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Antagonist patents



      

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




Date/App# patent app List of recent Antagonist-related patents
06/16/16
20160169918 
 Methods of diagnosis and treatment for pulmonary arterial hypertension patent thumbnailMethods of diagnosis and treatment for pulmonary arterial hypertension
Diagnostic and therapeutic agents for pulmonary arterial hypertension (pah) are provided. Circulating microparticles (mps) and/or the expression level of gpr75 are significantly increased in pah-pasmc, but not normal pasmc, thus, providing a non-invasive diagnostic method for pah.
The Regents Of The University Of California


06/16/16
20160168640 
 Therapeutic and diagnostic methods for il-33-mediated disorders patent thumbnailTherapeutic and diagnostic methods for il-33-mediated disorders
The invention relates to methods of treating a patient suffering from an il-33-mediated disorder, such as asthma, comprising administering to the patient an il-33 axis binding antagonist based on the genotype of the il1rl1 gene. The invention further relates to methods of determining whether a patient is at increased risk of an il-33-mediated disorder, as well as methods of determining whether a patient suffering from such a disorder is likely to respond to a treatment comprising an il-33 axis binding antagonist, based on the genotype of the il1rl1 gene..
Genentech, Inc.


06/16/16
20160168252 
 Antibodies, compounds and derivatives thereof for use in the treatment of male infertility patent thumbnailAntibodies, compounds and derivatives thereof for use in the treatment of male infertility
The present invention relates to antagonists or inhibitors, which bind selectively to rankl/opgbp and regulate the interaction between rankl/opgbp and rank/opg. In particular, the present invention relates to an antibody or antigen binding domain, fragment or derivative thereof, immunoreactive with a rankl/opgbppeptide for use in the treatment, prevention or alleviation of male infertility or reduced male fertility such as oligospermia or azospermia..
Rigshopitalet Copenhagen University Hospital


06/16/16
20160168244 
 Antagonist antibodies directed against calcitonin gene-related peptide and methods using same patent thumbnailAntagonist antibodies directed against calcitonin gene-related peptide and methods using same
The invention features methods for preventing or treating cgrp associated disorders such as vasomotor symptoms, including headaches (e.g., migraine, cluster headache, and tension headache) and hot flushes, by administering an anti-cgrp antagonist antibody. Antagonist antibody g1 and antibodies derived from g1 directed to cgrp are also described..
Labrys Biologics, Inc.


06/16/16
20160168243 
 Antagonists to il-6 to raise albumin and/or lower crp patent thumbnailAntagonists to il-6 to raise albumin and/or lower crp
The present invention is directed to therapeutic methods using il-6 antagonists such as antibodies and fragments thereof having binding specificity for il-6 to improve survivability or quality of life of a patient in need thereof. In preferred embodiments these patients will comprise those exhibiting (or at risk of developing) an elevated serum c-reactive protein level or a reduced serum albumin level prior to treatment.
Alderbio Holdings Llc


06/16/16
20160168240 
 Use of vegf antagonist in treating chorioretinal neovascular and permeability disorders in paediatric patients patent thumbnailUse of vegf antagonist in treating chorioretinal neovascular and permeability disorders in paediatric patients
The present invention relates to the use of a vegf antagonist in the treatment of chorioretinal neovascular or permeability disorders in children. In particular, the invention provides a vegf antagonist for use in a method for treating a child having cnv or me, wherein said method comprises administering to the eye of a child a vegf antagonist that either does not enter or is rapidly cleared from the systemic circulation.

06/16/16
20160168090 
 Novel indole derivatives and their use in neurodegenerative diseases patent thumbnailNovel indole derivatives and their use in neurodegenerative diseases
The present invention relates to indole compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of p2x7, and for the treatment of p2x7-related disorders.. .
Merck Patent Gmbh


06/16/16
20160166685 
 Combination therapy comprising ox40 binding agonists and pd-1 axis binding antagonists patent thumbnailCombination therapy comprising ox40 binding agonists and pd-1 axis binding antagonists
The invention provides compositions and methods for treating cancers. The method comprises administering a pd-1 axis binding antagonist and an ox40 binding agonist..
Genentech, Inc.


