 Patent Application Title |
Patent App Num. |
Date |
| Use of a new gene coding for a new member of the mcm2-8 family in pharmaceutical compositions | 20110023135 | 20110127 |
| The use of the human or animal MCM9 gene, or parts of the gene, or transcripts thereof, or antisense nucleic acids able to hybridize with part of the gene or transcripts, or silencing RNA derived from parts of the transcripts and able to repress the MCM9 gene, or proteins or peptidic fragments translated from the transcripts, or antibodies directed against the proteins or peptidic fragments, for the preparation of a pharmaceutical composition for the treatment of a human or animal pathology linked to a dysfunction of the expression of the MCM9 gene, or of human or animal cancers.
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| Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists | 20110021787 | 20110127 |
| in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
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| Novel indole derivatives as selective androgen receptor modulators (sarms) | 20110021785 | 20110127 |
| The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
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| Method of preparing stabilized pharmaceutical compositions comprising active ingredients susceptible to conversion to alternate polymorph forms | 20110021631 | 20110127 |
| A process is described for the preparation of a pharmaceutical comprising an active pharmaceutical ingredient capable of existing in multiple polymorphic forms, wherein the process comprises a step of preparation of a wet phase comprising the active pharmaceutical ingredient and microcrystalline cellulose and a liquid, wherein in the wet phase has a weight ratio of active pharmaceutical ingredient to microcrystalline cellulose above 1.0 or a weight ratio of active pharmaceutical ingredient to liquid above 1.0.
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| Encapsulation of vitamin c into water soluble dendrimers | 20110021626 | 20110127 |
| The invention relates to a conjugated dendrimer that comprises at least one water-soluble dendrimer and at least one vitamin C molecule. The conjugated dendrimer can be used e.g. for preparing cosmetic or pharmaceutical compositions. The dendrimers have a good vitamin C load capacity and are biocompatible.
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| 3-phenoxymethylpyrrolidine compounds | 20110021597 | 20110127 |
| where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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| Dual-acting antihypertensive agents | 20110021585 | 20110127 |
| wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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| Compounds which potentiate the ampa receptor and uses thereof in medicine | 20110021578 | 20110127 |
| Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; R1 is selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from C1-4alkyl and halogen; and R2 is selected from H and CH3 when n is 1 and R2 is H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, N and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
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| Antagonists of prostaglandin d2 receptors | 20110021573 | 20110127 |
| Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
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| Acyloxyalkyl carbamate prodrugs, methods of synthesis and use | 20110021571 | 20110127 |
| The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.
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| Pyridone glucokinase activators | 20110021570 | 20110127 |
| as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
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| Piperidine compounds, a process for their preparation and pharmaceutical compositions containing them | 20110021569 | 20110127 |
| Medicinal products containing the same which are useful in treating cognitive disorders associated with pathologies of the central nervous system.
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| Method of treating binge eating disorder and obesity resulting from binge eating behavior | 20110021564 | 20110127 |
| The invention provides methods of treating binge eating disorders, obesity resulting from binge eating behavior, and depression. The invention includes methods of treating certain co-morbidities in ADHD and ADD patients; for example the invention includes methods of treating generalized anxiety disorder, obsessional and ruminative thought disorders, and obsessive/compulsive behavior in ADHD and ADD patients. The invention also includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered with one or more other active agents. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.
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| Pyrrolidinyl derivatives and uses thereof | 20110021556 | 20110127 |
| The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.
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| Immunosuppressive macrolide powder for oral suspension | 20110021553 | 20110127 |
| The present invention describes pharmaceutical compositions that comprise a tacrolimus powder for oral suspension that exhibits great stability as a powder for suspension and also, once prepared, as the extemporaneous suspension, without the formation of cake-like clusters, same having a satisfactory flavour and a pleasant aroma. The invention also describes the method for preparing the pharmaceutical compositions, same being a dry method that comprises mixing tacrolimus and pre-sieved pharmaceutically acceptable carriers for a suitable length of time, and the use of the pharmaceutical compositions for treating and preventing rejection of transplanted organs and atopic dermatitis.
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| Pharmaceutical compositions comprising dextromethorphan and quinidine for the treatment of depression, anxiety, and neurodegenerative disorders | 20110021552 | 20110127 |
| Pharmaceutical compositions and methods for treating depression, anxiety, and neurodegenerative diseases and cognitive disorders, such as dementia and Alzheimer's disease, by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine.
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| Substantially pure and a stable crystalline form of bosentan | 20110021547 | 20110127 |
| Described is a highly stable crystalline form of bosentan having a water content in the range of about 3-4% by weight, based on the total weight of the bosentan, (bosentan crystalline form A5), a process for preparation thereof, and pharmaceutical compositions comprising the bosentan crystalline form A5. Provided also herein is a bosentan impurity, p-tert-butyl-N[6-hydroxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide (deshydroxyethyl bosentan impurity), and process for preparing and isolating thereof. Further provided are highly pure bosentan or a pharmaceutically acceptable salt thereof substantially free of deshydroxyethyl bosentan and bosentan dimer impurities, process for the preparation thereof, and pharmaceutical compositions comprising solid particles of highly pure bosentan or a pharmaceutically acceptable salt thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 300 microns.
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| Hydrochloride salt of ((1s,2s,4r)-4--2-hydroxycyclopentyl)methyl sulfamate | 20110021544 | 20110127 |
| crystalline forms thereof, and solvates thereof; pharmaceutical compositions comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and a pharmaceutically acceptable carrier or diluent; and the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting an E1 activating enzyme, particularly NAE, including, e.g., cancer.
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| Bis-(sulfonylamino) derivatives in therapy 066 | 20110021540 | 20110127 |
| The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
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| Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor | 20110021538 | 20110127 |
| The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
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| Crystalline forms and two solvated forms of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]quinolin-2(1h)-one lactic acid salts | 20110021536 | 20110127 |
| Crystalline forms or polymorphs of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one lactic acid salts, as well as to methods of making the same, pharmaceutical compositions comprising the same and methods of treatment using the same.
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| Cysteine prodrugs to treat schizophrenia and drug addiction | 20110021533 | 20110127 |
| The present invention provides cysteine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.
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| 2 -substituted- 3 -phenylpropionic acid derivatives and their use in the treatment of inflammatory bowel disease | 20110021534 | 20110127 |
| The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl) propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl) propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methylor ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.
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| Dual-acting oxazole antihypertensive agents | 20110021527 | 20110127 |
| wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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| Novel hydroxamates as therapeutic agents | 20110021528 | 20110127 |
| The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
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| Aryl sulfonamides | 20110021523 | 20110127 |
| Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
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| Fused heterocyclic compounds as ion channel modulators | 20110021521 | 20110127 |
| wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
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| Activators of executioner procaspases 3, 6 and 7 | 20110021522 | 20110127 |
| The present invention provides compounds as activators of procaspases 3, 6 and/or 7 and related derivatives, pharmaceutical compositions thereof, methods for their use, and methods for preparing these compounds. In one aspect, the compounds are useful for treating cancers and neoplastic diseases.
