|| List of recent Antagonist-related patents
|4-substituent-2-hydroxylmorpholine-3-one and preparation method thereof|
A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.. .
Shanghai Institute Of Pharmaceutical Industry
|Chimeric il-1 receptor type i agonists and antagonists|
Featured herein are non-naturally occuring cytokine domains that can be used, inter alia, to modulate cellular signalling responsive to interleukin-1 receptor i (il-1ri), to treat disorders, and to detect and/or bind to cellular receptors, as well as other agents. Exemplary cytokine domains can contain amino acid residues from at least two parental cytokines domains, for example, receptor binding features, surface features, β strands, and loops from at least two parental cytokines domains..
Eleven Biotherapeutics, Inc.
|G protein-coupled purinergic receptor gpr17 mediates orexigenic effects of foxo1 in agrp neurons|
G protein-coupled receptor (gpcr) gpr17 expressed in hypothalamic agouti-related peptide-expressing (agrp) neurons increases appetite and glucose tolerance and insulin sensitivity. By contrast, increasing gpr17 reduced glucose tolerance and increased appetite.
The Trustees Of Columbia University In The City Of New York
Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including type i and ii diabetes, insulin resistance and hyperglycemia.
Metabasis Therapeutics, Inc.
|Heterocyclic cgrp receptor antagonists|
The present invention is directed to heterocyclic compounds 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.
|Methods for treating gi tract disorders|
Provided herein are methods, compositions, and kits for the treatment of an enteric nervous system disorder. Such methods may comprise administering to a subject an effective amount of a phenothiazine compound, a peripherally restricted dopamine decarboxylase inhibitor, and/or a peripherally restricted dopamine d2 receptor antagonist that does not substantially inhibit herg channels..
|Cyclic amine derivatives as ep4 receptor antagonists|
The present invention therefore relates to novel compounds which are selective antagonists of the ep4 subtype of pge2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of prostaglandin e mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.. .
|Methods of altering bone growth by administration of sost or wise antagonist or agonist|
The present invention provides a method of promoting local bone growth by administering a therapeutic amount of a sost antagonist to a mammalian patient in need thereof. Preferably, the sost antagonist is an antibody or fab fragment selectively recognizing any one of seq id nos: 1-23.
|Alpha-4-beta-7 heterodimer specific antagonist antibody|
There are disclosed alpha4beta7 heterodimer-specific antigen binding proteins, nucleic acids encoding them, and methods of making and using them.. .
|Polypeptide binding to annexin a1 and use thereof|
A polypeptide binding to annexin a1, an antagonist against annexin a1 including the polypeptide, an anti-annexin a1 antibody including the polypeptide or an antigen-binding fragment thereof, and methods of preventing, treating and/or diagnosing a disease, including administering the antagonist and/or the antibody or an antigen-binding fragment thereof to a subject.. .
Samsung Electronics Co., Ltd.
Combination therapy for treating breast cancer
The invention provides compositions and methods for treating breast cancer. Specifically, the invention relates to administering a transforming growth factor beta (tgfβ) antagonist in combination with capecitabine and ixabepilone to treat breast cancer..
Use of survivin antagonists in polyomavirus-related disease
A method of treating a polyomavirus (+) cancer in which survivin is upregulated in a patient is provided, comprising administering to the patient a therapeutically effective amount of a composition that downregulates survivin expression or function in cells of the polyomavirus (+) cancer. A method of reducing growth of polyomavirus (+) cancer cells in which survivin is up-regulated is provided, comprising contacting the cells with an amount of a composition that downregulates survivin expression or function effective to reduce growth of the cells.
University Of Pittsburgh-of The Commonwealth System Higher Education
An element comprising a cup containing a thermally expanding material, a piston capable of translational movement along its axis, a rigid guide for guiding the translational movement of the piston, a seal for sealing in the thermally expanding material having an annular overall shape, centered on the axis and through which the piston passes axially right through, and which includes first and second opposite axial parts against which the guide and the cup press respectively in a substantially antagonistic manner so as to compress the seal around the piston, and an anti-extrusion washer mounted coaxially around the piston and axially interposed between the guide and the first part of the seal. The invention provides for including in this thermostatic element means for supercompressing the first part of the seal around the piston, which means are designed to make the degree of compression of the first part of the seal equal to a value strictly higher than that associated with an operational thermostatic element formed by the cup, the piston, the guide, the seal and the anti-extrusion washer assembled with one another without these supercompression means..
