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This page is updated frequently with new Antagonist-related patent applications.




Date/App# patent app List of recent Antagonist-related patents
07/21/16
20160209426 
 Use of biomarkers for assessing treatment of gastrointestinal inflammatory disorders with beta7 integrin antagonists patent thumbnailnew patent Use of biomarkers for assessing treatment of gastrointestinal inflammatory disorders with beta7 integrin antagonists
Methods of assessing or monitoring the effect, efficacy, responsiveness to treatment, and/or determining a dose or dosing regimen of therapeutic agents, such as integrin beta7 antagonists, for the treatment of gastrointestinal inflammatory disorders are provided. In certain aspects, methods of using integrin beta7 subunit-containing receptor occupancy by the integrin beta7 antagonist on colonic lymphocytes as an indicator (“biomarker”) of the effect, efficacy, or responsiveness to treatment, and/or as a means to determine dosing or dosing regimens of therapeutic agents such as beta7 integrin antagonists for the treatment of gastrointestinal inflammatory disorders are provided.
Genentech, Inc.


07/21/16
20160208215 
 Generation of endocrine progenitor cells from human pluripotent stem cells using small molecules patent thumbnailnew patent Generation of endocrine progenitor cells from human pluripotent stem cells using small molecules
The present invention relates to differentiation of stem cells into a homogeneous endocrine progenitor cell population suitable for further differentiation into pancreatic beta-cells. The present invention provides methods for obtaining ngn3/nkx2.2 double positive endocrine progenitor cells by exposing precursor cells to a tgf-β type i receptor inhibitor, a bmp antagonist, an adenylate cyclase activator and nicotinamide and/or exposing to the precursor cells to a selection of small molecules..
Takara Bio Europe Ab


07/21/16
20160208004 
 Il-17ra-il-17rb antagonists and uses thereof patent thumbnailnew patent Il-17ra-il-17rb antagonists and uses thereof
The present invention relates to interleukin-17 ligand and receptor family members and the discovery that il-17 receptor a and il-17 receptor c form a heteromeric receptor complex that is biologically active. Antagonists of the il-17ra-il-17rb heteromeric receptor complex are disclosed, as well as various methods of use..
Amgen Inc.


07/21/16
20160207930 
 Novel neurokinin 1 receptor antagonist compounds ii patent thumbnailnew patent Novel neurokinin 1 receptor antagonist compounds ii
The invention relates novel nk1 receptor antagonists represented in formula a, wherein r1 and r2 independently are selected from the group consisting of (c1-4)alkyl, (c1-4)haloalkyl, (c1-4)alkoxy, cd3 or halogen; r3 is selected from the group consisting of hydrogen, (c1-4)alkyl, (c1-4)haloalkyl and (c1-4)hydroxyalkyl; r4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; r5 and r6 are independently selected from the group consisting of hydrogen, (c1-4)alkyl, (c1-4) hydroxyalkyl and (c1-4)haloalkyl and x and y are independently selected from the group consisting of ch and n. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds..
Leo Pharma A/s


07/21/16
20160207891 
 Malignant and non-malignant disease treatment with ras antagonists patent thumbnailnew patent Malignant and non-malignant disease treatment with ras antagonists
The present disclosure describes new inhibitors or antagonists of ras useful for the treatment of conditions resulting from ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition.
Pisces Therapeutics, Llc


07/21/16
20160207880 
 Amide derivatives as lysophosphatidic acid receptor antagonists patent thumbnailnew patent Amide derivatives as lysophosphatidic acid receptor antagonists
Wherein r1, x, m, r2, y, r3, z, n, r4, a and b are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.. .

07/21/16
20160207194 
 Stabilization system for robotic technology patent thumbnailnew patent Stabilization system for robotic technology
A motor control system to be applied to robotic technology, the motor control system comprising at least two actuators that each include a first receiver and a second receiver. The system is comprised of a movement control system that communicates a first signal to the first receivers, the first signal indicative of a movement profile; and a stabilization control system that communicates a second signal to the second receivers, the second signal indicative of a stabilizing profile.

07/21/16
20160206679 
 Materials and methods for modulating disc1 turnover patent thumbnailnew patent Materials and methods for modulating disc1 turnover
The invention relates to the finding that turnover of disc1 (disrupted in schizophrenia 1) is mediated by the f-box-containing protein fbxw7 (f-box/wd repeat-containing protein 7). The sequence within disc1 that binds to fbxw7 and targets disc1 for turnover by the ubiquitin-proteasome system is identified.
The University Court Of The University Of Glasgow


07/21/16
20160206610 
 Methods for treating and/or preventing emesis and/or nausea including acute and/or delayed nausea and/or acute emesis and/or delayed emesis patent thumbnailnew patent Methods for treating and/or preventing emesis and/or nausea including acute and/or delayed nausea and/or acute emesis and/or delayed emesis
Methods for treating and/or preventing nausea and emesis including acute and/or delayed nausea and/or acute and/or delayed emesis in a subject are provided herein. The methods include administering to the subject in need thereof a therapeutically effective amount of a 5ht3 antagonist or a pharmaceutical composition thereof by nasal inhalation and/or oral inhalation..
Xoc Pharmaceuticals, Inc.


