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 Diagnostic methods for par4 antagonist therapy patent thumbnailDiagnostic methods for par4 antagonist therapy
The disclosure provides methods for identifying a par4 agonist responder or a par4 antagonist responder comprising contacting a par4 agonist with platelets in a sample obtained from a subject in need thereof. The methods also include administering a par4 antagonist to the subject identified as a par4 agonist responder or a par4 antagonist responder.
Cambridge Enterprise Limited


 Prevention and treatment of complement-associated eye conditions patent thumbnailPrevention and treatment of complement-associated eye conditions
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 d antagonists.. .
Genentech, Inc.


 Novel ceramide derivatives having agonistic effects on epidermal cannabinoid receptors, and pharmaceutical or cosmetic composition containing same patent thumbnailNovel ceramide derivatives having agonistic effects on epidermal cannabinoid receptors, and pharmaceutical or cosmetic composition containing same
The present invention relates to a novel pseudoceramide derivative, a pharmaceutically acceptable salt thereof or a solvate thereof, and a pharmaceutical or cosmetic composition containing the same as an active ingredient. The novel pseudoceramide derivative of the present invention is expected to be very useful for treating or preventing skin diseases by activating cannabinoid receptors.
Neopharm Co., Ltd.


 Combination therapy for treating cancer with a poxvirus expressing a tumor antigen and an antagonist and/or agonist of an immune checkpoint inhibitor patent thumbnailCombination therapy for treating cancer with a poxvirus expressing a tumor antigen and an antagonist and/or agonist of an immune checkpoint inhibitor
The present disclosure encompasses therapies, compositions, and methods for treatment of a human cancer patient using a recombinant poxvirus encoding a tumor-associated antigen in combination with one or more agonists or antagonists of immune checkpoint inhibitors.. .
Bavarian Nordic A/s


 Fused benzazepines for treatment of stuttering patent thumbnailFused benzazepines for treatment of stuttering
The present invention encompasses methods of treating a subject who stutters. The methods can include the steps of: (a) identifying a subject in need of treatment; and (b) administering to the subject a therapeutically effective amount of a composition comprising a d1/d5 receptor antagonist, a d1/d5 receptor partial agonist, or a mixture thereof.
Psyadon Pharmaceuticals ,inc.


 Methods and compositions for oral delivery of fts patent thumbnailMethods and compositions for oral delivery of fts
Disclosed are oral dosage forms containing a ras antagonist including fts and structural analogs thereof, and at least one pharmaceutically acceptable excipient other than a cyclodextrin, and methods of orally administering same to treat diseases and disorders responsive to the ras antagonists.. .
Kadmon Corporation, Llc


 Biological markers and methods for predicting response to b-cell antagonists patent thumbnailBiological markers and methods for predicting response to b-cell antagonists
Biological markers that predict patient responsiveness to b-cell antagonists are provided. Also provided are methods of using such biological markers.
Genentech, Inc.


 Methods for treating or preventing ophthalmological diseases patent thumbnailMethods for treating or preventing ophthalmological diseases
This invention relates to methods and compositions useful for the treatment or prevention of an ophthalmological disease, comprising administration of an effective amount of a pdgf antagonist and a vegf antagonist to a mammal in need thereof.. .
Ophthotech Corporation


 Methods for increasing adiponectin patent thumbnailMethods for increasing adiponectin
In certain aspects, the present invention provides compositions and methods for increasing adiponectin in a patient in need thereof by administering an antagonist of an actriib signaling pathway. Examples of such antagonists include actriib polypeptides, anti-actriib antibodies, anti-activin a and/or b antibodies, anti-myostatin antibodies, anti-gdf3 antibodies, and anti-bmp7 antibodies.
Acceleron Pharma Inc.


 Methods of reducing serum levels of fc-containing agents using fcrn antagonists patent thumbnailMethods of reducing serum levels of fc-containing agents using fcrn antagonists
Provided are novel methods of reducing the serum levels of fc-containing agents (e.g., antibodies and immunoadhesins) in a subject. These methods generally comprise administering to the subject an effective amount of an isolated fcrn-antagonist that binds specifically to fcrn with increased affinity and reduced ph dependence relative to the native fc region.
Argen-x N.v.


