This page is updated frequently with new Antagonist-related patent applications.
| Antagonists for abdominal vasopressin v2 receptor and uses thereof|
Provided herein are antagonists or binding agents of an abnormal vasopressin receptor v2 (e.g., abnv2), such as antibodies and antigen-binding portions thereof specific for the receptor, for identifying and targeting cancer cells expressing such abnormal vasopressin receptor v2. Additionally provided are methods of using said antagonists or binding agents, for example, to image cancer cells or in biological samples, or diagnose cancers, both in vivo and in vitro.
Woomera Therapeutics, Inc
| Dual receptor antagonistic antigen-binding proteins and uses thereof|
This disclosure relates to antagonistic dual receptor antigen-binding proteins, e.g. Antibodies and methods of using the dual receptor antibodies for treatment of pathological diseases.
| Provasopressin antagonists and uses thereof|
Provided herein are pro-vp antagonists, such as antibodies and antigen-binding portions thereof specific for pro-vp, for identifying and targeting expressing cancer cells. Applicants additionally provide methods of using said compositions, for example to image cancer cells in vivo and in biological samples.
Woomera Therapeutics, Inc.
| Delivery of therapeutic agents by a collagen binding protein|
Methods of delivering therapeutic agents by administering compositions including a bacterial collagen-binding polypeptide segment linked to the therapeutic agent to subjects in need of treatment with the therapeutic agent are provided. Methods of treating hyperparathyroidism, and hair loss using compositions comprising a collagen binding polypeptide and a pth/pthrp receptor agonist are provided.
Montefiore Medical Center
| Combination therapy for treating cancer with a poxvirus expressing a tumor antigen and an antagonist of tim-3|
The invention relates to compositions, kits, and methods for cancer therapy using recombinant poxviruses encoding a tumor-associated antigen in combination with a monoclonal antibody against immune checkpoint molecule tim-3.. .
Bavarian Nordic A/s
| Cenicriviroc for the treatment of hiv-2 infection|
Cenicriviroc (cvc) is an orally active antagonist of ligand binding to c—c chemokine receptor type 5 (ccr5) and c—c chemokine receptor type 2 (ccr2). Cvc blocks the binding of rantes, mip-1α, and mip-1β to ccr5, and of mcp-1/ccl2 to ccr2.
Tobira Therapeutics, Inc.
|Use of biomarkers for assessing treatment of gastrointestinal inflammatory disorders with beta7 integrin antagonists|
The present invention is directed to methods of using biomarkers to assess treatment of gastrointestinal inflammatory disorders with beta7 antagonists. More particularly, the present invention relates to methods of using the level of gut-homing lymphocytes in peripheral blood, the level of drug occupancy on gut-homing lymphocytes, and/or the level of beta7 integrin receptors on gut-homing lymphocytes as indicators (or biomarkers) of the effect, efficacy, safety, prognosis, and/or dosing of therapeutic agents, such as beta7 integrin antagonists, for the treatment of gastrointestinal inflammatory disorders..
|Modulation of human cytomegalovirus replication by micro-rna 132 (mir132), micro-rna 145 (mir145) and micro-rna 212 (mir212)|
The present invention relates to mir145, mir132, mir212, and the genes or gene products regulated by these mirnas. Mir145 is downregulated in cells infected with hcmv.
University Of Massachusetts
|Blockade of tim-1 for treating graft-versus-host disease|
Tim1 antagonists reduce gvhd by symptom score and show statistically significant improved survival.. .
The Board Of Trustees Of The Leland Stanford Junior University
|Fusion proteins of collagen-binding domain and parathyroid hormone|
Fusion proteins containing active agonist or antagonist fragments of parathyroid hormone (pth) and parathyroid hormone related peptide (pthrp) coupled to a collagen-binding domain are presented. The fusion proteins can be used to promote bone growth, to promote hair growth, to prevent cancer metastasis to bone, to promote immune reconstitution with a bone marrow stem cell transplant, to promote mobilization of bone marrow stem cells for collection for autologous stem cell transplant, and to treat renal osteodystrophy.