07/21/16
20160206593 
 Pharmaceutical for prophylaxis or treatment of hypertension patent thumbnailnew patent Pharmaceutical for prophylaxis or treatment of hypertension
A pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension. The pharmaceutical is characterized by comprising (i) a specific mineralocorticoid receptor antagonist and (ii) one or more components selected from the following components (a) to (c), for administration simultaneously or separately at a time interval: (a) an angiotensin ii receptor antagonist, (b) a calcium antagonist, and (c) a diuretic..
Daiichi Sankyo Company, Limited


07/14/16
20160201060 

Immune regulatory oligonucleotide (iro) compounds to modulate toll-like receptor based immune response


The invention provides immune regulatory oligonucleotides (iro) as antagonist of tlrs and methods of use thereof. These iros have unique sequences that inhibit tlr-mediated signaling in response to a tlr ligand or tlr agonist.
Idera Pharmaceuticals, Inc.


07/14/16
20160200818 

Methods of treating sporadic inclusion body myositis


The disclosure relates to the treatment of sporadic inclusion body myositis and other muscle wasting disorders with novel regimens, which employ a therapeutically effective amount of a myostatin antagonist, e.g., a myostatin binding molecule, e.g., a myostatin antibody or an actrii receptor binding molecule, an actrii receptor antibody, such as the bimagrumab antibody.. .
Novartis Ag


07/14/16
20160200808 

Method of treatment


A protocol for pain management includes a pharmaceutical composition and its use in ameliorating the sensation of pain. The protocol includes the use of a ccl17 signaling antagonist alone or in combination with another analgesic compound to treat pain associated with inflammatory conditions.
The University Of Melbourne


07/14/16
20160200718 

New cyclohexylamine derivatives having ß2 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.


07/14/16
20160200715 

Preparation and use of 7a-heterocycle substituted- 6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists


And the remaining variables are described herein. The compounds of the invention are effective inhibitors of the par-1 receptor.

07/14/16
20160200713 

Preparation and use of 3-pyridyl substituted- 6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists


The compounds of the invention are effective inhibitors of the par-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as asc, secondary prevention of myocardial infarction or stroke, or pad..

07/14/16
20160199949 

Positioner for tubes


Roller positioner for tubes comprising: a base structure; two lower support rollers rotating around respective axes positioned on said base structure; and an upper roller antagonist to said two lower support rollers; characterized by comprising a deformable quadrilateral for the movement of said upper roller suited for moving said upper roller along a rectilinear axis by a predetermined distance and then away from said rectilinear axis.. .
A. Narducci S.p.a.


07/14/16
20160199488 

Combination therapy for neoplasia treatment


The present invention relates to an insulin-like growth factor (igf) receptor antagonist for use in the treatment of prostate neoplasia, including benign prostatic hyperplasia (bph), prostate cancer, and particularly crpc, wherein the antagonist is used in combination with an androgen receptor antagonist. An embodiment of the invention is where the androgen receptor antagonist is enzalutamide..
Boehringer Ingelheim International Gmbh


07/14/16
20160199487 

Modulation of tumor immunity


Methods of treating proliferative disorders are described. In particular, combination treatment with a gitr agonist and a pd-1 antagonist are provided..
Merck Sharp & Dohme Corp.


07/14/16
20160199458 

Methods of promoting fat loss comprising administering an alk7 inhibitor


The invention relates to alk7 soluble receptors and their uses as antagonists of the function of certain ligands such as gdf-8 (myostatin) and gdf-11. The alk7 soluble receptor of the invention is useful as antagonists of gdf-8 and gdf-11 in the treatment of neuronal diseases or conditions such as stroke, spinal cord injury, and all peripheral nerve diseases.
Acceleron Pharma Inc.


