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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
04/28/16
20160116469 
 Immunologically active polypeptide patent thumbnailImmunologically active polypeptide
Disclosed are immunomodulatory polypeptides that behave as weak tlr2 and tlr4 agonists and as potent competitive antagonists of natural pathogenic ligands for human and murine tlr2 and tlr4, that identify a subset of neutrophils in human peripheral blood leukocytes, and that elicit an unusual induced cytokine profile. Also disclosed are compositions comprising such polypeptides, compositions comprising antibodies that specifically bind to such polypeptides, and methods of using the same, including for treating sepsis or reducing the severity or likelihood of occurrence of sepsis, in cancer treatment, in the treatment of autoimmune diseases, in organ transplantation and for reducing graft rejection, for promoting fertility, and for identifying a neutrophil subset and/or other cellular subset including by flow cytometry.
Institute Of Arthritis Research, Llc


04/28/16
20160115228 
 Antagonists of il-6 to prevent or treat thrombosis patent thumbnailAntagonists of il-6 to prevent or treat thrombosis
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 prevent or treat thrombosis in diseases associated with abnormal blood coagulation or fibrinolysis. In preferred embodiments these patients will comprise those exhibiting elevated d-dimer or other coagulation cascade related proteins and optionally will further exhibit elevated c reactive protein prior to treatment.
Alderbio Holdings Llc


04/28/16
20160113948 
 System and  diagnosis and treatment patent thumbnailSystem and diagnosis and treatment
This invention relates to a low cost rapid response diagnostic system to determine cortisol levels in patients selected as potential candidates for gcr (glucocorticoid receptor) antagonist therapy utilizing a gcr antagonist, such as org 34517. The rapid, sensitive, and inexpensive test can be used to determine patients who have non-normal cortisol production or disordered circadian rhythms as a method for selecting subjects for gcr antagonist therapy for whom it is likely to have beneficial and/or therapeutic effects, and can also be used to monitor changes in cortisol levels in response to treatment..
Pop Test Oncology Limited Liability Company


04/28/16
20160113928 
 Heterocyclic compounds as hedgehog signaling pathway inhibitors patent thumbnailHeterocyclic compounds as hedgehog signaling pathway inhibitors
This invention relates to novel compounds of formula (i). The compounds of the invention are hedgehog pathway antagonists.
Redx Pharma Plc


04/28/16
20160113923 
 Peripheral opioid receptor antagonists and uses thereof patent thumbnailPeripheral opioid receptor antagonists and uses thereof
Wherein x−, r1, and r2 are as defined herein, and compositions thereof.. .

04/28/16
20160113871 
 Compositions for delivery of drug combinations patent thumbnailCompositions for delivery of drug combinations
Compositions which comprise delivery vehicles having stably associated therewith non-antagonistic combinations of two or more agents, such as antineoplastic agents, are useful in achieving non-antagonistic effects when combinations of drugs are administered.. .
Celator Pharmaceuticals, Inc.


04/28/16
20160113286 
 Lactobacillus plantarum strain for the control of fire blight patent thumbnailLactobacillus plantarum strain for the control of fire blight
The present invention relates to the strain lactobacillus plantarum tc92, as well as to mutants thereof, and to the use of said strain as a pesticide for controlling fire blight in plants of the rosaceae family. Additional aspects of the invention relate to methods for producing the l.
Universitat De Girona


04/21/16
20160108116 
 Vegf-specific antagonists for adjuvant and neoadjuvant therapy and the treatment of early stage tumors patent thumbnailVegf-specific antagonists for adjuvant and neoadjuvant therapy and the treatment of early stage tumors
Disclosed herein are methods of treating benign, pre-cancerous, or non-metastatic tumors using an anti-vegf-specific antagonist. Also disclosed are methods of treating a subject at risk of developing benign, pre-cancerous, or non-metastatic tumors using an anti-vegf-specific antagonist.

04/21/16
20160106835 
 Combination therapies for cancer patent thumbnailCombination therapies for cancer
A novel combination comprising a b-raf inhibitor, particularly n-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, the mek inhibitor n-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2h-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and a pd-1 antagonist; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of mek and/or b-raf and/or immune modulation through pd-1 is beneficial, e.g., cancer.. .

04/21/16
20160106832 
 Treatment of cancer with naltrexone patent thumbnailTreatment of cancer with naltrexone
The present invention provides novel therapeutic applications of low dose naltrexone (ldn). Said applications have been determined in light of the discovery by the present inventors that naltrexone acts as an antagonist of toll-like receptor 9 (tlr9), an innate immune receptor which elicits the production of inflammatory cytokines when agonized.

