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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
01/29/15
20150031897
 Combined acetylcholinesterase inhibitor and quaternary ammonium antimuscarinic therapy to alter progression of cognitive diseases patent thumbnailnew patent Combined acetylcholinesterase inhibitor and quaternary ammonium antimuscarinic therapy to alter progression of cognitive diseases
A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression.
01/29/15
20150031893
 An h3 receptor antagonist for use in the treatment of alzheimer's disease patent thumbnailnew patent An h3 receptor antagonist for use in the treatment of alzheimer's disease
This disclosure relates to methods of using 2-(cyclohexylmethyl)-n-{2-[(2s)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide in a disease modifying therapy of alzheimer's disease, other tauopathies and related neurodegenerative diseases.. .
Sanofi
01/29/15
20150031728
 Cyclooxygenase inhibitor and calcium channel antagonist compositions and methods for use in urological procedures patent thumbnailnew patent Cyclooxygenase inhibitor and calcium channel antagonist compositions and methods for use in urological procedures
Compositions of a cyclooxygenase inhibitor and a calcium channel antagonist in a liquid carrier. The composition may be administered the urinary tract during urological diagnostic, interventional, surgical and other medical procedures.
Omeros Corporation
01/29/15
20150031718
 Pharmaceutical formulation containing opioid agonist, opioid antagonist and gelling agent patent thumbnailnew patent Pharmaceutical formulation containing opioid agonist, opioid antagonist and gelling agent
Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.. .
Purdue Pharmaceuticals L.p.
01/29/15
20150031716
 Piperidinone carboxamide azaindane cgrp receptor antagonists patent thumbnailnew patent Piperidinone carboxamide azaindane cgrp receptor antagonists
The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of cgrp receptors and 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..
Merck Sharp & Dohme Corp.
01/29/15
20150031715
 Integrin antagonist conjugates for targeted delivery to cells expressing vla-4 patent thumbnailnew patent Integrin antagonist conjugates for targeted delivery to cells expressing vla-4
The invention relates to compounds of formula i: wherein r1, r2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula i for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to vla-4 integrin antagonists to target cells expressing vla-4..
Hoffmann-la Roche Inc.
01/29/15
20150031705
 Ophthalmic formulations including selective alpha 1 antagonists patent thumbnailnew patent Ophthalmic formulations including selective alpha 1 antagonists
Ophthalmic formulations are provided. The ophthalmic formulations include one or more active agents that act to optimize pupil light reflex while minimizing, or effectively eliminating, any undesired eye redness in response to application thereof.
Ocularis Pharma, Llc
01/29/15
20150031689
 Peripherally restricted diphenyl purine derivatives patent thumbnailnew patent Peripherally restricted diphenyl purine derivatives
The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.. .
Research Triangle Institute
01/29/15
20150031688
 Compositions of dual thyrointegrin antagonists and use in vascular-associated disorders patent thumbnailnew patent Compositions of dual thyrointegrin antagonists and use in vascular-associated disorders
A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and αvβ3 integrin antagonist in the same molecule..
Vascular Vision Pharmaceutical Company
01/29/15
20150031605
 Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof patent thumbnailnew patent Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof
The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin o-acyltransferase (goat) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (vii): a11-a12-a13-gly-ser-a14-phe-leu-a15-a16-a17-a18, wherein each of a11, a12, and a13 is independently absent, an amino acid, or an amino protecting group; each of a15, a16, a17, and a18 is independently absent or an amino acid; and a14 is a serine conjugated with a —c(o)c1-c20alky or a diaminopropionic acid conjugated with a —c(o)c1-c20alkyl group, provided that at least one of a11, a12, or a13 is present..
The Administrators Of The Tulane Educational Fund
01/29/15
20150031083
new patent

Adenoviral-based biological delivery and expression system for use in the treatment of osteoarthritis


The invention relates to an adenoviral-based biological delivery and expression system for use in the treatment or prevention of osteoathritis in human or mammalian joints by long-term inducible gene expression of human or mammalian interleukin-1 receptor antagonist (il-1ra) in synovial cells, comprising a helper-dependent adenoviral vector containing a nucleic acid sequence encoding for human or mammalian interleukin-1 receptor antagonist (il-1ra), left and right inverted terminal repeats (l itr and r itr), the adenoviral packaging signal and non-viral, non-coding stuffer nucleic acid sequences, wherein the expression of the human or mammalian interleukin-1 receptor antagonist (il-1ra) gene within synovial cells is regulated by an inflammation-inducible promoter.. .
Baylor College Of Medicine
01/29/15
20150030561
new patent