07/14/16
20160199364 

Seizure treatment compositions and methods


A composition, a method for administering an anti-seizure composition, and a method for treating a seizure are described. In an implementation, a composition comprises a peroxisome proliferator activated receptor gamma (pparγ) antagonist that is administered to an individual, where the individual has been administered a ketogenic diet.
Creighton University


07/14/16
20160199309 

Nanoparticle and polymer formulations for thyroid hormone analogs, antagonists, and formulations and uses thereof


Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric nanoparticle form of thyroid hormone agonist, partial agonist or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Nanoparticle forms of thyroid hormone or thyroid hormone analogs as well as uses thereof are also disclosed..
Nanopharmaceuticals Llc


07/14/16
20160198654 

Growth of cryo-sprouts


The present description relates to cryo-sprouts that have been germinated, grown and shipped in the same container. Seeds are placed on a membrane in the container with sufficient water.
The Vista Institute Llc


07/07/16
20160194401 

Therapeutic agent for chronic arthritides diseases of childhood-related diseases


A therapeutic agent for chronic arthritides diseases of childhood-related diseases, for example chronic arthritides diseases of childhood, still's disease and the like, comprising an interleukin-6 (il-6) antagonist as an active ingredient.. .
Chugai Seiyaku Kabushiki Kaisha


07/07/16
20160194330 

Piperazine-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties


Disclosed are compounds of formula a: (structurally represented) where “rg1”, “rg2a”, “rg4”, “rg5”, “mg1”, “n” and “m” are defined herein which compounds are antagonists of a2a receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the a2a receptor in the potential treatment or prevention of neurological disorders and diseases in which a2a receptors are involved.
Merck Sharp & Dohme Corp.


07/07/16
20160194292 

Triazolone compounds and uses thereof


The invention disclosed herein is directed to compounds of formula (1a) and (1b) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocyticδ leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of formula (1a) or (1b), or a pharmaceutically acceptable salt thereof.
Inception 2, Inc.


07/07/16
20160193334 

Treating cancer with a combination of a pd-1 antagonist and dinaciclib


The present disclosure describes combination therapies comprising an antagonist of programmed death 1 receptor (pd-1) and the cdk inhibitor dincaciclib, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express pd-l1.. .
Merck Sharp & Dohme Corp.


07/07/16
20160193333 

Methods of treating generalized pustular psoriasis (gpp) using il-17 antagonists


The disclosure is directed to methods, treatment regimens, uses, kits and therapies for treating generalized pustular psoriasis (gpp). These methods, treatment regimens, uses, kits and therapies utilize, inter alia, administration of an il-17 antagonist, e.g., an il-17 antibody, such as secukinumab.
Novartis Ag


07/07/16
20160193294 

Compositions comprising e-selectin antagonists and uses therefor


This invention discloses the use of an e-selectin antagonist and a mobilizer of hematopoietic stem cells or progenitor cells in methods and compositions for treating or preventing immunocompromised conditions resulting from medical treatment. The present invention is particular relevant for prophylaxis and/or treatment of hematopoeitic disorders including neutropenia, agranulocytosis, anemia and thrombocytopenia in individuals receiving or proposed to receive treatments that target rapidly dividing cells or that disrupt the cell cycle or cell division..
The University Of Queensland


07/07/16
20160193285 

Oral octreotide administered in combination with other therapeutic agents


This invention relates to combination therapy of a subject suffering from acromegaly. The method of treatment comprises administration to the subject of a therapeutically effective amount of oral somatostatin receptor ligand (srl) e.g.
Chiasma Inc.


07/07/16
20160193238 

Hnf4-alpha antagonist and use thereof


Provided is a hepatocyte nuclear factor 4 alpha (hnf4-α) antagonist and a use thereof. The hnf4-α antagonist selected in the present invention was confirmed to specifically bind to the ligand binding domain of hnf4-α, thereby inhibiting the activity of hnf4-α.
National Cancer Center


07/07/16
20160193196 

Immediate-release tablet formulations of a thrombin receptor antagonist


Immediate-release formulations for oral administration of a thrombin receptor antagonist are provided. Certain formulations of higher api loading demonstrate sufficient moisture uptake after storage at stressed conditions to retard dissolution.
Merck Sharp & Dohme Corp.


07/07/16
20160193191 

Antagonists of chemokine receptors


Compounds are provided that act as potent antagonists of the ccr1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of ccr1-mediated diseases, and as controls in assays for the identification of competitive ccr1 antagonists..
Chemocentryx, Inc.


07/07/16
20160193190 

Targeting metabolic adaptive responses to chemotherapy


Methods for targeting adaptive responses to chemotherapy are described. In various embodiments, a method comprises administering at least one compound that inhibits s6k1, mtorc1 or upstream or downstream pathway components of s6k1 or mtorc1, in association with administration of at least one inhibitor of pparα, pparδ, or pgc1α.
University Of Cincinnati


07/07/16
20160193185 

Diazole amides


Compounds are provided that act as potent antagonists of the ccr1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of ccr1-mediated disease, and as controls in assays for the identification of competitive ccr1 antagonists..
Chemocentryx, Inc.


