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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
02/04/16
20160033478 
 Hemokinin-1 receptor and hemokinin-1-derived peptide patent thumbnailHemokinin-1 receptor and hemokinin-1-derived peptide
The present invention provides a peptide having antagonist activity against sp, pain control activity, anti-inflammation activity, and anti-pruritic activity. The present invention further provides a method for searching for a therapeutic agent for pain, a therapeutic agent for inflammation, and a therapeutic agent for pruritus using g protein coupled receptor (gpr) 83, which is an hk-1 specific receptor..
University Of Miyazaki


02/04/16
20160031990 
 Antagonists of pdl-1 and pd-1 for the treatment of hpv-negative cancers patent thumbnailAntagonists of pdl-1 and pd-1 for the treatment of hpv-negative cancers
Provided herein are methods of treating hpv-negative tumors comprising administering an effective amount of an antagonist of the pdl-1/pd-1 interaction (e.g., an anti-pdl-1 or anti-pd-1 antibody antigen binding fragment thereof).. .
Medlmmune, Llc


02/04/16
20160031944 
 A4b7 integrin thioether peptide antagonists patent thumbnailA4b7 integrin thioether peptide antagonists
The invention relates to thioether monomer and dimer peptide molecules which inhibit binding of α4β7 to the mucosal addressing cell adhesion molecule (madcam) in vivo.. .
Protagonist Therapeutics, Inc.


02/04/16
20160031908 
 Chemokine receptor antagonists and methods of use thereof patent thumbnailChemokine receptor antagonists and methods of use thereof
Or physiologically acceptable salt thereof.. .

02/04/16
20160031879 
 Novel indolizine derivatives and their use in neurodegenerative diseases patent thumbnailNovel indolizine derivatives and their use in neurodegenerative diseases
The present invention relates to indolizine compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of p2x7, and for the treatment of p2x7-related disorders.. .
Merck Patent Gmbh


02/04/16
20160031841 
 2,5-disubstituted arylsulfonamide ccr3 antagonists patent thumbnail2,5-disubstituted arylsulfonamide ccr3 antagonists
Provided herein are 2,5-disubstituted arylsulfonamide ccr3 antagonists, e.g., compounds of formula i, and pharmaceutical compositions thereof: also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a ccr3-mediated disorder, disease, or condition.. .
Axikin Pharmaceuticals, Inc.


02/04/16
20160031817 
 3-piperidone compounds and their use as neurokinin-1 (nk1) receptor antagonists patent thumbnail3-piperidone compounds and their use as neurokinin-1 (nk1) receptor antagonists
The invention relates to 3-piperidone compounds, and in particular, to (2s)-phenyl-3-piperidone and its synthesis method. Use of the thus-synthesized 3-piperidone compounds as potent neurokinin-1 (nk1) receptor antagonists is also provided..
Nanyang Technological University


02/04/16
20160031801 
 Deuterated 2-amino-3-hydroxypropanoic acid derivatives patent thumbnailDeuterated 2-amino-3-hydroxypropanoic acid derivatives
This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an nmda glycine-site antagonist..
Concert Pharmaceuticals, Inc.


02/04/16
20160030561 
 Methods of treating pancreatic cancer patent thumbnailMethods of treating pancreatic cancer
Novel methods of treating pancreatic cancer are provided. In one embodiment, the method comprises determining notch mrna expression levels in pancreatic cancer cells.
Oncomed Pharmaceuticals, Inc.


02/04/16
20160030513 
 Notch1 decoy antagonists protect from obesity-induced insulin resistance and fatty liver patent thumbnailNotch1 decoy antagonists protect from obesity-induced insulin resistance and fatty liver
(b) instructions for using the pharmaceutical composition of step (a) to treat the fatty liver disease.. .

02/04/16
20160030512 

Combination preparation comprising a cytokine antagonist and corticosteroid


The present invention relates to the treatment of patients with pharmaceutical compositions for a combination therapy with a cytokine antagonist and a corticosteroid. By means of the combination therapy diseases such as osteoarthritis, tendon injuries and/or degenerative spinal diseases can be treated..
Orthogen Ag