The Board Of Trustees Of The University Of Arkansas
Modulating gamma-c-cytokine activity
Embodiments relate to peptide antagonists of γc-family cytokines, which is associated with important human diseases, such as leukemia, autoimmune diseases, collagen diseases, diabetes mellitus, skin diseases, degenerative neuronal diseases and graft-versus-host disease (gvhd). Thus, inhibitors of γc-cytokine activity are valuable therapeutic and cosmetic agents as well as research tools.
Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists
Disclosed are chemical entities of formula (i) wherein x, y, z, r1, r3, r4, r5 and r6 are defined herein, as nr2b subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula (i), and methods of treating various diseases and disorders associated with nr2b antagonism, e.g., diseases and disorders of the cns, such as depression, by administering a chemical entity of formula i..
Rugen Holdings (cayman) Limited
Substituted prolines / piperidines as orexin receptor antagonists
The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as ox1 or ox2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention. For example, orexin receptor-modulatory compounds of the present invention can be used in treatment of an eating disorder, obesity, alcoholism or an alcohol-related disorder, drug abuse or addiction including addiction to cocaine, opiates, amphetamines, or nicotine, a sleep disorder, a cognitive dysfunction in a psychiatric or neurologic disorder, depression, anxiety, panic disorder, schizophrenia, alzheimer's disease, parkinson's disease, huntington's chorea, headache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases, cancer, hypertension, behavior disorder, mood disorder, manic depression, dementia, sex disorder, psychosexual disorder, or renal disease..
Eolas Therapeutics, Inc.
Androgen receptor antagonists
Disclosed herein are compositions and methods for modulating the androgen receptor.. .
The Regents Of The University Of California
Sweetness receptor antagonist
Wherein each symbol is described herein, are useful for the prophylaxis or treatment of metabolic syndrome, diabetes, obesity and the like.. .
Polyethylene glycol-modified integrin blocker hm-3 and use thereof
The present invention involves the pharmaceutical field, including integrin antagonists, which have the capacities of inhibiting angiogenesis of tumors, binding integrin. These antagonists are a kind of polypeptide, which was modified by polyethylene glycol and after modification, it can be used to treat tumors.
Chemical induction of lactation in prepubescent non-human mammals
The present invention describes a method of inducing lactation in non-human mammals by using a single administrations of an estrogen compound, a dopaminergic antagonist, and oxytocin. For example, the estrogen compound may be a long acting composition and is administered at least one week before the dopaminergic antagonist.
Compositions and methods for treating or preventing atrial fibrillation
The present invention provides compositions and methods for treating or preventing atrial fibrillation (af). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., m2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation..
Methods of treating diseases which are mediated by cutaneous lymphocyte antigen positive cells
The present invention relates to methods of treating patients suffering from itching and puritis mediated by cutaneous lymphocyte antigen positive t cell. In particular, diseases or disorders including contact dermatitis, drug induced delayed type cutaneous allergic reactions, toxic epidermal necrolysis, cutaneous t cell lymphoma, bullous pemphigoid, alopecia aereata, vitiligo, acne rosacea, prurigo nodularis, and herpes simplex virus, or combination thereof will benefit from the administration of an il-31 antagonist.
National Jewish Medical Research Center
Biomarkers related to interleukin-33 (il-33)-mediated diseases and uses thereof
The present invention relates to the identification of certain biomarkers for use in identifying patients who have, or are likely to develop an il-33 mediated disease or disorder and who are more likely to respond to therapy with an il-33 antagonist. The invention also relates to methods of treatment of an il-33-mediated disease or disorder in a patient by administering an il-33 antagonist to the patient in need thereof and monitoring the effectiveness of therapy using the biomarkers described herein.
Regeneron Pharmaceuticals, Inc.
Soluble tumor necrosis factor receptor treatment of medical disorders
The invention pertains to methods and compositions for treating medical disorders characterized by elevated levels or abnormal expression of tnfα by administering a tnfα antagonist, such as recombinant tnfr:fc.. .
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, Inc.
Antagonists acting at multiple prostaglandin receptors for the treatment of inflammation
Compounds, processes for their preparation, pharmaceutical compositions containing such compounds and their use in treating therapeutic conditions, in particular conditions mediated by the action of ligands on the fp, dp, ep1, ep4, ip, dp1, fp and tp prostaglandin (pg) receptors thereby providing a general anti-inflammatory response.. .