07/07/16
20160193168 

Treatment of pulmonary arterial hypertension with leukotriene inhibitors


Pulmonary arterial hypertension (pah) can be prevented in persons susceptible to the diseases and pah patients can be treated by administering an effective dose of a leukotriene inhibitor. Suitable inhibitors include leukotriene a4 hydrolase (lta4h) inhibitors, leukotriene b4 receptor (blt1/blt2) antagonists, 5-lipoxygenase (5-lo) inhibitors, and 5-lipoxgygenase activating protein (flap) inhibitors..
The Board Of Trustees Of The Leland Stanford Junior University


06/30/16
20160188904 

Method and system of privacy protection in antagonistic social milieu/dark privacy spots


An efficient and robust system 100 of privacy protection to provide security of a computing device by identifying and detecting unauthorized intrusion/peek problems related to computing device's environment/surrounding is disclosed. The system 100 includes a detector unit 102 for detecting data related to environment/surrounding of the computing device; a processing unit 104 for processing the detected data and a recommendation unit 106 to notify the user about the threat posed by environment/surrounding.

06/30/16
20160185872 

Compositions and methods for treating bone conditions


A method of treating a degenerative bone condition of a subject includes administering to hematopoietic progenitor cells or osteoclast progenitor cells of the subject at least one agent that substantially reduces the interaction of at least one of c3a or c5a with the c3a receptor (c3ar) and/or c5a receptor (c5ar), a stat3/il-6 signaling pathway antagonist, and a combination thereof, the agent being administered to the hematopoietic progenitor cells or osteoclast progenitor cells at an amount effective to inhibit osteoclast differentiation of hematopoietic progenitor cells or osteoclast progenitor cells.. .

06/30/16
20160185868 

Osteoarthritis treatment


The present invention relates generally to a method for the treatment and/or prophylaxis of osteoarthritis (oa). In accordance with the present invention, an antagonist of gm-csf can be effective in the treatment of osteoarthritis.

06/30/16
20160185867 

Use of c-fms antagonists


The present invention relates generally to a method for the treatment and/or prophylaxis of osteoarthritis (oa) and/or pain. In accordance with the present invention, an antagonist of c-fms is effective in the treatment of osteoarthritis and/or pain.

06/30/16
20160185866 

Methods for treating chronic sinusitis with nasal polyps by administering an il-4r antagonist


The present invention provides methods for decreasing a nasal polyp score in a subject. 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..

06/30/16
20160185864 

Methods of treating fgfr3 related conditions


Provided herein are biomarkers and therapies for the treatment of pathological conditions, such as cancer, and method of using fgfr3 antagonists. In particular, provided is fgfr3 as a biomarker 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..

06/30/16
20160185845 

Methods and compositions for the treatment and diagnosis of diseases characterized by vascular leak, hypotension, or a procoagulant state


Disclosed herein are methods for treating a vascular leak disorder, hypotension, or a procoagulant state using angiopoietin-2 (ang-2) antagonist compounds. Also disclosed are methods for treating a vascular leak disorder associated with high dose il-2 therapy using angiopoietin-2 antagonist compounds.

06/30/16
20160185843 

Treating alcohol-mediated disorders by inhibition of rgs6


The invention provides rgs6 antagonists and methods for their use in treating the effects of alcohol consumption.. .

06/30/16
20160185842 

14-3-3 antagonists for the prevention and treatment of arthritis


The invention provides compositions and methods for treating arthritis.. .

06/30/16
20160185801 

5-ht3 receptor antagonists


That are 5ht3 receptor antagonists and are therefore useful for the treatment of diseases treatable by inhibition of 5ht3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and gi disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds..

06/30/16
20160185768 

Thiazole orexin receptor antagonists


The present invention is directed to thiazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the thiazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.

06/30/16
20160185764 

Preparation and use of 7a-amide substituted- 6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists


And the remaining variables are described herein. The compounds of the invention are effective inhibitors of the par-1 receptor.

06/30/16
20160185756 

Substituted benzimidazoles and benzopyrazoles as ccr(4) antagonists


Benzimidazole, benzopyrazole and benzotriazole 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.. .

06/30/16
20160184383 

Method of treating cancer


The present invention provides a method of treating cancer in a subject wherein the method comprising administering to the subject an iap antagonist and a p38 and/or a mk2 inhibitor.. .

06/30/16
20160184339 

Compounds, compositions and methods using e-selectin antagonists for mobilization of hematopoietic cells


Methods are provided herein for use of e-selectin antagonists for mobilizing cells, such as hematopoietic cells, hematopoietic stem cells and progenitor cells, white blood cells, and malignant cells, and hematopoietic tumor cells from the bone marrow. More specifically, methods are provided for using e-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers, and peptides for mobilizing cells from the bone marrow to the peripheral vasculature and tissues..