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| Pyrrolotriazine derivatives useful for treating cancer through inhibition of aurora kinase | 20110021518 | 20110127 |
| This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly Cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly Cancer.
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| Monocyclic cgrp receptor antagonists | 20110021516 | 20110127 |
| The present invention is directed to compounds of the formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, G1, G2, G3, G4, J, Q, Ea, Eb, Ec, R6, R7, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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| Use of regulatory sequences for specific, transient expression in neuronal determined cells | 20110016547 | 20110120 |
| The present invention relates to the use of regulatory sequences for mediating specific, early transient expression in proliverative neuronal determined cells. Furthermore, the uses of recombinant nucleic acid molecules comprising said defined regulatory sequences for mediating specific, early transient expression in proliverative neuronal determined cells as well as for the generation of non-human transgenic organisms and/or host cells are disclosed. In addition, the invention provides for transgenic non-human animals and/or host cells comprising said regulatory sequences and/or recombinant nucleic acid molecules. The invention also describes methods for the preparation of such vectors, host cells and transgenic non-human animals as well as methods for the detection and/or isolation of neuronal determined cells. Additionally, methods for screening of compounds capable of regulating neuronal determined cell activity, neurogenesis, stimulating... |
| Combination therapies for the treatment of obesity | 20110015663 | 20110120 |
| Described are pharmaceutical compositions comprising sibutramine, metformin, topiramate, and at least one pharmaceutically acceptable carrier or excipient. Another aspect of the present invention relates to a method of treating a patient suffering from obesity or needing to lose weight, comprising the step of co-administering to said patient a therapeutically effective amount of sibutramine, metformin, and topiramate. In certain embodiments, an aforementioned method is practiced in conjunction or tandem with a medical procedure or the use of a medical device or both.
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| Inhibitors of interleukin-1 beta converting enzyme | 20110015371 | 20110120 |
| The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
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| Ampholytic copolymer, production thereof, and use of the same | 20110015280 | 20110120 |
| The present invention relates to an ampholytic copolymer, to a process for its preparation, to cosmetic or pharmaceutical compositions which comprise at least one such ampholytic copolymer, and to further uses of these copolymers.
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| Therapeutic delivery of carbon monoxide | 20110015263 | 20110120 |
| Compounds, pharmaceutical compositions and methods for the therapeutic delivery of carbon monoxide to humans and other mammals that employ transition metal complexes having at least a substituted cyclopentadienyl, indenyl or fluorenyl ligand and two or more carbonyl ligands.
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| Anti-malarial pharmaceutical composition | 20110015260 | 20110120 |
| The invention provides pharmaceutical compositions for the treatment and prophylaxis of malaria, comprising artemether and a medium chain triglyceride formulated for transmucosal sublingual, buccal or nasal delivery, especially by a spray. Also provided are delivery devices containing the compositions.
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| Hypoxia inducible vegf plasmid for ischemic disease | 20110015257 | 20110120 |
| Plasmids useful for treating ischemic disease, such as ischemic heart disease, are described. The plasmids express vascular endothelial growth factor (VEGF) under the control of a promoter (RTP801) that is up-regulated under hypoxic conditions. Pharmaceutical compositions for treating ischemic disease include mixtures of the hypoxia-regulated VEGF plasmids and pharmaceutically acceptable carriers. Methods for treating ischemic disease include administering such pharmaceutical compositions to a person in need of such treatment.
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| Bendamustine amphiphilic cationic compositions | 20110015245 | 20110120 |
| The present invention is directed to pharmaceutical compositions comprising bendamustine and one or more amphiphilic cationic compounds, which self assemble to form aggregates. The exhibiting enhanced stability in aqueous solutions, including plasma. The unexpectedly enhanced stability afforded by such aggregates permits patients to be treated with bendamustine in lower and/or with less frequent dosages or to improve its therapeutic effect while using the same as presently used treatment protocol.
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| Bendamustine amphiphilic anionic compositions | 20110015244 | 20110120 |
| The present invention is directed to pharmaceutical compositions comprising bendamustine and one or more amphiphilic anionic compounds and self assembled aggregates, which aggregates exhibit enhanced stability in aqueous solutions, including plasma, are disclosed. The unexpectedly enhanced stability afforded by such aggregates permits patients to be treated with bendamustine in lower and/or with less frequent dosages or to improve its therapeutic effect while using the same as presently used treatment protocol.
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| Co-solvent compositions and methods for improved delivery of dantrolene theraputic agents | 20110015243 | 20110120 |
| The present invention provides for methods of using tert-butyl alcohol (TBA) co-solvent systems in the formulation and production of a pharmaceutical agent with low solubility. The present invention also provides for pharmaceutical compositions made using the novel co-solvent system. In one embodiment, the invention provides for a method of making dantrolene sodium (DS) formulation for intravenous use (DS-IV). This instantaneous reconstitution of the DS-IV product constitutes a significant improvement in the pharmacotherapy of patients undergoing malignant hyperthermia during surgery.
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| Novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1]octane and their use as monoamine neurotransmitter re-uptake inhibitors | 20110015235 | 20110120 |
| This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1]octane useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
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| Isoxazole and isothiazole compounds useful in the treatment of inflammation | 20110015231 | 20110120 |
| The variables of Formulae (I), (I a), (VII) and (VII a) are described herein.
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| Novel compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and pharmaceutical compositions containing the same | 20110015230 | 20110120 |
| The present disclosure provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
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| Benzoquinolizinium salt derivatives as anticancer agents | 20110015222 | 20110120 |
| processes for the preparation of said compounds, pharmaceutical compositions containing said compounds and the use of said compounds for the manufacture of medicaments suitable for the treatment of cancerous diseases.
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| Tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, their salts, process for producing the compounds and their pharmaceutical use | 20110015214 | 20110120 |
| The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutically active agent and as pharmaceutical compositions for prophylaxis and/or treatment of proliferative diseases such as cancer.
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| Crystalline forms of 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester | 20110015215 | 20110120 |
| The present invention is directed to a novel crystalline forms of 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutical compositions containing said crystalline form and the use of said crystalline forms in the treatment of metabolic related disorders. The present invention is further directed to processes for the preparation of the crystalline forms of 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester.
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| Pharmaceutical compositions containing dopamine receptor ligands and methods of treatment using dopamine receptor ligands | 20110015208 | 20110120 |
| The present invention relates to pharmaceutical compositions containing dopamine receptor ligands and selective serotonin reuptake inhibitors and to methods of treating disorders such as schizophrenia, major depressive disorder and bipolar depression using combinations of dopamine receptor ligands and selective serotonin reuptake inhibitors. The present invention also relates to methods of treating depression using dopamine receptor ligands.