Compounds useful for inhibiting metastasis from cancer and methods using same


The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one cx3cr1 or fractalkine antagonist..
Alliance Discovery, Inc.


Pyrazolopyrimidone or pyrrolotriazone derivatives, preparing same, and pharmaceutical applications thereof


Pyrazolopyrimidone and pyrrolotriazone derivatives, methods of preparation thereof, and pharmaceutical uses thereof are described. Specifically, pyrazolopyrimidone and pyrrolotriazone derivatives represented by the general formula (i) and pharmaceutically acceptable salts thereof are described.
Jiangsu Hengrui Medicine Co., Ltd.


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.


Methods and compositions relating to leptin antagonists


Devices, methods and compositions for treating cardiovascular disorders are configured for sustained-release of leptin antagonist into a blood vessel in order to downregulate an expression or activity of leptin in a cardiovascular tissue that is affected by a disorder.. .

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.


Multidrug infusion for pain control


The present invention relates to a formulation comprising an opioid, a na channel blocker, an alpha2-receptor agonist, an opioid mu or delta receptor competitive antagonist and an intravenous anesthetic and/or a neurologic acting agent for use in pain control and/or cognitive function improvement.. .

Pharmaceutical formulation containing opioid agonist, opioid antagonist and irritant agent


Disclosed in certain embodiments is an oral dosage form comprising: a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and an irritant in an effective amount to impart an irritating sensation to an abuser upon administration of the dosage form after tampering.. .
Purdue Pharma Lp


Bioactive peptides having insecticide activity


Disclosed are novel bioactive peptides derived as antagonists to a fire ant receptor for a pheromone biosynthesis-activating neuropeptide/pyrokinin (pban/pyrokinin) gene derived neuropeptide ligand. Also disclosed are methods of controlling fire ants with the bioactive peptides disclosed herein.
The United States Of America, As Represented By The Secretary Of Agriculture


Methods of treating cancers using pd-1 axis binding antagonists and taxanes


The invention provides methods and compositions for treating cancer and for enhancing immune function in an individual having cancer. The methods comprise administering a pd-1 axis binding antagonist and a taxane..
Genentech, Inc.


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Modulators of resistant androgen receptor


The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (ar), compositions thereof, and methods of making and using the same.. .
Memorial Sloan-kettering Cancer Center


Radioligands for imaging the lpa-1 receptor


The present invention relates to radiolabeled lpa1 receptor antagonists or pharmaceutically acceptable salts thereof which are useful for the quantitative imaging of lpa1 receptors in mammals.. .
Yale University


Reactivation of axon growth and recovery in chronic spinal cord injury


Disclosed are methods of treating chronic nervous system diseases or injuries, e.g., chronic spinal cord injury, using nogo receptor antagonists, including nogo receptor-1 (ngr1) polypeptides, nogo receptor-1 antibodies and antigen-binding fragments thereof, soluble nogo receptors and fusion proteins thereof, and polynucleotides. Also disclosed are methods of noninvasively monitoring axonal growth during and after treatment with an axonal growth promoting agent..
Yale University


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.


Opioid receptor antagonist for use in treating patients with severe constipation induced by high opiate dosage regimen


The present invention relates to a pharmaceutical composition comprising an opioid receptor antagonist, or a derivative or a pharmaceutically acceptable salt thereof, as an active substance, wherein the composition releases the active substance in a prolonged manner. The composition that is suitable for an administration period of at least twelve-hours for the treatment of severe opioid-induced constipation in patients receiving a daily dosage of opioid equivalent to at least 80 mg of morphine..
Develco Pharma Schweiz Ag


Composition of opioid receptor antagonists for use in treatment of constipation with highly increased whole gut transit time


The present invention relates to a composition comprising an opioid receptor antagonist in an extended release formulation for use in treating a patient with severe constipation characterised by a defined whole gut transit time.. .
Develco Pharma Schweiz Ag


Dosage of naloxone


The present invention relates to a pharmaceutical composition comprising a μ-receptor antagonist as an active substance, wherein the antagonist is prepared in an extended release formulation. The composition is intended for the treatment of patients with opioid-induced constipation, wherein the dosage of the μ-receptor agonist is independent of the opioid dosage.
Develco Pharma Schweiz Ag


Compositions of buprenorphine and u antagonists


.. .