06/30/16
20160184294 

Nasal drug products and methods of their use


Drug products adapted for nasal delivery, comprising a pre-primed device filled with a pharmaceutical composition comprising an opioid receptor antagonist, are provided. Methods of treating opioid overdose or its symptoms with the inventive drug products are also provided..

06/30/16
20160184265 

Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders


In which n, m, x, y1, r1, r2, r3, r4 and r5 are defined in the summary of the invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity..

06/30/16
20160183606 

Resistance exercise clothing


A method and apparatus for exercising a muscle in a given agonist and antagonist muscle pair of a user's human body by providing an elongated elastic band having a first length when no external forces are applied thereto, elongating the elastic band to a second length that is greater than the first length, securing the elastic band to a garment in a manner whereby when the elastic band is installed on the garment an axial force is imposed on the body of the user and the elastic band is disposed in aligned proximate relationship with at least one of the muscles in a given pair of muscles comprising an agonist muscle and antagonist muscle pair.. .

06/23/16
20160176974 

Method for treating joint damage


Methods of treating joint damage in a subject eligible for treatment are provided involving administering an antagonist that binds to a b-cell surface marker, such as cd20 antibody, to the subject in an amount effective to slow progression of the joint damage as measured by radiography. Further provided are articles of manufacture useful for such methods..

06/23/16
20160176972 

Prion protein as a receptor for amyloid-beta oligomers


The invention provides methods of inhibiting suppression of long term potentiation, improving acute memory retention and spatial memory performance and treating alzheimer's disease by administration of a prpc antagonist or combinations thereof. Additionally, this invention provides pharmaceutical kits comprising, and methods for making and using, such combinations, as well as methods of identifying molecules that could function as prpc antagonists..

06/23/16
20160176871 

Tgf beta r antagonists


The invention relates generally to compounds that modulate the activity of tgfβr-1 and tgfβr-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.. .

06/23/16
20160176863 

8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists


Wherein r1, r2, r3, a, and g are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds..

06/23/16
20160176858 

Oxazole orexin receptor antagonists


The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.

06/23/16
20160176851 

Antagonists of prostaglandin ep3 receptor


Provided herein are antagonists of prostaglandin ep3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.. .

06/23/16
20160176841 

Selectively substituted quinoline compounds


Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (sle) and lupus nephritis.. .

06/23/16
20160176831 

11-oxo-10,11-dihydrodibenzo[b,f][1,4]thiazepine s-oxide derivatives and their use as dopamine d2 receptor antagonists


The disclosure includes compounds and pharmaceutically acceptable salts of formula (i). Certain compounds and salts of formula (i) are selective inhibitors of the dopamine d2 receptor.

06/23/16
20160176816 

Novel biphenyl derivative and preparing same


The present invention provides novel biphenyl derivatives, isomers thereof, or pharmaceutically acceptable salts thereof, methods for preparing the same, and a pharmaceutical composition containing the same. The novel biphenyl derivatives, isomers thereof, or pharmaceutically acceptable salts thereof, as disclosed in the present invention, act as muscarinic m3 receptor antagonists, and thus are useful for the prevention or treatment of a disease selected from the group consisting of chronic obstructive pulmonary disease, asthma, irritable bowel syndrome, urinary incontinence, rhinitis, spasmodic colitis, chronic cystitis, alzheimer's disease, senile dementia, glaucoma, schizophrenia, gastroesophageal reflux disease, cardiac arrhythmia, and hyper-salivation syndromes..

06/23/16
20160175485 

Combination therapy to promote wound healing


Methods for increasing and/or promoting wound healing, wound re-epithelialization and dermal regeneration of epithelial tissues and cutaneous wounds by administration to a subject of an extracellular matrix scaffold or scaffold for dermal regeneration (sdr) populated with beta adrenergic receptor antagonist pre-conditioned mesenchymal stem cells (mscs) are provided. Compositions and kits comprising an extracellular matrix scaffold (ecms) populated with beta adrenergic receptor antagonist pre-conditioned mesenchymal stem cells (mscs) are also provided..

06/23/16
20160175439 

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..

06/23/16
20160175328 

Compositions and treatments of heart failure in non-human mammal animals


The invention relates to new compositions comprising an aldosterone antagonist according to a particular posology for the treatment of heart failure in non-human mammal animals.. .

06/23/16
20160175308 

Therapeutic agents for modulating thymic function and/or growth and/or treating various disorders


The present disclosure relates to a therapeutic agent for use in a method for modulating the function and/or growth of a thymus in a subject, wherein the therapeutic agent comprises an her2 or her1 pathway antagonist or agonist, and/or a ccr/ccl5 antagonist the method involving administering the therapeutic agent to the subject. Also disclosed herein is a therapeutic agent for use in a method for treating a disorder in a subject, the disorder selected from systemic autoimmunity, peripheral autoimmunity and systemic lupus erythematosus,.