Use of cxcr4 antagonists


Presently disclosed are methods and compositions for treating or preventing whim syndrome and certain other disorders or conditions with a certain cxcr4 antagonist.. .
University Of Washington Center For Commercialization
01/22/15
20150025237

Methods and compounds useful in the synthesis of orexin-2 receptor antagonists


The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.. .
Eisai R&r Management Co. Ltd.
01/22/15
20150025224

Antagonists of neuropilin receptor function and use thereof


The present invention relates to antagonists of neuropilin receptor function and use thereof in the treatment of cancer, particularly metastatic cancer, and angiogenic diseases.. .
Children's Medical Center Corporation
01/22/15
20150025223

System and producing interleukin receptor antagonist (ira)


The present invention relates to a system and method for producing high levels of autologous il-1ra cytokine, comprising: a blood collection vessel (1), a cover (4), a portion of separation gel (2), an anticoagulant portion (3), a plasma collection syringe comprising a sharp needle (9), a buffy coat collection syringe (11) and an incubation tube with cover (15). The vessel is adapted such that, when containing the whole blood (5), and centrifuged after treatment, yields separation fractions comprising, a first fraction of rbcs sediment (6), a second fraction of said gel (2), a third fraction comprising wbcs, platelets and), and fourth fraction of plasma solution (8)..
Estar Technologies Ltd
01/22/15
20150025153

Small molecule cmklr1 antagonists in demyelinating disease


Compounds and methods are provided for decreasing demyelinating inflammatory disease in a subject by inhibiting the activity of chemokine-like receptor 1 (cmklr1). In some embodiments such methods include treating demyelinating inflammatory disease in a subject by administering an agent that antagonizes the activity of chemokine-like receptor 1 (cmklr1) and/or a cmklr1 ligand (e.g., chemerin or other endogenous cmklr1 ligands).
The Board Of Trustees Of The Leland Stanford Junior University
01/22/15
20150025101

Opioid agonist/antagonist combinations


The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome)..
Purdue Pharma L.p.
01/22/15
20150025075

Heterocyclic amide derivatives as p2x7 receptor antagonists


Wherein r1, r2, r3, x and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.. .
01/22/15
20150025064

Novel benzodiazepinones as modulators of metabotropic glutamate receptor functions and neurological uses thereof


Wherein r1, r2, r4, r6, r7, r8, r9, and r10 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, methods of use of such compounds and compositions, and methods for preparing the compounds and compositions.
01/22/15
20150025061

Gabaa receptor antagonists affecting ganglion cell function and visual acuity


The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic gabaa receptor antagonist. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the extrasynaptic gabaa receptor antagonist..
Allergan, Inc.
01/22/15
20150025046

Preparation and use of bicyclic himbacine derivatives as par-1 receptor antagonists


The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: x is —o—, —n(r), —c(r8)(r9) or —c(o)—; and y is —o—, —n(r), —c(r8)(r9) or —c(o)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the par-1 receptor.
Merck Sharp & Dohme Corp.
01/22/15
20150025017

Compositions and methods for treating cancer


The present disclosure provides compositions and methods for treating cellular hyperproliferative disorders with a phf5α inhibitor, such as sirna, shrna, antisense oligonucleotides, or pharmaceutical compounds. Exemplary cellular hyperproliferative disorders that can be treated with the phf5α antagonists of the present disclosure include cancers, such as gliomas, adenocarcinomas, cervical cancer or prostate cancer..
Fred Hutchinson Cancer Research Center
01/22/15
20150025013

Compositions and methods of use for (pro)renin receptor


Disclosed are methods of treating kidney disease, infectious or inflammatory diseases, acute kidney injury and hypertension by administering a (pro)renin receptor (prr) antagonist. In some instances the prr antagonist is a polypeptide.
University Of Utah
01/22/15
20150024058

Pharmaceutical compositions for the deterrence and/or prevention of abuse


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..
Alpharma Pharmaceuticals Llc
01/22/15
20150023957

Saa domain-specific antibodies and peptide antagonists and use thereof to treat inflammatory diseases


Isolated saa peptides, fusion proteins and compositions comprising such are provided as are domain-specific saa antibodies. Methods of treating sepsis and endotoxemia are also provided..
The Feinstein Institute For Medical Research
01/15/15
20150018553