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| Nitrogen-containing bycyclic compounds active on chronic pain conditions | 20110015200 | 20110120 |
| The invention refers to compounds of general formula (I) wherein the R groups are, independently, H, C1-6alkyl, aryl, CF3; Y is CH2, C═O; X is bond, C═O, SO2, or C═N—CN; m is 0, 1; n is 0, 1; A is a heterocycle, or a phenyl group optionally substituted as defined in the specification. The compounds are active on chronic pain conditions of different origin; they can be administered alone or with other drugs. Most of these compounds are new. The invention include a process to prepare said compounds, and pharmaceutical compositions suitable for their administration to a patient.
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| Gpr119 agonists | 20110015199 | 20110120 |
| and pharmaceutical compositions for the treatment of diabetes and obesity.
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| Lupeol-type triterpene derivatives as antivirals | 20110015196 | 20110120 |
| The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
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| Organic compounds | 20110015191 | 20110120 |
| Novel polymorph form III of Aprepitant and a method for preparation of novel form III is disclosed. New processes for the preparation of Aprepitant form II are disclosed. The processes involve transformation of form III to form II by heating in decalin and the precipitation of form II from a solvent or solvent mixture by cooling and/or addition of addition of seed crystals or an anti solvent. Solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A process for the preparation of the solid dispersion by evaporation of a solution of Aprepitant and the carrier in a suitable solvent is disclosed. Stable Aprepitant form II is disclosed. Further pharmaceutical compositions containing Aprepitant form II, III or solid dispersions containing Aprepitant form II in... |
| Benzofuran compounds | 20110015185 | 20110120 |
| P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
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| Methods and compositions for protecting and treating neuroinjury | 20110015186 | 20110120 |
| A method and composition for protecting and/or treating neuroinjury are disclosed. In one aspect, the present application discloses a method for protecting and/or treating a subject from organophosphate-induced neuronal injury. The method comprises administering to a subject an effective amount of 4R cembranoid, 4S cembranoid or a cembranoid analogue. In another aspect, the application discloses neuroprotective pharmaceutical compositions for protecting and/or treating a subject from organophosphate-induced neuronal injury. A kit for protecting and treating a subject from organophosphate-induced neurodamage is also disclosed.
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| Substituted pyrazole sigma receptor antagonists | 20110015183 | 20110120 |
| and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.
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| Amido-thiophene compounds and their use | 20110015178 | 20110120 |
| The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
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| Crystalline freebase forms of a biphenyl compound | 20110015163 | 20110120 |
| The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.
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| Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 | 20110015157 | 20110120 |
| This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih); (Ii); (Ij), (Ik), (II) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
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| Method for preparing gynostemma pentaphyllum extract with increasing damulin a and damulin b contents, and pharmaceutical compositions of the same for treating metabolic disease | 20110015142 | 20110120 |
| Disclosed is an AMPK activating material used for improving and treating metabolic syndrome, in which AMPK (AMP-activated protein kinase) is a main enzyme for regulating an energy sensor and lipid/glucose metabolism in the body. The activation of AMPK inhibits the synthesis of fat and cholesterol, and accelerates the reduction of body fat and blood glucose, thereby improving obesity, diabetes, and hyperlipidaemia. The disclosed AMPK activating material contains, as active ingredients having an improving and treating effect on metabolic syndrome, including obesity, diabetes, and hyperlipidaemia, a novel compound 2α,3β,12β-trihydroxydammar-20(22)-E,24-diene-3-O-[β-D-glucopyranosyl-(1→)-β-D-glucopyranoside], named Damulin A, and a novel compound 2α,3β,12β-trihydroxydammara-20,24-diene-3-O-[β-D-glucopyranosyl-(1→)-β-D-glucopyranoside], named Damulin B. Herein, the contents of damulin A and damulin B (as active indicator ingredients for AMPK activation) can be increased by treating a Gynostemma pentaphyllum extract with high... |
| Targeting complement factor h for treatment of diseases | 20110015127 | 20110120 |
| The invention provides a CR2-FH molecule comprising a CR2 portion comprising CR2 protein or a fragment thereof and a FH portion comprising a factor H protein or a fragment thereof, and pharmaceutical compositions comprising a CR2-FH molecule. Also provided are methods of using the compositions for treatment diseases in which the alternative complement pathway is implicated, such as age-related macular degeneration, rheumatoid arthritis, and ischemia reperfusion.
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| Novel semi-synthetic glycopeptides as antibacterial agents | 20110015119 | 20110120 |
| Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the... |
| Novel polymorphs of azabicyclohexane | 20090326245 | 20091231 |
| The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.
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| Benzothiazole cyclobutyl amine derivatives | 20090326222 | 20091231 |
| are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
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| Enantiomers of o-desmethyl venlafaxine | 20090326075 | 20091231 |
| This invention provides pharmaceutically active enantiomers of the venlafaxine metabolite O-Desmethyl venlafaxine, R(−)-4-[2-(Dimethylamino-1-(1-hydroxycyclo-hexyl)ethyl]phenol or R(−)1-[2-(dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclo-hexanol, and S(+)-1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclohexanol or S(+)-4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol, or one or more pharmaceutically acceptable salts or salt hydrates thereof, as well as pharmaceutical compositions utilizing these enantiomers and methods of using the enantiomers to treat, inhibit or control central nervous system disorders.
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| Alkoxy compounds for disease treatment | 20090326074 | 20091231 |
| The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
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| Vinyl substituted fatty acids | 20090326070 | 20091231 |
| Activated fatty acids, pharmaceutical compositions including activated fatty acids, methods for using activated fatty acids to treat a variety of diseases, and methods for preparing activated fatty acids are provided herein.
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| Levodopa prodrug mesylate, compositions thereof, and uses thereof | 20090326067 | 20091231 |
| (2R)-2-Phenylcarbonyloxypropyl(2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.
... |
| Carvedilol | 20090326033 | 20091231 |
| This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.
... |
| Pharmaceutical compositions comprising nk1 receptor antagonists and sodium channel blockers | 20090326032 | 20091231 |
| as a combined preparation for simultaneous or sequential administration, and to the use of such compositions in the treatment of certain disorders, including epilepsy and mood disorders.
... |
| Non-cyclic substituted benzimidazole thiophene benzyl ether compounds | 20090326029 | 20091231 |
| The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
... |
| New pharmaceutical composition | 20090326025 | 20091231 |
| The invention provides a new pharmaceutical compositions for treating cardiovascular disease, which contains the active component 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxy)carbonyloxy]methyl ester dispersing in pharmaceutically acceptable carriers. The composition can be prepared to solid dosage forms e.g. powders, granules, dripping pills, micro-pellets, tablets, capsules, lozenges etc. by mouth or other way e.g. sublingual administration etc.
... |
| Salts of imidazole-5-carboxylic acid derivatives, a method for preparing same and pharmaceutical compositions comprising same | 20090326024 | 20091231 |
| The present invention provides pharmaceutically acceptable salts of imidazole-5-carboxylic acid derivatives, methods for preparing same and pharmaceutical compositions comprising same. The salts obtained by the present invention can be easily dissolved in common solvents, such as water and methanol. The bioavailability thereof is good in animal body. Thereby it is applicable to be developed as a normal preparation for treating hypertension.
