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This page is updated frequently with new Antagonist-related patent applications. Subscribe to the Antagonist RSS feed to automatically get the update: related Antagonist RSS feeds. RSS updates for this page: Antagonist RSS RSS


Date/App# patent app List of recent Antagonist-related patents
11/13/14
20140336383
 Prolyl hydroxylase inhibitors patent thumbnailProlyl hydroxylase inhibitors
Which are antagonists of hif prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.. .
11/13/14
20140336381
 Fast-dissociating dopamine 2 receptor antagonists patent thumbnailFast-dissociating dopamine 2 receptor antagonists
The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects..
11/13/14
20140336374
 Process and intermediates for the production of ccr2 antagonists patent thumbnailProcess and intermediates for the production of ccr2 antagonists
The present invention relates to a process for the production of novel antagonists for ccr2 (cc chemokine receptor 2) and intermediates thereof.. .
11/13/14
20140336365
 Cdr regions of monoclonal antibody that antagonize sphinogosine 1-phosphate and related methods patent thumbnailCdr regions of monoclonal antibody that antagonize sphinogosine 1-phosphate and related methods
Materials and method for treating cancer and screening for anti-neoplastic agents are provided. These materials and methods can include sphingosine 1-phosphate antagonists that bind to sphingosine-1 phosphate receptor subtype 3.
11/13/14
20140336266
 Method for administering an nmda receptor antagonist to a subject patent thumbnailMethod for administering an nmda receptor antagonist to a subject
Compositions and methods for administering memantine to a subject are provided. In particular, a solid pharmaceutical composition in a unit dosage form for once daily oral administration is provided.
11/13/14
20140336258
 Anti-virulence compositions and methods patent thumbnailAnti-virulence compositions and methods
A method of reducing the virulence of a bacterium that expresses accessory gene regulator a (agra) includes administering to the bacterium an amount of agra antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.. .
11/13/14
20140336224
 Mineralocorticoid receptor antagonists patent thumbnailMineralocorticoid receptor antagonists
Compounds of the formula (i) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the formula (i), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the formula (i) are disclosed..
11/13/14
20140336212
 Combination analgesic employing opioid agonist and neutral antagonist patent thumbnailCombination analgesic employing opioid agonist and neutral antagonist
In some embodiments, the invention provides a non-addictive analgesic co-formulation comprising an opioid agonist in an amount sufficient to confer analgesia in a mammalian subject (such as a human) and a neutral opioid antagonist in an amount sufficient to inhibit peripheral effects of the opioid agonist, and insufficient to block substantial central effects of the opioid agonist in the subject. The formulation may be formulated for oral administration to the subject.
11/13/14
20140336183
 Compositions and method for treatment of ischemic neuronal reperfusion injury patent thumbnailCompositions and method for treatment of ischemic neuronal reperfusion injury
A method and composition for the treatment of ischemic neuronal reperfusion injury are provided. The composition may include at least a benzodiazepine class material.
11/13/14
20140336172
 Novel 2h-indazoles as ep2 receptor antagonists patent thumbnailNovel 2h-indazoles as ep2 receptor antagonists
The present invention relates to novel 2h-indazoles of the general formula (i), methods for the preparation thereof and the use thereof for the production of pharmaceutical agents for the treatment of diseases and indications which are linked with the ep2-receptor.. .
11/13/14
20140336158
Nk1 antagonists
Wherein ar1 and ar2 are optionally substituted phenyl or heteroaryl, x1 is an ether, thio or imino linkage, r4 and r5 are not both h or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions.
11/13/14
20140336142
Method for treatment of macular degeneration by modulating p2y12 or p2x7 receptors
Provided is a method of treating or preventing age-related macular degeneration (amd) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal ph (phl), or acidifying an abnormally elevated phl, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (rpe) cells of the eye of the patient. Further, this method is achieved by modulating the action of the p2x7 and/or p2y12 receptors of the rpe cells, specifically decreasing the acidity (phl) of the rpe lysosomes by administering selected receptor antagonists affecting the action of the p2x7 and/or p2y12 receptors of the rpe.
11/13/14
20140336117
Modified receptor fusion proteins
We disclose growth hormone fusion proteins that have increased in vivo stability and activity; nucleic acid molecules encoding said proteins and methods of treatment of growth hormone related diseases that would benefit from growth hormone agonists or antagonists.. .