02/04/16
20160030482 

Compositions and methods for enhancing the therapeutic potential of stem cells


The invention encompasses compositions and method of treating a vascular disease such as peripheral artery disease, the methods involve—administering to a patient in need thereof, an effective amount of a composition comprising a population of cells such as mesenchymal stem cells (mscs) and a non-muscle myosin 0 antagonist such as blebbistatin. Non-muscle myosin ii antagonists are disclosed to surprisingly and dramatically accelerate msc-triggered regeneration of damaged tissues arid unexpectedly and drastically reduce severe complications of stem cell treatment..
Lonza Cologne Gmbh


02/04/16
20160030478 

Materials and methods to enhance hematopoietic stem cells engraftment procedures


This disclosure is directed to the methods of enhancing hematopoietic stem cells (hspc) and progenitor cell (hspc) engraftment procedure. Treatment in vivo of a hspc donor with compounds that reduce pge2 biosynthesis or pge2 receptor antagonists alone, or in combination with other hematopoietic mobilization agents such as amd3100 and g-csf, increases the circulation of available hspcs.
Indiana University Research And Technology Corp.


02/04/16
20160030474 

Brain, spinal and nerve injury treatment


A treatment for brain, spinal and nerve injury comprising use of a substance p receptor antagonist optionally in combination with a magnesium compound. There is also provided a formulation for use in this treatment comprising a substance p receptor antagonist and a magnesium compound..
Eustralis Pharmaceuticals Limited


02/04/16
20160030442 

Novel compounds


Wherein r1 is 2-indanyl, r2 is 1-methylpropyl, r3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, r4 represents methyl and r5 represents hydrogen or methyl or, r4 and r5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.. .

02/04/16
20160030430 

Tetrahydropyrazolopyrimidine compounds


Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine 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. .
Eisai R&d Management Co., Ltd.


02/04/16
20160030422 

Rbp4 antagonists for the treatment of age-related macular degeneration and stargardt disease


A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in a mammal afflicted therewith, comprising administering to the mammal an effective amount of a compound having the structure of any one of formulas i-iv described herein, or a pharmaceutically acceptable salt thereof.. .

02/04/16
20160030418 

Method for decreasing low density lipid protein


The present invention further relates to a composition for treating bipolar ii disorder, which comprises valproic acid and at least one agent selected from the group of dextromethorphan and memantine, wherein the dose of dextromethorphan or memantine is a low dose not sufficient to work as a n-methyl-d-aspartate (nmda) receptor antagonist.. .

02/04/16
20160030397 

Compositions and methods of using (r)-pramipexole


Pharmaceutical compositions of (r)-pramipexole and one or more secondary therapeutic agents such as, for example, dopamine agonists, dopaminergic agonists, comt inhibitors, moa inhibitors, excitatory amino acid antagonists, growth factors, neurotrophic factors, antioxidants, anti-inflammatory agents, immunomodulators, anti-glutamatergics, ion channel blockers, α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (ampa) receptor antagonists, heat shock protein inducers/protein disaggregators and downregulators, monoamine oxidase type b (moab) inhibitors, multi-target agents, kinase inhibitors, bcl inducers, histone deacetylase (hdac) mediators, glial modulators, mitochondrial energy promoting agents, myostatin inhibitors, caspase inhibitors and combinations thereof or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.. .
Knopp Biosciences Llc


02/04/16
20160030386 

Prevention of rosacea inflammation


The disclosure demonstrates the role of mast cell stabilizers in treating rosacea. The disclosure also shows the role of mast cells, cathelicidin, serine protease and/or vitamin d3 in rosacea pathology and the use of antagonists and inhibitors thereof to treat rosacea..
The Regents Of The University Of California


01/28/16
20160025746 

Methods of screening compounds that can modulate nr2f6 by displacement of a reference ligand


The current invention discloses compositions of matter, protocols and methods of screening test compounds to identifying agonists and antagonists of the orphan nuclear receptor nr2f6 by measuring the ability of a test compound to occupy the active site of nr2f6, in the presence of a reference compound.. .
Regen Biopharma, Inc


01/28/16
20160024224 

Anti-factor b antibodies and their uses


The invention concerns the prevention and treatment of complement-associated eye conditions, such as choroidal neovascularization (cnv) and age-related macular degeneration (amd), by administration of factor b antagonists.. .
Genentech, Inc.


01/28/16
20160024201 

Methods of treating diseases which are mediated by cutaneous lymphocyte antigen positive cells


The present invention relates to methods of treating patients suffering from itching and puritis mediated by cutaneous lymphocyte antigen positive t cell. In particular, diseases or disorders including contact dermatitis, drug induced delayed type cutaneous allergic reactions, toxic epidermal necrolysis, cutaneous t cell lymphoma, bullous pemphigoid, alopecia aereata, vitiligo, acne rosacea, prurigo nodularis, and herpes simplex virus, or combination thereof will benefit from the administration of an il-31 antagonist.
Zymogenetics, Inc.