04/21/16
20160106821 

Functional ghrelin receptor antagonism during pregnancy to prevent stress-associated mental illness in offspring and mothers


The invention relates to methods of protecting against elevated ghrelin levels in a fetus by antagonizing ghrelin or ghrelin receptor. The invention also encompasses methods of treating postpartum depression by administering ghrelin antagonists..

04/21/16
20160106803 

Use of tight junction antagonists in the treatment of acute lung injury and acute respiratory distress


The present application provides compositions and methods for treating acute lung injury and acute respiratory distress syndrome. The methods include administering one or more tight junction antagonists to the lung of a subject in need thereof..

04/21/16
20160106802 

Methods of diagnosing and treating asthma


The present invention provides materials and methods to diagnose asthma. In some embodiments, the present invention provides a method of diagnosing asthma by measuring the zonulin level of a subject.

04/21/16
20160106752 

Use of cb1 antagonists and/or inverse agonists for the preparation of drugs that increase motor neuron excitability


Use of a cb1 receptor antagonist and/or inverse agonist, preferably rimonabant, for the preparation of drugs useful for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level, as well as a method for increasing motor neuron excitability through the administration of a cb1 antagonist/ inverse agonist receptors, and to the use of a pharmaceutical composition which comprises a cb1 receptor antagonist and/or inverse agonist, preferably rimonabant, for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level.. .

04/21/16
20160106749 

Fatty liver disease treatment using glucocorticoid and mineralocorticoid receptor antagonists


The present invention provides treatment of fatty liver disease using a class of pyrimidinedione cyclohexyl compounds.. .

04/21/16
20160106726 

Pharmaceutical composition for treating alcohol dependency


A compound having an antagonistic action on the alpha1-noradrenergic receptors selected from prazosin, alfuzosin, terazosin and tamsulosin.. .

04/14/16
20160102311 

Protection against ionizing radiation and chemotherapy toxicity via latexin regulation


The present invention relates to methods for protecting against damage caused by radiation and/or chemotherapy, and methods for treating bone marrow damage by reducing/inhibiting latexin expression and/or latexin activity. The methods comprise administering to a subject in need thereof a pharmaceutical composition comprising an antagonist that reduces expression and/or activity of latexin, wherein latexin is a latexin polynucleotide variant and/or a latexin polypeptide variant that binds to the antagonist..

04/14/16
20160102145 

Antagonists of il-6 to prevent or treat cachexia, weakness, fatigue, and/or fever


The present invention is directed to therapeutic methods using antibodies and fragments thereof having binding specificity for il-6 to prevent or treat cachexia, fever, weakness and/or fatigue in a patient in need thereof. In preferred embodiments, the anti-il-6 antibodies will be humanized and/or will be aglycosylated.

04/14/16
20160102073 

2-hydroxymethyl-substituted orexin receptor antagonists


The present invention is directed to 2-hydroxymethyl 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.

04/14/16
20160101152 

Use of a vegf antagonist to treat angiogenic eye disorders


The present invention provides methods for treating angiogenic eye disorders by sequentially administering multiple doses of a vegf antagonist to a patient. The methods of the present invention include the administration of multiple doses of a vegf antagonist to a patient at a frequency of once every 8 or more weeks.

04/14/16
20160101099 

H3 receptor antagonist for use in the treatment of alzheimer's disease


This disclosure relates to methods of using 2-(cyclohexylmethyl)-n-{2-[(2s)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide in a disease modifying therapy of alzheimer's disease, other tauopathies and related neurodegenerative diseases.. .

04/07/16
20160096899 

Methods for treating juvenile arthritis with anti-bile salt-stimulated lipase (bssl) antibodies


It provides methods and pharmaceutical compositions comprising antagonists to the protein bile salt-stimulated lipase (bssl) for the prevention, prophylaxis and treatment of inflammatory diseases, such as rheumatoid arthritis. It further relates to pharmaceutical compositions comprising bssl antagonists and their use in methods for the prevention, prophylaxis and treatment of inflammatory diseases, such as rheumatoid arthritis.
Lipum Ab


04/07/16
20160096803 

Crystal of pyrrole derivative and producing the same


The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (i) [wherein r1 represents a methyl group or a trifluoromethyl group, r2 represents a hydrogen atom or a c1-c3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (s)-1-(2-hydroxyethyl)-4-methyl-n-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1h-pyrrole-3-carboxamide..
Daiichi Sankyo Company, Limited


04/07/16
20160095897 

Par-4 antagonists for use in the treatment or prevention of influenza virus type a infections


The present invention provides methods and compositions (such as pharmaceutical compositions) comprising par4 antagonists for treating or preventing influenza virus type a infections, in particular h1n1 infection. Par4 antagonists may be combined with a par2 agonist or a par1 antagonist..
Universite Claude Bernard Lyon 1


04/07/16
20160095854 

Arylpiperazine opioid receptor antagonists


Where r, y3, r1, r2, r3, r4 and r5 are as defined herein.. .