06/23/16
20160175295 

Combinations comprising maba compounds and corticosteroids


A combination which comprises (a) corticosteroid and (b) a dual muscarinic antagonist-β2 adrenergic agonist compound, or any pharmaceutically acceptable salt or solvate thereof.. .

06/23/16
20160175283 

Oxytocin receptor antagonist therapy in the luteal phase for implantation and pregnancy in women undergoing assisted reproductive technologies


The present invention relates to the use of an oxytocin receptor antagonist in females undergoing embryo transfer as part of an assisted reproductive technology. In particular, methods are provided for increasing ongoing implantation rate, increasing ongoing pregnancy rate, increasing clinical pregnancy rate, and/or increasing live birth rate in a female subject undergoing embryo transfer.

06/23/16
20160175266 

Nmda receptor antagonist formulation with reduced neurotoxicity


The present invention is directed to pharmaceutical compositions of effective amounts of nmda receptor antagonists and preservative for the administration to a patient in need of effective analgesia and anesthesia. The compositions of the invention advantageously do not cause any significant neurotoxicity.

06/16/16
20160169918 

Methods of diagnosis and treatment for pulmonary arterial hypertension


Diagnostic and therapeutic agents for pulmonary arterial hypertension (pah) are provided. Circulating microparticles (mps) and/or the expression level of gpr75 are significantly increased in pah-pasmc, but not normal pasmc, thus, providing a non-invasive diagnostic method for pah.
The Regents Of The University Of California


06/16/16
20160168640 

Therapeutic and diagnostic methods for il-33-mediated disorders


The invention relates to methods of treating a patient suffering from an il-33-mediated disorder, such as asthma, comprising administering to the patient an il-33 axis binding antagonist based on the genotype of the il1rl1 gene. The invention further relates to methods of determining whether a patient is at increased risk of an il-33-mediated disorder, as well as methods of determining whether a patient suffering from such a disorder is likely to respond to a treatment comprising an il-33 axis binding antagonist, based on the genotype of the il1rl1 gene..
Genentech, Inc.


06/16/16
20160168252 

Antibodies, compounds and derivatives thereof for use in the treatment of male infertility


The present invention relates to antagonists or inhibitors, which bind selectively to rankl/opgbp and regulate the interaction between rankl/opgbp and rank/opg. In particular, the present invention relates to an antibody or antigen binding domain, fragment or derivative thereof, immunoreactive with a rankl/opgbppeptide for use in the treatment, prevention or alleviation of male infertility or reduced male fertility such as oligospermia or azospermia..
Rigshopitalet Copenhagen University Hospital


06/16/16
20160168244 

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..
Labrys Biologics, Inc.


06/16/16
20160168243 

Antagonists to il-6 to raise albumin and/or lower crp


The present invention is directed to therapeutic methods using il-6 antagonists such as antibodies and fragments thereof having binding specificity for il-6 to improve survivability or quality of life of a patient in need thereof. In preferred embodiments these patients will comprise those exhibiting (or at risk of developing) an elevated serum c-reactive protein level or a reduced serum albumin level prior to treatment.
Alderbio Holdings Llc


06/16/16
20160168240 

Use of vegf antagonist in treating chorioretinal neovascular and permeability disorders in paediatric patients


The present invention relates to the use of a vegf antagonist in the treatment of chorioretinal neovascular or permeability disorders in children. In particular, the invention provides a vegf antagonist for use in a method for treating a child having cnv or me, wherein said method comprises administering to the eye of a child a vegf antagonist that either does not enter or is rapidly cleared from the systemic circulation.

06/16/16
20160168090 

Novel indole derivatives and their use in neurodegenerative diseases


The present invention relates to indole compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of p2x7, and for the treatment of p2x7-related disorders.. .
Merck Patent Gmbh


06/16/16
20160166685 

Combination therapy comprising ox40 binding agonists and pd-1 axis binding antagonists


The invention provides compositions and methods for treating cancers. The method comprises administering a pd-1 axis binding antagonist and an ox40 binding agonist..
Genentech, Inc.


06/16/16
20160166684 

Treatment of fibrotic diseases


The present invention relates to rspo and lgr antagonists, and methods of using the rspo and lgr antagonists for treating or preventing fibrotic diseases.. .
Oncomed Pharmaceuticals, Inc.


