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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
05/21/15
20150141481
 Treatment of chronic obstructive pulmonary disease with nebulized beta 2-agonist or combined nebulized beta 2-agonist and anticholinergic administration patent thumbnailnew patent Treatment of chronic obstructive pulmonary disease with nebulized beta 2-agonist or combined nebulized beta 2-agonist and anticholinergic administration
Inhalation solutions for administration of beta 2-agonists or combinations of muscarinic antagonists and beta 2-agonists for the treatment of breathing disorders, such as copd, are provided. The inhalation solutions are administered by nebulization, particularly with a high efficiency nebulizer..
Sunovion Respiratory Development, Inc.
05/21/15
20150141477
 Pyrazole derivatives and their use as lpar5 antagonists patent thumbnailnew patent Pyrazole derivatives and their use as lpar5 antagonists
The present invention relates to compounds of the formula (i), wherein the residues r1 to r5, v, g and m have the meanings indicated in the claims. The compounds of the formula (i) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses.
Sanofi
05/21/15
20150141471
 Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation patent thumbnailnew patent Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation
The present invention relates to compounds of the formula (i), wherein the residues r1 to r6, v, g and m have the meanings indicated in the claims. The compounds of the formula i are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses.
Sanofi
05/21/15
20150141452
 Compositions for affecting weight loss patent thumbnailnew patent Compositions for affecting weight loss
Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (mc3-r) or a melanocortin 4 receptor (mc4-r) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-msh activity..
Orexigen Therapeutics, Inc.
05/21/15
20150141432
 Piperidin-4-yl-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists patent thumbnailnew patent Piperidin-4-yl-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists
The present invention relates to compounds 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..
Janssen Pharmaceutica N.v.
05/21/15
20150141425
 C5ar antagonists patent thumbnailnew patent C5ar antagonists
Compounds are provided that are modulators of the c5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of c5a receptors..
Chemocentryx, Inc.
05/21/15
20150141416
 Hydroxybupropion analogues for treating drug dependence patent thumbnailnew patent Hydroxybupropion analogues for treating drug dependence
The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes.
Virginia Commonwealth University
05/21/15
20150141397
 Substituted anilines as ccr(4) antagonists patent thumbnailnew patent Substituted anilines as ccr(4) antagonists
Aniline compounds are provided which bind to ccr(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.. .
Chemocentryx, Inc.
05/21/15
20150141387
 Pharmaceutical product comprising a p38 kinase inhibitor and a second active ingredient patent thumbnailnew patent Pharmaceutical product comprising a p38 kinase inhibitor and a second active ingredient
The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is n-cyclopropyl-3-fluoro-4-methyl-5-[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-1(2h)-pyrazinyl]-benzamide or a salt thereof, and a second active ingredient selected from: a non-steroidal glucocorticoid receptor (gr receptor) agonist; an antioxidant; a β2 adrenoceptor agonist; a ccr1 antagonist; a chemokine antagonist (not ccr1); a corticosteroid; a crth2 antagonist; a dpi antagonist; an histone deacetylase activator; an ikk2 kinase inhibitor; a cox inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a maba compound; an mpo inhibitor; a muscarinic antagonist; a pde4 inhibitor; a pparγ agonist; a protease inhibitor; a statin; a thromboxane antagonist; a vasodilator; or, an enac blocker (epithelial sodium-channel blocker); and its use in the treatment of respiratory disease.. .
Astrazeneca Ab
05/21/15
20150140124
 Method of diagnosing, treating and determining progression and survival of cancer cells using bcl-2 antagonist of cell death (bad) pathway gene signature patent thumbnailnew patent Method of diagnosing, treating and determining progression and survival of cancer cells using bcl-2 antagonist of cell death (bad) pathway gene signature
The present invention relates to the bad pathway's influence on development, progression, chemo-sensitivity, and overall survival for multiple human cancers and its potential as a therapeutic target to increase chemo-sensitivity. Bad pathway expression was associated with the development and/or progression of breast, colon, and endometrial cancers, relapse-free survival from breast cancer, and overall survival from ovarian, colon, and brain cancers.
H. Lee Moffitt Cancer Center And Research Institute, Inc.
05/21/15
20150140087
new patent

Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists


Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists or a pharmacologically acceptable salt thereof are disclosed. The compositions contain the therapeutic active compound with non-ionic polymer and ionic polymer, binder and fillers in either matrix pellet, matrix tablet or coated pellets.
F. Hoffmann-la Roche Ag
05/21/15
20150140086
new patent

Tamper resistant co-extruded dosage form containing an active agent and an adverse agent and process of making same


The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms arc useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid.
Purdue Pharma L.p.
05/21/15
20150140082
new patent

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.
05/21/15
20150140081
new patent

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.
05/21/15
20150140080
new patent

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.
05/21/15
20150140079
new patent

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.
05/21/15
20150140078
new patent

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.
05/21/15
20150140077
new patent

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.
05/21/15
20150140076
new patent

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.
05/21/15
20150140075
new patent

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.
05/21/15
20150140016
new patent

Molecular determinants of myeloma bone disease and uses thereof


The present invention is drawn to understanding lytic bone diseases. In this regard, the present invention discloses mechanism by which wnt signaling antagonist inhibits bone differentiation.
Board Of Trustees Of The University Of Arkansas
05/21/15
20150139999
new patent

Interferon antagonists, antibodies thereto, and associated methods of use


Described are compositions and methods useful for modulating the immune system of a subject. Also included are diagnostic methods for monitoring an immunologic condition.
Rutgers, The State University Of New Jersey
05/21/15
20150139916
new patent

Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity


Compounds of formula (i) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.. .
Chiesi Farmaceutici S.p.a.
05/14/15
20150133637

P2x7 receptor antagonists and agonists


The present invention relates to biological materials against p2x7 and more in particular to polypeptides, nucleic acids encoding such polypeptides; to methods for preparing such polypeptides; to host cells expressing or capable of expressing such polypeptides; to compositions and in particular to pharmaceutical compositions that comprise such polypeptides, for prophylactic, therapeutic or diagnostic purposes. In particular, the biological materials of the present invention inhibit the biological activity of the p2x7 receptor, such as activation by atp..
05/14/15
20150133512

N-aryltriazole compounds as lpar antagonists


Provided herein are compounds of the formula (i): 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 inflammatory diseases and disorders such as, for example, pulmonary fibrosis..
05/14/15
20150133511

N-alkyltriazole compounds as lpar antagonists


Provided herein are compounds of the formula (i): 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 inflammatory diseases and disorders such as, for example, pulmonary fibrosis .
05/14/15
20150133491

Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity


Compounds of formula (i) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.. .
05/14/15
20150133411

Compounds with trpv4 activity, compositions and associated methods thereof


Compounds, compositions and methods useful for treating ocular diseases are provided. In particular, antagonists of trpv4, their synthesis, pharmaceutical compositions thereof and methods of treating ocular diseases such as glaucoma, are disclosed.
05/14/15
20150133399

Composition and uses of galectin antagonist


The present invention is directed to methods and compositions for augmenting treatment of cancers and other proliferative disorders. In particular embodiments, the invention combines the administration of an agent that inhibits the anti-apoptotic activity of galectin-3 (e.g., a “galectin-3 inhibitor”) so as to potentiate the toxicity of a chemotherapeutic agent.
05/14/15
20150133372

Methods and compositions for the induction of hypothermia


Provided herein are methods for the induction of hypothermia and the treatment of clinical insults in a subject through the administration of a regulated hypothermic multidrug combination. The compositions or multidrug combinations of the invention comprise a regulated hypothermic compound or a dopamine receptor agonist; a vasoactive compound; and an antiarrhythmic compound or a serotonin 5-ht3 receptor antagonist.
05/14/15
20150132790

Screen to identify agents that can modulate heme transporter


Provided are compositions and methods related to heme transporters and high-throughput methods of identifying agents that can modulate heme transporters. An approach for identifying a modulator of a eukaryotic heme transporter involves adding a toxic heme analog and at least one test agent to a culture of cells, wherein the cells express a recombinant heterologous eukaryotic heme transporter.
05/14/15
20150132304

Methods of preventing or treating pain using anti-ngf antibodies that selectively inhibit the association of ngf with trka, without affecting the association of ngf with p75


Ngf antagonists including antibodies and antibody fragments thereof having binding specificity to human nerve growth factor (“ngf”), and methods of treating pain. Methods of treating pain or eliciting an analgesic effect in an individual comprising administering an effective amount of an ngf antagonist inhibits the association of ngf with trka without inhibiting the association of ngf with p75.
05/14/15
20150132300