06/16/16
20160166684 
 Treatment of fibrotic diseases patent thumbnailTreatment of fibrotic diseases
The present invention relates to rspo and lgr antagonists, and methods of using the rspo and lgr antagonists for treating or preventing fibrotic diseases.. .
Oncomed Pharmaceuticals, Inc.


06/16/16
20160166652 
 Novel n- and c-terminal substituted antagonistic analogs of gh-rh patent thumbnailNovel n- and c-terminal substituted antagonistic analogs of gh-rh
There is provided a novel series of synthetic analogs of hgh-rh(1-29)nh2 (seq id no: 1) and hgh-rh(1-30)nh2. Of particular interest are those carrying phac, n-me-aib, dca, ac-ada, fer, ac-amc, me-nh-sub, phac-ada, ac-ada-d-phe, ac-ada-phe, dca-ada, dca-amc, nac-ada, ada-ada, or ch3—(ch2)10—co-ada, at the n-terminus and β-ala, amc, apa, ada, ae2a, ae4p, ε-lys(α-nh2), agm, lys(oct) or ahx, at the c-terminus.
U.s.a., Represented By The Department Of Veterans Affairs


06/16/16
20160166590 

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


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


06/16/16
20160166566 

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


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


06/16/16
20160166555 

Cyclooxygenase inhibitor and calcium channel antagonist compositions and methods for use in urological procedures


Compositions of a cyclooxygenase inhibitor and a calcium channel antagonist in a liquid carrier. The composition may be administered the urinary tract during urological diagnostic, interventional, surgical and other medical procedures.
Omeros Corporation


06/16/16
20160166506 

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


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


06/16/16
20160166503 

Nasal drug products and methods of their use


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


06/09/16
20160161494 

Methods and compositions for treating and diagnosing diseases


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


06/09/16
20160160213 

Methods of treating cancer and preventing cancer drug resistance


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


06/09/16
20160159927 

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


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


06/09/16
20160159914 

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


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


06/09/16
20160159893 

Use of a vegf antagonist in treating retinopathy of prematurity


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

06/09/16
20160159878 

Nogo receptor antagonists


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


06/09/16
20160159875 

Targeting of cytokine antagonists


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


06/09/16
20160159862 

Novel a4b7 peptide monomer and dimer antagonists


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


06/09/16
20160159790 

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


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


06/09/16
20160159779 

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


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


06/09/16
20160159744 

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


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

06/09/16
20160158360 

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


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


06/09/16
20160158325 

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


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


06/09/16
20160158236 

Pharmaceutical composition comprising a trpa1 antagonist and a steroid


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


06/09/16
20160158222 

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


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


06/09/16
20160158217 

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


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

06/09/16
20160158211 

Dosage and use of an a2a antagonist


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


06/09/16
20160158204 

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


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


06/09/16
20160158198 

Compositions and methods for ameliorating cachexia


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


06/09/16
20160158136 

Composition for reduction of trpa1 and trpv1 sensations


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


06/02/16
20160153043 

Method for predicting a treatment response to a crhr1 antagonist and/or a v1b antagonist in a patient with depressive and/or anxiety symptoms


The present invention relates to a method for predicting a treatment response to a corticotropin releasing hormone receptor type 1 (crhr1) antagonist and/or a vasopressin receptor 1b (v1b) antagonist in a patient with depressive and/or anxiety symptoms. The present invention furthermore relates to a v1b receptor antagonist and/or crhr1 antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a patient.
Max-planck-gesellschaft Zur FÖrderung Der Wissenschaften E.v.


06/02/16
20160152915 

Mechanical part coated with a layer of amorphous carbon for sliding in relation to a less hard component


A mechanical part provided with an amorphous carbon coating (with at least 70 wt. % of carbon not including hydrogen) and used to cooperate slidingly with an antagonistic part having a surface hardness which is a maximum of two thirds of that of the coating.
H.e.f.


06/02/16
20160152734 

Treatment with anti-pcsk9 antibodies


The present invention concerns dosages for the treatment of human patients susceptible to or diagnosed with a disorder characterized by marked elevations of low density lipoprotein particles in the plasma with a pcsk9 antagonist antiboyd alone or in combination with a statin.. .
Pfizer Inc.