11/13/14
20140335190
New non-abusable pharmaceutical composition comprising opioids
There is provided pharmaceutical compositions for the treatment of pain comprising a pharmacologically-effective amount of an opioid analgesic, or a pharmaceutically-acceptable salt thereof, presented in particulate form upon the surfaces of carrier particles comprising a pharmacologically-effective amount of an opioid antagonist, or a pharmaceutically-acceptable salt thereof, which carrier particles are larger in size than the particles of the opioid analgesic. The compositions are also useful in prevention of opioid abuse by addicts..
11/13/14
20140335105
Methods of generating hyper inos expressing cells and uses thereof
A method of generating a hyper inos expressing cell includes administering to a myeloid derived cell an amount of a pparγ agonist and an il-6/stat3 signaling pathway antagonist effective to substantially inhibit stat3 activation in the cell and administering an inflammatory insult to the cell to stimulate hyper inos expression from the cell.. .
11/13/14
20140335077
Compositions and methods for the treatment of cancer using igf-ir antagonists and mapk/erk inhibitors
The present invention relates generally to the field of cancer therapy. More specifically the present invention relates a combination therapy where igf-1r antagonists are combined with mapk/erk pathway inhibitors.
11/06/14
20140331362
Dominant negative mutant krp protein protection of active cyclin-cdk complex inhibition by wild-type krp
Disclosed are mutant cdk inhibitor (cki) polypeptides having dominant negative antagonist activity against wild-type cki proteins, as well as related compositions, including nucleic acids and vectors encoding the mutant cki polypeptides and transformed host cells and transgenic plants comprising such nucleic acids and vectors. Also disclosed are related methods for using the mutant proteins to modulate cell division in cells, particularly plant cells..
11/06/14
20140329862
Glucagon receptor modulators
Or a pharmaceutically acceptable salt thereof wherein r1, r2, r3, a1, a2, a3, a4, l, b1, b2, b3 and b4 are as defined herein. The compounds of formula i have been found to act as glucagon antagonists or inverse agonists.
11/06/14
20140329858
Cyclic urea derivatives as androgen receptor antagonists
The present invention is directed to compounds of formula (i) wherein r1, r2, r3, and a are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (i) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer..
11/06/14
20140329857
Quaternary ammonium compounds useful as muscarinic receptor antagonists
In salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein r1-6, a, z and q are as defined in the specification. These compounds are muscarinic receptor antagonists.
11/06/14
20140329846
Morphinan compounds
This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has nmda antagonist activity..
11/06/14
20140329845
3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists
Wherein r1, r2, r3, r4, r5, and r6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds..
11/06/14
20140329844
Method of restoring the incretin effect
The present invention relates to methods of treating metabolic syndrome, type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion.
11/06/14
20140329829
Trpv1 antagonists including dihydroxy substituent and uses thereof
And pharmaceutically acceptable derivatives thereof, where r1, r4, r8, r9, and m are as defined herein, compositions comprising an effective amount of a compound of formula (i) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, ui, an ulcer, ibd, and ibs, comprising administering to an animal in need thereof an effective amount of a compound of formula (i) or a pharmaceutically acceptable derivative thereof.. .
11/06/14
20140329811
Methods of modulating cell proliferation and cyst formation in polycystic kidney and liver diseases
The present invention provides a method for preferentially reducing the proliferation of cystic epithelial cells in the kidney or bile duct in a mammal in need thereof by administering a 20-hete synthesizing enzyme inhibitor or a 20-hete antagonist to the mammal in an amount sufficient to preferentially reduce the proliferation of cystic epithelial cells over normal epithelial cells such as tubule epithelial cells in the kidney or bile duct. The present invention also provides a method for preventing or treating autosomal dominant polycystic kidney disease (adpkd), autosomal recessive polycystic kidney disease (arpkd), arpkd associated congenital hepatic fibrosis, arpkd associated caroli's disease, or cholangiocarcinoma in a mammal in need thereof by administering a 20-hete synthesizing enzyme inhibitor or a 20-hete antagonist to the mammal in an amount sufficient to prevent or treat the disease..
11/06/14
20140329759
Polyethylene glycol-modified integrin blocker hm-3 and use thereof
The present invention involves the pharmaceutical field, including integrin antagonists, which have the capacities of inhibiting angiogenesis of tumors, binding integrin. These antagonists are a kind of polypeptide, which was modified by polyethylene glycol and after modification, it can be used to treat tumors.
11/06/14
20140329752
Peptide antagonists of the calcitonin cgrp family of peptide hormones and their use
The embodiments provide a modified calcitonin gene-related peptide antagonist including an n-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the n-terminal fragment are cysteine (cys) and at least one amino acid comprises a non-threonine substitution of a threonine (thr) residue; a central core where the central core comprises an oc-helix; and a c-terminal fragment of modified calcitonin gene-related peptide or related protein family member comprising a c-terminal amide and where at least one amino acid of the c-terminal fragment is phenylalanine (phe), proline (pro), tyrosine (tyr) or hydroxyproline (hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition..
