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Antagonist patents

      

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




 Method for mobilizing stem and/or progenitor cells patent thumbnailnew patent 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


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


new patent

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.


new patent

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.


new patent

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.


new patent

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


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..

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.


Use of biomarkers for assessing treatment of gastrointestinal inflammatory disorders with beta7 integrin antagonists


Methods of assessing or monitoring the effect, efficacy, responsiveness to treatment, and/or determining a dose or dosing regimen of therapeutic agents, such as integrin beta7 antagonists, for the treatment of gastrointestinal inflammatory disorders are provided. In certain aspects, methods of using integrin beta7 subunit-containing receptor occupancy by the integrin beta7 antagonist on colonic lymphocytes as an indicator (“biomarker”) of the effect, efficacy, or responsiveness to treatment, and/or as a means to determine dosing or dosing regimens of therapeutic agents such as beta7 integrin antagonists for the treatment of gastrointestinal inflammatory disorders are provided.
Genentech, Inc.


Generation of endocrine progenitor cells from human pluripotent stem cells using small molecules


The present invention relates to differentiation of stem cells into a homogeneous endocrine progenitor cell population suitable for further differentiation into pancreatic beta-cells. The present invention provides methods for obtaining ngn3/nkx2.2 double positive endocrine progenitor cells by exposing precursor cells to a tgf-β type i receptor inhibitor, a bmp antagonist, an adenylate cyclase activator and nicotinamide and/or exposing to the precursor cells to a selection of small molecules..
Takara Bio Europe Ab


Il-17ra-il-17rb antagonists and uses thereof


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


Novel neurokinin 1 receptor antagonist compounds ii


The invention relates novel nk1 receptor antagonists represented in formula a, wherein r1 and r2 independently are selected from the group consisting of (c1-4)alkyl, (c1-4)haloalkyl, (c1-4)alkoxy, cd3 or halogen; r3 is selected from the group consisting of hydrogen, (c1-4)alkyl, (c1-4)haloalkyl and (c1-4)hydroxyalkyl; r4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; r5 and r6 are independently selected from the group consisting of hydrogen, (c1-4)alkyl, (c1-4) hydroxyalkyl and (c1-4)haloalkyl and x and y are independently selected from the group consisting of ch and n. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds..
Leo Pharma A/s


Malignant and non-malignant disease treatment with ras antagonists


The present disclosure describes new inhibitors or antagonists of ras useful for the treatment of conditions resulting from ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition.
Pisces Therapeutics, Llc


Amide derivatives as lysophosphatidic acid receptor antagonists


Wherein r1, x, m, r2, y, r3, z, n, r4, a and b are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.. .

Stabilization system for robotic technology


A motor control system to be applied to robotic technology, the motor control system comprising at least two actuators that each include a first receiver and a second receiver. The system is comprised of a movement control system that communicates a first signal to the first receivers, the first signal indicative of a movement profile; and a stabilization control system that communicates a second signal to the second receivers, the second signal indicative of a stabilizing profile.

Materials and methods for modulating disc1 turnover


The invention relates to the finding that turnover of disc1 (disrupted in schizophrenia 1) is mediated by the f-box-containing protein fbxw7 (f-box/wd repeat-containing protein 7). The sequence within disc1 that binds to fbxw7 and targets disc1 for turnover by the ubiquitin-proteasome system is identified.
The University Court Of The University Of Glasgow


Methods for treating and/or preventing emesis and/or nausea including acute and/or delayed nausea and/or acute emesis and/or delayed emesis


Methods for treating and/or preventing nausea and emesis including acute and/or delayed nausea and/or acute and/or delayed emesis in a subject are provided herein. The methods include administering to the subject in need thereof a therapeutically effective amount of a 5ht3 antagonist or a pharmaceutical composition thereof by nasal inhalation and/or oral inhalation..
Xoc Pharmaceuticals, Inc.