Processes for the preparation of uracil derivatives


The present invention relates to processes and intermediates for preparing gonadotropin-releasing hormone (gnrh) receptor antagonists of structure (vi); and stereoisomers and pharmaceutically acceptable salts thereof.. .
Neurocrine Biosciences, Inc.
01/15/15
20150018399

Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use


Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions.
Merck Sharp & Dohme Corp.
01/15/15
20150018366

Trpv1 antagonists including dihydroxy substituent and uses thereof


And pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula ia or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, ui, an ulcer, ibd and ibs, comprising administering to an animal in need thereof an effective amount of a compound of formula ia or a pharmaceutically acceptable derivative thereof.. .
01/15/15
20150018363

Benzimidazole derivatives as mch receptor antagonists


Wherein each symbol as defined in the specification, or a salt thereof.. .
01/15/15
20150018360

Compositions and methods for treating metabolic disorders


The present invention provides, inter alia, compositions containing enantiomerically pure (r)(+)-amisulpride or enantiomerically pure (r)(+)-sulpiride, optionally with dopamine receptor modulators. The present invention also provides compositions containing racemic (rs)-amisulpride or (rs)-sulpiride in combination with dopamine receptor modulators.
Biomed Valley Discoveries, Inc.
01/15/15
20150018345

Novel neurokinin 1 receptor antagonist compounds


The present invention relates to a compound according to formula (a) wherein n is 1 or 2; r1 and r2 are independently hydrogen, c1-4 alkyl, c1-4 haloalkyl, c1-4 alkoxy, cd3 or halogen; r3 is hydrogen, c(═o)or7 or c1-4 alkyl optionally substituted with hydroxy or nr8r9; r4 is hydrogen or oxo; r5 and r6 are independently hydrogen, hydroxy, nr8r9, c(═o)r7, c(═o)or7, c(═o)nr8r9, c1-4 alkyl, wherein said c1-4 alkyl is optionally substituted with hydroxy, nr8r9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with c1-4 alkyl or c(═o)r7; or r5 and r6, together with the carbon atom to which they are attached, form ═ch2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with c1-4 alkyl; r7 is hydrogen or c1-4 alkyl; r8 and r9 are independently hydrogen or c1-4 alkyl, or r8 and r9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments..
Leo Pharma A/s
01/15/15
20150018337

N-(2-(hetaryl)aryl)arylsulfonamides and n-(2-(hetaryl)hetaryl)arylsulfonamides


Compounds are provided that act as potent antagonists of the ccr9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for ccr9.
Chemocentryx, Inc.
01/15/15
20150018285

Antagonists of bcl-2 and uses thereof in induction of apoptosis


The present invention provides an antagonist of a bcl-2 pro survival protein containing a bh3-like domain. The antagonist of the invention comprises arts and any fragment or peptide that comprises a bh3-like domain.
Carmel-haifa University Economic Corporation Ltd.
01/15/15
20150017263

Fn14 antagonists and therapeutic uses thereof


The present disclosure is directed to methods of using fibroblast growth factor-inducible 14 (fn14) antagonists to modulate activity at a tnf-like weak inducer of apoptosis (tweak) binding site on a cysteine-rich domain (crd) of fn14. The present disclosure also provides pharmaceutical compositions comprising synergistic combinations fn14 antagonists and chemotherapeutic agents..
The Translational Genomics Research Institute
01/15/15
20150017247

Compositions for pulmonary delivery of long-acting b2 adrenergic receptor agonists and associated methods and systems


Compositions, methods and systems are provided for pulmonary delivery of long-acting muscarinic antagonists and long-acting β2 adrenergic receptor agonists via a metered dose inhaler. In particular embodiments, the compositions include a suspension medium, active agent particles, and suspending particles, in which the active agent particles and suspending particles form a co-suspension within the suspension medium..
Pearl Therapeutics, Inc.
01/15/15
20150017182

Methods for treating nasal polyposis by administering an il-4r antagonist


The present invention provides methods for treating nasal polyposis. The methods include administering to a subject in need thereof a therapeutic composition comprising an interleukin-4 receptor (il-4r) antagonist such as an anti-il-4r antibody or antigen binding fragment thereof..
Regeneron Pharmaceuticals, Inc.
01/15/15
20150017173

Antibodies to human transmembrane proteins


The invention provides human transmembrane proteins (htmpn) and polynucleotides which identify and encode htmpn. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists.
Incyte Corporation
01/15/15
20150017171