... |
| Compounds for treatment of cancer | 20090326020 | 20091231 |
| where Q is S, N, or O; X is optional, and can be O═, S═, ═N—NH2, ═N—OH, or —OH; Y is optional and can be —N(H)—, O, or C1 to C20 hydrocarbon; and R1 and R2 are each independently substituted or unsubstituted single-, fused- or multiple-ring aryl or (hetero)cyclic ring systems. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.
... |
| 3,4-bicyclic pyrrolidine antivirals | 20090326019 | 20091231 |
| which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
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| Isomers of inositol niacinate and uses thereof | 20090326013 | 20091231 |
| An ester formed from an inositol or an inositol derivative and niacin, wherein the inositol or the inositol derivatives comprises a stereoisomer selected from allo-inositol, cis-inositol, epi-inositol, muco-inositol, neo-inositol, scyllo-inositol, D-chiro-inositol and L-chiro-inositol, or pharmaceutically acceptable salts thereof. Examples of esters include inositol hexaniacinates such as allo-inositol hexaniacinate and cis-inositol hexaniacinate. The esters can be used to treat any disorder that is treatable with niacin therapy such as dyslipidemia, hypercholesterolemia, hyperlipidemia or cardiovascular disease. The esters can be administered with other agents such as HMG-CoA reductase inhibitors, statins, fibrates, activators of peroxisome proliferator activated receptors poli-cosanol, phytosterols, tocotrienols, calcium, bile acid sequestrants, guar gum and free niacin. The invention includes pharmaceutical compositions containing these compounds.
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| Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors | 20090326006 | 20091231 |
| The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.
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| Muscarinic receptor antagonists | 20090326004 | 20091231 |
| The present invention relates generally to muscarinic receptor antagonist, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and the method for treating diseases mediated through muscarinic receptors. Also provided herein are pharmaceutical composition comprising one or more muscarinic receptor antagonists and at least one other active ingredients include, but are not limited to, corticosteroids, beta agonists, leukotriene antagonists, 5-lipoxygenase inhibitors, anti-histamines, antitussives, dopamine receptor antagonists, chemokine inhibitors, p38 MAP Kinase inhibitors, and PDE-IV inhibitors.
... |
| Thieno [2,3-b] pyridine compounds with mglur activity | 20090326002 | 20091231 |
| Provided herein are Thieno[2,3-b]pyridine compounds with mGluR activity. Also provided herein are processes and intermediates for the preparation of the Thieno[2,3-b]pyridine compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in treatment, therapy, and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.
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| Thienopyridine derivatives as modulators of metabotropic glutamate receptors | 20090326001 | 20091231 |
| The present invention relates to new mGluR1 and niGluR5 receptor subtype preferring ligands of formula (I): wherein X represents a group selected from (CH2)n, CH═CH, NH, N(CH3), NHCH2, N(CH3)CH2, O, OCH2, CH2COO, NHCH2COO; n is an integer of 0 to 2; Y represents a subtituent selected from H, CH3, F, Cl, Br; Z is H or CH3; R is alkyl, cycloalkyl, an optionally substituted phenyl or an optionally substituted heteroaryl, and/or geometric isomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of... |
| Pharmaceutical compositions for the treatment of capillary arteriopathy | 20090325997 | 20091231 |
| The present invention relates to the use of ergot derivatives or ergolines, and in particular of lisuride and terguride for the prophylaxis and treatment of constrictive capillary arteriopathy. Constrictive capillary arteriopathy refers to the diseases pulmonary arterial hypertension, endogenously induced or exogenously induced glomeruloscleroses as well as secondary Raynaud's syndrome.
... |
| Camptothecin derivatives and their use | 20090325996 | 20091231 |
| New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines.
... |
| Glyt1 transporter inhibitors and uses thereof in treatment of neurological and neuropsychiatric disorders | 20090325993 | 20091231 |
| wherein R1, R2, R3, R4, R5, R6, R7, R9, R10, X, n, p and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further discloses pharmaceutical compositions and combinations comprising the compounds.
... |
| Spirolactam bicyclic cgrp receptor antagonists | 20090325991 | 20091231 |
| (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
... |
| Indazolyl derivatives useful as potassium channel modulating agents | 20090325989 | 20091231 |
| Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular respiratory diseases, epilepsy, convulsions, seizures, absence seizures, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, erectile dysfunction, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, autism, ataxia, traumatic brain injury, Parkinson's disease, bipolar disorder, psychosis, schizophrenia, anxiety, depression, mania, mood disorders, dementia, memory and attention deficits, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, arrhythmia, hypertension, myotonic muscle dystrophia, spasticity, xerostomi, diabetes type II, hyperinsulinemia, premature labour, baldness, cancer, irritable bowel syndrome, immune suppression, migraine and pain.
... |
| Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof | 20090325988 | 20091231 |
| wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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| Quinazolinedione derivatives as trpa1 modulators | 20090325987 | 20091231 |
| The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
... |
| Diketopiperidine derivatives as hiv attachment inhibitors | 20090325985 | 20091231 |
| Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketopiperidine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.
... |
| Deazapurine analogs of 1'-aza-l-nucleosides | 20090325986 | 20091231 |
| The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds.
... |
| New purine derivatives | 20090325983 | 20091231 |
| A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
... |
| Compounds and compositions as lxr modulators | 20090325981 | 20091231 |
| The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
... |
| Piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid mtp inhibiting compounds | 20090325980 | 20091231 |
| The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
... |
| Methods for treating multiple myeloma using 4-(amino)-2-(2,6-dioxo(3-piperidyl))-isoindoline-1,3dione | 20080317708 | 20081225 |
| Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
... |
| Methods for treating head or neck cancer using 4-(amino)-2-(2,6-dioxo(3-piperidyl))-isoindoline-1,3-dione | 20080317709 | 20081225 |
| Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
... |
| Arylpiperidinyl and arylpyrrolidinyl tripeptide hepatitis c serine protease inhibitors | 20080317712 | 20081225 |
| which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
... |
| Anti-hepatitis b virus ribozymal nucleic acid | 20080317717 | 20081225 |
| This invention relates to ribozymes which cleave Hepatitis B Virus (HBV) at CUC sites. Suitable ribozymes may, for example, cleave at GGCUCUCUCGUCCC, CCUCAGCUCUGUAUCG or GAGGACUCUUGGA recognition sequences in HBV RNA. Ribozymal DNA, vector systems and pharmaceutical compositions are provided which may be useful, for example, in the treatment of HBV infection.
... |
| Compounds and methods for treatment and diagnosis of chlamydial infection | 20080317772 | 20081225 |
| Compounds and methods for the diagnosis and treatment of Chlamydial infection are disclosed. The compounds provided include polypeptides that contain at least one antigenic portion of a Chlamydia antigen and DNA sequences encoding such polypeptides. Pharmaceutical compositions and vaccines comprising such polypeptides or DNA sequences are also provided, together with antibodies directed against such polypeptides. Diagnostic kits containing such polypeptides or DNA sequences and a suitable detection reagent may be used for the detection of Chlamydial infection in patients and in biological samples.