Pyrazole-substituted arylamides as p2x3 and p2x2/3 antagonists
Or a pharmaceutically acceptable salt thereof, wherein, r1 is optionally substituted pyrazolyl, 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..
Diamide compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
Or a pharmaceutically acceptable salt thereof. Such compounds possess both muscarinic receptor antagonist and β2 adrenergic receptor agonist activities.
Diaminopyrimidines as p2x3 and p2x2/3 antagonists
Or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein x is o, d, y, r1, r2, r3, r4, r5, r6, r7 and r8 are as defined herein.. .
Novel n-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective nk-3 receptor antagonists, pharmaceutical composition, methods for use in nk-3 receptor-mediated disorders
Or a pharmaceutically acceptable solvate thereof.. .
Heteroaryl sulfonamides and ccr2/ccr9
Compounds are provided that act as potent antagonists of the ccr2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for ccr2.
Distinguishing antagonistic and agonistic anti b7-h1 antibodies
Materials and methods for distinguishing agonistic anti-b7-h1 antibodies from antagonistic anti-b7-h1 antibodies, and for treating subjects diagnosed with clinical conditions such as cancer, pathogenic infection, or autoimmune disease.. .
Mayo Foundation For Medical Education And Research
Preventing, treating, and reducing (persistent) post-traumatic headache
Disclosed herein are methods of treating or reducing incidence of post-traumatic headache and/or at least one secondary symptom associated with post-traumatic headache in a subject comprising administering to the subject a monoclonal antibody that modulates the cgrp pathway. Compositions for use in the disclosed methods are also provided.
Teva Pharmaceuticals International Gmbh
Methods for treating osteoarthristis pain by administering a nerve growth factor antagonist and compositions containing the same
The invention concerns anti-ngf antibodies (such as anti-ngf antagonist antibodies), and polynucleotides encoding the same. The invention further concerns use of such antibodies and/or polynucleotides in the treatment and/or prevention of pain, including post-surgical pain, rheumatoid arthritis pain, and osteoarthritis pain..
Rinat Neuroscience Corp.
Novel crystal structure and ligand binding sites of trail receptor
A composition comprising a trail-r2 receptor or fragment thereof bound to a ligand in crystalline form is presently provided along with novel binding sites and binding agents of a trail receptor. Also provided are methods of designing a compound, protein or peptide and identifying a binding agent that interacts with a trail receptor.
La Jolla Institute For Allergy And Immunology
Glycoproteins having lipid mobilizing properties and therapeutic uses thereof
The invention provides formulations and methods for ameliorating symptoms associated with metabolic disorders, such as cachexia, hypoglycemia, obesity, diabetes, and the like by administering zn-α2-glycoproteins or a functional fragment thereof, alone or in combination with additional agents, such as β adrenergin receptor agonists, β adrenergin receptor antagonists, and/or glycemic control agents.. .
Triazolo[4,5-d] pyramidine derivatives and their use as purine receptor antagonists
Compounds of formula (i) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. Disclosed.
Vernalis (r&d) Limited
Method and composition for the treatment of opioid induced constipation
The invention relates to a method of treatment using a solid oral pharmaceutical dosage form comprising an opioid receptor antagonist for use in the treatment of opioid induced constipation comprising the opioid antagonist equivalent to 24 mg of naloxone hydrochloride as twice daily formulation or equivalent to 48 mg of naloxone hydrochloride as once daily formulation, characterized in that the opioid antagonist has a rapid first pass metabolism with a plasma half-life of 2 hours or less in humans within the first 3 hours of oral administration of a solution, wherein the steady state pharmacokinetics result in a constant level of naloxone in the bloodstream, wherein the pharmacokinetics are independent of whether the dosage is administered once or twice daily, wherein the oral dosage form releases the opioid antagonist in a prolonged manner, wherein the in vitro release rate of the opioid antagonist measured using the paddle stirrer method according to ph. Eur.