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 polypeptide antagonists of plvap proteins, including humanized and chimeric antibodies that specifically bind plvap proteins, as well as compositions and kits comprising such polypeptide antagonists..
China Synthetic Rubber Corporation
01/15/15
20150017164

Combination of blys and/or april inhibition and immunosuppressants for treatment of autoimmune disease


The invention relates to novel combination therapies involving blys or blys/april inhibition and immunosuppressants for the treatment of autoimmune diseases. One preferred method is where the blys and/or april antagonist is a fc-fusion protein which can be a taci-fc-fusion protein comprising the extracellular domain of taci or a functional fragment thereof, a baff-r-fc-fusion protein comprising the extracellular domain of baff-r or a functional fragment thereof, or a bcma-fc-fusion protein comprising the extracellular domain of bcma or a functional fragment thereof.
Ares Trading S.a.
01/15/15
20150017163

Methods for treating or preventing ophthalmological conditions


The present invention relates to methods for treating and preventing ophthalmological disease and disorders, comprising administering antagonist a or another pharmaceutically acceptable salt thereof, optionally in combination with another treatment, to a subject in need thereof. The present invention also relates to methods for treating and preventing ophthalmological disease and disorders, comprising administering an anti-c5 agent (e.g., arc1905), optionally in combination with another treatment, to a subject in need thereof..
Ophthotech Corporation
01/08/15
20150011597

Dual-acting antihypertensive agents


Wherein ar, r, r3, x, and r5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula i have at1 receptor antagonist activity and neprilysin inhibition activity.
01/08/15
20150011566

N-phenylpiperazine derivatives that are antagonists of a1a, a1d adrenoceptors and 5-ht1a receptors for the treatment of benign prostate hyperplasia, pharmaceutical compositions containing the same


The present invention provides n-phenylpiperazine derivatives for use as multiple binders and/or antagonists of α1a adrenoceptors, α1d adrenoceptors and 5-ht1a serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions..
UniÃo Brasiliense De EducaÇÃo E Cultura - Ubec
01/08/15
20150011560

Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3


The present invention relates to the treatment or prevention of skeletal disorders, in particular skeletal diseases, developed by patients that display abnormal increased activation of the fibroblast growth factor receptor 3 (fgfr3), in particular by expression of a constitutively activated mutant or fgfr3.. .
Institut National De La Sante Et De La Recherche Medicale (inserm)
01/08/15
20150011557

Benzyl piperidine compounds as lysophosphatidic acid (lpa) receptor antagonist


The invention provides novel substituted benzyl piperidine compounds according to formula (i) as lysophosphatidic acid (lpa) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.. .
Merck Patent Gmbh
01/08/15
20150011496

Methods and compositions for stimulating bone regeneration


The invention provides methods and compositions for stimulating or promoting bone regeneration or repairing bone fracture or for stimulating or increasing differentiation or activation of osteoblasts by administering to a subject a therapeutically effective amount of an adenosine receptor agonist, or an analog, derivative or combination thereof, an adenosine receptor antagonist, or an analog, derivative or combination thereof, or adenosine or a compound that upregulates, increases the amount of or increases the biological activity of adenosine. The invention also extends to pharmaceutical compositions such as those comprising an agent that modulates an adenosine receptor such as an adenosine a2a agonist or a1 antagonist..
New York University
01/08/15
20150011477

Ccr2 antagonist peptides


The invention relates to a peptide comprising the following amino acid sequence thr-phe-leu-lys or thr-phe-leu-lys-cys, useful as a ccr2 non competitive antagonist peptide.. .
Universite Pierre Et Marie Curie
01/08/15
20150010932

Methods for assaying protein-protein interactions


Provided herein is an assay for interrogating transient and dynamic protein-protein interactions and for screening and characterizing agents as agonists or antagonists of protein-protein interactions. The methods can provide a single assay for simultaneously assessing the bioavailability and efficacy of a test compound for increasing or decreasing a protein-protein interaction of interest..
Salk Institute For Biological Studies
01/08/15
20150010917

Method to identify ligands for sigma-1 receptors


An assay for identifying ligands of the σ1 receptor based on a fusion protein comprising the σ1 receptor flanked by two fluorophores, so that said fluorophores are capable of producing constitutive fret when no ligand is bound to the σ1 receptor. The fusion protein of the invention also allows the simultaneous determination whether the newly determined ligand is an agonist or an antagonist.
Laboratorios Del Dr. Esteve S.a.
01/08/15
20150010570