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


The disclosure relates to the compound 2-(cyclohexylmethyl)-n-{2-[(2s)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide or a pharmaceutically acceptable salt thereof, intended for the treatment of alzheimer's disease and other types of dementia.. .
Sanofi


Method and compositions for treatment or prevention of inflammatory conditions


Pharmaceutical compositions and methods for treating or preventing an inflammatory condition in a patient are disclosed. The pharmaceutical compositions and methods include the use of vincamine or a vincamine derivative, either alone or in combination with one or more additional therapeutic agents, including a steroid (preferably a corticosteroid), an angiotensin ii receptor (type 1) antagonist, an angiotensin-converting enzyme (ace) inhibitor, and a non-steroidal anti-inflammatory drug..
University Of Rochester


Micrornas modulating the effect of glucocorticoid signaling


The present invention discloses micrornas (mir) involved in the regulation of the lipid and glucose metabolism. Several conserved mir molecules were found as direct targets of the glucocorticoid hormone/glucocorticoid receptor signaling axis.
Ruprecht-karls-universitat Heidelberg


Combination of angiopoietin-2 antagonist and of vegf-a, kdr and/or flt1 antagonist for treating cancer


The invention relates to agents which possess anti-antigenic activity and are accordingly useful in methods of treatment of disease states associated with angiogenesis in the animal or human body. More specifically the invention concerns a combination of an antagonist of the biological activity of angiopoietin-2 and an antagonist of the biological activity of vegf-a, and/or kdr, and/or flt1, and uses of such antagonists..
Medimmune Limited


5-ht3 receptor antagonists


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

Agonist/antagonist compositions and methods of use


The present invention relates to novel compositions comprising an agonist and an antagonist, in certain ratios which allow for the onset of agonist action followed quickly by alleviation by antagonist action, and methods of use in personal defense and law enforcement.. .
The United States Of America, As Represented By The Secretary, Dept. Of Health & Human Services


Composition-of-matter and treating cardiovascular disorders


A composition-of-matter for treating cardiovascular disorders and a method of using same are provided the composition-of-matter includes a leptin antagonist and a carrier configured for localized release of the leptin antagonist.. .

Methods of treating and preventing cancer drug resistance


Provided herein are combination therapies for the treatment of pathological conditions, such as cancer, using an antagonist of fgfr signaling.. .
Genentech, Inc.


Orexin-control of bone formation and loss


The use of orexin 1 receptor antagonists and/or orexin 2 receptor agonists thereof in the treatment of bone loss diseases is described. Such conditions include osteoporosis, rheumatoid arthritis and other bone wasting diseases..
The Board Of Regents Of The University Of Texas System


Methods and compositions for treatment of epithelial wounds


The invention relates to treatment of epithelial wounds. In particular, the invention relates to methods and formulations for treating epithelial wounds based on application of an opioid antagonist such as naltrexone..
The Penn State Research Foundation


Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use


Glucagon receptor antagonist compounds are disclosed which are of long duration of action. The compounds are useful for treating type 2 diabetes and related conditions.
Merck Sharp & Dohme Corp.


Method for mobilizing stem and/or progenitor cells


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


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Methods for predicting the progression and treating a chronic kidney disease in a patient


The present invention relates to a method for predicting the progression of chronic kidney disease (ckd) in a patient and also to an inhibitor of ngal gene expression or an ngal antagonist for use in the prevention or the treatment of ckd.. .
Institut National De La Sante Et De La Recherche Medicale


Vegf antagonist formulations suitable for intravitreal administration


Ophthalmic formulations of a vascular endothelial growth factor (vegf)-specific fusion protein antagonist are provided suitable for intravitreal administration to the eye. The ophthalmic formulations include a stable liquid formulation and a lyophilizable formulation.
Regeneron Pharmaceuticals, Inc.


Vegf antagonist formulations


Formulations of a vascular endothelial growth factor (vegf)-specific fusion protein antagonist are provided including a pre-lyophilized formulation, a reconstituted lyophilized formulation, and a stable liquid formulation. Preferably, the fusion protein has the sequence of seq id no:4..
Regeneron Pharmaceuticals, Inc.