04/07/16
20160095840 

Combinations of a muscarinic receptor antagonist and a beta-2 adrenoreceptor agonist


Combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, and methods of using them are provided.. .
Glaxo Group Limited


03/31/16
20160090420 

Antagonist of the btla/hvem interaction for use in therapy


antagonist of the btla/hvem interaction for use in therapy the present invention relates to an antagonist of the btla/hvem interaction for use in therapy, wherein said antagonist increases the proliferation of vγ9vδ2 t cells.. .
Centre National De La Recherche Scintifique- Cnrs


03/31/16
20160090359 

Crystalline forms of an nk-1 antagonist


The present invention is related to crystalline forms of 2-(3,5-bis(trifluoromethyl)phenyl)-n,2-dimethyl-n-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide which is an nk-1 antagonist useful in the treatment of induced vomiting and other disorders.. .
Helsinn Healthcare Sa


03/31/16
20160090357 

Processes and intermediates in the preparation of c5ar antagonists


Intermediates and methods are provided for the preparation of selected c5ar antagonist compounds.. .
Chemocentryx, Inc.


03/31/16
20160089379 

Treatment of neurological and other disorders


Methods and implants for treating neurological, muscular and other cells having an electrical potential, with an infusion of antagonists or inverse agonists (such as flumazenil for the benzodiazepine receptor, or naltrexone for the opiate receptor or other antagonist for other receptor) at rates that are so low that only a small percentage of receptors have the antagonist effect at any one time.. .
Palmaya Pty Ltd


03/31/16
20160089378 

Treatment of osteoarthritis pain


This invention discloses a method of treatment of osteoarthritis pain by administration of a histamine h3 receptor antagonist, described herein, a salt thereof, or a composition comprising such compound or salt.. .
Abbvie Inc.


03/31/16
20160089364 

Pharmaceutical composition and the use thereof, and application regime of said pharmaceutical composition for on-demand contraception


The invention relates to a pharmaceutical composition for non-hormonal, on-demand contraception and to processes for preparing this pharmaceutical composition. The latter comprises 2h-indazole as novel ep2 receptor antagonists in combination with cox inhibitors.
Bayer Pharma Aktiengesellschaft


03/31/16
20160089313 

Method for searching for malodor control agent, malodor control agent, and malodor control method


Provided are a method for searching for a malodor inhibitor by using the response of an olfactory receptor as an indicator; a method for inhibiting malodor based on the antagonism of olfactory receptors; and a malodor inhibitor. Disclosed are a method for searching for a malodor inhibitor, the method including: adding a test substance and a malodor-causing substance to any one olfactory receptor selected from the group consisting of or51e1, or2w1, or10a6, or51i2, and or51l1, measuring the response of the olfactory receptor to the malodor-causing substance, identifying the test substance that suppresses the response of the olfactory receptor on the basis of the measured response, and selecting the identified test substance as a malodor inhibitor; an antagonist to any one olfactory receptor selected from the group consisting of or51e1, or2w1, or10a6, or51i2, and or51l1; a method for inhibiting malodor using the antagonist..
Kao Corporation


03/24/16
20160083733 

Novel treatment of metabolic diseases


Antagonists of mammalian sterile 20-like kinase (mst) 1 for use in the treatment and prevention of metabolic diseases, in particular diabetes and obesity are described.. .
University Of Bremen


03/24/16
20160083472 

Vista antagonist and methods of use


The present invention is directed to synergic or additive therapies comprising the administration of a vista antagonist and a pd-1, pd-l1 or pod-l3 antagonist; or the combination of a vista agonist and a -1, pd-l1 or pod-l3 agonist which combinations respectively elicit an additive or synergistic effect at promoting t cell immunity or inhibiting t cell immunity, i.e., cd4, cd8 or th1 immunity. The agonists and antagonists may be in the same or separate compositions and may be administered together or separately administered in either order..

03/24/16
20160083468 

Compositions comprising antibodies to lingo or fragments thereof


Endogenous lingo-1 is a negative regulator for neuronal survival, axon regeneration, oligodendrocyte differentiation and myelination. Molecules that block endogenous lingo-1 function, such anti-lingo-1 antibodies can be used as therapeutics for the treatment of neuron and oligodendrocyte dysfunction.
Biogen Ma Inc.


03/24/16
20160083430 

Peptide and peptidomimetic inhibitors


The present invention provides inhibitors and/or antagonists of plasma kallikrein. Also provided are methods of utilizing the inhibitors as therapeutics..
Ra Pharmaceuticals, Inc.