06/02/16
20160152717 

Methods for treating dry eye disease by administering an il-6r antagonist


The present invention provides methods for treating dry eye disease by administering an il-6r antagonist to a subject in need thereof.. .
Regeneron Pharmaceuticals, Inc.


06/02/16
20160152710 

Milk fat globule epidermal growth factor 8 regulates fatty acid uptake


Methods and compositions for regulating fatty acid uptake and/or decreasing gastric motility in an animal are provided. The method comprises administering an antagonist of integrin αvβ3 or αvβ5 to an animal in an amount sufficient to reduce fatty acid uptake in the animal, thereby reducing fatty acid uptake in the animal.
Regents Of The University Of California


06/02/16
20160152709 

Compositions and methods for treatment of stroke


The invention relates, inter alia, to methods of treating stroke, e.g., ischemic stroke, e.g., acute ischemic stroke, and methods of reducing infarct size and/or other neurological deficits associated with stroke, e.g., ischemic stroke, e.g., acute ischemic stroke, using a vla-4 antagonist such as natalizumab. It was discovered that vla-4 antagonists such as natalizumab can effectively reduce the infarct size and other associated neurological deficits of a stroke, e.g., an ischemic stroke; e.g., an acute ischemic stroke, e.g., when administered within a specified time period after the onset of the stroke.
Biogen Ma Inc.


06/02/16
20160152708 

Method of inhibiting binding or activity of mif by administering a mif antagonist


Methods and compositions for using the mhc class ii invariant chain polypeptide, ii (also known as cd74), as a receptor for macrophage migration inhibitory factor (mif), are disclosed. These include methods and compositions for using this receptor, as well as agonists and antagonists of mif which bind to this receptor, or which otherwise modulate the interaction of mif with cd74 or the consequences of such interaction, in treatment of conditions characterized by locally or systemically altered mif levels, particularly inflammatory conditions and cancer..
Baxalta Gmbh


06/02/16
20160152698 

Anti-ngf antibodies and methods using same


The invention concerns anti-ngf antibodies (such as anti-ngf antagonist antibodies), and polynucleotides encoding the same. The invention further concerns use of such antibodies and/or polynucleotides in the treatment and/or prevention of pain, including post-surgical pain, rheumatoid arthritis pain, and osteoarthritis pain..
Rinat Neuroscience Corp.


06/02/16
20160152664 

Novel a4b7 peptide monomer and dimer antagonists


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


06/02/16
20160152592 

Imidazole diketone compound and use thereof


Provided are imidazolidinedione compounds of formula (i), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne..
Hinova Pharmaceuticals Inc.


06/02/16
20160151921 

Improved agonist - antagonist actuated joint


An actuated joint comprising a first element and a second element movable one with respect to the other, a first actuator and a second actuator connected to said first and second element for controlling the movement of said joint in an agonist-antagonist way, wherein said first actuator has a nominal or maximum power greater than that of said second actuator and said second actuator comprises at least a first elastic element extendable so as to store a maximum amount of elastic energy greater than that storable by said first actuator.. .
Fondazione Istituto Italiano Di Technologia


06/02/16
20160151449 

Use of tight junction antagonists to treat inflammatory bowel disease


The present invention provides materials and methods for the treatment of inflammatory bowel disease (e.g., crohn's disease and ulcerative colitis). Materials of the invention may include compositions comprising one or more tight junction antagonists and optionally one or more therapeutic agents.
Alba Therapeutics Corporation


06/02/16
20160151412 

Combination of xenon with an nmda receptor antagonist for fighting a neurodegenerative disease


The invention relates to a gaseous medication containing xenon, preferably in an amount of less than 75% by volume, for use by inhalation, in combination with at least one nmda receptor antagonist in the form of a liquid or solid, in particular memantine, for treating, slowing or preventing neurological deterioration consequent upon a neurodegenerative disease, in particular alzheimer's disease, in a human patient.. .
L'institut Du Cerveau Et De La Moelle Epiniere


06/02/16
20160151388 

Methods and compositions related to glucocorticoid receptor antagonism and prostate cancer


Methods are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity..
The University Of Chicago


06/02/16
20160151359 

Method of treating dyskinesia


Methods of treating patients with dyskinesias, by administering a therapeutically effective amount of a dual-action μ-opioid receptor antagonist/κ-opioid receptor agonists or prodrug thereof to a subject in need thereof, sufficient to mitigate the dyskinesia. Alternatively, a combination of both a mu-opioid receptor antagonist or prodrug thereof, and a kappa-opioid receptor agonist or prodrug thereof can be administered, either together or separately..
Rutgers, The State University Of New Jersey


06/02/16
20160151354 

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.