Fused cyclopentyl antagonists of ccr2
Wherein: r0, r1, r2, r3, r4, r5, and a are as defined in the specification.. .
Combination of 4- benzamide and a nmda receptor antagonist and pharmaceutical compositions containing the same
Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and neurodegenerative diseases.. .
Compositions and methods for minimizing or reversing agonist-induced desensitization
Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient.
Pharmorx Therapeutics, Inc.
Triazolone compounds and uses thereof
The invention disclosed herein is directed to compounds of formula (i) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of formula (i), or a pharmaceutically acceptable salt thereof.
Inception 2, Inc.
Pyridinyl amides as p2x3 and p2x2/3 inhibitors
Or a pharmaceutically acceptable salt thereof, wherein, r1 is optionally substituted phenyl or optionally substituted pyridinyl, and r2, r3, r4, r5, r6, r7, r8 and r9 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..
Combinations comprising antimuscarinic agents and pde4 inhibitors
Combinations comprising (a) a pde4 inhibitor and (b) an antagonist of m3 muscarinic receptors which is 3(r)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion x, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary diseases.. .
Compounds are provided that act as potent antagonists of the ccr9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for ccr9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of ccr9-mediated diseases, and as controls in assays for the identification of ccr9 antagonists..
Modulation of bacterial quorum sensing with synthetic ligands
The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect.
Wisconsin Alumni Research Foundation
Application of initial doses of lhrh analogues and maintenance doses of lhrh antagonists for the treatment of hormone-dependent cancers and corresponding pharmaceutical kits
Lhrh analogues and lhrh antagonists for use in the treatment or prophylaxis of hormone-dependent cancers, in particular prostate cancer, prostate carcinoma and/or advanced prostate carcinoma, by administering an initial dose of an lhrh analogue over a first period sufficient to effect hormonal castration, then administering a maintenance dose of an lhrh antagonist over a second period, the dose being insufficient to achieve and/or maintain hormonal castration.. .
Aeterna Zentaris Gmbh
Sustained release formulations of peptidomimetic drugs and uses thereof
The invention provides sustained release formulations comprising a c5a receptor antagonist. In certain embodiments the sustained-release formulations include microparticles that comprise a complement c5ar antagonist and a biodegradable polymeric matrix.
Jerini Ophthalmic, Inc.
Mechanism, diagnostic, and treatments for complications of renal failure
Mechanisms for complications of renal failure and processes for treating the same are disclosed. They include contacting a biological fluid (e.g.
Anti-neoplastic uses of artemin antagonists
The invention relates to methods for the prophylaxis and treatment of breast cancer using one or more antagonists of artemin function, such as anti-artemin polynucleotides or anti-artemin antibodies and antibody fragments, and uses of these antagonists. In particular, the invention relates to the resensitisation of therapy-resistance breast cancer cells to anti-cancer therapies by antagonism of artemin functionality..
Auckland Uniservices Limited
Treatment of acute inflammation in the respiratory tract
This invention relates to the field of molecular physiology. Specifically, this invention relates to the prevention and/or treatment of acute inflammation of the respiratory tract, especially acute lung injury (ali) or acute respiratory distress syndrome (ards).
Ucl Business Plc
Vegf antagonist formulations
Formulations of a vascular endothelial growth factor (vegf)-specific fusion protein antagonist are provided including a pre-lyophilized formulation, a reconstituted lyophilized formulation, and a stable liquid formulation. Preferably, the fusion protein has the sequence of seq id no:4..
Regeneron Pharmaceuticals, Inc.
Methods for treatment of brain injury utilizing biologics
A method of using biologics to treat chronic brain injury or spasticity due to stroke, trauma and other causes. Preferred embodiments include perispinal, parenteral, transepidermal or intranasal use of tnf antagonists.
Tact Ip Llc
Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
The present invention also relates to the method of prophylaxis or treatment of 5-ht2a serotonin receptor mediated disorders in combination with a dopamine d2 receptor antagonist such as haloperidol, administered separately or together.. .
Use of phosphorylation pathway-related factor in regulating function of regulatory t cell
A method for the treatment and/or the prevention of a disease or a symptom related to dysfunction of regulatory t cell immunomodulation includes administering to a subject in need thereof compositions that regulate regulatory t cell immunomodulatory function, in which the compositions may be prepared by contacting starting materials with phosphorylation pathway-related factors, the agonists or the antagonists thereof. The phosphorylation pathway-related factors are selected from: proto-oncogene protein pim1 and the coding sequence thereof.