01/28/16
20160024092 

Intravenous formulations of neurokinin-1 antagonists


Or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein..

01/28/16
20160024064 

Azetidine amide derivatives as orexin receptor antagonists


The present invention relates to azetidine amide derivatives derivatives of formula (i) wherein rings a1 a2 and a3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to pharmaceutical compositions containing one or more compounds of formula (i), and to their use as pharmaceuticals, especially to their use as orexin receptor antagonists.. .
Actelion Pharmaceuticals Ltd


01/28/16
20160024009 

Novel sulfonamide trpa1 receptor antagonists


The invention discloses compounds of formula (i). The compounds of formula (i) are trpa1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of trpa1 receptors..
Ario Pharma Limited


01/28/16
20160022814 

Combination of a pd-1 antagonist and a listeria-based vaccine for treating prostate cancer


The present disclosure describes combination therapies comprising an antagonist of programmed death 1 receptor (pd-1) and a listeria based strain that expresses prostate-tissue specific antigen (psa), and the use of the combination therapies for the treatment of prostate cancer.. .
Merck Sharpe And Dohme Corp.


01/28/16
20160022772 

Cytokine receptors as targets for hypertension therapy and methods of use


The present disclosure provides methods of treating or ameliorating hypertension in a subject comprising administering a therapeutically effective amount of an il-1 receptor antagonist.. .
Duke University


01/28/16
20160022757 

Therapeutic methods for treating solid tumors and related diagnostic methods


The present invention provides a method for treating a subject afflicted with a cancer which comprises administering to the subject (i) a proteasome antagonist and (ii) a pi3k signal transduction pathway antagonist, each of (i) and (ii) in an amount such that when both (i) and (ii) are administered, the administration is effective to treat the subject. The present invention also provides a method for treating a subject afflicted with a cancer which comprises administering to the subject (i) a proteasome antagonist, and (ii) an oligonucleotide which decreases the amount of pi3k, mtor, torc1, torc2, akt, or jnk produced by cells of the cancer.
Icahn School Of Medicine At Mount Sinai


01/28/16
20160022708 

Methods and compositions for the treatment of glutamine-addicted cancers


Provided herein are methods for a novel combination therapy for treating a glutamine-addicted cancer in a subject in need thereof, which comprises the administration of a glutaminase antagonist and a pro-apoptotic compound. Specific glutaminase antagonists and pro-apoptotic compounds are provided.
St. Jude Children's Research Hospital


01/28/16
20160022653 

Methods and pharmaceutical compositions for the treatment of symptoms of anxiety and panic using beta adrenergic receptor antagonist and muscarinic receptor antagonist combinations


The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist.

01/28/16
20160022652 

Methods and pharmaceutical compositions for the treatment of symptoms of anxiety and panic using beta adrenergic receptor antagonist and muscarinic receptor antagonist combinations


The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist.

01/28/16
20160022635 

Use of arginine vasopressin receptor antagonists for the treatment of prostate cancer


Described herein are methods of decreasing the proliferation of prostate cancer cells in a mammalian subject by administering to a subject in need thereof a composition comprising an avpr antagonist in amount effective to decrease proliferation of the cancer cells. Also provided are methods of inducing prostate cancer cell death (or decreasing invasion migration of the prostate cancer cells) in a mammalian subject by administering to a subject in need thereof a composition comprising an avpr antagonist..
University Of Miami


01/28/16
20160022614 

Compositions and methods for treating cancer


Compositions containing one or more cox inhibitors in combination with one or more antagonists of 20-hete (20-hydroxyeicosatetraeonic acid), and optionally a pharmaceutically acceptable excipient are provided. Preferred compositions include rofecoxib in combination with het0016.
Georgia Regents Research Institute, Inc.


01/21/16
20160017053 

Non-antagonistic egfr-binding molecules and immunoconjugates thereof


Novel anti-cancer agents, including, but not limited to, antibodies and immunoconjugates, that bind to egfr are provided. Methods of using the agents, antibodies, or immunoconjugates, such as methods of inhibiting tumor growth are further provided..
Immunogen, Inc.