06/02/16
20160151353 

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.


06/02/16
20160151351 

Non-abusable pharmaceutical composition comprising opioids


There is provided pharmaceutical compositions for the treatment of pain comprising a pharmacologically-effective amount of an opioid analgesic, or a pharmaceutically-acceptable salt thereof, presented in particulate form upon the surfaces of carrier particles comprising a pharmacologically-effective amount of an opioid antagonist, or a pharmaceutically-acceptable salt thereof, which carrier particles are larger in size than the particles of the opioid analgesic. The compositions are also useful in prevention of opioid abuse by addicts..
Orexo Ab


06/02/16
20160151132 

Occlusion estimation in dental prosthesis design


Herein are provided methods, systems, computer-readable media, techniques and processes for occlusion estimation in dental prosthesis design. These include determining a first contact point between antagonist teeth, then simulating motion in order to determine additional contact points.
Biocad Medical, Inc.


05/26/16
20160145333 

Cb-1 receptor antigen-binding proteins and uses thereof


This disclosure relates to cb1 receptor antigen-binding proteins, e.g. Antibodies and methods of using the cb1 receptor antibodies.
Amgen Inc.


05/26/16
20160145315 

Peptide antagonists of the calcitonin cgrp family of peptide hormones and their use


The embodiments provide a modified calcitonin gene-related peptide antagonist including an n-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the n-terminal fragment are cysteine (cys) and at least one amino acid comprises a non-threonine substitution of a threonine (thr) residue; a central core where the central core comprises an a-helix; and a c-terminal fragment of modified calcitonin gene-related peptide or related protein family member comprising a c-terminal amide and where at least one amino acid of the c-terminal fragment is phenylalanine (phe), proline (pro), tyrosine (tyr) or hydroxyproline (hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition..

05/26/16
20160145294 

Antagonists of cb1 receptor


The invention relates to an antagonist of cb1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.. .
Universite De Bordeaux


05/26/16
20160145290 

E-selectin antagonist compounds, compositions, and methods of use


Methods and compositions using e-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of e-selectin to an e-selectin ligand. Described herein are e-selection antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation..
Glycomimetics, Inc.


05/26/16
20160145259 

Cxcr7 antagonists


Or pharmaceutically acceptable salts, hydrates or n-oxides thereof are provided and are useful for binding to cxcr7, and treating diseases that are dependent, at least in part, on cxcr7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient..

05/26/16
20160145215 

Process for preparing a pyrimidine intermediate


The present invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula i-2 or a salt thereof. Said compound of formula i-2 or its salt can be used to prepare macitentan.
Actelion Pharmaceuticals Ltd.


05/26/16
20160145213 

Heterocyclic compounds and methods of their use


The present invention relates generally to compounds that are useful in antagonizing the angiotensin ii type 2 (at2) receptor. More particularly, the invention relates to substituted isoquinoline compounds and their use as at2 receptor antagonists.
Novartis Ag


05/26/16
20160144025 

Methods and formulations for treating vascular eye diseases


The present invention provides methods for treating, preventing or reducing the severity of an eye disease. The methods of the present invention comprise administering to a subject in need thereof a therapeutic composition comprising an angiopoietin-2 (ang-2) inhibitor such as an anti-ang-2 antibody in combination with a vascular endothelial growth factor (vegf) antagonist (e.g., aflibercept)..
Regeneron Pharmaceuticals, Inc.