Methods of antagonizing signal transduction in spinal cord cells using an il-31ra or osmr-b antagonist


Use of antagonists to il-31ra and osmrb are used to treat inflammation and pain by inhibiting, preventing, reducing, minimizing, limiting or minimizing stimulation in neuronal tissues. Such antagonists include soluble receptors, antibodies and fragments, derivative, or variants thereof.
05/14/15
20150132299

Methods of treating neuronal inflammation using an il-31 monoclonal antibody


Use of antagonists to il-31 are used to treat inflammation and pain by inhibiting, preventing, reducing, minimizing, limiting or minimizing stimulation in neuronal tissues. Such antagonists include antibodies and fragments, derivative, or variants thereof.
05/14/15
20150132226

Treatment of cancer


This invention relates to the field of molecular physiology. Specifically, this invention relates to the prevention and/or treatment of cancer.
05/07/15
20150126501

Fused ring compound for use as mineralocorticoid receptor antagonist


The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by formula (i) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of x, y1, y2, y3, r1, r2a, r2b, r3a, r3b, r4, cy and n are as presented in the description..
Kbp Biosciences Co., Ltd.
05/07/15
20150126498

Orexin receptor antagonists


The disclosures herein relate to novel compounds of formula wherein w, x and y1, y2, y3 and y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.. .
Heptares Therapeutics Limited
05/07/15
20150126494

Non-retinoid antagonists for treatment of age-related macular degeneration and stargardt disease


A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.. .
The Trustees Of Columbia University In The City Of New York
05/07/15
20150126486

Phenyl derivative


Wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human s1p2 antagonistic activity. The compound may therefore be used as a therapeutic agent for s1p2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases..
05/07/15
20150126482

Pharmaceutical composition or group of compositions for inhibiting autocrine hcg production in adult human cells


A pharmaceutical composition for use as medicament that inhibits inhibits autocrine human chorionic gonadotropin (hcg) production and thus carcinogenesis in adult human cells, the composition comprising at least a first pharmaceutically acceptable carrier and an active agent that is a competitively binding progesterone antagonist binding to steroid receptors of human cells, wherein the composition is provided in units designed for the monthly, semi-annual or annual application of the active agent in annual dosages in the range between 0.1 mg to 10.0 mg per kg of person/body-weight.. .
Flamina Holding Ag
05/07/15
20150126474

Broad spectrum pro-quorum-sensing molecules as inhibitors of virulence in vibrios


Using a whole-cell high-throughput screen, eleven molecules were identified that activate v. Cholerae quorum sensing (qs).
The Trustees Of Princeton University
05/07/15
20150126446

Vascular endothelial growth factor antagonists and methods for their use


The present invention provides variant vegf polypeptides which have been altered in their c-terminal heparin binding region to lower their heparin binding affinity. These variants have been found to act as receptor antagonists for vegf receptors and antagonize angiogenesis.
The United States Of America, As Represented By The Secretary, Dept. Of Health & Human Services
05/07/15
20150125863

Cxcl5 as a marker of hormone escape in prostate cancer


The invention relates to the use of cxcl5 as a marker for assessing hormone escape in prostate cancer cells. The invention further provides diagnostic methods and kits for assessing hormone escape in prostate cancer cells, and cxcl5 antagonists for use in the treatment or prevention of prostate cancer and/or hormone escape in prostate cancer..
Institut National De La Sante Recherche Medicale (inserm)
05/07/15
20150125857

Cancer patient selection for administration of wnt signaling inhibitors using rnf43 mutation status


Disclosed are biomarkers, methods and assay for the identification of cancer patients who are predicted to benefit from the therapeutic administration of wnt antagonist. The biomarkers include detection of rnf43 and znrf3 gene deletion, reduced rnf43 and znrf3 mrna expression, reduced rnf43 and znrf3 protein expression, rnf43 and znrf3 inactivation mutation, phosphorylated lrp6, phophorylated dishevelleds, and the expression of frizzleds.
Irm Llc
05/07/15
20150125468