03/24/16
20160083363 

Substituted indoles as selective protease activated receptor 4 (par-4) antagonists


Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition..
Vanderbilt University


03/24/16
20160083350 

A nk3 receptor antagonist compound (nk3ra) for use in a the treatment of polycystic ovary syndrome (pcos)


A method for treating polycystic ovarian syndrome and related conditions with a compound (i): or a pharmaceutically acceptable salt thereof.. .
Astrazeneca Uk Limited


03/24/16
20160082079 

Wnt antagonist and methods of treatment and screening


The present invention relates to compositions comprising wnt antagonists and methods of treating wnt-associated diseases and disorders, such as cancer, inducing differentiation, and reducing the frequency of cancer stem cells, as well as novel methods of screening for such wnt antagonists. In particular, the invention discloses soluble fzd, sfrp and ror receptors and their use..
Oncomed Pharmaceuticals, Inc.


03/24/16
20160082073 

Novel use


The present invention relates to a combination comprising at least one compound selected from the group consisting of an α-adrenergic antagonist, an anthelmintic agent, an antifungal agent, an antimalarial agent, an antineoplastic agent, an antipsychotic agent, an antioxidant, a vasodilator, a vitamin, or a pharmaceutically acceptable derivative thereof; and an antimicrobial compound.. .
Helperby Therapeutics Limited


03/24/16
20160082071 

Methods of treating myeloid leukemia


There is provided a method of treating a myeloid leukemia. The method includes the step of administering to a subject in need thereof a therapeutically effective amount of a cxcr4-antagonistic peptide and a therapeutically effective amount of a chemotherapeutic agent..
Biokine Therapeutics Ltd.


03/24/16
20160082020 

Methods and compositions for stimulating reepithelialisation during wound healing


The present invention relates to methods and compositions for stimulating reepithelialisation during wound healing. More particularly, the present invention relates to a mineralocorticoid receptor antagonist or an inhibitor of mineralocorticoid receptor gene expression for use in a method for stimulating reepithelialisation of the skin or of the cornea during wound healing..
Universite Paris Descartes


03/24/16
20160081995 

Selective nr2b antagonists


The disclosure generally relates to compounds of formula i, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the nr2b receptor and may be useful for the treatment of various disorders of the central nervous system..
Bristol-myers Squibb Company


03/24/16
20160081946 

4:3 naltrexone: 5-methyl-2-furaldehyde cocrystal


A 4:3 naltrexone: 5-methyl-2-furaldehyde cocrystal and its use as an opioid antagonist are disclosed. The invention also relates to a drug-in-adhesive transdermal patch containing the analgesic fentanyl, a mu opioid agonist, or an analog thereof and a 4:3 naltrexone: 5-methyl-2-furaldehyde cocrystal, as an opioid antagonist.
Pain Therapeutics, Inc.


03/24/16
20160081926 

Stable high strength pharmaceutical composition of levoleucovorin


The administration of levoleucovorin is useful as an antidote to drugs which act as folic acid antagonists and in combination chemotherapy with 5-fu. The most often used calcium salt of levoleucovorin has a limited solubility in water and forms almost insoluble degradation products.
Aprofol Ag


03/24/16
20160081901 

Compositions and methods for hair growth


The present invention provides compositions comprising a bradykinin receptor b2 agonist or an angiotensin ii receptor (atir) antagonist, and methods using such compositions to increase/promote hair growth or reduce/delay hair loss.. .
Wuhan Optics Valley Bridgebiomed International Corporation


03/17/16
20160077113 

Methods of identifying candidate compounds of the human g protein-coupled receptor, gpr50, as modulators of body mass or adiposity


The present invention relates to methods of using a g protein-coupled receptor (gpcr) to screen one or more candidate compounds as a modulator of body mass or of adiposity or of percentage body fat in a subject or as a pharmaceutical agent for obesity and conditions related thereto. Inverse agonists and antagonists of the invention are useful as therapeutic agents for the prevention or treatment of obesity and conditions related thereto, including hypertension, insulin resistance, metabolic syndrome, type 2 diabetes, dyslipidemia, atherosclerosis, coronary heart disease, and stroke.
Arena Pharmaceuticals, Inc.