01/21/16
20160017028 

Pharmaceutical composition containing antagonist of egf family ligand as component


The present inventors identified inhibition of a combination of egfr ligands that serve as targets for inhibition of cancer cell proliferation. More specifically, ereg antagonists and tgfα antagonists were found to be useful as inhibitors of cell growth.
Chugai Seiyaku Kabushiki Kaisha


01/21/16
20160017024 

Fam150a, fam150b, and fam150 antagonists and uses thereof


Methods of identifying and using fam150a agents, fam150b agents, and fam150 antagonists are provided. Methods of identifying and using ltk agonists (including ltk agonist antibodies, fam150a agents, and fam150b agents) and fam150 antagonists are provided.
Five Prime Therapeutics, Inc.


01/21/16
20160017010 

Methods and compositions for delivering interleukin-1 receptor antagonist


Methods and compositions generating and using an interleukin-1 receptor antagonist (il-1ra)-rich solution. Methods for generating and isolating interleukin-1 receptor antagonist include incubating a liquid volume of white blood cells and platelets with polyacrylamide beads to produce interleukin-1 receptor antagonist.
Biomet Biologics, Llc


01/21/16
20160016965 

Novel mixed μ agonist/ δ antagonist opioid analgesics with reduced tolerance liabilities and uses thereof


An opioid narcotics used for the treatment of moderate-to-severe pain that primarily exert their analgesic effects through μ receptors. Although, traditional μ agonists can cause undesired side effects, including tolerance, addition of δ antagonists can attenuate said side effects.
West Virginia University


01/21/16
20160016935 

2-pyridyloxy-4-ether orexin receptor antagonists


The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether 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.


01/21/16
20160016920 

Analogs of peroxisome proliferator activated receptor (ppar) agonists, and methods of using the same


Analogs of ppar5 and analogs of 20-oh-pge2, which are ppar5 agonists and 20-oh-pge2 antagonists, respectively, and methods of using the same for inducing osteogenesis or chondrogenesis, are disclosed.. .
The University Of Toledo


01/21/16
20160016900 

Thromboxane receptor antagonists


The invention generally relates to compounds that function as tp antagonists for treating thrombosis and other cardiovascular, renal, or pulmonary diseases. In some embodiments, the invention provides a compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group.
University College Dublin, National University Of Ireland, Dublin


01/21/16
20160015895 

Devices and methods for delivering opioid antagonists including formulations for naloxone


An apparatus includes a container, a needle, and an actuation assembly. The container contains a dose of a naloxone composition having a delivered volume of at least about 0.34 ml.
Kaleo, Inc.


01/21/16
20160015779 

Immunomodulating tumor necrosis factor receptor 25 (tnfr25) agonists, antagonists, and immunotoxins


This document provides novel compositions and methods utilizing immunomodulating agents that can stimulate or indirectly augment the immune system, or can have an immunosuppressive effect. Tnfr25 agonists disclosed herein have an anti-inflammatory and healing effect.
University Of Miami


01/21/16
20160015760 

Newcastle disease viruses and uses thereof


Described herein are chimeric newcastle disease viruses engineered to express an agonist of a co-stimulatory signal of an immune cell and compositions comprising such viruses. Also described herein are chimeric newcastle disease viruses engineered to express an antagonist of an inhibitory signal of an immune cell and compositions comprising such viruses.
Memorial Sloan Kettering Cancer Center


01/21/16
20160015704 

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.. .
Almirall, S.a.


01/21/16
20160015701 

Methods of treating acute kidney injury


Methods are provided for treating acute kidney injury in a subject, particularly ischemia-induced kidney injury and/or hypoxia-induced kidney injury. The methods comprise administering to the subject an eta receptor antagonist, such as atrasentan or a pharmaceutically acceptable salt thereof.
Fred Hutchinson Cancer Research Center


01/21/16
20160015644 

Gastro-retentive sustained-release oral dosage form of a bile acid sequestrant


Disclosed herein are novel compositions and methods for controlling the release of bile acid sequestrant to the stomach in order to treat or prevent upper gi tract disorders or disorders of the throat. 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 dispersed in a polymeric matrix.
Ironwood Pharmaceuticals, Inc.