Pharmaceutical for prophylaxis or treatment of hypertension


A pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension. The pharmaceutical is characterized by comprising (i) a specific mineralocorticoid receptor antagonist and (ii) one or more components selected from the following components (a) to (c), for administration simultaneously or separately at a time interval: (a) an angiotensin ii receptor antagonist, (b) a calcium antagonist, and (c) a diuretic..
Daiichi Sankyo Company, Limited


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


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


Methods of treating sporadic inclusion body myositis


The disclosure relates to the treatment of sporadic inclusion body myositis and other muscle wasting disorders with novel regimens, which employ a therapeutically effective amount of a myostatin antagonist, e.g., a myostatin binding molecule, e.g., a myostatin antibody or an actrii receptor binding molecule, an actrii receptor antibody, such as the bimagrumab antibody.. .
Novartis Ag


Method of treatment


A protocol for pain management includes a pharmaceutical composition and its use in ameliorating the sensation of pain. The protocol includes the use of a ccl17 signaling antagonist alone or in combination with another analgesic compound to treat pain associated with inflammatory conditions.
The University Of Melbourne


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.


Preparation and use of 7a-heterocycle substituted- 6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists


And the remaining variables are described herein. The compounds of the invention are effective inhibitors of the par-1 receptor.

Preparation and use of 3-pyridyl substituted- 6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists


The compounds of the invention are effective inhibitors of the par-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as asc, secondary prevention of myocardial infarction or stroke, or pad..

Positioner for tubes


Roller positioner for tubes comprising: a base structure; two lower support rollers rotating around respective axes positioned on said base structure; and an upper roller antagonist to said two lower support rollers; characterized by comprising a deformable quadrilateral for the movement of said upper roller suited for moving said upper roller along a rectilinear axis by a predetermined distance and then away from said rectilinear axis.. .
A. Narducci S.p.a.


Combination therapy for neoplasia treatment


The present invention relates to an insulin-like growth factor (igf) receptor antagonist for use in the treatment of prostate neoplasia, including benign prostatic hyperplasia (bph), prostate cancer, and particularly crpc, wherein the antagonist is used in combination with an androgen receptor antagonist. An embodiment of the invention is where the androgen receptor antagonist is enzalutamide..
Boehringer Ingelheim International Gmbh


Modulation of tumor immunity


Methods of treating proliferative disorders are described. In particular, combination treatment with a gitr agonist and a pd-1 antagonist are provided..
Merck Sharp & Dohme Corp.


Methods of promoting fat loss comprising administering an alk7 inhibitor


The invention relates to alk7 soluble receptors and their uses as antagonists of the function of certain ligands such as gdf-8 (myostatin) and gdf-11. The alk7 soluble receptor of the invention is useful as antagonists of gdf-8 and gdf-11 in the treatment of neuronal diseases or conditions such as stroke, spinal cord injury, and all peripheral nerve diseases.
Acceleron Pharma Inc.


Seizure treatment compositions and methods


A composition, a method for administering an anti-seizure composition, and a method for treating a seizure are described. In an implementation, a composition comprises a peroxisome proliferator activated receptor gamma (pparγ) antagonist that is administered to an individual, where the individual has been administered a ketogenic diet.
Creighton University


Nanoparticle and polymer formulations for thyroid hormone analogs, antagonists, and formulations and uses thereof


Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric nanoparticle form of thyroid hormone agonist, partial agonist or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Nanoparticle forms of thyroid hormone or thyroid hormone analogs as well as uses thereof are also disclosed..
Nanopharmaceuticals Llc


Growth of cryo-sprouts


The present description relates to cryo-sprouts that have been germinated, grown and shipped in the same container. Seeds are placed on a membrane in the container with sufficient water.
The Vista Institute Llc


Therapeutic agent for chronic arthritides diseases of childhood-related diseases


A therapeutic agent for chronic arthritides diseases of childhood-related diseases, for example chronic arthritides diseases of childhood, still's disease and the like, comprising an interleukin-6 (il-6) antagonist as an active ingredient.. .
Chugai Seiyaku Kabushiki Kaisha


Piperazine-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties


Disclosed are compounds of formula a: (structurally represented) where “rg1”, “rg2a”, “rg4”, “rg5”, “mg1”, “n” and “m” are defined herein which compounds are antagonists of a2a receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the a2a receptor in the potential treatment or prevention of neurological disorders and diseases in which a2a receptors are involved.
Merck Sharp & Dohme Corp.