05/26/16
20160143999 

Combination therapy


The present disclosure relates to a method for treatment or prevention of diseases have an increased level of insulin-like growth factor i (igf-i). The method comprises administration of a growth hormone (gh) variant having antagonistic activity in combination with an oligonucleotide targeted to growth hormone receptor (ghr) to a subject in need..
Antisense Therapeutics Ltd


05/26/16
20160143995 

Method of treating intracellular infection


The present invention provides a method of treating an intracellular infection in a subject wherein the method comprising administering to the subject an iap antagonist. In certain embodiments the iap antagonist is a smac mimetic..
Tetralogic Pharamceuticals Corporation


05/26/16
20160143917 

Compositions and methods for modulating hiv activation


A pharmaceutical composition for inducing reactivation of latent provirus in an hiv infected cell includes an esr-1 antagonist or an esr-1 coactivator antagonist and a pharmaceutically acceptable carrier.. .
Case Western Reserve University


05/26/16
20160143915 

New cyclohexylamine derivatives having ß2 adrenergic agonist and m3 muscarinic antagonist activities


The present invention relates to novel compounds having β2 adrenergic agonist and m3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.. .
Almirall, S.a.


05/26/16
20160143910 

Methods of treating cancer and preventing cancer drug resistance


Provided herein are methods of treating and/or preventing cancer drug resistance using antagonists of kdm5.. .
Genentech, Inc.


05/26/16
20160143890 

Method and composition for treating alzheimer-type dementia


There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (achei) in a patient suffering from an alzheimer type dementia by decreasing concomitant adverse effects by administration of said achei in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the cns of said patient is achieved and alleviation of the symptoms of alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of alzheimer type dementia in combination with an acetyl choline esterase inhibitor (achei) and pharmaceutical compositions comprising (a) a 5ht3 receptor antagonist, a dopamine antagonist, a h1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described..
Chase Pharmaceuticals Corporation


05/26/16
20160143882 

Use of nk-1 receptor antagonist serlopitant in pruritus


The invention relates to methods for treating pruritus with nk-1 receptor antagonists such as serlopitant. The invention further relates to pharmaceutical compositions comprising nk-1 receptor antagonists such as serlopitant.
Tigercat Pharma, Inc.


05/19/16
20160138027 

Treatment of diseases and conditions associated with dysregulation of mammalian target of rapamycin complex 1 (mtorc1)


Compositions and methods for treating diseases and conditions associated with dysregulation of mammalian target of rapamycin complex 1 (mtorc1) are disclosed. The invention is based in part on the discovery that protein mediator of amino acid signaling to mtor (mortor) is involved in amino acid-induced translocation of mtorc1 to lysosomes where mortor forms a signaling complex with mtorc1, ragulator, and rag gtpases, which controls protein synthesis.
The Board Of Trustees Of The Leland Stanford Junior University


05/19/16
20160138022 

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


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


05/19/16
20160137737 

Integrin alpha-v beta8 neutralizing antibody


The present invention relates to αvβ8 antagonists, anti-αvβ8 antibodies or immunoconjugates for reducing tgfβ activation in an individual. Further provided are compositions comprising one of the αvβ8 antagonists, anti-αvβ8 antibodies or immunoconjugates, methods for using the compositions, and related subject matter..
The Regents Of The University Of California


05/19/16
20160137717 

Use of a vegf antagonist in treating choroidal neovascularisation


The present invention relates to the use of a non-antibody vegf antagonist, in the treatment of choroidal neovascularisation secondary to diseases other than age-related macular degeneration and pathologic myopia.. .

05/19/16
20160137629 

Compounds for binding to the platelet specific glycoprotein iib/iiia and their use for imaging of thrombi


The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (pet) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body.
Piramal Imaging Sa


05/19/16
20160136248 

Methods and materials for modulating deubiquitinases and ubiquitinated polypeptides


This document relates to methods and materials involved in modulating deubiquitinases (e.g., usp10 polypeptides) and/or ubiquitinated polypeptides (e.g., tumor suppressor polypeptides or mutant versions of tumor suppressor polypeptides). For example, methods and materials for increasing deubiquitinase (e.g., a usp10 polypeptide) expression or activity, methods and materials for decreasing deubiquitinase (e.g., a usp10 polypeptide) expression or activity, methods and materials for stabilizing tumor suppressor polypeptides (e.g., wild-type p53 polypeptides), methods and materials for de-stabilizing mutant versions of tumor suppressor polypeptides (e.g., mutant p53 polypeptides), and methods and materials for reducing cancer cell proliferation, increasing cancer cell apoptosis, and/or treating cancer (e.g., cancers having reduced levels of wild-type p53 polypeptides or cancers having increased levels of mutant p53 polypeptides) are provided.
Mayo Foundation For Medical Education And Research