Institut Pasteur Of Shanghai, Chinese Academy Of Sciences
Pyrrolidine derivatives as oxytocin/vasopressin v1a receptors antagonists
The present invention relates to a compound of formula (3z,5s)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one o-methy19243-yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin v1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.. .
Aza-aryl 1h-pyrazol-1-yl benzene sulfonamides
Compounds are provided that act as potent antagonists of the ccr(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for ccr(9).
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..
Concert Pharmaceuticals, Inc.
Substituted b-amino acid derivatives as cxcr3 receptor antagonists
That are useful for the preventive and/or therapeutic treatment of diseases caused by abnormal activation of cxcr3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds..
Treatment of male sexual dysfunction
A composition comprising a selective oxytocin antagonist for use in the treatment and/or prevention of a male ejaculatory disorder; which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.. .
Substituted 2,3-dihydro-1h-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis
The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the retinoic acid-related orphan nuclear receptor γt (rorγt)/rorγ. The compounds of the present invention are useful for modulating rorγt)/rorγ activity and for treating diseases or conditions mediated by rorγt)/rorγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as multiple sclerosis (ms), rheumatoid arthritis (ra), inflammatory colitis, psoriasis, copd, pain, obesity, diabetes, dyslipidemia, osteoporosis, asthma, neurodegenerative diseases and cancer..
Arrien Pharmaceuticals Llc
Compositions and methods for regulating hair growth
The invention relates to compositions and methods for regulating hair growth. Specifically, the invention relates to regulating hair growth by regulating the activity one of the prostaglandin d2 (pgd2) receptors, dp-2 (gpr44).
The Trustees Of The University Of Pennsylvania
Novel cholesterol metabolite, 5-cholesten, 3beta-25-diol, disulfate (25hcds) for therapy of metabolic disorders, hyperlipidemia, diabetes, fatty livers diseases and atherosclerosis
5-cholesten, 3β, 25-diol, disulfate (25hcds) has been found to be an authentic pparγ agonist and lxr antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic diseases.. .
Virgini Commonwealth University
Lisurid, terguride and derivatives thereof for use in the prophylaxis and/or treatment of fibrotic changes
The present invention relates to the use of 5-ht2 receptor antagonists and in particular of 8-α-ergolines such as lisuride, terguride and the derivatives thereof as 5-ht2b and 5-ht2a receptor antagonists and antioxidants in preferably higher-dosed and preferably continuous use for the treatment, progression prophylaxis and general prophylaxis of organ fibroses and other pathological organ remodeling caused by mesenchymal proliferation. .
Sinoxa Pharma Gmbh
Methods and compositions to regulate hepcidin expression
The present invention provides new systems and strategies for the regulation of iron metabolism in mammals. In particular, methods of using agonists and antagonists of tgf-β superfamily members to modulate the expression or activity of hepcidin, a key regulator of iron metabolism, are described.
The General Hospital Corporation
Treatment of ischemic retinopathies
The present invention relates to the field of ischemic retinopathies. More specifically, the present invention provides methods and compositions useful for treating ischemic retinopathies including diabetic macular edema (dme).
University Of Maryland, Baltimore
Anti-cd28 humanized antibodies
The invention relates to humanized antibodies directed against the human lymphocyte receptor cd28. When used in a monovalent form these antibodies are antagonists, i.e.
Institut National De La Sante Et De La Recherche Medicale (inserm)
Biomarkers and methods of treating pd-1 and pd-l1 related conditions
Provided herein are biomarkers for the treatment of pathological conditions, such as cancer, and method of using pd-1/pd-l1 pathway antagonists. In particular, provided are biomarkers for patient selection and prognosis in cancer, as well as methods of therapeutic treatment, articles of manufacture and methods for making them, diagnostic kits, methods of detection and methods of advertising related thereto..
Antagonistic peptides for frizzled-1 and frizzled-2
The invention is in the field of molecular medicine. It provides antagonistic compounds for frizzled-1 and/or frizzled-2 receptors, which may be useful in molecular imaging of the wound healing process after myocardial infarction and in therapeutic intervention into wound healing after remodeling of the heart, thereby ameliorating the consequences of myocardial infarction.