06/16/16
20160166652 

Novel n- and c-terminal substituted antagonistic analogs of gh-rh


There is provided a novel series of synthetic analogs of hgh-rh(1-29)nh2 (seq id no: 1) and hgh-rh(1-30)nh2. Of particular interest are those carrying phac, n-me-aib, dca, ac-ada, fer, ac-amc, me-nh-sub, phac-ada, ac-ada-d-phe, ac-ada-phe, dca-ada, dca-amc, nac-ada, ada-ada, or ch3—(ch2)10—co-ada, at the n-terminus and β-ala, amc, apa, ada, ae2a, ae4p, ε-lys(α-nh2), agm, lys(oct) or ahx, at the c-terminus.
U.s.a., Represented By The Department Of Veterans Affairs


06/16/16
20160166590 

Compositions comprising rank/rankl antagonists and related compounds for treating pain


Disclosed herein are methods of treating pain using comprising rank/rankl antagonists.. .
Antecip Bioventures Ii Llc


06/16/16
20160166566 

Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1h)-one derivatives having both muscarinic receptor antagonist and beta2 adrenergic receptor agonist activities


The present invention is directed to crystalline addition salts of (ii) 8-hydroxyquinolin-2(1h)-one derivatives and (ii) a dicarboxylic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.. .
Almirall, S.a.


06/16/16
20160166555 

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


06/16/16
20160166506 

Method and system for the treatment of chronic obstructive pulmonary disease with nebulized anticholinergic administrations


A method is provided for improving lung function in copd by administering a muscarinic antagonist with a high efficiency nebulizer.. .
Sunovion Respiratory Development Inc.


06/16/16
20160166503 

Nasal drug products and methods of their use


Drug products adapted for nasal delivery, comprising a pre-primed device filled with a pharmaceutical composition comprising an opioid receptor antagonist, are provided. Methods of treating opioid overdose or its symptoms with the inventive drug products are also provided..
Lightlake Therapeutics, Inc.


06/09/16
20160161494 

Methods and compositions for treating and diagnosing diseases


Methods and compositions for diagnosing and treating diseases, particularly cancer, associated with differential expression of cancer-associated targets (cat) in disease cells compared to healthy cells are provided. Also provided are antagonists and agonists of cat, and methods for screening agents that modulate cat level or activity in vivo or in vitro..
Celera Corporation


06/09/16
20160160213 

Methods of treating cancer and preventing cancer drug resistance


Provided herein are methods of treating and/or preventing cancer drug resistance using modulators of chromatin modifiers (e.g., antagonists of chromatin modifiers) described herein.. .
Genentech, Inc.


06/09/16
20160159927 

Identification of vsig8 as the putative vista receptor (v-r) and use thereof to produce vista/vsig8 agonists and antagonists


The receptor for vista is identified (vsig8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of vsig8 and/or vista and/or the vsig8/vista binding interaction. These antagonists may be used to suppress vista's suppressive effects on t cell immunity, and more particularly used in the treatment of cancer, or infectious disease.
Immunext, Inc.


06/09/16
20160159914 

Il-17 receptor a is required for il-17c biology


The present invention relates to interleukin-17 ligand and receptor family members and the discovery that il-17 receptor a and il-17 receptor e form a heteromeric receptor complex that is biologically active, and that il-17c activity requires the il-17ra-il-17re heteromeric receptor complex. Antagonists of the il-17ra-il-17re heteromeric receptor complex are disclosed, as well as various methods of use..
Amgen Inc.


06/09/16
20160159893 

Use of a vegf antagonist in treating retinopathy of prematurity


The present invention relates to the use of a vegf antagonist in the treatment of retinal neovascular disorders in infants. In particular, the invention provides a method for treating an infant having retinopathy of prematurity (rop), wherein said method comprises administering to the eye of an infant a vegf antagonist that either does not enter or is rapidly cleared from the systemic circulation.

06/09/16
20160159878 

Nogo receptor antagonists


Disclosed are immunogenic nogo receptor-1 polypeptides, nogo receptor-1 antibodies, antigen-binding fragments thereof, soluble nogo receptors and fusion proteins thereof and nucleic acids encoding the same. Also disclosed are nogo receptor antagonist polynucleotides.
Biogen Ma Inc.


06/09/16
20160159875 

Targeting of cytokine antagonists


The present invention relates to a fusion protein, comprising a cytokine antagonist and a targeting moiety, preferably an antibody or anti-body like molecule. In a preferred embodiment, the cytokine antagonist is a modified cytokine which binds to the receptor, but doesn't induce the receptor signalling.
Centre Hospitalier Regional Universitaire De Montpellier


06/09/16
20160159862 

Novel a4b7 peptide monomer and dimer antagonists


The invention relates to peptide dimer compounds and peptide monomer compounds that potently inhibit binding of α4β7 to the mucosal addressin cell adhesion molecule (madcam) in vivo, possess high selectivity against α4β1 binding, and have high stability under gastrointestinal conditions.. .
Protagonist Therapeutics, Inc.