Develco Pharma Schweiz Ag
Method of modulating fibroblast accumulation or collagen deposition
The invention provides methods and compositions for reducing or preventing fibrosis in a subject suffering from a fibrotic disorder by administering a therapeutically effective amount of at least one antagonist to the cytokine thymic stromal lymphopoietin to the subject. In one embodiment, the methods and compositions further comprise administering at least one additional antagonist to an additional profibrotic cytokine, growth factor or chemokine..
Antagonist anti-cd40 monoclonal antibodies and methods for their use
Compositions and methods of therapy for treating diseases mediated by stimulation of cd40 signaling on cd40-expressing cells are provided. The methods comprise administering a therapeutically effective amount of an antagonist anti-cd40 antibody or antigen-binding fragment thereof to a patient in need thereof.
Novartis Vaccines And Diagnostics, Inc.
Anti-il-17 antibodies, producing same and using same
The present invention relates to the field of medicine, and specifically to the field of monoclonal antibodies against human il-17. More specifically, the invention relates to monoclonal antibodies/antagonists of il-17a, which bind with high affinity to an il-17 epitope, wherein the antibodies contain amino acid substitutions in hypervariable regions of heavy and light chains.
Closed Joint Stock Company "biocad"
Antagonist antibodies directed against calcitonin gene-related peptide and methods using same
The invention features methods for preventing or treating cgrp associated disorders such as vasomotor symptoms, including headaches (e.g., migraine, cluster headache, and tension headache) and hot flushes, by administering an anti-cgrp antagonist antibody. Antagonist antibody g1 and antibodies derived from g1 directed to cgrp are also described..
Teva Pharmaceuticals International Gmbh
Antagonists of bcl-2 and uses thereof in induction of apoptosis
The present invention provides an antagonist of a bcl-2 prosurvival 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.
Peptide antagonist of ll-37
This disclosure is related to the peptide antagonist of ll-37, an antimicrobial peptide that has multiple functions in both innate and adaptive immune response. Specifically, the identified peptide antagonists of ll-37 provide inhibition to detrimental autoimmune inflammatory response, whereas at the same time retain ll-37's antibacterial activity..
Janssen Biotech, Inc.
Inhibitor of apoptosis protein (iap) antagonists
Provided herein are compounds that modulate the activity of inhibitor of apoptosis proteins (iapb), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.. .
Sanford-burnham Medical Research Institute
Thiadiazole-substituted arylamides as p2x3 and p2x2/3 antagonists
Or a pharmaceutically acceptable salt thereof, wherein, r1 is optionally substituted thiadiazolyl, 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..
Prostaglandin receptor ep2 antagonists, derivatives, compositions, and uses related thereto
The disclosure relates to prostaglandin receptor ep2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which ep2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof..
P2x4 receptor antagonist
The present invention relates to a compound represented by the following general formula (i), which has a p2x4 receptor antagonistic activity (in the formula, r1, r2 and r3 represent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, a halogen atom, and the like, x represents c or n, y represents n or c(═o), provided that when x is c, y represents n, and when x is n, y represents c(═o), the double line consisting of the solid line and the broken line represents a single bond or double bond, n represents an integer of 0 to 6, z represents o, s, or an atomic bond, and a represents benzene ring, pyridine ring, and the like).. .
Compounds and compositions for the treatment of ocular disorders
The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.. .
Graybug Vision, Inc.
Methods and formulations for treating vascular eye diseases
The present invention provides methods for treating, preventing or reducing the severity of an eye disease. The methods of the present invention comprise administering to a subject in need thereof a therapeutic composition comprising an angiopoietin-2 (ang-2) inhibitor such as an anti-ang-2 antibody in combination with a vascular endothelial growth factor (vegf) antagonist (e.g., aflibercept)..
Regeneron Pharmaceuticals, Inc.
Method and composition of thyroid hormone analogues and nanoformulations thereof for treating anti-inflammatory disorders
Thyroid hormone antagonists and their nanoparticle formulations (nanotetrac™ or nanotriac™) act at a cell surface receptor to block angiogenesis and tumor cell proliferation. The complex anti-angiogenic performs actions on specific cytokines and chemokines.
Pharmaceutically Acceptable Salt
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