05/19/16
20160136245 

Methods of treating pain using protein solutions


Methods and compositions for treating pain in mammalian subjects are provided. The methods include obtaining blood or a fraction of blood from the subject, measuring a therapeutic indicator in the blood or in the fraction blood, and administering an anti-inflammatory composition to the subject if the therapeutic indicator is equal to or above a threshold level.

05/19/16
20160136196 

Methods for treating pulmonary hypertension


The present invention relates to methods for treating or preventing pulmonary hypertension, reducing mortality in a subject experiencing pulmonary hypertension, or inhibiting adp-mediated vasoconstriction of pulmonary arteries in a subject, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a reversible p2y12 receptor antagonist. Also provided are related medicaments, pharmaceutical compositions, and methods for preparing the medicaments..
The Medicines Company


05/19/16
20160136194 

Pharmaceutical composition comprising a proton pump inhibitor and a prebiotic for the treatment of ulcerous lesions of the stomach and duodenum


A pharmaceutical composition including proton pump inhibitors and prebiotics is proposed for the treatment of gastric and duodenal ulcer, this allowing effective ulcer treatment and eradication of h. Pylori from the gastric and duodenal mucosa to be carried out without using wide-spectrum antibiotics.

05/19/16
20160136183 

Pharmaceutical compositions for preventing glucocorticoid-induced corneal or skin thinning


The present invention relates to method and pharmaceutical compositions for preventing glucocorticoid-induced corneal or skin thinning. In particular, the present invention relates to a mineralocorticoid receptor antagonist for topical use in a method for preventing or reducing glucocorticoid-induced corneal or skin thinning in a subject in need thereof.
Assistance Publique-hopitaux De Paris (aphp)


05/19/16
20160136157 

Intranasal naloxone compositions and methods of making and using same


Disclosed herein are compositions containing an opioid antagonist such as naloxone and one or more pharmaceutically acceptable excipients. The compositions may be used for intranasal delivery of naloxone for the treatment of, for example, opioid overdose in an individual in need thereof.
Antiop, Inc.


05/19/16
20160136153 

Diversion-resistant opioid formulations


The present invention provides a composition comprising an opioid agonist, and a polymer-antagonist conjugate. The polymer-antagonist conjugate preferably does not hydrolyze upon administration to a patient, and does not bind to the opioid receptors.
Elysium Therapeutics, Inc.


05/19/16
20160136145 

Bitopic muscarinic agonists and antagonists and methods of synthesis and use thereof


Compositions for treating a condition associated with activity of a muscarinic receptor (e.g., one or more of m1, m2, m3, m4, m5) and for anesthetizing a subject include a bitopic muscarinic antagonist or agonist. A bitopic muscarinic antagonist named jb-d4 was discovered.
Barry University, Inc.


05/19/16
20160136119 

Dp2 antagonist and uses thereof


Described herein is the dp2 antagonist [2′-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4′-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the dp2 antagonist, or a pharmaceutically acceptable salt thereof.
Brickell Biotech, Inc.


05/19/16
20160136079 

A3 adenosine receptor ligands for modulation of pigmentation


The present invention relates to compositions and methods for modulating melanin production, secretion and/or accumulation in human skin cells. In particular, the present invention relates to the use of a3 adenosine receptor antagonists in compositions and methods for the treatment and amelioration of hyper-pigmentation conditions and for the lightening of skin, and to the use of a3 adenosine receptor agonists in compositions and methods for the treatment and amelioration of hypo-pigmentation conditions and for the tanning of skin..
Oradin Pharmaceutical Ltd.