... |
| Novel anti-inflammatory androstane derivatives | 20080317833 | 20081225 |
| in admixture with one or more physiologically acceptable diluents or carriers.
... |
| Oral dosage forms for propiverine or pharmaceutically acceptable salts thereof having prolonged release of the active agent | 20080317848 | 20081225 |
| By suitable retardation oral pharmaceutical compositions containing propiverine or one or several pharmaceutically acceptable salts thereof in an amount of 4 mg to 60 mg propiverine and having a prolonged release of the active agent are produced. Preferably a blend of active agent and optionally one or more acidic substances having a pKa value of less than 6.65 are provided with a retarding coating or are embedded in a matrix which is then optionally coated with further retarding layers.
... |
| Method for improving the medical treatment of pain | 20080317849 | 20081225 |
| Methods for improving pain management in a mammal, the methods comprising administering a combination of a strontium-containing compound and a second therapeutically and/or prophylactically active substance selected from the group consisting of analgesic agents, anti-inflammatory agents and palliative agents to the mammal. Pharmaceutical compositions for use in such methods, comprising a strontium-containing compound and a second therapeutically and/or prophylactically active substance selected from the group consisting of analgesic agents, anti-inflammatory agents and palliative agents.
... |
| Pharmaceutical compositions useful in the transmucosal administration of drugs | 20080317863 | 20081225 |
| There is provided pharmaceutical compositions in the form of homogeneous interactive mixtures, which compositions comprise a pharmacologically-effective amount of an active ingredient in the form of microparticles of a size between about 0.5 μm and about 10 μm, which particles are attached to the surfaces of larger carrier particles with a size range of between about 10 and about 100 μm. The carrier particle material is preferably bio- and/or mucoadhesive in its nature.
... |
| Compositions and methods for the intracellular disruption of vegf and vegfr-2 by intraceptors | 20080318857 | 20081225 |
| The present invention provides an intraceptor that interacts with and decreases activity of with VEGF and/or a VEGFR for the treatment of angiogenesis-related conditions. The present invention further provides pharmaceutical compositions, and methods of use thereof, for the treatment and prevention of an angiogenesis-related condition using said intraceptors. The invention further provides for nucleic acids encoding said intraceptors.
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| Use of mycobacterial mannosylated lipoglycans peptide mimotopes for treating inflammation | 20080318868 | 20081225 |
| The present invention is based on the discovery that biological peptide-based mimotopes of mannose-containing cell-wall compounds of Mycobacterium tuberculosis, specifically, ManLAM, have an anti-inflammatory effect and immunoregulator effect in animal models of inflammation. Such models include animal models of allergic peritonitis, allergic asthma and septic shock model (mice injected with LPS) and in Crohn's disease model (TNBS-induced colitis). Thus, the present invention concerns the use a molecule, particularly, an amino acid based molecule for the production of a pharmaceutical composition for the treatment of an inflammatory condition, the amino acid comprising one or more peptides characterized in that it can bind to ManLAM binding antibodies; and/or it can elicit an immune response in a subject inoculated therewith, giving rise to production of ManLAM-binding antibodies. The invention... |
| Antibacterial agents | 20080318878 | 20081225 |
| The present invention provides acylide derivatives, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed to by Gram-positive, Gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds disclosed herein, pharmaceutical compositions thereof, and method of treating bacterial infections.
... |
| 20-cyclopropyl, 26,27-alkyl/haloalkyl vitamin d3 compounds and methods of use thereof | 20080318911 | 20081225 |
| The invention provides vitamin D3 analogs of cholecalciferol, substituted at carbon 20 with cycloalkyl, e.g., cyclopropyl, wherein carbon-16 is a double bond, and carbon-23 is a single, double, or triple bond. Various alkyl or haloalkyl substitutions are incorporated as carbon-25. The invention provides pharmaceutically acceptable esters, salts, and prodrugs thereof. Methods for using the compounds to treat vitamin D3 associated states, and pharmaceutical compositions containing the compounds are also disclosed.
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| Tricyclic 6-alkylidene-penems as beta-lactamase inhibitors | 20080318921 | 20081225 |
| The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
... |
| Substituted monocyclic cgrp receptor antagonists | 20080318927 | 20081225 |
| (wherein variables A1, A2, A2, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
... |
| Pyrimidine derivatives useful as inhibitors of pkc-theta | 20080318929 | 20081225 |
| Disclosed are novel compounds of formula (I) wherein R1, R2, R3, and R4 and A are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
... |
| Sodium channel blocker compositions and the use thereof | 20080318932 | 20081225 |
| Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.
... |
| Di-amino-substituted heterocyclic compounds and methods of use | 20080318946 | 20081225 |
| wherein R1-6, X and Y are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
... |
| Dual-acting benzoimidazole antihypertensive agents | 20080318951 | 20081225 |
| wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
... |
| New utilities of tricyclic compounds | 20080318958 | 20081225 |
| in which X1 and X1 are independently an aryl or heteroaryl that may be optionally substituted, a hydrogen, a halogen, or the like; ring A is a benzene ring or 6-membered aromatic heterocyclic ring containing 1 to 3 N atoms that may be optionally condensed with another aromatic ring; R1 to R4 are independently a hydrogen, a halogen, a lower alkyl, a lower alkoxy or the like; a prodrug thereof, a pharmaceutically acceptable salt or solvate of them are disclosed.
... |
| Chemical compounds | 20080318968 | 20081225 |
| wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).
... |
| Indolylmaleimide derivatives | 20080318975 | 20081225 |
| wherein R, R1, and R2, ring A and ring B are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
... |
| Novel compounds 480 | 20080318981 | 20081225 |
| wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
... |
| Method of treating pain utilizing controlled release oxymorphone pharmaceutical compositions and instruction on dosing for hepatic impairment | 20080318993 | 20081225 |
| The invention pertains to a method of using oxymorphone in the treatment of pain by providing a patient with an oxymorphone dosage form and informing the patient or prescribing physician that the bioavailability of oxymorphone may be increased in patients with hepatic impairment.
... |
| Method of treating pain utilizing controlled release oxymorphone pharmaceutical compositions and instruction on dosing for renal impairment | 20080318994 | 20081225 |
| The invention pertains to a method of using oxymorphone in the treatment of pain by providing a patient with an oxymorphone dosage form and informing the patient or prescribing physician that the bioavailability of oxymorphone is increased in patients with renal impairment.
... |
| 6-amino(aza)indane compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor | 20080318996 | 20081225 |
| The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R6 and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising... |
| Alkyloxy substituted thiazoloquinolines and thiazolonaphthyridines | 20080318998 | 20081225 |
| Thiazoloquinolines and thiazolonaphthyridines with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
... |
| Xanthine derivatives a useful as muscarinic receptor antagonists | 20080319002 | 20081225 |
| This present invention generally relates to xanthine derivatives as muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.