Quinine compounds, and optical isomers, preparation method and medical use thereof


The present invention discloses a class of quinine compounds and pharmaceutically acceptable salts, solvates, prodrugs or optical isomers thereof. Also disclosed in the present invention are that the above compounds have a selective antagonistic effect on the receptor subtypes of m1 and m3, but have no significant effect on m2 receptor subtype, and the above compounds are characterized by rapid action, long-lasting efficacy, and low toxic and side-effects when used to treat rhinitis, post-cold rhinitis, chronic trachitis, airway hyperresponsiveness, asthma, chronic obstructive pulmonary diseases, cough, urinary incontinence, frequent urination, unstable bladder syndrome, bladder spasms, bladder inflammation and gastrointestinal diseases such as irritable bowel syndrome, spastic colitis, as well as duodenal and gastric ulcers..
Beijing Fswelcome Technology Development Co., Ltd


P2x4 receptor antagonist


The present invention relates to a compound represented by the following general formula (ii), wherein, in the formula, r1a to r6a represent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and the like, xa represents c or n, ya represents n or c(═o), provided that when xa is c, ya represents n, and when xa is n, ya represents c(═o), the double line consisting of the solid line and the broken line represents a single bond or double bond, aa represents benzene ring, pyridine ring, and the like, da represents tetrazole ring, imidazole ring, and the like, ea represents —(cr9ar10a)p-ta-, and ga represents benzene ring, pyridine ring, and the like, which has a p2x4 receptor antagonistic activity.. .
Kyushu University


Carbazole derivatives acting on 5-ht7 receptor


Disclosed are carbazole derivatives and pharmaceutically acceptable salts thereof that act on the 5-ht7 receptor. The carbazole derivatives and the pharmaceutically acceptable salts thereof have high binding affinities for the 5-ht7 serotonin receptor and antagonistic activities against the 5-ht7 serotonin receptor.
Korea Institute Of Science And Technology


Methods and compositions comprising a combination of a vegf antagonist and an anti-ctla-4 antibody


The present invention provides pharmaceutical compositions comprising a vegf antagonist and an anti-ctla-4 antibody, and methods of use thereof. The compositions and methods of the present invention are useful for the treatment of cancers and other diseases and disorders in which anti-angiogenic therapies and/or targeted immune responses may be beneficial..
Regeneron Pharmaceuticals, Inc.


Tweak antagonists for treating lupus nephritis and muscle atrophy


Methods and compositions for treating lupus nephritis and muscle atrophy with anti-tweak antibodies are provided. Methods that include administering therapeutically effective amounts of anti-tweak antibodies to human subjects already receiving a standard treatment for lupus nephritis are also encompassed.
Biogen Ma Inc.


Methods for treating cancers comprising k-ras mutations


Methods of inhibiting tumor growth, methods of treating cancer, and methods of reducing the frequency of cancer stem cells in a tumor are described. Particularly, the methods are directed to tumors or cancers that comprise a k-ras mutation.
Oncomed Pharmaceuticals, Inc.


Methods of treating acute myeloid leukemia with a flt3 mutation


There is provided a method of treating acute myeloid leukemia (aml). The method includes the step of administering to a patient having aml with a fms-like tyrosine kinase 3 (flt3)-mutation a therapeutically effective amount of a cxcr4-antagonistic peptide..
Biolinerx Ltd.


Methods and compositions for treating and/or preventing mucositis


Methods for treating and/or preventing mucositis comprising administering to a subject in need thereof an effective amount of at least one compound chosen from e-selectin antagonists, pharmaceutically acceptable salts of e-selectin antagonists, prodrugs of e-selectin antagonists, and pharmaceutically acceptable salts of prodrugs of e-selectin antagonists, and compositions comprising at least one of such compound.. .
Glycomimetics, Inc.


Methods of treating cancer using compositions comprising perillyl alcohol derivative


A method for treating brain metastases of a cancer in a mammal includes administering to the mammal a therapeutically effective amount of a perillyl alcohol carbamate, such as tmz−poh. The brain metastases can be originated or spread from breast cancer.
Neonc Technologies Inc.