Methods and compositions for using mhc class ii invariant chain polypeptides as a receptor for macrophage migration inhibitory factor


Methods and compositions for using the mhc class ii invariant chain polypeptide, ii (also known as cd74), as a receptor for macrophage migration inhibitory factor (mif), are disclosed. These include methods and compositions for using this receptor, as well as agonists and antagonists of mif which bind to this receptor, or which otherwise modulate the interaction of mif with cd74 or the consequences of such interaction, in treatment of conditions characterized by locally or systemically altered mif levels, particularly inflammatory conditions and cancer..
Baxter Healthcare S.a.
01/08/15
20150010563

Methods for treating corneal and conjunctival inflammation and inflammatory disorders


Provided herein are methods for reducing corneal inflammation, reducing inflammatory cell (e.g., dendritic cell) recruitment to the cornea, and treating an corneal inflammatory disorder in a subject that include administering to the subject one or more of a madc am-1 antagonist, an α4β7 integrin antagonist, a l-selectin antagonist, and an e-selectin antagonist. Also provided are compositions containing one or more of a madc am-1 antagonist, an α4β7 integrin antagonist, a l-selectin antagonist, and an e-selectin antagonist, and kits containing these compositions..
Massachusetts Eye & Ear Infirmary
01/08/15
20150010554

Methods for treating interleukin-6 related diseases


A pharmaceutical composition for the treatment of interleukin-6 (il-6) related diseases, comprising an interleukin-6 antagonist (il-6 antagonist) and immunosuppressants. The il-6 antagonist is preferably an antibody to an interleukin-6 receptor (il-6r)..
Chugai Seiyaku Kabushiki Kaisha
01/08/15
20150010525

Catalytic tagging system to study macro-molecular interactions using engineered ubiquitin ligase and ubiquitin-like proteins to facilitate substrate identification


The present invention describes an unbiased catalytic tagging system to search for target substrates. Identification of substrates for specific baits is accomplished by utilizing an orthogonal system consisting of an e1 activating enzyme, an e2 ubiquitin-like conjugating enzyme, and baits that are fused to the e2 ubiquitin-like conjugating enzyme.
The Regents Of The University Of California
01/08/15
20150010503

Methods and compositions related to glucocorticoid receptor antagonism and prostate cancer


Methods are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity..
The University Of Chicago
01/08/15
20150010477

Method for the treatment of multiple sclerosis


A method for treating a subject with multiple sclerosis is disclosed herein. In one embodiment, a method is provided for treating a subject with multiple sclerosis that includes administering to the subject a therapeutically effective amount of an il-21 receptor antagonist, wherein the subject has failed to respond treatment with beta interferon, thereby treating the subject..
The Government Of The United States Of America As Represented By The Secretary Of The Department Of
01/01/15
20150005338

Ccr1 antagonists and methods of use thereof


Wherein r1 is halogen. The invention also provides compositions comprising the compounds, and methods of treating diseases or disorders that comprise administering one or more of the compounds to a subject in need thereof.
01/01/15
20150005336

Opioid agonist/opioid antagonist/acetaminophen combinations


The invention is directed in part to oral dosage forms comprising a combination of an opioid agonist, acetaminophen and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome)..
Purdue Pharma L.p.
01/01/15
20150005330

Piperidinone carboxamide azaindane cgrp receptor antagonists


The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of cgrp receptors and 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..
Merck Sharp & Dohme Corp.
01/01/15
20150005315

1-substituted 4-arylpiperazine as kappa opioid receptor antagonists


Provided are compounds represented by the formula: where r, y3, r1, r2, r3, r4, r6, g, r7, e1, e2, a, b, w, x, y and z are as defined herein.. .
Research Triangle Institute
01/01/15
20150005292

Method and composition for treating alzheimer-type dementia


There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (achei) in a patient suffering from an alzheimer type dementia by decreasing concomitant adverse effects by administration of said achei in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the cns of said patient is achieved and alleviation of the symptoms of alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of alzheimer type dementia in combination with an acetyl choline esterase inhibitor (achei) and pharmaceutical compositions comprising (a) a 5ht3 receptor antagonist, a dopamine antagonist, a h1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described..
Chase Pharmaceuticals Corporation
01/01/15
20150004259