03/17/16
20160077102 

Diagnostic biomarker to predict women at risk for preterm delivery


The invention relates to biomarkers associated with preterm delivery. More specifically, the invention provides methods of measuring biomarkers including but not limited to cytokines, cytokine receptors, cytokine receptor antagonists, chemokines, chemokine receptors, and/or chemokine receptor antagonists found in women that are at risk for preterm delivery.
Cedars-sinai Medical Center


03/17/16
20160075791 

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


03/17/16
20160075786 

Use of antagonists of the interaction between hiv gp120 and a4b7 integrin


Methods are provided for the treatment of a hiv infection. The methods can include administering to a subject with an hiv infection a therapeutically effective amount of an agent that interferes with the interaction of gp120 and α4 integrin, such as a α4β1 or α4β7 integrin antagonist, thereby treating the hiv infection.
The United States Of America, As Represented By The Secretary, Department Of Health And Human Serv


03/17/16
20160075772 

Treatment of fibrodysplasia ossificans progressiva


Methods for treating fibrodysplasia ossificans progressiva (fop) are provided. Such methods involve administering to a subject having fop an effective regime of an activin receptor type 2a (acvr2a) and/or an activin receptor type 2b (acvr2b) antagonist or an activin receptor type 1 (acvr1) antagonist.
Regeneron Pharmaceuticals, Inc.


03/17/16
20160075752 

B-type plexin antagonists and uses thereof


The present invention concerns the field of cancer therapy. In particular, it relates to an antagonist of a b-type plexin which prevents the interaction of the b-type plexin with erbb-2 for use as a medicament, in particular, for treating metastasizing cancer.
Max-planck-gesellschaft Zur Förderung Der Wissenschaften E.v.


03/17/16
20160075713 

Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists


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..

03/17/16
20160075711 

Compounds for the inhibition of indoleamine-2,3-dioxygenase


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


03/17/16
20160075698 

Fluorinated integrin antagonists


The present invention relates to fluorinated compounds of formula i and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (dr), macular edema, diabetic macular edema (dme), and macular edema following retinal vein occlusion (rvo), by administering these compounds and pharmaceutical compositions to subjects in need thereof..
Scifluor Life Sciences, Inc.


03/17/16
20160075650 

Crystalline polymorphic forms of an antidiabetic compound


This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included..

03/17/16
20160074413 

Substituted diketopiperazines and their use as oxytocin antagonists


Wherein r1 is 2-indanyl, r2 is 1-methylpropyl, r3 is 2-methyl-1,3-oxazol-4-yl and r4 and r5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.. .

03/17/16
20160074402 

Stable pharmaceutical composition containing folates


The administration of leucovorin as well as other active, reduced folates is useful as an antidote to drugs which act as folic acid antagonists and in combination chemotherapy with 5-fu. The most often used calcium salts of the folates have a low solubility in water and form almost insoluble degradation products.
Aprofol Ag


03/17/16
20160074400 

Wnt modulators for the protection, mitigation and treatment of radiation injury


Provided are composition and methods for treating radiation-induced cell damage, and in particular aspects to methods for protecting, mitigating or otherwise treating radiation-induced induced depletion of tissue stem cells and injury to the supportive stem cell niche, and in even more particular aspects to methods for protecting, mitigating or otherwise treating radiation-induced gastrointestinal syndrome (rigs), comprising sequential administration of a wnt pathway activator/agonist (e.g., rspo1 or a small molecule inducer thereof) that amplifies the surviving intestinal stem cell (isc) pool post-radiation exposure, followed by a selective antagonist of the β-catenin-cbp interaction (e.g., icg-001 or other exemplary compounds disclosed herein) that accelerates differentiation of the stimulated (e.g., rspo1-stimulated) isc in crypt-villi axis, promoting villous regeneration and intestinal restitution, thereby mitigating rigs. Adjunctive and combination therapy embodiments are encompassed..
Albert Einstein College Of Medicine Of Yeshiva University


03/10/16
20160068823 

Chimeric newcastle disease viruses and uses thereof


Described herein are chimeric newcastle disease viruses engineered to express a heterologous interferon antagonist and compositions comprising such viruses. The chimeric newcastle disease viruses and compositions are useful in the treatment of cancer..
Memorial Sloan-kettering Cancer Center


03/10/16
20160068599 

Method for treating neuroendocrine cancer


Methods for decreasing proliferation and preventing or treating a neuroendocrine cancer using an n-methyl d-aspartate-associated (nmda) glutamate receptor antagonists or binding agent, such as an antibody, antibody fragment or peptide aptamer specific for a nmda glutamate receptor, are disclosed.. .
Trustees Of Dartmouth College


03/10/16
20160068557 

Platinum compounds, compositions, and uses thereof


The present teachings relate to compounds and compositions for treatment of cancers. In some embodiments, the composition comprises a platinum (iv) complex having at least one reacting group for reacting with a functional group on a protein, engineered protein, antibody, antibody fragment, peptide, agonist, antagonist, aptamer or ligand which may be capable of recognizing a selected target cell population, and/or derivatives/analogs/mimics thereof..
Blend Therapeutics, Inc.