... |
| Nitroxides for use in treating or preventing diabetes | 20080319014 | 20081225 |
| Pharmaceutical compositions are provided that are useful in treating diabetes. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of genes related to diabetes. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of diabetes. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl).
... |
| Non-anilinic derivatives of isothiazol-3(2h)-thione 1,1-dioxides as liver x receptor modulators | 20080319017 | 20081225 |
| to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
... |
| Method and composition for enhancing bone formation | 20070297985 | 20071227 |
| A method for screening for an osteogenic compound that is a PTEN antagonist. Also included are methods for enhancing bone formation and pharmaceutical compositions therefore, as well as methods for treating conditions associated with bone loss.
... |
| Pharmaceutical compositions and methods for reducing body fat | 20070298025 | 20071227 |
| The invention concerns a method of reducing body fat content of a subject in need thereof, the method comprising administering to the subject an agent capable of down-regulating activity and/or expression of at least one component participating in protein digestion and/or absorption. Such agents may be (i) an oligonucleotide directed to an endogenous nucleic acid sequence expressing said at least one component participating in said protein digestion and/or absorption or (ii) a protease inhibitor directed to said at least one component participating in protein digestion and/or absorption. The invention is particularly directed to a method of reducing body fat content of a subject in need thereof, the method comprising administering to the subject serine protease inhibitor inhibiting both enteropeptidase and trypsin activity.
... |
| Novel target for antiderpressant therapy | 20070298027 | 20071227 |
| The present invention relates to a method of classifying an individual comprising analyzing the nucleic acid of a sample taken from said patient for nucleotide polymorphisms in a haplotype block comprising the gene encoding FKBP51 and/or determining the expression level of FKBP51 in said sample. In a preferred embodiment, the invention provides a method of predicting the response to antidepressant therapy. Furthermore, a method of developing an anti-depressant drug, and pharmaceutical compositions are provided.
... |
| Diagnostics and therapeutics for diseases associated with kallikrein 3 (klk3) | 20070298028 | 20071227 |
| The invention provides a human KLK3 which is associated with the endocrine system and hormone disorders, cardiovascular disorders, metabolic diseases, cancer disorders, neurological disorders, urological disorders and reproduction disorders. The invention also provides assays for the identification of compounds useful in the treatment or prevention of endocrine system and hormone disorders, cardiovascular disorders, metabolic diseases, cancer disorders, neurological disorders, urological disorders and reproduction disorders. The invention also features compounds which bind to and/or activate or inhibit the activity of KLK3 as well as pharmaceutical compositions comprising such compounds.
... |
| Pharmaceutical compositions comprising ascomycin | 20070298058 | 20071227 |
| The invention relates to pharmaceutical compositions comprising an ascomycin in dissolved form and a pharmaceutically acceptable cellulose derivative for prevention or reduction of crystal growth.
... |
| Compressed pharmaceutical compositions comprising peg and electrolytes | 20070298100 | 20071227 |
| The invention provides a compressed pharmaceutical composition comprising polyethylene glycol of molecular weight from 2000 to 4500, wherein the polyethylene glycol makes up from 80 to 99.5% by weight of the composition, one or more electrolytes for the treatment of constipation, faecal impaction, faecal retention, intestinal gas and cramping, or flatulence; or for orthostatic lavage, colon evacuation or colon cleansing. It has been found, surprisingly, that a compressed pharmaceutical composition comprising PEG for example a solid tablet, is significantly more palatable than previously proposed compositions and is effective when administered. The compressed pharmaceutical composition of the invention comprising polyethylene glycol has been found to have a more agreeable taste and a more agreeable mouthfeel than previously proposed liquid or dry powder or granular compositions.
... |
| Pharmaceutical compositions of mirtazapine | 20070298107 | 20071227 |
| The present invention relates to pharmaceutical compositions of mirtazapine or its pharmaceutically acceptable salts. More particularly, the present invention relates to solid unit dosage forms of anhydrous mirtazapine or its pharmaceutically acceptable salts suitable for oral administration. The present invention also relates to a process for the preparation of pharmaceutical compositions of mirtazapine or its pharmaceutically acceptable salts.
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| Crystalline forms of a biphenyl compound | 20070298112 | 20071227 |
| The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
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| Methods and compositions for use in evaluating and treating neoplastic disease conditions | 20070298444 | 20071227 |
| Methods and compositions for use in a evaluating and treating neoplastic disease conditions are provided. In certain embodiments of the subject invention, the presence of at least one target protein associated with cellular locomotion is determined in a cell to make an evaluation regarding the cell and/or host from which the cell was obtained. In yet other embodiments, the activity certain embodiments, the target protein is part of a nucleus-associated ribbon-like structure. Also provided are kits and pharmaceutical compositions that find use in various embodiments invention finds use in a variety of different applications, including both diagnostic and therapeutic applications.
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| Novel receptor that causes cell death | 20070298460 | 20071227 |
| Isolated apoptosis inducing receptors, DNAs encoding such receptors, and pharmaceutical compositions made therefrom, are disclosed. The isolated receptors can be used to regulate an immune response. The receptors are also useful in screening for inhibitors thereof.
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| Vascular endothelial growth factor d(vegf-d) antibodies and vectors, and methods of uses | 20070298493 | 20071227 |
| VEGF-D, a new member of the PDGF family of growth factors, which among other things stimulates endothelial cell proliferation and angiogenesis and increases vascular permeability, as well as nucleotide sequences encoding it, methods for producing it, antibodies and other antagonists to it, transfected or transformed host cells for expressing it, pharmaceutical compositions containing it, and uses thereof in medical and diagnostic applications.
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| Analogs of parathyroid hormone | 20070299009 | 20071227 |
| The present invention is directed to peptide analogues of fragment of parathyroid hormone (PTH) or parathyroid hormone-related protein (PTHrP), a method of using said analogues alone or in combination with a bisphosphonate or calcitonin to treat osteoporosis and pharmaceutical compositions comprising said analogues alone or in combination with a bisphosphonate or calcitonin.
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| Exosite-directed thrombin inhibitors | 20070299013 | 20071227 |
| Disclosed are an amino acid sequence of the human blood clotting factor Va, peptides containing such sequence, and additional peptides of interest that significantly inhibit thrombin generation. Also disclosed are pharmaceutical compositions containing these peptides and related therapeutic methods for inhibiting thrombin generation and treating blood coagulation disorders.
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| Macrolides and methods for producing same | 20070299019 | 20071227 |
| This invention relates, in part, to macrolide compounds, actinomycete strains for producing them, and pharmaceutical compositions containing them.
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| Methods for treatment of ovarian, colorectal or pancreatic cancer using 4-(aminno)-2(2,6-dioxo(3-piperidyl)-isoindoline-1,3-dione | 20070299020 | 20071227 |
| Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
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| P185neu-encoding dna and therapeutical uses thereof | 20070299023 | 20071227 |
| Plasmids containing sequences encoding different fragments of p185neu oncoprotein, able to induce an immune response against tumours expressing oncogenes of the ErbB family, and pharmaceutical compositions thereof.