Nitroxyl progenitors in the treatment of heart failure


Administration of an hno/no+ donating compound, such as angeli's salt, increases myocardial contractility while concomitantly lowering left ventricular preload in subjects experiencing heart failure. Moreover, administration of the hno/no− donating compound isopropylamine (ipa)/no (na(ch3)2chnhn(o)no) surprisingly exhibited positive inotropic effects in subjects experiencing heart failure that were superior to those caused by the hno/no− donating compound angeli's salt.
The Johns Hopkins University
01/01/15
20150004186

Modulation of t cell signaling threshold and t cell sensitivity to antigens


Micrornas (mirnas) are a diverse and abundant class of ˜22-nucleotide (nt) endogenous regulatory rnas that play a variety of roles in animal cells by controlling gene expression at the posttranscriptional level. Increased mir-181a expression in mature t cells is shown to cause a marked increase in t cell activation and augments t cell sensitivity to peptide antigens.
The Board Of Trustees Of The Leland Stanford Junior University
01/01/15
20150004183

Novel anti-malignant tumor agent


The present invention provides an antitumor agent having high safety, which is a molecular target drug against malignant tumors. An anti-malignant tumor agent characterized by containing, as an active ingredient, a substance targeting ribosomal proteins shows increased expression in malignant tumor cells.
National University Corporation Okayama University
01/01/15
20150004165

Secreted proteins


The invention provides human secreted proteins (secp) and polynucleotides which identify and encode secp. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists.
Incyte Corporation
12/25/14
20140378680

Spiro-oxindole mdm2 antagonists


Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and mdm2, and their use as therapeutics for the treatment of cancer and other diseases..
The Regents Of The University Of Michigan
12/25/14
20140378531

Inhibition of pattern recognition receptors in pancreatic cancer treatment using tlr inhibitors


The disclosure herein relates to the novel finding that pattern recognition receptor activation is central to pancreatic cancer progression, and provides antagonists of pattern recognition receptors (prrs), including the tlrs 4, 7, and 9, and the clr dectin-1, for treatment and prevention of pancreatic cancer and pancreatic inflammation. The inventors have discovered that cancer development and progression can be prevented by pattern recognition receptor inhibition, a powerful finding with important clinical and therapeutic implications..
New York University
12/25/14
20140378521

Use of nk-1 receptor antagonists in pruritus


The invention relates to methods for treating pruritus with an nk-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising nk-1 receptor antagonist..
Tigercat Pharma, Inc.
12/25/14
20140378512

Composition for improving cognition and memory


The invention relates to a pharmacologically active combination, having utility in treating insomnia patients, which comprises: (a) at least one first active ingredient selected from melatonin, other melatonergic agents, melatonin agonists and melatonin antagonists; and (b) at least one second active ingredient selected from nicotine and nicotine receptor agonists; to use of a medicament containing component (a) with or without component (b) for alleviation of at least one adverse effect which occurs in a patient in the course of nicotine replacement therapy, or otherwise, selected from impairment of the quality of sleep, impairment of cognition and impairment of memory, as well as to a kit having utility in treating insomnia patients, which comprises components (a) and (b) in unit dosage form.. .
Neurim Pharmaceuticals (1991) Ltd.
12/25/14
20140378506

Compositions and methods for treatment


The present invention provides compounds and methods for the treatment of lfa-1 mediated diseases. In particular, lfa-1 antagonists are described herein and these antagonists are used in the treatment of lfa-1 mediated diseases.
Sarcode Bioscience Inc.
12/25/14
20140378460

Compositions and methods for treating neurodegenerative disease


This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor..
Cognition Therapeutics, Inc.
12/25/14
20140378421

New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities


The present invention relates to novel compounds having β2 adrenergic agonist and m3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.. .
Almirall, S.a.
12/25/14
20140378379

Combination therapy


The present disclosure relates to a method for treatment or prevention of diseases have an increased level of insulin-like growth factor i (igf-i). The method comprises administration of a growth hormone (gh) variant having antagonistic activity in combination with an oligonucleotide targeted to growth hormone receptor (ghr) to a subject in need..
Antisense Therapeutics Ltd
12/25/14
20140378303

Plant seed assemblies comprising bacterial/fungal anatagonists


A seed treated with a fungal/bacterial antagonist combination and a seed assembly comprising a seed and a fungal/bacterial antagonist combination. The fungal/bacterial antagonist combination comprises a trichoderma virens fungal antagonist and a bacillus amyloliquefaciens bacterial antagonist for controlling plant pathogens as a biocontrol agent, bio-pesticide or bio-fungicide.
Novozymes Bioag A/s


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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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