03/10/16
20160068540 

Crystal forms of (r)-n-methylnaltrexone bromide and uses thereof


The present invention provides a new forms of (r)—n-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.. .
Wyeth Llc


03/10/16
20160068514 

Halo and trifluoromethyl substituted orexin receptor antagonists


The present invention is directed to halo and trifluoromethyl substituted 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.
Merck Sharp & Dohme Corp.


03/10/16
20160068510 

Hydroxy-substituted orexin receptor antagonists


The present invention is directed to hydroxy 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.
Merck Sharp & Dohme Corp.


03/10/16
20160067337 

Combination of dr5 agonist and anti-pd-1 antagonist and methods of use


Provided are methods and compositions for treating cancer using an effective amount of a pd-1 antagonist (e.g., an antibody) in combination with a dr4 or dr5 agonist (e.g., an antibody).. .
Bristol-myers Squibb Company


03/10/16
20160067301 

Antagonism of abcg4, lyn kinase, and c-cbl e3 ligase to increase platelet count as therapy for thrombocytopenia


The present invention provides a method of treating a subject to increase the subject's platelet count which comprises administering to the subject an amount of one or more of an antagonist or inhibitor of abcg4, lyn kinase or c-cbl effective to antagonize or inhibit such abcg4, lyn kinase or c-cbl so as to thereby increase the subject's platelet count.. .
The Trustees Of Columbia University In The City Of New York


03/10/16
20160067261 

Serca inhibitor and calmodulin antagonist combination


The present invention relates to novel combinations of active ingredients for use in the prevention and/or treatment of tumors. The tumors treated by the composition according to the invention overexpress sec62 gene and overproduce sec62 protein.
Universitaet Des Saarlandes


03/10/16
20160067235 

Antagonists of the cannabinoid receptor cb1 for use in the treatment of diseases associated with neuronal dendritic abnormalities


The invention relates to antagonists of the cannabinoid receptor cbi for use in the treatment and prevention of diseases associated with neural dendritic abnormalities, such as down's syndrome, angelman's syndrome, rett syndrome and tuberous sclerosis. More specifically, the invention provides a method of treatment or prevention of such diseases by the administration of the compound rimonabant..
Universitat Pompeu Fabra


03/10/16
20160067212 

Use of insulin signaling antagonists, optionally in combination of transfection of non-beta cells, for inducing insulin production


The invention relates to methods of inducing insulin production in non-beta-cells or converting non-beta-cells into insulin producing cells, as well as methods of preventing and/or treating diabetes and methods of predicting the susceptibility of a diabetic subject to a treatment.. .
Universite De Geneve


03/10/16
20160067175 

Intrathecal multidrug infusion for pain control


The present invention relates to an intrathecal (it) formulation comprising an opioid, a na channel blocker, an alpha2-receptor agonist, an opioid mu or delta receptor competitive antagonist and an intravenous anesthetic.. .

03/10/16
20160066514 

Methods for modulating photosynthetic activity


A method is provided for modulating transpiration in an organism that is capable of photosynthesis, where the method includes contacting the organism with a composition including an effective amount of an oxygen antagonist. Also provided is an apparatus for modulating transpiration in an organism that is capable of photosynthesis..
Elwha Llc


03/03/16
20160063085 

System and anticipating criminal behaviour


A system and method for anticipating criminal behaviour. The system includes or is connectable to a database including records, each record including data representative of a criminal incident.

03/03/16
20160061812 

Diagnosis and treatment of arthritic conditions


Provided is a method of determining the likelihood that a patient, with a disorder treatable with a tnf antagonist, will respond to administration of a tnf-antagonist. The method comprises determining the likelihood of the patient's response to said antagonist based on a metabolic profile of a urine sample from said patient.
The University Of Birmingham


03/03/16
20160060623 

Method of regulating nfatc2 activity in lymphocytes


A method of decreasing nfatc2 activity in a lymphocyte includes administering to the lymphocyte an amount of an nfatc2 mrna antagonist that binds to a binding site on the 3′utr of nfatc2 mrna effective to decrease the activity of nfatc2 mrna in the lymphocyte.. .
Case Western Reserve University


03/03/16
20160060351 

Use of c5ar antagonists


C5a and c5ar stimulate the inflammatory response and c5ar antagonist can counteract this function performing as an anti-inflammatory agents. This functionality is considered useful in treatment of inflammatory diseases including auto immune diseases.
Novo Nordisk A/s


03/03/16
20160060343 

Cancer treatment


The present invention relates to methods of treating cancer, such as melanoma, by administering a ctla4 antagonist to a subject with a serum c-reactive protein (crp) concentration that is less than or equal to some amount. The invention further relates to methods of treating cancer by determining the level of serum crp concentration in a subject, and then administering a ctla4 antagonist if the crp concentration is less than or equal to a certain amount.
Pfizer Inc.