01/14/16
20160009792 

Apolipoprotein c3 (apociii) antagonists and methods of their use to remove apociii inhibition of lipoprotein lipase (lpl)


Provided herein are methods of increasing lipoprotein lipase (lpl) activity, by inhibiting apolipoprotein c3 (apociii), which removes the apociii inhibition of lpl, and permits vldl to be converted to ldl. Also provided are methods for treating or preventing a lipid metabolism disorder, such as type 2 diabetes by use of an apociii antagonist.
Imetabolic Biopharma, Llc


01/14/16
20160009773 

Rspondins as modulators of angiogenesis and vasculogenesis


The present invention relates to the use of rspondins, particularly rspondin2 (rspo2) or rspondin3 (rspo3) or rspondin nucleic acids, or regulators or effectors or modulators of rspondin, e.g. Rspo2 and/or rspo3 to promote or inhibit angiogenesis and/or vasculogenesis, respectively.
Deutsches Krebsforschungszentrum Stiftung Des Öffentlichen Rechts


01/14/16
20160009698 

Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1h)-one derivatives having both β2 adrenergic receptor agonist and m3 muscarinic receptor antagonist activities


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


01/14/16
20160009697 

Pyridine derivatives as 5-ht6 receptor antagonists


Compounds of formula (i), wherein x, y, z, r1-r7, m and n are as defined herein, exhibit 5-ht6 antagonistic activity and are thus useful for the treatment of certain cns disorders. Methods of use of said compounds are also provided..
Selvita S.a.


01/14/16
20160009645 

H3 antagonists containing phenoxypiperidine core structure


The present invention relates to new histamine h3 (h3) receptor subtype selective ligands of the general formula (i) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of h3 receptors.
Richter Gedeon Nyrt.


01/14/16
20160009639 

Novel antagonists of the glucagon receptor


The present invention provides for novel compounds of formula (i) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including type i and ii diabetes, insulin resistance and hyperglycemia.
Metabasis Therapeutics, Inc.


01/14/16
20160008419 

Methods and compositions for the prevention and treatment of parasitic disease


Compositions and methods are provided for treating or preventing a parasitic disease in a subject. Aspects of the methods include administering an aldh antagonist to a subject that is infected with a parasite or that is at risk for being infected with a parasite.
The Board Of Trustees Of The Leland Stanford Junior University


01/14/16
20160008351 

Abuse-resistant controlled-release opioid dosage form


Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally.
Purdue Pharma L.p.


01/14/16
20160008350 

Pharmaceutical formulation containing opioid agonist, opioid antagonist and gelling agent


Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.. .
Purdue Pharmaceuticals L.p.


01/14/16
20160008346 

Abuse-resistant controlled-release opioid dosage form


Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally.
Purdue Pharma L.p.


01/14/16
20160008343 

Compounds and methods of prophylaxis and treatment regarding nicotinic receptor antagonists


It is an object of the present invention that the novel nicotinic receptor antagonists disclosed herein may be used in a broad array of clinical or medicinal facets. For example, it is a contemplated use of the present invention that the novel nicotinic receptor antagonists be used to inhibit the growth cycle of non-small cell lung cancer cells.

01/14/16
20160008323 

Nicotinic receptor non-competitive antagonists


The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.. .
Targacept, Inc.


01/14/16
20160008297 

Compounds for preventing, reducing and/or alleviating itchy skin condition(s)


The present invention primarily relates to the use of one or more specific compounds and/or one or more respective salt(s) thereof for preventing, reducing or alleviating itchy skin condition(s), and/or as par-2 antagonist. Furthermore, the present invention relates to compositions (products or, respectively, formulations), in particular for topical administration, preferably cosmetic or pharmaceutical compositions, in particular for preventing, reducing or alleviating one or more itchy skin conditions and/or for providing a par-2 antagonistic effect, comprising or consisting of an effect amount of such compound(s) and/or salt(s) and one or more cosmetically and/or pharmaceutically acceptable carriers..
B.r.a.i.n. Biotechnology Research And Information Network Ag


01/14/16
20160008277 

Co-packaged drug products


Provided herein are drug products comprising a combination of an opioid receptor agonist and an opioid receptor agonists, including co-packaged drug products comprising an opioid receptor agonist and an opioid receptor antagonist in a delivery device selected from a hand-held auto-injector and a pre-primed nasal delivery device, and methods of prescribing and dispensing same. Methods of lowering opioid overdose risk by providing a combination of an opioid receptor agonist and an opioid receptor agonists, for example by co-packaging an opioid receptor agonist and an opioid receptor antagonist in a delivery device, are also provided..
Lightlake Therapeutics Inc.


01/07/16
20160002340 

Zcytor17 heterodimeric cytokine receptor monoclonal antibodies


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.