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| Pharmaceutical co-crystal compositions and related methods of use | 20070299033 | 20071227 |
| The present invention comprises pharmaceutical compositions comprising a co-crystal of an API and a co-crystal former, and methods of making and using the same.
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| Combination of sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression | 20070299055 | 20071227 |
| One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering... |
| N3 alkylated benzimidazole derivatives as mek inhibitors | 20070299063 | 20071227 |
| and pharmaceutically acceptable salts thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
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| Quinoline and isoquinoline derivatives as phosphodiesterase 10 inhibitors | 20070299067 | 20071227 |
| The present invention is directed to certain quinoline and isoquinoline compounds that are PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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| Methods for treating hepatitis c | 20070299068 | 20071227 |
| The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
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| Methods for treating hepatitis c | 20070299069 | 20071227 |
| The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
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| Substituted phenyl methanone derivatives | 20070299071 | 20071227 |
| wherein R1, R2, R3, X, n, and m are as defined herein and to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them, and to methods for treating neurological and neuropsychiatric disorders.
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| Aryl-substituted polycyclic amines, method for the production thereof, and use thereof as a medicament | 20070299077 | 20071227 |
| where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.
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| Quinoxalinyl macrocyclic hepatitis c virus serine protease inhibitors | 20070299078 | 20071227 |
| which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
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| Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase | 20070299081 | 20071227 |
| Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): Formula (I) where x, y, G, J, L, M, V, W, R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8, and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
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| 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline hydrochloric acid salts | 20070299083 | 20071227 |
| The present invention relates to hydrochloric acid salt and crystalline forms of the 5-HT1A binding agent 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline, as well as pharmaceutical compositions thereof, and methods of use thereof.
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| Indole derivatives useful for treating resistance to antitumor agents | 20070299084 | 20071227 |
| The use of a group of indole compounds of formula (I) is described for treating tumours which have developed resistance to antitumour drugs. The compounds of formula (I) can be used in monotherapy, to treat tumours affected by drug resistance, or in co-therapy, as synergistic enhancers of the action of the aforesaid antitumour drugs. In addition, pharmaceutical compositions are described which comprise the indole derivatives of formula (I) in association with antitumour drugs the activity of which is to be enhanced.
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| Therapeutic agent for neuropathic pain | 20070299098 | 20071227 |
| The present invention provides therapeutic agents for neuropathic pain, the agents having excellent therapeutic effects on neuropathic pain, which is an intractable disorder. More specifically, the invention provides therapeutic agents for neuropathic pain comprising, as the active ingredient, an opioid receptor antagonist (particularly naloxone, naltrexone, naloxonazine, naltrindole, etc.), pharmaceutical compositions for treating neuropathic pain comprising an opioid receptor antagonist as the active ingredient, and a method for treating neuropathic pain using opioid receptor antagonists.
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| Niacin receptor agonists, compositions containing such compounds and methods of treatment | 20070299101 | 20071227 |
| The present invention relates to niacin receptor agonists of formula: (I); as well as pharmaceutically acceptable salts and solvates. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included.
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| Methods for preparing pharmaceutical compositions | 20060292081 | 20061228 |
| The present invention relates to improvements in dry powder formulations comprising a pharmaceutically active agent for administration by inhalation, and in particular to methods of preparing dry powder compositions with improved properties. In particular, spray drying processes are adapted and adjusted to obtain active particles with higher fine particle fractions and fine particle doses.
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| Allergen vaccine proteins for the treatment and prevention of allergic diseases | 20060292138 | 20061228 |
| The present invention provides fusion proteins comprising an allergen sequence linked via an IgG hinge region to another polypeptide sequence capable of specifically binding to a native IgG inhibitory receptor containing an immune receptor tyrosine based inhibitory motif (ITIM). They are designed to cross-link an Fc receptor for IgE (e.g., FcεR1) and an IgG inhibitory receptor (e.g., FcγRIIb), thereby inhibiting the IgE-driven mediators released from mast cells and basophils. In addition, the present invention provides nucleic acid molecules encoding the fusion proteins, vectors and host cells for producing the fusion proteins, pharmaceutical compositions comprising the fusion proteins, and methods for ameliorating or reducing the risk of IgE-medicated allergic diseases.
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| Novel t-cell membrane protein (tirc7), peptides and antibodies derived therefrom and uses thereof | 20060292143 | 20061228 |
| Described are generally a T cell immune response cDNA 7 (TIRC7) encoding a novel T-cell transmembrane protein as well as peptides und polypeptides derived therefrom and antibodies recognizing said (poly)peptides. More particularly, peptide and polypeptide as well as antibodies being capable of inhibiting T-cell stimulation through the T-cell membrane protein (TIRC7) are provided. Furthermore, vectors comprising the aforementioned polynucleotides and host cells transformed therewith as well as their use in the production of the above-defined proteins, peptides or polypeptides are described. Additionally, pharmaceutical and diagnostic compositions are provided comprising any one of the afore described polynucleotide, vector, protein, peptide, polypeptide, or antibody. Furthermore, methods and uses for modulating immune responses through the novel TIRC7 membrane protein as well as pharmaceutical compositions comprising agents which act on... |
| Variable antibodies | 20060292149 | 20061228 |
| The present invention discloses inhibitory antibodies against Factor VIII with modified glycosylation, either by enzymatic deglycosylation or by site directed mutagenesis. Said antibodies with modified glycosylation have equal affinity for FVIII but show different inhibiting properties. The use of one or a mixture of said antibodies allow modulation of the inhibition of factor VII to levels between 40 and 95%. The present invention further disclosed pharmaceutical compositions comprising inhibitory antibodies against Factor VIII with modified glycosylation, combinations of these antibodies and methods for treating haemostasis disorders using said antibodies and antibody mixtures.
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| Diagnostics and therapeutics for diseases associated with mosaic serine protease (msp) | 20060292155 | 20061228 |
| The invention provides a human MSP which is associated with the cardiovascular diseases, endocrinological diseases, metabolic diseases, cancer, inflammation, gastroenterological diseases, hematological diseases, respiratory diseases, neurological diseases, urological diseases and reproduction disorders. The invention also provides assays for the identification of compounds useful in the treatment or prevention of cardiovascular diseases, endocrinological diseases, metabolic diseases, cancer, inflammation, gastroenterological diseases, hematological diseases, respiratory diseases, neurological diseases, urological diseases and reproduction disorders. The invention also features compounds which bind to and/or activate or inhibit the activity of MSP as well as pharmaceutical compositions comprising such compounds.
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| Interferon-beta gene therapy using an improved, regulated expression system | 20060292609 | 20061228 |
| The present invention provides an improved, expression system for the regulated expression of an encoded protein or nucleic acid therapeutic molecule in the cells of a subject, for use in the treatment of disease. In particular, the present invention provides an improved, regulated gene expression system, and pharmaceutical compositions and uses thereof for treatment of disease.