Academisch Ziekenhuis Maastricht
Dual-acting antihypertensive agents
Wherein: ar, r, y, z, q, w, x, and r5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have at1 receptor antagonist activity and neprilysin inhibition activity.
Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.. .
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.
Neurendo Pharma, Llc
Integrin antagonist conjugates for targeted delivery to cells expressing lfa-1
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 lfa-1 integrin antagonists to target cells expressing lfa-1..
Hoffmann-la Roche Inc.
The present invention provides compounds of formula (i) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein x is nh, or o; q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: c1-c4 alkyl, halogen, halo c1-c4 alkyl, c1-c4 alkoxy, cn; a is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: c1-c4 alkyl, halogen, halo c1-c4 alkyl, c1-c4 alkoxy, cn; b may assume different meanings from a and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: c1-c4 alkyl, halogen, halo c1-c4 alkyl, c1-c4 alkoxy, cn; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the orexin 1 and orexin 2 receptors.. .
Rottapharm Biotech S.r.l.
Triazole-substituted arylamides as p2x3 and p2x2/3 modulators
Or a pharmaceutically acceptable salt thereof, wherein, r1 is optionally substituted triazolyl, and r2, r3, r4, r5, r6, r7 and r8 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..
Heterocyclic compounds and methods of use
This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.. .
Medivation Technologies, Inc.
Tetrazole-substituted arylamides as p2x3 and p2x2/3 antagonists
Or a pharmaceutically acceptable salt thereof, wherein, r1 is optionally substituted tetrazolyl, r2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and r3, r4, r5, r6 r7 and r8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the p2x3 and/or a p2x2/3 receptor antagonist and methods of making the compounds..
4-aminopyridine as a therapeutic agent for spinal muscular atrophy
It has been discovered that pharmacological inhibition of k+ channels (using the fda-approved broad-spectrum k+ channel antagonist 4-ap) positively benefitted smn mutant phenotypes, a result that is consistent with the defective excitability of motor circuits by their interneuron or sensory neuron inputs being a critical consequence of smn depletion. Based on these observations, certain embodiments of the invention are directed to methods of treatment of sma by administering therapeutically effective amounts of one or more potassium channel antagonists, including 4-aminopyridine, 4-(dimethylamino)pyridine, 4-(methylamino)pyridine, and 4-(aminomethyl)pyridine.
The Trustees Of Columbia University In The City Of New York
Oral film containing opiate enteric-release beads
A control release and abuse-resistant opiate drug delivery oral wafer or edible oral film dosage to treat pain and substance abuse is provided. The drug delivery oral wafer or edible oral film dosage includes a controlled release layer containing enteric-release beads dispersed in a polymer matrix.
Lts Lohmann Therapie-systeme Ag
Methods and compositions for 6-phosphogluconate dehydrogenase (6-pgd) as a target for lung cancer therapy
The present invention relates to methods, compositions, and diagnostic tests for treating and diagnosing a proliferative disease that result in dysregulation of 6-phosphogluconate dehydrogenase. In particular, the methods and compositions include treatment of gefitinib/erlotinib resistant proliferative diseases such as lung cancer using a 6-phosphogluconate dehydrogenase antagonist..
Beth Israel Deaconess Medical Center, Inc.
Methods of treating psoriatic arthritis (psa) using il-17 antagonists and psa response or non-response alleles
The disclosure is directed to predictive methods and personalized therapies for treating psoriatic arthritis (psa). Specifically, this disclosure relates to methods of treating a patient having psa by selectively administering an il-17 antagonist, e.g., an il-17 antibody, such as secukinumab, to the psa patient on the basis of that patient being predisposed to have a favorable response to treatment with the il-17 antagonist.
Method of treating cancer with dll4 antagonist and chemotherapeutic agent
The invention provides methods for treating various types of cancer/tumor by administering the combination of dll4 antagonists, in particular, dll4 antibodies and fragments thereof that specifically bind human dll4, and chemotherapeutic agents. Such combination therapies exhibit synergistic effects compared to the treatment with either agent alone.
Regeneron Pharmaceuticals, Inc.
Fibrosis suppression by inhibiting integrin alpha-8 beta-1 function
Novel and effective anti-fibrosis agents are obtained. An anti-fibrosis agent containing an antagonist for integrin α8β1 is used.
Methods of treating liver conditions using notch2 antagonists
Methods and compositions for the treatment of liver conditions are provided, such methods and compositions comprising notch2 antagonists, e.g., anti-notch2 antibodies. Liver conditions include, but are not limited to, chronic liver disease..