Il-6 antagonists and uses thereof


Il-6 antagonists are provided that are specific for binding to site ii of il-6. Methods of using such inhibitors to treat il-6 related diseases, e.g., disease of the eye such as diabetic macular edema are disclosed..
Eleven Biotherapeutics, Inc.
05/07/15
20150125462

Methods of treating ankylosing spondylitis using il-17 antagonists


The disclosure is directed to novel personalized therapies and methods for treating ankylosing spondylitis (as). Specifically, this disclosure relates to methods of treating a patient having as by selectively administering an il-17 antagonist, e.g., an il-17 antibody, such as secukinumab, to the as patient on the basis of that patient being predisposed to have a favorable response to treatment with the il-17 antagonist.
05/07/15
20150125452

Combination treatments comprising c-met antagonists and b-raf antagonists


The present invention relates generally to the fields of molecular biology and growth factor regulation. More specifically, the invention relates to therapies for the treatment of pathological conditions, such as cancer..
Genentech, Inc.
05/07/15
20150125435

Compositions for controlling plant parasitic nematodes and methods for using same


Aspects of the invention include compositions for controlling plant parasitic nematodes. Compositions according to certain embodiments include a carbon skeleton energy compound, a chelating agent, macronutrients, micronutrients, an ionophore, exotic micronutrients and a plant parasitic nematode antagonist.
04/30/15
20150119450

Compositions for use in treating or diagnosing bone disorders and/or cardiovascular disorders


Compositions of an inhibitor of a polynucleotide for use in treating or preventing bone disorders such as osteoporosis, osteopenia, bone fracture, bone cancer, as well as impaired bone homeostasis. Preferred compounds to be used in these medical interventions are antagonistic compounds, like nucleic acid molecules, directed against mir-31 and derivatives thereof.
Universitat Fur Bodenkultur Wien
04/30/15
20150119381

Use of ghrelin receptor inverse agonists or antagonists for treating sleep disorders


The present invention relates to methods of treating sleep disorders in patients comprising administration of a ghrelin receptor inverse agonist or antagonist. The invention also includes methods of treating sleep disorders comprising the administration of a pharmaceutical composition comprising a ghrelin receptor inverse agonist or antagonist and at least one pharmaceutically acceptable carrier, diluent, or excipient..
Pfizer Inc.
04/30/15
20150119351

Therapy of tumors and infectious agents deficient in methylthioadenosine phosphorylase


Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents.
04/30/15
20150119329

Modulation of angiotensin ii receptors for the prevention and treatment of malaria cerebral


The present invention is directed to a composition for the treatment or prevention of cerebral malaria that comprises an angiotensin receptor type-2 agonist and an antimalaria drug. The present invention is further directed to methods for treating and preventing cerebral malaria that involve administering an angiotensin receptor type-2 agonist and/or an angiotensin receptor type-1 antagonist..
New York University
04/30/15
20150119327

Drug screening platform for rett syndrome


The invention provides a method for restoring a neural cell having a deficiency or alteration in glutamatergic pathway affecting neuron and/or glial function comprising contacting the cell with a nmda receptor antagonist(s) and/or modulator(s) of a glutamatergic pathway, thereby restoring the neural cell having a deficiency or alteration in glutamatergic pathways affecting neuron and/or glial function.. .
The Regents Of The University Of California
04/30/15
20150118241

Lingo-2 antagonists for treatment of conditions involving motor neurons


The invention provides methods of treating diseases, disorders or injuries involving motor neuron survival and axonal growth, including amylotrophic lateral sclerosis, by the administration of a lingo-2 antagonist. An exemplary method for promoting survival of a motor neuron, comprising contacting said motor neuron with an effective amount of a composition comprising a lingo-2 antagonist selected from the group consisting of: (i) a soluble lingo-2 polypeptide; (ii) a lingo-2 antibody or antigen-binding fragment thereof; (iii) a lingo-2 antagonist polynucleotide; (iv) a lingo-2 aptamer; and (v) a combination of two or more of said lingo-2 antagonists..
Biogen Idec Ma Inc.
04/30/15
20150118232

Therapeutic combination and methods of treatment with a dll4 antagonist and an anti-hypertensive agent


Methods for treating cancer comprising administering a dll4 antagonist and one or more anti-hypertensive agents are described. Also described are pharmaceutical compositions comprising a dll4 antagonist and one or more anti-hypertensive agents, and kits comprising the same..
Oncomed Pharmaceuticals, Inc.
04/23/15
20150112067