06/09/16
20160159790 

Pyrroloquinoline derivatives as 5-ht6 antagonists, preparation method and use thereof


This invention concerns pyrroloquinoline derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, parkinson's disease, huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, irritable bowel syndrome.
Universite De Montpellier


06/09/16
20160159779 

Co-crystal of the par-1 receptor antagonists vorapaxar and asprin


This invention relates to a co-crystal of vorapaxar and aspirin. The inventive co-crystal antagonizes the par-1 receptor.
Merck Sharp & Dohme Corp.


06/09/16
20160159744 

Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2-negative allosteric modulators, compositions, and their use


Wherein ring a, rq, -l-, r1, n, r2, and r3 are as defined herein. The compounds of the invention are useful as non-competitive mglur2 antagonists, or mglur2 negative allosteric modulators (nams), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mglur2-nam receptor is involved, including potentially alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.

06/09/16
20160158360 

Methods and compositions for treating cancer using pd-1 axis antagonists and hpk1 antagonists


Compositions and methods for enhancing an immune response and treating cancer are provided. Compositions comprise pd-1 axis antagonists and hpk1 antagonists.
Genentech, Inc.


06/09/16
20160158325 

Method of treating fibroproliferative disorders including dupuytren's disease with one or more specific human matrix metalloproteinase and a tnf antagonist


The subject invention also provides a method of treating a subject afflicted with a fibroproliferative disorder comprising periodically administering to the patient an amount of one or more human matrix metalloproteinase, wherein the one or more human matrix metalloproteinase are selected from human metalloproteinase-1 (mmp-1), human metalloproteinase-2 (mmp-2), human metalloproteinase-3 (mmp-3), human metalloproteinase-7 (mmp-7), human metalloproteinase-8 (mmp-8), human metalloproteinase-9 (mmp-9), human metalloproteinase-10 (mmp-10), human metalloproteinase-11 (mmp-11), metalloproteinase-12 (mmp-12), and human metalloproteinase-13 (mmp-13), and wherein the amount is effective to treat the subject. In an embodiment, the invention further comprises periodically administering to the subject an amount of tnf antagonist, wherein the amount of one or more the human matrix metalloproteinase and the amount of tnf antagonist when taken together are effective to treat the subject..
180 Therapeutics Lp


06/09/16
20160158236 

Pharmaceutical composition comprising a trpa1 antagonist and a steroid


The present patent application relates to a pharmaceutical composition comprising a transient receptor potential ankyrin-1 receptor (“trpa1”) antagonist and a glucocorticoid.. .
Glenmark Pharmaceuticals S.a.


06/09/16
20160158222 

Combinations of opioid/tlr4 antagonist and a cyclooxygenase (cox) inhibitor for use in the treatment of pain


Disclosed are compositions for treatment of pain comprising a first compound and a second compound, the first compound is an opioid antagonist that treats pain by blocking toll-like receptor 4 (tlr4) and the second compound is a cyclooxygenase (cox) inhibitor that enhances the pain treatment effect of the first compound. Examples of opioid antagonist include naltrexone and naloxone.
Allodynic Therapeutics, Inc.


06/09/16
20160158217 

Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2-negative allosteric modulators, compositions, and their use


Wherein ring a, rq, -l-, r1, n, r2, and r3 are as defined herein. The compounds of the invention are useful as non-competitive mglur2 antagonists, or mglur2 negative allosteric modulators (nams), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mglur2-nam receptor is involved, including potentially alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.

06/09/16
20160158211 

Dosage and use of an a2a antagonist


The present invention relates to specific dosages of an a2a antagonist for use as a medicament and in particular useful for the treatment of parkinson disease and attention deficit/hyperactivity disorder.. .
H. Lundbeck A/s


06/09/16
20160158204 

Pharmacological stimulation to facilitate and restore standing and walking functions in spinal cord motor disorders


The invention relates to the selective targeting of specific α2 adrenergic receptor subtypes for facilitating and also restoring standing and walking in a subject affected by spinal cord disorders, in particular spinal cord injury. In particular, the improvement of locomotion by targeting specific receptor subtypes can be achieved by stimulation of the α2c receptor subtype using an α2c specific agonist or by blocking the α2a receptor subtype using α2a antagonists.
Ecole Polytechnique Federale De Lausanne (epfl)


06/09/16
20160158198 

Compositions and methods for ameliorating cachexia


The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (nsaid), an angiotensin-converting enzyme (ace) inhibitor, an angiotensin receptor blocker (arb), an anabolic steroid, a natural oil or fatty acid or any combination thereof..
Vicus Therapeutics Llc


06/09/16
20160158136 

Composition for reduction of trpa1 and trpv1 sensations


A personal care composition and method of using a personal care composition having menthol and/or hydrogen peroxide and a trpa1 and/or trpv1 receptor antagonists.. .
The Procter & Gamble Company




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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