Diagnostic methods and compositions for treatment of glioblastoma
The invention provides methods and compositions to detect expression of one or more biomarkers for identifying and treating patients having glioblastomas who are likely to be responsive to vegf antagonist therapy. The invention also provides kits and articles of manufacture for use in the methods..
Anti-cd40 antibody mutants
A mutant of a potentially therapeutic anti-cd40 antibody is provided which mutant has reduced adcc and cdc activities designed to be optimized as a pharmaceutical agent. A mutant of an agonistic anti-cd40 antibody, comprising mutation and/or substitution of at least one amino acid in the constant region to reduce the adcc and/or cdc activities therein, and a mutant of an antagonistic anti-cd40 antibody, comprising at least one mutation or substitution in the constant region to reduce the adcc and/or cdc activities therein, both mutants having at least a hinge region derived from a human igg2..
Kyowa Hakko Kirin Co., Ltd.
Compound, use and method
The present invention relates to the use of an antagonist of kisspeptin in the manufacture of a medicament for the treatment of a condition induced and/or worsened by kisspeptin activity in an individual. The invention also provides certain defined peptide molecules, which may act as an antagonist of kisspeptin, which are of use in treating a condition induced and/or worsened by kisspeptin activity in an individual.
Medical Research Council
Methods for the treatment of tinnitus induced by cochlear excitotoxicity
The invention relates to methods for the prevention and/or treatment of tinnitus induced by cochlear excitotoxicity. In these methods, a pharmaceutical composition comprising an nmda receptor antagonist is administered to an individual in need of such treatment by appropriate devices and/or formulations for local administration to the inner ear.
Auris Medical Ag
Novel cellular targets for hiv infection
Methods and compositions are provided for treating hiv infection and for inhibiting hiv infection, and for identifying purinergic receptor antagonists or panx 1 hemi-channel blockers useful therefor. The invention provides a method of treating a mammalian subject having an hiv infection, or suspected of having been exposed to hiv, comprising administering to the mammalian subject an amount of (i) an antagonist of a panx 1 hemichannel, or (ii) of an inhibitor of a purinergic receptor, effective to inhibit (a) hiv fusion with a target cell, or (b) hiv replication, or (c) hiv entry into a target cell, or two or more of (a), (b) and (c)..
Albert Einstein College Of Medicine Of Yeshiva University
Proline sulfonamide derivatives as orexin receptor antagonists
Wherein r1 and r2 are as described in the description, or pharmaceutically acceptable salts thereof, for use in the prevention or treatment of diseases or disorders related to the orexin system. The present invention also relates to the use of (s)-proline sulfonamide compounds of formula (ii) as pharmaceuticals, to pharmaceutical compositions comprising compounds of formula (ii), and especially their use in the prevention or treatment of diseases or disorders related to the orexin system..
Compounds containing s-n-valeryl-n--valine and (2r,4s)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester moieties and cations
A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a nepi.. .
Novartis Pharmaceuticals Corporation
The present invention provides a method of selection of a patient, who is a candidate for treatment with an nmda antagonist drug, such as (s)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the nmda antagonist. The invention provides a method for determining the sequence of gabr-a2 at any of four single nucleotide polymorphism (snp) sites known as rs3756007, rs11503016, rs17537359 or rs1372472.
Methods for treatment of 16p11.2 microdeletion syndrome
Subjects that have a 16p11.2 microdeletion syndrome are treated by administering compositions that include mglur inhibitors, including mglur antagonists that include mglur negative allosteric modulators. Administration of compositions employed in the methods of the invention can treat psychiatric, including neuropsychiatric disorders, cognitive impairments, attention, obesity, intellectual disability and seizure disorders..
Massachusetts Institute Of Technology
Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3 -arylpropyl)imidazolidin-1-yl)-3 -arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described..
Scifluor Life Sciences, Llc
Composition and neuropeptide s receptor (npsr) antagonists
Neuropeptide s receptor antagonists are provided that bind in functional assays to neuropeptide s receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide s receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide s receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide s receptor.. .
Research Triangle Institute
Use of nk-1 receptor antagonists in pruritus
The invention relates to methods for treating pruritus with nk-1 receptor antagonists such as serlopitant. The invention further relates to pharmaceutical compositions comprising nk-1 receptor antagonists such as serlopitant.
Tigercat Pharma, Inc.