01/07/16
20160002335 

Therapeutic use of anti-cs1 antibodies


The present invention is directed to antagonists of cs1 that bind to and neutralize at least one biological activity of cs1. The invention also includes a pharmaceutical composition comprising such antibodies or antigen-binding fragments thereof.
Abbvie Biotherapeutics Inc.


01/07/16
20160002329 

Treatment of conditions involving demyelination


The invention provides methods of treating diseases, disorders or injuries involving demyelination and dysmyelination, including multiple sclerosis, by the administration of an sp35 antagonist. Additional methods include methods for inhibiting the binding of the sp35 polypeptide with the erbb2 polypeptide and a method for increasing erbb2 phosphorylation by contacting oligodendrocytes with an effective amount of a composition comprising an sp35 antagonist of the invention.
Biogen Ma Inc.


01/07/16
20160002312 

Oral composition comprising a tnf antagonist and use thereof


This application further describes a method of treating, preventing or reducing liver diseases, the method comprising, administering to the subject a therapeutically effective amount of a tnf antagonist molecule.. .

01/07/16
20160002220 

Muscarinic acetylcholine receptor antagonists


Methods of using muscarinic acetylcholine receptor antagonists are provided.. .
Glaxo Group Limited


01/07/16
20160002174 

Cxcr4 antagonists for the treatment of medical disorders


The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine cxcr4 receptor for the treatment of proliferative conditions mediated by cxcr4 receptors. The compounds provided interfere with the binding of sdf1 to the receptor.
Emory University


01/07/16
20160000877 

Compositions and methods for modulating gamma-c-cytokine activity


The γc-family cytokines, interleukin-2 (il-2), interleukin-4 (il-4), interleukin-7 (il-7), interleukin-9 (il-9), interleukin-15 (il-15), and interleukin-21 (il-21), are associated with important human diseases, such as leukemia, autoimmune diseases, collagen diseases, diabetes mellitus, skin diseases, degenerative neuronal diseases and graft-versus-host disease (gvhd). Thus, inhibitors of γc-cytokine activity are valuable therapeutic and cosmetic agents as well as research tools.
Bioniz, Llc


01/07/16
20160000870 

Methods and compositions for delivering interleukin-1 receptor antagonist


Methods, systems, and compositions related to generating and using a solution rich in interleukin-1 receptor antagonist are provided. Methods include contacting a liquid comprising white blood cells with a solid extraction material and stimulating with an electromagnetic field to activate production of interleukin-1 receptor antagonist.
Biomet Biologics, Llc


01/07/16
20160000817 

Treatment of ocular disorders


The invention includes a method of treating an intraocular disorder in a mammal, the method comprising administering to the mammal a very late antigen-4 (vla-4) antagonist for the treatment of selected ocular disorders.. .
Massachusetts Eye And Ear Infirmary


01/07/16
20160000814 

Treatment of cystic diseases


The invention described herein pertains to the treatment of cystic diseases. More particularly, the invention described herein relates to methods for treating cystic disease using one or more lysophosphatidic acid antagonists, tmem16a inhibitors, and/or peroxisome proliferator-activated receptor modulators..
Indiana University Research And Technology Corporation


01/07/16
20160000790 

Drug combination


The invention provides a composition which comprises (a) a pde3/pde4 inhibitor which is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2h-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a muscarinic receptor antagonist.. .
Verona Pharma Plc


01/07/16
20160000777 

Methods of using histamine receptor agonists and antagonists


This invention relates to a transdermal drug formulation that includes a pharmaceutically suitable carrier; an effective amount of a therapeutic agent; and a histamine type 4 receptor (“h4r”) agonist, as well as a transdermal vaccine formulation that includes a pharmaceutically suitable carrier; an effective amount of an antigen or antigen-encoding nucleic acid molecule present in the carrier, and optionally one or more adjuvants; and an h4r agonist. The present invention also relates to transdermal delivery device including such formulations and methods of administering such formulations.
University Of Rochester


01/07/16
20160000733 

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.

01/07/16
20160000578 

Intervertebral implant with integrated fixation


A system for spinal surgery includes a prosthesis comprising a plurality of bone anchors which engage an intervertebral construct for fusion or motion preservation. The fusion construct comprises a spacer optionally encircled by a jacket.
Howmedica Osteonics Corp.