Opioid antagonist formulations


In certain embodiments, the present invention is directed to a solid controlled-release dosage form comprising a core comprising a core portion of an opioid antagonist and a shell encasing the core and comprising a shell portion of the opioid antagonist, wherein the release profile of the core portion of opioid antagonist is different than the release profile of the shell portion of opioid antagonist.. .
Purdue Pharma L.p.


Toll-like receptor 9 antagonist and methods of use thereof


The invention provides antagonist of tlr9 and methods of use thereof. These compounds inhibit or suppress tlr9-mediated signaling.
Idera Pharmaceuticals, Inc.


Renal progenitor cells


A method is provided for simultaneously producing both nephron progenitor cells and ureteric epithelial progenitor cells including the step of contacting intermediate mesoderm cells with: fibroblast growth factor (9) and/or fibroblast growth factor (20) and optionally, one or more selected from the group consisting of. Bone morphogenic protein 7; heparin: a wnt agonist; retinoic acid; and an ra antagonist.
The University Of Queensland


Organic compounds


The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer..
Intra-cellular Therapies, Inc.


Diarylalkylamine rev-erb antagonists and their use as medicaments


The present invention relates to compounds of formula (i) or pharmaceutically acceptable salts or solvates thereof: it further discloses a pharmaceutical composition comprising the compounds of formula (i) and their uses as anti-proliferative and pro-apoptotic agents for cancer therapy.. .
Fondazione Istituto Italiano Di Tecnologia


Novel substituted n, n-dimethylaminoalkyl ethers of isoflavanone oximes as h1-receptor antagonists


The present invention relates to compounds of formula (i), and salts thereof and the pharmaceutical composition containing them in treatment of various diseases, as allergic rhinitis where r1 and r2 are, independently, hydrogen, halogen, c1_3 alkyl or c1-3alkoxy; r3 is phenyl optionally substituted by r4 and r5 which are, independently hydrogen, halogen, c1-3 alkyl, c1-3-alkoxy, fluoro-, difluoro- and trifluoromethyl, nitrile group, n,n-dic1-3alkyl-amide, carboc1-3 alkoxy or c1-3alkylsulphone groups; r3 is pyridyl group containing nitrogen at various positions in the benzene ring, n is one of the integers 1 or 2.. .
Polfarmex S.a.


Histamine-3 receptor antagonists


The invention is directed to a compound of formula i, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula i; and a method of treatment of a disorder or condition selected from the list consisting of acute myocardial infarction; memory processes disorders; dementia; cognition disorders such as alzheimer's disease; attention deficit disorder (add); attention-deficit hyperactivity disorder (adhd); cancers such as cutaneous carcinoma, medullary thyroid carcinoma and melanoma; meniere's disease; gastrointestinal disorders; inflammation; migraine; motion sickness; obesity; pain; septic shock; respiratory disorders (including allergic rhinitis, nasal congestion and allergic congestion) in a mammal, including a human, that may be effected by administering to said mammal a pharmacologically effective amount of a compound of formula i, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.. .
Medisynergics, Llc


Method for producing pyrrole derivative, and intermediate thereof


The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (b) [wherein r1 represents a c1-c4 alkyl group, and r2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate..
Daiichi Sankyo Company, Limited


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Methods of treating neuroendocrine tumors using frizzled-binding agents


Novel methods of treating neuroendocrine tumors are provided. In one embodiment, the method comprises administering to a subject in need thereof a therapeutically effective dose of a wnt antagonist.
Oncomed Pharmaceuticals, Inc.


Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity


Compounds of formula i, defined herein, act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for treating broncho-obstructive and inflammatory diseases.. .
Chiesi Farmaceutici S.p.a.


Processes for preparing a solid polymer matrix containing a core material by pressure cycling of supercritical fluid


There is provided a supercritical fluid-based process for preparing a solid polymer matrix containing a core material, wherein the process includes the step of mixing the polymer, core material and supercritical fluid in a mixing vessel, followed at least one cycle of, without recovering the solid polymer matrix, (i) converting the supercritical fluid in the mixing vessel to a sub-critical state, and then (ii) returning the fluid to the supercritical state, provided that the core material does not comprise any of gonadotropin releasing hormone (gnrh), a gnrh agonist and a gnrh antagonist.. .
Critical Pharmaceuticals Limited