03/03/16
20160060323 

Zcytor17 heterodimeric cytokine receptor


Novel polypeptide combinations, polynucleotides encoding the polypeptides, and related compositions and methods are disclosed for zcytor17-containing multimeric or heterodimer cytokine receptors that may be used as novel cytokine antagonists, and within methods for detecting ligands that stimulate the proliferation and/or development of hematopoietic, lymphoid and myeloid cells in vitro and in vivo. The present invention also includes methods for producing the multimeric or heterodimeric cytokine receptor, uses therefor and antibodies thereto..
Zymogenetics, Inc.


03/03/16
20160060273 

Heterocyclic compound


Provided is a compound represented by the following formula (1) or a salt thereof, which has an sstr5 antagonistic action: wherein each symbol has the same definition as in the specification.. .
Takeda Pharmaceutical Company Limited


03/03/16
20160058895 

Radiolabeled gnrh antagonists as pet imaging agents


Provided herein is technology relating to imaging agents for positron emission tomography (pet) and particularly, but not exclusively, to a gonadotropin-releasing hormone (gnrh) antagonist radiolabeled with positron emitting nuclides and to methods of visualizing gnrh receptors in the central nervous system by pet from administration of such compounds to warm-blooded animals for diagnostic purposes.. .
Oslo Universitetssykehus Hf


03/03/16
20160058851 

Use of antagonists of ghrelin or ghrelin receptor to prevent or treat stress-sensitive psychiatric illness


The invention relates to methods of protecting against chronic stress in a subject and treating stress sensitive disorders in a subject by antagonizing ghrelin or ghrelin receptor.. .
Massachusetts Institute Of Technology


03/03/16
20160058785 

Galactose-pronged polysaccharides in a formulation for antifibrotic therapies


Methods and compositions for reducing fibrosis and cirrhosis are provided in which an effective dose of an admixture of a polysaccharide compound and, for example, a compound selected from the group consisting of antibodies specific to intracellular or cell-surface: (i) beta-pdgf receptors; (ii) synaptophysin; (iii) zvegf3; (iv) ccr1 receptors; (v) connective tissue growth factor; (vi) alpha 1-smooth muscle actin; (vii) matrix metalloproteinases mmp 2 and mmp9; (viii) matrix metalloproteinase inhibitors timp1 and tmp2; (ix) integrins; (x) tfg-β1; (xi) endothelin receptor antagonists; and (xii) collagen synthesis and degradation modulating compounds; (xiii) actin synthesis and degradation modulating compounds; and (xiv) tyrosine kinases is administered to an animal in order to treat fibrosis.. .
Galectin Therapeutics, Inc.


03/03/16
20160058755 

Pharmaceutical composition


Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided.
Alpharma Pharmaceuticals Llc


03/03/16
20160058748 

Antitumor agent


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.
Tochigi Institute Of Clinical Pathology


03/03/16
20160058736 

Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes


The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.. .
Jenrin Discovery


02/25/16
20160053012 

Compositions and methods for preserving cells of the eye


The invention provides a method of preserving ocular cells in a patient having or at risk of developing glaucoma. In particular, microglial cell activation can be decreased, oligodendrocyte loss can be reduced, and/or the viability of retinal ganglion cells can be preserved by administering a selective tnfr2 antagonist to an individual having or at risk of developing glaucoma..
Massachusetts Eye And Ear Infirmary


02/25/16
20160052985 

Thymic stromal lymphopoietin fragments and uses thereof


The present invention relates to a compound selected in the group consisting of: a) a polypeptide consisting of the c-terminus amino acid sequence of the human thymic stromal lymphopoietin (tslp) long isoform (seq id no: 2), derivatives and fragments thereof; b) a polynucleotide coding for said polypeptide; d) a vector comprising said polynucleotide; c) a host cell genetically engineered expressing said polypeptide, or d) a tslp long isoform (seq id no:2) antagonist for use in the treatment or/and prevention and/or diagnosis and/or monitoring of a disorder or pathology characterized by an inflammatory response.. .
Ieo - Istituto Europeo Di Oncologia Srl


02/25/16
20160052936 

Spiroindoline derivatives for use as gonadotropin-releasing hormone receptor antagonists


Spiroindoline derivatives, processes for their preparation and pharmaceutical compositions thereof, their use for the treatment of diseases, and their use for the manufacture of medicaments for the treatment of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine leiomyoma (fibroids), polycystic ovarian disease, menorrhagia, dysmenorrhea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception, infertility and assisted reproductive therapy such as in vitro fertilization. The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (gnrh) receptor antagonists..
Bayer Pharma Aktiengesellschaft