12/31/15
20150377888 

Methods for predicting and preventing metastasis in triple negative breast cancers


In particular the present invention relates to a method for predicting the risk of relapse and distant metastasis in a patient suffering from a triple negative breast cancer comprising the step of i) determining the level of soluble cd95l in a blood sample obtained from the patient ii) comparing the level determined at step i) with a predetermined reference value and iii) concluding that the patient will exhibit an increased risk of relapse and distant metastasis when the level determined at step i) is higher than the predetermined reference value or concluding that the patient will exhibit a decreased risk of relapse and distant metastasis when the level determined at step i) is lower than the predetermined reference value. The present invention also relates to a method of preventing metastases in a subject suffering from triple negative breast cancer comprising the steps consisting of i) predicting the risk of relapse and distant metastasis by the method according to the invention and ii) administering the subject with a therapeutically effective amount of a cd95 antagonist when it is concluded at step i) that the subject will exhibit an increased risk of relapse and distant metastasis..
Universite Des Antilles Et De La Guyane


12/31/15
20150376292 

Anti c-met antibodies


The present invention relates to antibodies that specifically bind to the human c-met receptor protein and that act as strict antagonists of hepatocyte growth factor (hgf)-mediated activation of the c-met receptor and also inhibit hgf-independent activation of the human c-met protein.. .
Argen-x N.v.


12/31/15
20150376291 

Anti c-met antibodies


The present invention relates to antibodies that specifically bind to the human c-met receptor protein and that act as strict antagonists of hepatocyte growth factor (hgf)-mediated activation of the c-met receptor and also inhibit hgf-independent activation of the human c-met protein.. .
Argen-x N.v.


12/31/15
20150376272 

Inhibition of angiogenesis in refractory tumors


The present invention relates generally to the inhibition of tumor angiogenesis. In particular, the invention concerns the prevention or treatment of tumor angiogenesis and the suppression of tumor growth in tumors refractory to an anti-vascular endothelial growth factor (vegf) treatment, using il-17 antagonists, such as anti-il-17 antibodies and other antagonists..
Genentech, Inc.


12/31/15
20150376271 

Dual pdgf/vegf antagonists


The invention provides a dual vegf/pdgf antagonist comprising a vegf antagonist linked to a pdgf antagonist. The vegf antagonist is an antibody to a vegf or vegfr or is a vegfr extracellular trap segment (i.e., a segment from the extracellular region of one or more vegfr receptors that inhibits binding of at least one vegfr to at least one vegf).
Oligasis, Llc


12/31/15
20150376130 

N-prop-2-ynyl carboxamide derivatives and their use as trpa1 antagonists


Compounds of formula i, wherein a, b, x, z and r1-r6, are as defined in the claims, exhibit trpa 1 activity and are thus useful as trpa1 modulators.. .
Orlon Corporation


12/31/15
20150374836 

Analgesic conjugates


The invention provides analgesic conjugates having a mu opioid receptor agonist linked to a mglur5 antagonist, and to methods for producing analgesia using such compounds.. .
Regents Of The University Of Minnesota


12/31/15
20150374721 

Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies


Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer.
Tokai Pharmaceuticals, Inc.


12/31/15
20150374718 

Zhankuic acid a and analogs thereof and their use as an anti-inflammatory agent


Zhankuic acid a (zaa) is the major pharmacologically active compound of taiwanofungus camphoratus. We analyzed the structure of human tlr4/md-2 complex with zaa by x-score and hotlig modeling approaches.
National Cheng Kung University


12/31/15
20150374695 

6-piperazinyl-3,4-dihydroquinazolin-2(1h)-ones


A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1h)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent d2 receptor antagonist and 5-ht1a receptor agonist properties.
King Abdulaziz City For Science And Technology


12/31/15
20150374684 

Composition and treatment of depression and psychosis in humans


Compositions and methods for the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an nmdar antagonist.
Glytech, Llc


12/24/15
20150368338 

Interferon alpha and omega antibody antagonists


The present invention relates to antibodies that broady neutralize interferon-α and interferon-ω, polynucleotides encoding the antibodies or fragments, and methods of making and using the foregoing.. .
Janssen Biotech, Inc.