Preservative-free ophthalmic pharmaceutical formulation


The present invention relates to a process for manufacturing an ophthalmic formulation of a carbonic anhydrase inhibitor, hydroxyl ethyl cellulose (hec), and a beta-adrenergic antagonist for use in the treatment of ocular hypertension and glaucoma wherein the ophthalmic pharmaceutical formulation is devoid of benzalkonium chloride or any other preservatives. The present process for manufacturing is simpler, cost effective process to prepare the pharmaceutical ophthalmic formulation in a single tank, without the use of additional tanks that can be sterile filtered..
Sentiss Pharma Private Limited


Antagonist anti-il-7 receptor antibodies and methods


The present invention provides antagonizing antibodies that bind to interleukin-7 receptor (il-7r). The invention further provides a method of obtaining such antibodies and antibody-encoding nucleic acids.
Rinat Neuroscience Corp.


C5ar antagonists


Compounds are provided that are modulators of the c5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of c5a receptors..
Chemocentryx, Inc.


Robot device, robot control method, program, and recording medium


A joint torque computing unit computes a joint torque t1 of a joint necessary to move a joint angle to a target joint angle. A summing unit obtains a sum value u1 indicating the sum of generated forces generated at actuators, from a target stiffness.
t1


Transdiscal administration of specific inhibitors of pro-inflammatory cytokines


The present invention relates to injecting a high specificity cytokine antagonist into a diseased intervertebral disc.. .
Depuy Synthes Products, Inc.


Microparticles comprising gnrh made by pgss


A pharmaceutical formulation comprising a solid matrix of one or more biodegradable polymers, the solid matrix including a pharmaceutically active substance or a pharmaceutically acceptable salt thereof distributed homogeneously or substantially homogeneously within the matrix; wherein the pharmaceutically active substance is, for example, a gonadotropin releasing hormone (gnrh), a gnrh agonist or a gnrh antagonist.. .
Ferring B.v.


Novel inhibitors of mammalian tight junction opening


The present invention provides novel peptides that inhibit and/or reduce the opening of mammalian tight junctions, i.e. Peptide tight junction antagonists.
Alba Therapeutics Corporation


Nitroxyl progenitors in the treatment of heart failure


Administration of an hno/no− donating compound, such as angeli's salt, increases myocardial contractility while concomitantly lowering left ventricular preload in subjects experiencing heart failure. Moreover, administration of the hno/no− donating compound isopropylamine (ipa)/no (na(ch3)2chnhn(o)no) surprisingly exhibited positive inotropic effects in subjects experiencing heart failure that were superior to those caused by the hno/no− donating compound angeli's salt.
The Johns Hopkins University


Method and pharmaceutical composition for use in the treatment of epilepsy


The present invention relates to a compound which is an antagonist of the gluk2/gluk5 receptor or an inhibitor of the gluk2/gluk5 receptor expression for use in the treatment or the prevention of epilepsy.. .
Centre National De La Recherche Scientifique (cnrs)


Methods for treating cancer with trka receptor tyrosine kinase antagonists


The disclosure further concerns the use of such compounds in the treatment and/or prevention of certain types of cancers, pain, inflammation, restenosis, atherosclerosis, psoriasis, thrombosis, alzheimer's, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination.. .

Combined biomarker measurement of fibrosis


Provided herein is a sandwich immunoassay for detecting cross-linked piiinp that has at least two strands of piiinp joined together by inter-strand cross-linking each having a c-terminal neo-epitope of piiinp that is generated by n-protease cleavage of intact type iii procollagen. A biological sample having the cross-linked piiinp is contacted with a first surface-bound monoclonal antibody and then by a second monoclonal antibody, both specifically reactive with a neoepitope in the c-terminal sequence of piiinp, and then binding of the second monoclonal antibody is determined.
Nordic Bioscience A/s


Anti-cd40 antibodies


The present invention relates to new humanized antagonistic anti-cd40 antibodies and therapeutic and diagnostic methods and compositions for using the same.. .
Boehringer Ingelheim International Gmbh


Method treating neuronal tissue inflammation using an il-31ra monoclonal antibody


Use of antagonists to il-31ra and osmrb are used to treat inflammation and pain by inhibiting, preventing, reducing, minimizing, limiting or minimizing stimulation in neuronal tissues. Such antagonists include soluble receptors, antibodies and fragments, derivative, or variants thereof.
Zymogenetics, Inc.