11/06/14
20140328930
Pharmaceutical compositions
Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided..
11/06/14
20140328861
Combination of crth2 antagonist and a proton pump inhibitor for the treatment of eosinophilic esophagitis
Disclosed are methods and compositions for preventing, treating, or ameliorating eosinophilic esophagitis (eoe) in an individual, comprising administering to the individual a therapeutically effective amount of at least one crth2 antagonist or a pharmaceutically acceptable salt thereof and at least one proton pump inhibitor (ppi) or a pharmaceutically acceptable salt thereof. Also disclosed are compositions comprising at least one crth2 antagonist or a pharmaceutically acceptable salt thereof and at least one proton pump inhibitor or a pharmaceutically acceptable salt thereof..
11/06/14
20140328845
Methods for increasing thermogenic adipocytes
In certain aspects, the present invention provides compositions and methods for increasing thermogenic adipocytes (e.g., brown adipocytes or other ucp-1 expressing adipocytes) by administering an antagonist of an actriib signaling pathway. Examples of such antagonists include actriib polypeptides, anti-actriib antibodies, anti-myostatin antibodies, anti-gdf3 antibodies, anti-noda1, anti-activin, and anti-gdf11 antibodies.
10/30/14
20140323983
Vegf antagonist formulations for intravitreal administration
Ophthalmic formulations of a vascular endothelial growth factor (vegf)-specific fusion protein antagonist are provided suitable for intravitreal administration to the eye. The ophthalmic formulations include a stable liquid formulation and a lyophilizable formulation.
10/30/14
20140323733
Diamide compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
Or a pharmaceutically acceptable salt thereof. Such compounds possess both muscarinic receptor antagonist and β2 adrenergic receptor agonist activities.
10/30/14
20140323594
Methods and compositions for diagnosis and prognosis of renal injury and renal failure
The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in subjects suffering from or suspected of having a renal injury. In particular, the invention relates to using assays that detect one or more markers selected from the group consisting of cytoplasmic aspartate aminotransferase, soluble tumor necrosis factor receptor superfamily member 5, soluble cd40 ligand, soluble c-x-c motif chemokine 16, s100-a12, eotaxin, soluble e-selectin, fibronectin, granulocyte colony-stimulating factor, granulocyte-macrophage colony-stimulating factor, heparin-binding growth factor 2, soluble hepatocyte growth factor receptor, interleukin-1 receptor antagonist, interleukin-1 beta, interleukin-10, interleukin-15, interleukin-3, myeloperoxidase, nidogen-1, soluble oxidized low-density lipoprotein receptor 1, pappalysin-1, soluble p-selectin glycoprotein ligand 1, antileukoproteinase, soluble kit ligand, tissue inhibitor of metalloproteinase 1, tissue inhibitor of metalloproteinase 2, soluble tumor necrosis factor, soluble vascular cell adhesion molecule 1, and vascular endothelial growth factor a as diagnostic and prognostic biomarkers in renal injuries..
10/30/14
20140323535
5-oxo-ete receptor antagonist compounds
The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ete receptors, such as the oxe receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases.
10/30/14
20140323499
Oxazolone and pyrrolidinone-substituted arylamides as p2x3 and p2x2/3 antagonists
Or a pharmaceutically acceptable salt thereof, wherein, x, y, r1, r2, r3, r4, r5, r6 and r7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with p2x3 and/or a p2x2/3 receptor antagonists and methods of making the compounds..
10/30/14
20140323492
Ccr2 receptor antagonists
The present invention relates to novel antagonists for ccr2 (cc chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and copd.. .
10/30/14
20140323487
Novel compounds as antagonists or inverse agonists at opioid receptors
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.. .
10/30/14
20140323426
Use of opioid antagonists to attenuate endothelial cell proliferation and migration
The invention provides methods of attenuating, e.g., inhibiting or reducing, cellular proliferation and migration, particularly endothelial cell proliferation and migration, including that associated with angiogenesis, using opioid antagonists, including, but not limited to, those that are peripherally restricted antagonists.. .
10/30/14
20140323399
Compositions and methods for increasing insulin sensitivity
Methods and compositions for treating a blood glucose condition involve identifying a suitable subject and administering an effective amount of a composition that contains one or more of an opioid antagonist, an anticonvulsant, and a psychotherapeutic agent. The compositions can include insulin.