12/24/15
20150368337 

Anti-il-6 antibodies for the treatment of oral mucositis


The present invention is directed to therapeutic methods using il-6 antagonists such as anti-il-6 antibodies and fragments thereof having binding specificity for il-6 to prevent or treat mucositis (e.g., oral mucositis) including persons on a treatment regimen with a drug or chemotherapy and/or radiation for cancer (e.g., head and neck cancer) that is associated with increased risk of mucositis, including oral mucositis.. .
Alderbio Holdings Llc


12/24/15
20150368330 

Methods of preventing or treating pain using anti-ngf antibodies that selectively inhibit the association of ngf with trka, without affecting the association of ngf with p75


This invention pertains to ngf antagonists including antibodies and antibody fragments thereof having binding specificity to human nerve growth factor (“ngf”), and methods of treating pain. Methods of treating pain or eliciting an analgesic effect in an individual comprising administering an effective amount of an ngf antagonist inhibits the association of ngf with trka without inhibiting the association of ngf with p75.
Alderbio Holdings Llc


12/24/15
20150368318 

Mutants of interleukin-1 receptor antagonist and uses thereof


The invention provides an isolated polypeptide comprising a variant amino acid sequence of seq id no: 1, or a fusion or derivative of said polypeptide, or a fusion of a said derivative thereof, wherein the polypeptide, fusion or derivative retains a biological activity of wild type il-ira. In one embodiment, the isolated polypeptide, fusion or derivative is or comprises a polypeptide variant of amino acid sequence seq id no: 1 comprising or consisting of substitutions at one or more of the following amino acid mutations of seq id no: 1: q29k, p38y, p38r, l42w, d47n, e52r, h54r, e90y, q129l, q129n, m136n, m136d and q149k.
Alligator Bioscience Ab


12/24/15
20150366943 

Mobilization of hematopoietic stem cells from bone marrow to blood using a combination of a robo4 receptor antagonist and a cxcr4 antagonist or hrvegf-165 and a cxcr4 antagonist


The invention herein disclosed provides for compositions, methods for synthesizing said compositions, and methods for using said compositions, wherein the compositions and methods may be used in clinical treatment using hematopoietic transplantation, particularly to those relating to treatment of cancer and metastasis. The compositions regulate mobilization of hematopoietic stem cells (hscs) between bone marrow (bm) and the peripheral blood (pb)..
The Regents Of The University Of California


12/24/15
20150366930 

Treatment of disorders with altered vascular barrier function


The present invention provides methods of using rasip1 agonists and antagonists to modulate vascular barrier function and regulate new vessel formation, and to treat related disorders.. .
Genentech, Inc.


12/24/15
20150366920 

Method for preventing and/or treating infections, colonisations, or illnesses related to staphylococcus aureus, pseudomonas aeruginosa, streptococcus pyogenes, enterococcus faecium, enterobacter cloacae, proteus mirabilis, bacteroides fragilis, staphylococcus epidermidis, propionibacterium acnes, candida albicans and/or malassezia furfur


The subject matter of the present invention is a bacterium or a mixture of bacteria having an antagonistic activity with respect to strains of s. Aureus, p.
Laboratoires Urgo


12/24/15
20150366882 

System and diagnosis and treatment


This invention relates the use of cortisol blockers (glucocorticoid receptor [gr] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.. .
Pop Test Oncology Limited Liability Company


12/24/15
20150366881 

System 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


12/24/15
20150366855 

Muscarinic antagonists and combinations thereof for the treatment of airway disease in horses


The invention relates to the field of medicine, in particular to the field of veterinary medicine. The invention specifically relates to muscarinic antagonists (including long acting muscarinic antagonists (lamas)) for the treatment of airway disease, such as pulmonary disease, preferably recurrent airway obstruction (rao), summer pasture associated obstructive pulmonary disease (spaopd), and inflammatory airway disease (iad) in animals, preferably equines such as horses..
Boehringer Ingelheim Vetmedica Gmbh


12/24/15
20150366811 

Pharmaceutical products


Disclosed in certain embodiments is a dosage form comprising a plurality of extruded particles comprising an adverse agent or antagonist and a layer disposed about the particles.. .
Purdue Pharma L.p.


12/24/15
20150366549 

Exposure posterior spinal minimally invasive screw placement surgery


An exposure apparatus for posterior spinal minimally invasive screw placement surgery includes a transverse process refractor and a facet joint retractor, is provided. The apparatus separates a gap between a multifidus muscle and a longissimus muscle, easily and atraumatically reach a screw placement position on a pedicle, accurately place the retractors, and thereafter locally form a screw placement tunnel space that externally extends 10 to 15 degrees.
The First Affiliated Hospital Of Nanjing Medical University




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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