Biomarkers and methods of treating pd-1 and pd-l1 related conditions


Provided herein are biomarkers for the treatment of pathological conditions, such as cancer, and method of using pd-1/pd-l1 pathway antagonists. In particular, provided are biomarkers for patient selection and prognosis in cancer, as well as methods of therapeutic treatment, articles of manufacture and methods for making them, diagnostic kits, methods of detection and methods of advertising related thereto..
Genentech, Inc.


Use of an il-31 monoclonal antibody for antagonizing signal transduction in spinal cord cells


Use of antagonists to il-31 are used to treat inflammation and pain by inhibiting, preventing, reducing, minimizing, limiting or minimizing stimulation in neuronal tissues. Such antagonists include antibodies and fragments, derivative, or variants thereof.
Zymogenetics, Inc.


Thiazole and oxazole-substituted arylamides as p2x3 and p2x2/3 antagonists


And x, r2, r3, r4, r5, r6, ra and rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a p2x3 and/or a p2x2/3 receptor antagonist and methods of making the subject compounds..

Trpv1 antagonists including dihydroxy substituent and uses thereof


And pharmaceutically acceptable derivatives thereof, where r1, r4, r8, r9, and m are as defined herein, compositions comprising an effective amount of a compound of formula (i) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, ui, an ulcer, ibd, and ibs, comprising administering to an animal in need thereof an effective amount of a compound of formula (i) or a pharmaceutically acceptable derivative thereof.. .

N-acylpyrrolidine ether tropomyosin-related kinase inhibitors


Described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as trk antagonists.. .

Pyrrolidine derivatives as oxytocin/vasopressin v1a receptors antagonists


The present invention relates to a compound of formula (3z,5s)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one o-methl9243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin v1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.. .
Obseva S.a.


Intermediates for macrocyclic compounds


Wherein r1, r2, r3, r4, r5, r6, n1, m, p z1, z2, and z3 are as described in the specification. The invention also relates to compounds of formula (i) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction..

Devices, systems, and methods for spg block and neuro-modulation


Neuro-modulation of the spg is achieved by direct delivery of medication that includes a cgrp receptor antagonist using a trans-nasal drug delivery device with delivery features that may include an ergonomic grip, directional control and indicators, or radiopaque portions.. .

Compositions and methods for treatment of diabetic retinopathy


The present invention provides compounds and methods for the treatment of diabetic retinopathy. In particular, lfa-1 antagonists are described herein to be used in the treatment of diabetic retinopathy.
Sarcode Bioscience Inc.


Methods of modulating erythropoiesis with arginine vasopressin receptor 1b molecules


Disclosed are methods of modulating erythropoiesis with arginine vasopressin receptor 1b (avpr1b) molecules, such as avpr1b agonists or antagonists. In one example, a method of stimulating erythropoiesis is disclosed including administering an effective amount of an avpr1b stimulatory molecule to a subject in need thereof, thereby stimulating erythropoiesis.
The Usa, As Represented By The Secretary, Departm- Ent Of Health And Human Service


Method for treating or preventing hot flushes


The invention provides a neurokinin 3 receptor (nkr3) antagonist for use in the treatment, prevention or amelioration of hot flushes in a human subject, for example a menopausal woman or a patient undergoing cancer therapy which affects secretion of sex steroids. The invention also provides a nkr3 antagonist together with a further active agent, and a composition and a kit comprising a nkr3 antagonist and a further active agent.
Imperial Innovations Limited


Formulations for cgrp receptor antagonists


The instant invention relates to liquid pharmaceutical compositions containing cgrp receptor antagonists. The cgrp receptor antagonist liquid pharmaceutical compositions of the instant invention are alcohol-free, low volume liquid pharmaceutical compositions that can be taken without water for the treatment of migraine headache..
Merck Sharp & Dohme Corp.


Biphenyl compounds useful as muscarinic receptor antagonists


Wherein a, b, c, d, m, n, p, s, t, w, ar1, r1, r2, r3, r4, r6, r7, and r8 are as defined in the specification. The compounds of formula i are muscarinic receptor antagonists.