Process for making cgrp receptor antagonists


The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are cgrp receptor antagonists, useful for the treatment of migraine. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of formulae b (after salt break) and c with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent..
Merck Sharp & Dohme
04/23/15
20150111920

Selective ep4 receptor antagonistic substance for treatment of cancer


This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin e2 receptor (ep4 receptor) and is represented by the following general formula (i), (ii), (iii), or (iv), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer.
Raqualia Pharma Inc.
04/23/15
20150111914

Spirolactam cgrp receptor antagonists


The present invention is directed to spirolactam analogues which are antagonists of cgrp receptors and 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..
Merck Sharp & Dohme Corp.
04/23/15
20150111908

Methods of diagnosing, preventing, and treating bone mass diseases


The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are tph1 inhibitors or serotonin receptor antagonists..
04/23/15
20150111895

Substituted triazolo-pyridazine derivatives


This invention relates to novel substituted triazolo-pyridazines, their derivatives, 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 an α1-gaba-a receptor antagonist and/or a α2, α3 and α5 gaba-a receptor agonist..
Concert Pharmaceuticals Inc.
04/23/15
20150111889

Benzo[1,3]dioxine derivatives and their use as lpar5 antagonists


The present invention relates to compounds of the formula (i), wherein the residues a, r1 to r5, z1 and z2 have the meanings indicated in the claims. The compounds of the formula (i) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses.
Sanofi
04/23/15
20150111828

Dipeptide mimetics of ngf and bdnf neurotrophins


The invention relates to compounds having either agonist or antagonist activities for the neurotrophins ngf and bdnf and represented by monomeric or dimeric substituted dipeptides that are analogs of the exposed portions of loop 1 or loop 4 regions of these neurotrophins near or at a beta-turn of the respective loop. N-acylated substituents of these dipeptides are biostereoisomers of the amino acid residues preceding these dipeptide sequences in the neurotrophin primary structure.
Uchrezhdenie Rossiiskoi Akademii Meditsynskikh Nauk Nauchno-issledovatelsky Institut Farmakologii
04/23/15
20150110879

Opioid agonist formulations with releasable and sequestered antagonist


Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.. .
Purdue Pharma L.p.
04/23/15
20150110865

Cns stimulant and opioid receptor antagonist combination as a non-addictive, non-aversive and synergistic anti-obesity treatment


Combinations comprise a therapeutically effective amount of one or more stimulants and and/or pharmaceutically acceptable analogs, salts, or hydrates of the one or more stimulants, and one or more non-selective opioid receptor antagonists, and/or pharmaceutically acceptable analogs, salts or hydrates of the one or more non-selective opioid receptor antagonists. These combinations may be used for treating obesity via administration to a subject having a need thereof..
The General Hospital Corporation
04/23/15
20150110808

E-selectin antagonist compounds, compositions, and methods of use


Methods and compositions using e-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of e-selectin to an e-selectin ligand. Described herein are e-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation..
Glycomimetics, Inc.
04/23/15
20150110787

Polypeptide specifically binding to vegf-c and use thereof


A polypeptide, antagonist, and antibody that specifically bind to and inhibit vegf-c and uses thereof in a method of inhibiting angiogenesis and a method of preventing, treating, and/or diagnosing a disease associated with activation and/or overexpression of vegf-c, using the antibody, and a method of detecting the presence of vegf-c in a sample.. .
Samsung Electronics Co., Ltd.
04/23/15
20150110783

Antagonist anti-cd40 antibody pharmaceutical compositions


Stable liquid pharmaceutical compositions comprising an antagonist anti-cd40 antibody as a therapeutically or prophylactically active component and methods useful in their preparation are provided. These compositions comprise the antagonist anti-cd40 antibody, a buffering agent to maintain the ph of the composition between about ph 5.0 and about ph 7.0, and an amount of arginine-hcl sufficient to render the liquid composition near isotonic.
Novartis Ag
04/23/15
20150110669

Inhibitor of odor caused by sotolone


It is intended to provide a substance inhibiting an odor caused by sotolone. The present invention provides an inhibitor of an odor caused by sotolone, comprising an antagonist of an olfactory receptor or8d1 as an active ingredient..
Kao Corporation


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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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