10/30/14
20140323348
Expression of g-protein coupled receptors (gpcrs)
Disclosed are methods of promoting and/or enhancing g-protein coupled receptor (gpcr) localization to the cell membrane and/or cell surface; methods of promoting and/or enhancing gpcr functional expression; and methods and assays for screening or identifying ligands (e.g., agonists or antagonists) that bind gpcrs. Also provided are vectors, recombinant cells, and stable cell lines for use in the methods and assays..
10/30/14
20140322366
Htrpa1-activating composition and use thereof
A coniferyl alcohol or a compositae family, brassicaceae family, umbelliferae family, lamiaceae family, liliaceae family or amaranthaceae plant extract provides various uses associated with htrpa1 activation, and, being a natural compound, involves relatively few side effects in the body and has substantial industrial applicability. The coniferyl alcohol or the compositae family, brassicaceae family, umbelliferae family, lamiaceae family, liliaceae family or amaranthaceae plant extract of the present invention not only will be a novel medical or food raw material which is helpful in maintaining homeostasis in the body associated with htrpa1 activation, but can also be used to advantage in htrpa1 antagonist screening..
10/30/14
20140322332
Antagonists of muc1
The present invention is directed to improved compositions for cellular delivery of peptides. Using segments of only 3-5 positively-charged residues, one can effectively transfer peptides, including therapeutic peptides, into cells.
10/30/14
20140322313
Pharmaceutical compositions of ibuprofen and an h2 receptor antagonist
Pharmaceutical compositions of a h2 receptor antagonist and ibuprofen are provided herein. The compositions comprise, e.g., a core and a shell separated by a barrier layer, bilayered or trilayered compositions, or liquid formulations.
10/30/14
20140322238
Il-17ra-il-17rb antagonists and uses thereof
The present invention relates to interleukin-17 ligand and receptor family members and the discovery that il-17 receptor a and il-17 receptor c form a heteromeric receptor complex that is biologically active. Antagonists of the il-17ra-il-17rb heteromeric receptor complex are disclosed, as well as various methods of use..
10/30/14
20140322222
Compounds and methods for the modulation of beta-1 integrin function to mediate tissue repair
The present invention provides methods and compositions that modulate beta 1 integrin activity by functioning as allosteric antagonists. In particular, the present invention provides methods for mediating tissue repair where insult or injury has occurred by antagonising the allosteric function of beta 1 integrin..
10/30/14
20140322215
Methods of inhibiting tumor growth by antagonizing il-6 receptor
The present invention provides methods for inhibiting or attenuating tumor growth in a subject by administering an il-6 antagonist to the subject. In certain embodiments, the methods of the invention are used to inhibit the growth of an anti-vegf-resistant tumor in a subject.
10/30/14
20140322131
Methods and agents for the diagnosis and treatment of hepatocellular carcinoma
The present invention relates to methods of diagnosing and methods of treating hepatocellular carcinoma in a subject. The invention also relates to antagonists of plvap proteins, such as antibodies that specifically bind plvap proteins, as well as compositions and kits comprising antagonists of plvap proteins.
10/23/14
20140316575
Robot device, robot control method, program, and recording medium
A joint torque computing unit computes a joint torque t1 of a joint necessary to move a joint angle to a target joint angle. A summing unit obtains a sum value u1 indicating the sum of generated forces generated at actuators, from a target stiffness.
10/23/14
20140316142
Process for the preparation of angiotensin ii antagonists and intermediates thereof
Preferably a phosphite salt of formula-4′.h3po3. .
10/23/14
20140315957
Androgen receptor antagonists and uses thereof
The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism.. .
10/23/14
20140315940
Morphinan compounds
This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has nmda antagonist activity..
10/23/14
20140315932
Quinazolinone derivatives useful as vanilloid antagonists
The present specification relates to the use of a quinazolinone compound of the formula (i) wherein r1, r2, r3, r4, r5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form.. .
10/23/14
20140315922
Method of treating parkinson's disease with a diarylmethylpiperazine compounds exhibiting delta opioid receptor agonist activity
Compositions and methods for treatment of parkinson's disease to reduce the negative side effects of the disease by administering a therapeutically effective diarylmethylpiperazine compound which exhibits delta opioid receptor agonist activity, and optionally, mu receptor antagonist activity.. .
10/23/14
20140315900
Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a dihydropyrazino-pyrazine compound and an effective amount of an androgen receptor antagonist to a patient having a cancer.. .
10/23/14
20140315877
Nicotinic receptor non-competitive antagonists
The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.. .