02/25/16
20160052925 

Method of treatment or prophylaxis inftammatory pain


A method of treatment, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals, particularly in human subjects, comprising administering angiotensin ii receptor 2 (at2 receptor) antagonists is disclosed. The at2 receptor antagonist may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory pain..
Novartis Ag


02/25/16
20160052913 

Substituted benzimidazoles as nociceptin receptor modulators


The invention provides modulators of the nociceptin receptor (nop), including both agonists and antagonists. A compound of the invention can be a selective modulator of nop with respect to the μ- and κ-opioid receptors (mop and kop), thus providing a therapeutic method for the treatment of conditions wherein selective nop modulation is medically indicated and mop or kop modulation may be less desirable.
The Scripps Research Institute


02/25/16
20160051689 

Supramolecular aggregates comprising maleimido cores


The invention relates to a supramolecular aggregate of formula (vi) wherein a is an active substance, and x1, x2, x3 and x4, independently to each other, are a moiety of formula (i) containing a maleimido functionalization and at least one among x1, x2, x3 and x4 is present in formula (vi). In a preferred embodiment the maleimido-funzionalized core is pwt2.
Ufpeptides S.r.l.


02/25/16
20160051673 

Compositions and methods for increasing the serum half-life of a therapeutic agent targeting complement c5


The disclosure features compositions and methods for increasing the half-life of a therapeutic agent (e.g., a c5 antagonist) in the serum of a subject (e.g., a human). Also featured are compositions and methods for: (i) decreasing the frequency by which a therapeutically effective amount of a therapeutic agent must be administered to a human having, suspected of having, or at risk for developing, a medical condition for which the therapeutic agent is effective and (ii) decreasing the dosage of the therapeutic agent required for therapeutic efficacy in a human having, suspected of having, or at risk for developing, a medical condition for which the therapeutic agent is effective.
Alexion Pharmaceuticals, Inc.


02/25/16
20160051672 

Methods of treatment with antagonists against pd-1 and pd-l1 in combination with radiation therapy


This application provides a method of treating cancer in a patient comprising administering at least one dose of radiation therapy and at least one pd-1 and/or pd-l1 antagonist, wherein at least one pd-1 and/or pd-l1 antagonist is administered on the same day as a dose of radiation therapy or up to and including 4 days later.. .
The University Of Manchester


02/25/16
20160051671 

Combination of blys inhibition and anti-cd 20 agents for treatment of autoimmune disease


The invention relates to novel combination therapies involving blys or blys/april inhibition and anti-cd20 agents for the treatment of autoimmune diseases. One preferred method is where the blys antagonist is a fc-fusion protein which can be a taci-fc-fusion protein comprising the extracellular domain of taci or a functional fragment thereof, a baff-r-fc-fusion protein comprising the extracellular domain of baff-r or a functional fragment thereof, or a bcma-fc-fusion protein comprising the extracellular domain of bcma or a functional fragment thereof.
Zymogenetics, Inc.


02/25/16
20160051577 

Compositions comprising bile acid sequestrants for treating esophageal disorders


Disclosed herein are novel compositions and methods for treating or preventing upper gi tract disorders and protecting stratified squamous epithelium against injury by a noxious substance. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising at least one bile acid sequestrant, alone or in combination with at least one proton pump inhibitor, and optionally one or more agent chosen from antacids, histamine h2-receptor antagonists, γ-aminobutyricacid-b (gaba-b) agonists, prodrugs of gaba-b agonists, and protease inhibitors..
Ironwood Pharmaceuticals, Inc.


02/25/16
20160051549 

Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3


The present invention relates to the treatment or prevention of skeletal disorders, in particular skeletal diseases, developed by patients that display abnormal increased activation of the fibroblast growth factor receptor 3 (fgfr3), in particular by expression of a constitutively activated mutant of fgfr3.. .
Imagine


02/25/16
20160051539 

Opioid agonist/antagonist combinations


The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome)..
Purdue Pharma L.p.


02/25/16
20160051537 

Combinations of opioid/tlr4 antagonist and acetyl-para-aminophenol (apap) for use in the treatment of pain


Disclosed are compositions for the treatment of pain comprising a first compound and a second compound, the first compound is an opiod antagonist that treats pain by blocking toll-like receptor 4 (tlr4) and the second compound is acetyl-para-aminophenol (apap) that enhances the pain treatment effect of the first compound. Examples of opioid antagonist include naltrexone and naloxone, synergistic pharmaceutical compositions thereof, and their use in the treatment, prevention, and reversal of neuropathic and nociceptive pain..
Allodynic Therapeutics, Inc.




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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