Methods and compositions for treating anxiety


Methods of treating a trpc5 mediated disorder in a subject by administering an effective amount of a trpc5 antagonist, such as a compound disclosed herein, are described.. .
Hydra Biosciences, Inc.


G protein coupled receptors and uses thereof


The present invention provides gpcr polypeptides and polynucleotides, recombinant materials, and transgenic mice, as well as methods for their production. The polypeptides and polynucleotides are useful, for example, in methods of diagnosis and treatment of diseases and disorders.
Omeros Corporation


Methods of modulating lymphangiogenesis, e.g., to treat corneal transplant rejection, in a subject


Methods of modulating the occurrence of lymphangiogenesis in a subject are provided. In some instances, the method includes reducing antigen presenting cell function, such as cell trafficking to draining lymph nodes.
The Regents Of The University Of California


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.


2,2-difluorodioxolo a2a receptor antagonists


The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of a2a receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which a2a receptor are involved.
Merck Sharp & Dohme Corp.


Novel benzimidazole derivatives as ep4 antagonists


The present invention relates to novel benzimidazole derivatives of the general formula (i), processes for their preparation and their use for the production of pharmaceutical compositions for the treatment of diseases and indications that are connected with the receptor ep4.. .
Bayer Pharma Aktiengesellschaft


2-pyridyloxy-4-ester orexin receptor antagonists


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


Use of lingo-4 antagonists in the 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 a lingo-4 antagonist.. .
Biogen Ma Inc.


Orexin receptor antagonists


The disclosures herein relate to novel compounds of formula wherein w, x and y1, y2, y3 and y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.. .
Heptares Therapeutics Limited


Substituted 2,3-dihydro-1h-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis


The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the retinoic acid-related orphan nuclear receptor γt (rorγt)/rorγ. The compounds of the present invention are useful for modulating rorγt)/rorγ activity and for treating diseases or conditions mediated by rorγt)/rorγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as multiple sclerosis (ms), rheumatoid arthritis (ra), inflammatory colitis, psoriasis, copd, pain, obesity, diabetes, dyslipidemia, osteoporosis, asthma, neurodegenerative diseases and cancer..
Arrien Pharmaceuticals Llc


Phenyl derivative


Wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human s1p2 antagonistic activity. The compound may therefore be used as a therapeutic agent for s1p2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases..

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Substituted 2,3-dihydro-1h-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis


The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the retinoic acid-related orphan nuclear receptor γt (rorγt)/rorγ. The compounds of the present invention are useful for modulating rorγt)/rorγ activity and for treating diseases or conditions mediated by rorγt)/rorγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as multiple sclerosis (ms), rheumatoid arthritis (ra), inflammatory colitis, psoriasis, copd, pain, obesity, diabetes, dyslipidemia, osteoporosis, asthma, neurodegenerative diseases and cancer..
Arrien Pharmaceuticals Llc


Dry powder inhalers comprising a carrier other than lactose and a ternary component


This invention relates to novel pharmaceutical compositions for inhalation comprising separately, sequentially or together, drugs having amine in the form of a dry powder in admixture with a pharmaceutically acceptable carrier, other than lactose, and its use in the treatment of respiratory condition selected from asthma and chronic obstructive pulmonary disease (copd) and other obstructive airways diseases. More particulary, the invention relates to pharmaceutical composition for inhalation further comprising a ternary component.
Arven Ilac Sanayi Ve Ticaret Anonim Sirketi


Vegf antagonist formulations suitable for intravitreal administration


Ophthalmic formulations of a vascular endothelial growth factor (vegf)-specific fusion protein antagonist are provided suitable for intravitreal administration to the eye. The ophthalmic formulations include a stable liquid formulation and a lyophilizable formulation.
Regeneron Pharmaceuticals, Inc.




Antagonist topics:
  • Antagonist
  • Recurrence
  • Proliferative Disorder
  • Proliferative
  • Antibodies
  • Progesterone
  • Dicyclomine
  • Scopolamine
  • Extracellular
  • Pharmaceutically Acceptable Salt
  • Metalloprotein
  • Nucleic Acids
  • Polynucleotide
  • Nucleic Acid
  • Monoclonal


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