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Antagonist

Antagonist-related patent applications - as published by the U.S. Patent and Trademark Office (USPTO).


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Molecular flux rates through critical pathways measured by stable isotope labeling in vivo, as biomarkers ...
The Regents Of The University Of California
December 07, 2017 - N°20170350903

The methods described herein enable the evaluation of compounds on subjects to assess their therapeutic efficacy or toxic effects. The target of analysis is the underlying biochemical process or processes (i. E., metabolic process) thought to be involved in disease pathogenesis. Molecular flux rates within the one or more biochemical processes serve as biomarkers and are quantitated and compared with ...
Methods and compositions for treating and diagnosing diseases
Celera Corporation
December 07, 2017 - N°20170350897

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.
Combination therapy of t cell activating bispecific antigen binding molecules and pd-1 axis binding antagonists
Hoffmann-la Roche Inc.
December 07, 2017 - N°20170349666

The present invention generally relates to t cell activating bispecific antigen binding molecules, pd-1 axis binding antagonists, and in particular to combination therapies employing such t cell activating bispecific antigen binding molecules and pd-1 axis binding antagonists, and their use of these combination therapies for the treatment of cancer.
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Anti-axl antagonistic antibodies
Bergenbio As
December 07, 2017 - N°20170349658

Described are antibodies that specifically bind to the axl protein and inhibit the interaction between axl and the axl-ligand, gas6. Also disclosed are methods for the production and use of the anti-axl antibodies.
Use of il-20 antagonists for treating pancreatic cancer
National Cheng Kung University
December 07, 2017 - N°20170349656

Methods for treating pancreatic cancer using an il-20 antagonist, which can be an antibody that binds il-20 or an il-20 receptor, thereby blocking the signaling pathway mediated by il-20.
Wnt antagonists and their use in the diagnosis and treatment of wnt-mediated disorders
Genentech, Inc.
December 07, 2017 - N°20170349639

The present invention provides for chimeric wnt antagonists comprising a frz domain component derived from a frizzled protein, a secreted frizzled related protein or ror protein and an fc immunoglobulin component, and their use in the treatment and diagnostic detection of cellular wnt signaling and wnt-mediated disorders, including cancer.
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Antagonist Patent Applications
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8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
Genentech, Inc.
December 07, 2017 - N°20170349578

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.
Novel chemokine cxcr1 and cxcr2 receptor antagonist compounds, and use thereof in the treatment of ...
Galderma Research & Development
December 07, 2017 - N°20170349575

Novel chemokine cxcr1 and cxcr2 receptor antagonist compounds of general formula (i) are described. Also described, are pharmaceutical compositions including the compounds, and use of the compounds and the compositions for the treatment of chemokine-mediated pathologies, more specifically in the field of dermatology.
Hedgehog antagonists having zinc binding moieties
Genentech, Inc.
December 07, 2017 - N°20170349573

The present invention provides compounds which antagonize hedgehog signaling and inhibit hdac activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.
5-ht2b antagonists
Genentech, Inc.
December 07, 2017 - N°20170349559

And related methods for treating a person having a disorder characterized by undesirable 5-ht2b receptor signaling, such as migraine, irritable bowel syndrome (ibs), pulmonary arterial hypertension (pah), fibrosis, hepatocellular cancer, a small intestinal neuroendocrine tumor, cardiovascular disorders, and gastrointestinal (gi) tract disorders.
Compositions and methods for treating neurodegenerative disease
Cognition Therapeutics, Inc.
December 07, 2017 - N°20170349554

This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated ...
Non-cleavable polymer conjugated with alpha v beta 3 integrin thyroid antagonists
Nanopharmaceuticals, Llc
December 07, 2017 - N°20170348425

Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward and classified as anti-angiogenic thyrointegrin antagonists, which may be capable of reacting with one or more cell surface receptors of the integrin αvβ3 receptor family. Anti-angiogenic thyrointegrin antagonists or derivatives thereof are conjugated via a non-cleavable linker having an amine, ...
Dislodgement and release of hsc from the bone marrow stem cell niche using alpha9 integrin ...
Commonwealth Scientific And Industrial Research Organisation
December 07, 2017 - N°20170348375

Haematopoietic stem cell mobilization is a process whereby haematopoietic stem cells are stimulated out of the bone marrow space. Before hsc can mobilize, they must be dislodged and released from the bm stem cell niche in which they reside and are retained by adhesive interactions. Accordingly, in an aspect of the present invention there is provided a method for enhancing ...
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Antitumor agent
Tochigi Institute Of Clinical Pathology
December 07, 2017 - N°20170348299

Pharmaceuticals which are effective for treatment, prevention, and the like of cancer and have less side effects are disclosed. The antitumor agent of the present invention comprises as an effective ingredient at least one leukotriene inhibitor. Examples of the leukotriene inhibitor includes leukotriene production inhibitors and leukotriene receptor antagonists, and preferred specific examples of the leukotriene inhibitor include montelukast, zafirlukast, ...
Method of treating liver fibrosis
Chemocentryx, Inc.
December 07, 2017 - N°20170348293

A method of treating liver fibrosis with ccr2 antagonists is provided. The liver fibrosis may be associated with non-alcoholic steatohepatitis (nash), non-alcoholic fatty liver disease (nafld), emerging cirrhosis, non-cirrhotic hepatic fibrosis, type 2 diabetes mellitus (t2dm) or metabolic syndrome (ms).
Use of nk-1 receptor antagonists in pruritus
Menlo Therapeutics Inc.
December 07, 2017 - N°20170348283

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. In addition, the invention encompasses treatment of a pruritus-associated condition with serlopitant and an additional antipruritic agent, and the use of serlopitant as a sleep aid, optionally in combination with an ...
Use of nk-1 receptor antagonist serlopitant in pruritus
Menlo Therapeutics Inc.
December 07, 2017 - N°20170348282

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. In addition, the invention encompasses treatment of a pruritus-associated condition with serlopitant and an additional antipruritic agent, and the use of serlopitant as a sleep aid, optionally in combination with an ...
Anti-ngf antibodies and methods using same
Rinat Neuroscience Corp.
November 30, 2017 - N°20170342143

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.
Triazolo[4,5-d] pyramidine derivatives and their use as purine receptor antagonists
Vernalis (r&d) Limited
November 30, 2017 - N°20170342081

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. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
Crystal forms of a ccr5 antagonist
Merck Sharp & Dohme B.v.
November 30, 2017 - N°20170342053

The present disclosure relates to forms of a ccr5 inhibitory compound, (4,6-dimethylpyrimidin-5-yl)(4-((3s)-4-((1r)-2-methoxy-1-(4-(trifluoromethyl)phenyl)ethyl)-3-methyl-piperazin-1-yl)-4-methylpiperidin-1-yl)methanone.
Pyrrolidine orexin receptor antagonists
Merck Sharp & Dohme Corp.
November 30, 2017 - N°20170342052

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