Triazolone compounds and uses thereof


The invention disclosed herein is directed to compounds of formula (1a) and (1b) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocyticδ leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of formula (1a) or (1b), or a pharmaceutically acceptable salt thereof.
Inception 2, Inc.


Treating cancer with a combination of a pd-1 antagonist and dinaciclib


The present disclosure describes combination therapies comprising an antagonist of programmed death 1 receptor (pd-1) and the cdk inhibitor dincaciclib, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express pd-l1.. .
Merck Sharp & Dohme Corp.


Methods of treating generalized pustular psoriasis (gpp) using il-17 antagonists


The disclosure is directed to methods, treatment regimens, uses, kits and therapies for treating generalized pustular psoriasis (gpp). These methods, treatment regimens, uses, kits and therapies utilize, inter alia, administration of an il-17 antagonist, e.g., an il-17 antibody, such as secukinumab.
Novartis Ag


Compositions comprising e-selectin antagonists and uses therefor


This invention discloses the use of an e-selectin antagonist and a mobilizer of hematopoietic stem cells or progenitor cells in methods and compositions for treating or preventing immunocompromised conditions resulting from medical treatment. The present invention is particular relevant for prophylaxis and/or treatment of hematopoeitic disorders including neutropenia, agranulocytosis, anemia and thrombocytopenia in individuals receiving or proposed to receive treatments that target rapidly dividing cells or that disrupt the cell cycle or cell division..
The University Of Queensland


Oral octreotide administered in combination with other therapeutic agents


This invention relates to combination therapy of a subject suffering from acromegaly. The method of treatment comprises administration to the subject of a therapeutically effective amount of oral somatostatin receptor ligand (srl) e.g.
Chiasma Inc.


Hnf4-alpha antagonist and use thereof


Provided is a hepatocyte nuclear factor 4 alpha (hnf4-α) antagonist and a use thereof. The hnf4-α antagonist selected in the present invention was confirmed to specifically bind to the ligand binding domain of hnf4-α, thereby inhibiting the activity of hnf4-α.
National Cancer Center


Immediate-release tablet formulations of a thrombin receptor antagonist


Immediate-release formulations for oral administration of a thrombin receptor antagonist are provided. Certain formulations of higher api loading demonstrate sufficient moisture uptake after storage at stressed conditions to retard dissolution.
Merck Sharp & Dohme Corp.


Antagonists of chemokine receptors


Compounds are provided that act as potent antagonists of the ccr1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of ccr1-mediated diseases, and as controls in assays for the identification of competitive ccr1 antagonists..
Chemocentryx, Inc.


Targeting metabolic adaptive responses to chemotherapy


Methods for targeting adaptive responses to chemotherapy are described. In various embodiments, a method comprises administering at least one compound that inhibits s6k1, mtorc1 or upstream or downstream pathway components of s6k1 or mtorc1, in association with administration of at least one inhibitor of pparα, pparδ, or pgc1α.
University Of Cincinnati


Diazole amides


Compounds are provided that act as potent antagonists of the ccr1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of ccr1-mediated disease, and as controls in assays for the identification of competitive ccr1 antagonists..
Chemocentryx, Inc.


Treatment of pulmonary arterial hypertension with leukotriene inhibitors


Pulmonary arterial hypertension (pah) can be prevented in persons susceptible to the diseases and pah patients can be treated by administering an effective dose of a leukotriene inhibitor. Suitable inhibitors include leukotriene a4 hydrolase (lta4h) inhibitors, leukotriene b4 receptor (blt1/blt2) antagonists, 5-lipoxygenase (5-lo) inhibitors, and 5-lipoxgygenase activating protein (flap) inhibitors..
The Board Of Trustees Of The Leland Stanford Junior University




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


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