05/12/16
20160130337 

Methods for treating ocular diseases


A method is provided for reducing the treatment burden for patients who have an intraocular neovascular disorder, the method comprising administering a therapeutically effective amount of vegf antagonist on a dosing schedule that includes treatment intervals of 8 and/or 12 weeks.. .
Novartis Ag


05/12/16
20160130332 

Antibodies to human signal peptide-containing proteins


The invention provides a human signal peptide-containing proteins (sigp) and polynucleotides which identify and encode sigp. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists.
Incyte Corporation


05/12/16
20160130321 

Use of a vegf antagonist in treating macular edema


The present invention relates to the use of a non-antibody vegf antagonist in the treatment of macular edema secondary to diseases or conditions other than diabetes or retinal vein occlusion.. .

05/12/16
20160130320 

Modified chimeric polypeptides with improved pharmacokinetic properties


The present invention provides vegf antagonists with improved pharmacokinetic properties. According to certain embodiments, a fusion polypeptide capable of antagonizing vegf activity is provided comprising a modified extracellular ligand binding domain of a vegf receptor fused to a multimerizing component..
Regeneron Pharmaceuticals, Inc.


05/12/16
20160130318 

Interleukin 15 (il-15) antagonists and uses thereof for the treatment of autoimmune diseases and inflammatory diseases


The present relates to interleukin 15 (il-15) antagonists and uses thereof, in particular for the treatment of autoimmune diseases and inflammatory diseases. In particular, the present invention relates to an il-15 mutant polypeptide having the amino acid sequence as set forth in seq id no:1 wherein the leucine residue at position 45 is substituted by an aspartic acid residue, the asparagines residue at position 65 is substituted by a lysine residue and the leucine residue at position 69 is substituted by an arginine residue.
Universite D'angers


05/12/16
20160130273 

Process for making cgrp receptor antagonists


The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are cgrp receptor antagonists useful for the treatment of migraine.. .
Merck Sharp & Dohme Corp.


05/12/16
20160130270 

Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives


The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described..
Scifluor Life Sciences, Inc.


05/12/16
20160130262 

N-substituted azetidine derivatives


The present invention relates to novel n-substituted azetidine derivatives<of the formula (i); wherein sermf is a selective estrogen receptor modilator fragment; x is no atom, o, s, ch2, carbonyl, n—r5; r1 is h, (c1-8)alkyl, (c3-8)cycloalkyl, (c3-6)heterocycloalkyl, (c2-6)alkenyl, (c2-6)alkynyl, (c1-4)alkylcarbonyl, (c1-4)alkoxy(c2-4)alkyl, (c3-6)cycloalkyl(c1-3)-alkyl, (c3-6)heterocycloalkyl(c1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (c1-2)alkyl; r5 is h, (c1-3)alkyl, optionally substituted with one or more fluorine; r17, r18 and r19 are independently of each other h, fluorine, nitrile or (c1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, >to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular er-positive breast cancer, more in particular er-positive, hormone treatment-resistant breast cancer. Said n-substituted azetidine derivatives have estrogen receptor alpha (erα) antagonistic and—in certain embodiments—selective estrogen receptor downregulating (serd) activity in er-positive breast cancer cells..

05/12/16
20160130255 

Ethynyl derivatives


The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, fragile-x syndrome, autism spectrum disorders, parkinson's disease, and gastroesophageal reflux disease (gerd).. .
Hoffmann-la Roche Inc.


05/12/16
20160130254 

Novel cyp17 inhibitors/antiandrogens


Wherein r1 to r8, a, b, z1, and z2 are as defined in the claims and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds of formula (i) possess utility as androgen receptor antagonists (inhibitors) and/or cytochrome p450 monooxygenase 17α-hydroxylase/17,20-lyase (cyp17) inhibitors.

05/12/16
20160130232 

4-alkynyl imidazole derivative and medicine comprising same as active ingredient


There are provided 4-alkynylimidazole derivatives represented by the following general formula (i) or phamaceutically acceptable salts thereof; the derivatives have a superior ep4 receptor antagonistic action and are useful as pharmaceuticals for the treatment of diseases associated with the ep4 receptor, for example, as anti-inflammatory and/or analgesic drugs for inflammatory diseases and diseases that involve various kinds of pains, and further as pharmaceuticals for the treatment of immune diseases that result from inflammations as evoked by tissue destruction due to the activation of th1 cells and/or th17 cells:. .
Kaken Pharmaceutical Co., Ltd.




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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