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| Recognition molecules for the treatment and detection of tumours | 20060292643 | 20061228 |
| The invention relates to recognition molecules directed towards tumors, and it also relates to pharmaceutical compositions comprising said recognition molecules, methods for the production of said recognition molecules, and to the use of said recognition molecules in the diagnosis and therapy of tumor diseases.
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| Pharmaceutical compositions comprising an active agent and chitosan for sustained drug release or mucoadhesion | 20060293216 | 20061228 |
| The invention provides a pharmaceutical composition comprising a physiologically active agent and a release sustaining or mucoadhesive agent, characterized in that said release sustaining or mucoadhesive agent comprises a chitosan having a FA of from 0.25 to 0.80.
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| Pharmaceutical formulations for sustained release | 20060293217 | 20061228 |
| Sustained delivery pharmaceutical compositions comprising a solid ionic complex of a pharmaceutically active compound and an ionic macromolecule are provided by the present invention. The pharmaceutical compositions of the invention allow for loading of high concentrations of pharmaceutically active compounds and for delivery of a pharmaceutically active compound for prolonged periods of time, e.g., one month, after administration. Methods for preparing these pharmaceutical compositions, as well as methods of using them to treat a subject are also provided.
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| Inactivation resistant factor viii | 20060293238 | 20061228 |
| The present invention provides novel purified and isolated nucleic acid sequences encoding procoagulant-active FVIII proteins. The nucleic acid sequences of the present invention encode amino acid sequences corresponding to known human FVIII sequences, wherein residue Phe309 is mutated. The nucleic acid sequences of the present invention also encode amino acid sequences corresponding to known human FVIII sequences, wherein the APC cleavage sites, Arg336 and Ile562, are mutated. The nucleic acid sequences of the present invention further encode amino acid sequences corresponding to known human FVIII sequences, wherein the B-domain is deleted, the von Willebrand factor binding site is deleted, a thrombin cleavage site is mutated, an amino acid sequence spacer is inserted between the A2- and A3-domains. Methods of producing the FVIII proteins of the invention,... |
| Human sef isoforms and methods of using same for cancer diagnosis and gene therapy | 20060293240 | 20061228 |
| A method and pharmaceutical compositions useful for inhibiting the growth of solid tumors are provided. Specifically, the method is effected by administering to a subject in need thereof an agent capable of upregulating the expression level and/or activity of at least a functional portion of Sef, wherein the functional portion being capable of inhibiting RTK-mediated cell proliferation. Also provided are methods and kits for diagnosing and staging of cancer by detecting the expression level of hSef in a tissue sample, wherein a decrease in hSef expression level is indicative of cancer.
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| Stable, buffered, pharmaceutical compositions including motilin-like peptides | 20060293243 | 20061228 |
| Stable, pharmaceutical compositions including a synthetic motilin-like peptide in a buffered solution are disclosed. The composition provides for a peptide that remains stable and substantially retains its initial potency during extended storage and after steam sterilization.
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| Anti-inflammatory compounds and uses thereof | 20060293244 | 20061228 |
| The present invention provides anti-inflammatory compounds, pharmaceutical compositions thereof, and methods of use thereof for treating inflammatory disorders. The present invention also provides methods of identifying anti-inflammatory compounds and methods of inhibiting NF-κB-dependent target gene expression in a cell.
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| N²-quinoline or isoquinoline substituted purine derivatives | 20060293274 | 20061228 |
| wherein W represents a hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C3-6 cycloalkyl, or an optionally substituted C1-6 haloalkyl, Y represents a hydrogen, or a saccharide, Q represents a quinoline or isoquinoline. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same.
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| Salmeterol and ciclesonide combination | 20060293293 | 20061228 |
| The invention relates to pharmaceutical compositions containing combinations of salmeterol and ciclesonide and the use of such pharmaceutical compositions in medicine, in particular, the prophylaxis and treatment of respiratory disease.
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| Oxazolidinone derivatives as antimicrobials | 20060293307 | 20061228 |
| The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
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| Pyridyl derivatives and their use as therapeutic agents | 20060293308 | 20061228 |
| Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein W, V, x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
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| Intermediates of novel heterocyclic compounds having antibacterial activity and process for their preparation | 20060293315 | 20061228 |
| The present invention also relates to a process for the preparation of the above said novel compounds, their stereoisomers, their salts and pharmaceutical compositions.
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| Therapeutic amides | 20060293333 | 20061228 |
| wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.
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| P2x7 receptor antagonists and their use | 20060293337 | 20061228 |
| The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
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| Biaryl substituted 6-membered heterocycles as sodium channel blockers | 20060293339 | 20061228 |
| Biaryl substituted pyridine, pyrimidine and pyrazine compounds are sodium channel blockers useful for the treatment of pain. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
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| Tie-2 modulators and methods of use | 20060293342 | 20061228 |
| The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
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| Therapeutic compounds | 20060293344 | 20061228 |
| pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
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| Pyrimidine derivatives and their use as cb2 modulators | 20060293354 | 20061228 |
| The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
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| Niacin receptor agonists, compositions containing such compounds and methods of treatment | 20060293364 | 20061228 |
| as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
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| Benzopyran derivatives substituted with a benzimidazole derviative, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them | 20060293376 | 20061228 |
| The present invention relates to benzopyran derivatives substituted with a benzimidazole derivative, or pharmaceutically acceptable salts thereof, a preparation method of the same and pharmarceutical compositions containing them. Benzopyran derivatives substituted with a benzimidazole derivative, represented in Formula (1), have the function of protecting heart from ischemia-reperfusion without side effect like vasodilation, so that a pharmaceutical composition containing benzopyran derivatives substituted with a benzimidazole derivative or pharmaceutically acceptable salts thereof of the present invention as an effective ingredient can be effectively used for the protection of tissues influenced by ischemia-reperfusion, for example, for the protection of heart, nervous cells, brain, retinal cells, storage organs, etc. and for the treatment of diseases caused by ischemia-reperfusion.
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| Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease | 20060293380 | 20061228 |
| which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
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| Fungicidal effect by regulating signal transduction pathways | 20060293381 | 20061228 |
| The present invention concerns methods of treating fungal infections and methods of screening compounds for activity in treating fungal infections. Methods of the invention include using an active compound such as fludioxonil to treat a Cryptococcus neoformans infection. Also included are methods and pharmaceutical compositions useful for treating fungal infections using a Hog1 activator such as fludioxonil and a calcineurin inhibitor in combination.
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| Benzamide derivatives and uses related thereto | 20060293392 | 20061228 |
| wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.
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| Methods for treating a mammal before, during and after cardiac arrest | 20060293395 | 20061228 |
| Methods for treating mammals before, during and after cardiac arrest are disclosed. Pharmaceutical compositions comprising levosimendan useful for such treatment also are disclosed.
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