10/23/14
20140315866
Methods and compositions related to glucocorticoid receptor antagonists and breast cancer
Embodiments of the invention are directed to methods of determining the prognosis of a breast cancer patient by evaluating the activity of the glucocorticoid receptor in tumor cells. Other embodiment include methods of treating breast cancer cells, particularly, chemo-resistant cells, with a glucocorticoid receptor antagonist and an anticancer agent or compound..
10/23/14
20140315741
Methods and materials for modulating deubiquitinases and ubiquitinated polypeptides
This document relates to methods and materials involved in modulating deubiquitinases (e.g., usp10 polypeptides) and/or ubiquitinated polypeptides (e.g., tumor suppressor polypeptides or mutant versions of tumor suppressor polypeptides). For example, methods and materials for increasing deubiquitinase (e.g., a usp10 polypeptide) expression or activity, methods and materials for decreasing deubiquitinase (e.g., a usp10 polypeptide) expression or activity, methods and materials for stabilizing tumor suppressor polypeptides (e.g., wild-type p53 polypeptides), methods and materials for de-stabilizing mutant versions of tumor suppressor polypeptides (e.g., mutant p53 polypeptides), and methods and materials for reducing cancer cell proliferation, increasing cancer cell apoptosis, and/or treating cancer (e.g., cancers having reduced levels of wild-type p53 polypeptides or cancers having increased levels of mutant p53 polypeptides) are provided.
10/23/14
20140315250
Humanized antibodies against tl1a
Disclosed are humanized antibodies that bind specifically to tnf superfamily member 15 (tnfsf15), also known as tl1a. Methods of making and using the anti-tl1a antibodies are also described.
10/23/14
20140314767
Methods for treating visceral pain by administering antagonist antibodies directed against calcitonin gene-related peptide
The invention features methods for preventing or treating visceral pain, including pain associated with functional bowel disorder, inflammatory bowel disease and interstitial cystitis, by administering an anti-cgrp antagonist antibody.. .
10/23/14
20140314744
Mcam antagonists and methods of treatment
Described herein are mcam antagonists, including mcam antagonist antibodies capable of inhibiting the interaction between mcam and it ligand, a laminin α4 chain, e.g., an α4 chain of laminin 411. These mcam antagonists, e.g., anti-mcam antibodies, may be useful to treat neuroinflammatory conditions, for example, multiple sclerosis and parkinson's disease, by inhibiting the infiltration of mcam-expressing cells into the central nervous system (cns), e.g., extravasation of th17 cells into the cns..
10/23/14
20140314669
Compounds for binding to the platelet specific glycoprotein iib/iiia and their use for imaging of thrombi
The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (pet) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body.
10/23/14
20140314665
Nanoparticle and polymer formulations for thyroid hormone analogs, antagonists, and formulations thereof
Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric nanoparticle form of thyroid hormone agonist, partial agonist or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed..
10/16/14
20140309311
Pharmaceutical combination
A pharmaceutical combination comprising as components (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and (b) at least one nmda-antagonist, a pharmaceutical formulation and a dosage form comprising such a combination, and a method of treating pain, e.g. Inflammatory pain or neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, with component (a) being administered either before or after component (b), and with components (a) or (b) being administered to the mammal either via the same pathway of administration or via different pathways of administration..
10/16/14
20140309254
Pyrrolopyridine derivatives and their use as crth2 antagonists
In free or salt form, wherein r1, r2, r3, r4, r5, r6, q, w, x, m, n and p are as described in the specification, process for preparing them, and their use as pharmaceuticals.. .
10/16/14
20140309252
Compositions and methods for reducing food cravings
Disclosed are compositions for reducing food cravings, comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound is an α-msh agonist. Also disclosed are methods of reducing food cravings, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-msh activity..
10/16/14
20140309251
Spirothienopyran-piperidine derivatives as orl-1 receptor antagonists for their use in the treatment of alcohol dependence and abuse
For the treatment of alcohol use disorders is described.. .
10/16/14
20140309227
Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2-negative allosteric modulators, compositions, and their use
The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (i) wherein ring a, rq, -l-, r1, n, r2, and r3 are as defined herein. The compounds of the invention are useful as non-competitive mglur2 antagonists, or mglur2 negative allosteric modulators (nams), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mglur2-nam receptor is involved, such as alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.


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Antagonist topics: Antagonist, Recurrence, Proliferative Disorder, Proliferative, Antibodies, Progesterone, Dicyclomine, Scopolamine, Extracellular, Pharmaceutically Acceptable Salt, Metalloprotein, Nucleic Acids, Polynucleotide, Nucleic Acid, Monoclonal

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