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537 results about "NK1 receptor antagonist" patented technology

Neurokinin 1 (NK₁) antagonists (-pitants) are a novel class of medications that possesses unique antidepressant, anxiolytic, and antiemetic properties. NK-1 antagonists boost the efficacy of 5-HT3 antagonists to prevent nausea and vomiting. The discovery of neurokinin 1 (NK₁) receptor antagonists was a turning point in the prevention of nausea and vomiting associated with cancer chemotherapy.

1-Amino-alkylcyclohexane NMDA receptor antagonists

Certain 1-aminoalkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking / unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti-Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-aminoalkylcyclohexane compounds involved.
Owner:MERZ PHARMA GMBH & CO KGAA

Bicyclic derivatives serving as CRTH2 receptor antagonist

The invention belongs to the technical field of medicine, and particularly relates to bicyclic derivatives (shown in a general formula (I)) serving as CRTH2 receptor antagonist and pharmaceutically acceptable salt and stereoisomeride thereof, wherein in the general formula (I), X1, X2, X3, X4, X5, X6, X7, X8, Y, Z, R1 and R2 are as defined in the specification. The invention also relates to a preparation method of these compounds, a pharmaceutical preparation and pharmaceutical composition containing these compounds, and application of these compounds in preparation of medicaments for treating and / or preventing diseases related to CRTH2 activity.
Owner:KBP BIOSCIENCES CO LTD

Transdermal Delivery of Hydrophobic Bioactive Agents

A method and related compositions, including the use of N-acyl derivatives of sarcosine, provide for the delivery of bioactive agents through tissue surfaces such as the skin. The method and composition are particularly well suited for hydrophobic active agents such as serotonin (5HT3) receptor antagonists (e.g., ondansetron), antipsychotic agents (e.g., risperidone), benzodiazepines (e.g., flumazenil), and progestins (e.g., levonorgestrel).
Owner:DERMATRENDS INC

Treatment of sexual dysfunction

InactiveUS20020169101A1BiocideDisease diagnosisSexual functioningBombesin receptor
Bombesin receptor antagonists have been found to be useful in the treatment of sexual dysfunction in both males and females. They may be selective BB1 antagonists or mixed BB1 / BB2 antagonists. Combinations are disclosed of bombesin receptor antagonists with a range of other active compounds, for example PDE5 inhibitors, NEP inhibitors and lasofoxifene.
Owner:WARNER-LAMBERT CO

Novel compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and pharmaceutical compositions containing the same

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1 )antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.
Owner:AMOREPACIFIC CORP

Androgen receptor antagonist for resisting prostate cancer

ActiveCN101817787AOrganic active ingredientsOrganic chemistryDiseaseSex hormone receptor
The invention provides an androgen receptor antagonist for resisting the prostate cancer, relates to a sulfoimidazoledione with substituted groups on two nitrogen atoms, and relates to a use of such the compounds as a medicament for treating the diseases or disorders related to the androgen receptor, such as prostate cancer, alopecia or whelk.
Owner:SUZHOU KINTOR PHARMA

Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors

The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and / or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and / or long term regulation of energy balance; short-, medium- and / or long term regulation (stimulation and / or inhibition) of food intake; adipogenesis, adiposity and / or obesity; body weight gain and / or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and / or gastrectomy (ghrelin replacement therapy).
Owner:ZENTARIS GMBH +3

Pyrrolidine derivatives-CCR-3 receptor antagonists

This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I): that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Owner:SYNTEX (USA) LLC

Bicyclic compounds as NR2B receptor antagonists

This invention provides a compound of the formula (I): wherein R<1 >and R<2 >independently represent a hydrogen atom or the like; X represents a covalent bond or the like: A represents a bicyclic, aromatic, saturated or partially unsaturated heterocyclic or carbocyclic group having from 8 to 12 ring atoms; or the like: B represents a phenyl group or a heteroaryl group having from 5 to 6 ring atoms or the like: These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
Owner:ANDO KAZUO +5

Il-23 receptor antagonists and uses thereof

InactiveUS20100190710A1Efficacy excessiveExcessive side effectSenses disorderPeptide/protein ingredientsNK1 receptor antagonistAgonist
The present invention relates to IL-23 receptor antagonists and agonists. The use of IL-23 receptor antagonists in treating autoimmune and inflammatory disorders, as well as methods of identifying IL-23 receptor antagonists and agonists.
Owner:VALORISATION HSJ LLP

Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists

This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
Owner:DIRECT CURSUS TECH LLC +1

Compositions And Methods For Lipo Modeling

InactiveUS20090317376A1Conducive to survivalReduce adverse metabolic consequence of obesityBiocidePeptide/protein ingredientsFat graftingNK1 receptor antagonist
Methods for lipomodeling by peripherally administering a modulator of a Y receptor are provided. Methods may comprise reduction of a fat depot by administering a Y receptor antagonist proximally and / or directly to the site of the fat depot. Other methods comprise increasing or stabilizing a fat depot or fat graft by administering a Y receptor agonist proximally and / or directly to the site of the fat depot or fat graft. Also provided are methods for stimulating wound healing by administering a Y receptor agonist proximally to a wound site.
Owner:GEORGETOWN UNIV

Tricyclic diazepines tocolytic oxytocin receptor antagonists

This invention provides novel tricyclic diazepine compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including treatment of preterm labor, dysmenorrhea, endometritis, and for suppressing labor prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
Owner:WYETH LLC

Methods for inhibiting angiogenesis by EphB receptor antagonists

InactiveUS20040136983A1Senses disorderPeptide/protein ingredientsEphB ReceptorMammal
The present application describes methods of inhibiting or stimulating angiogenesis in a mammal comprising administering to the mammal an effective amount of an Eph receptor antagonist or agonist, respectively. Articles of manufacture for use in relation to these methods are also described.
Owner:AGUET MICHEL

Glucagon receptor antagonists

The present invention relates to glucagon receptor polypeptide antagonists which inhibit the binding of the hormone glucagon to its receptor. More particularly, the present invention relates to high affinity glucagon receptor antibodies or Fab fragments thereof that inhibit binding of glucagon to its receptor and their use in the treatment or prevention of type 2 diabetes (NIDDM) and related disorders in mammalian species.
Owner:ELI LILLY & CO

Chemokine receptor antagonists and methods of use therefor

Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and / or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: ##STR1## and physiologically acceptable salts thereof.
Owner:KYOWA HAKKO KOGYO CO LTD +1

Calcitonin gene related peptide receptor antagonists

The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors ('CGRP-receptor'), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
Owner:BRISTOL MYERS SQUIBB CO

Particles containing an opioid receptor antagonist and methods of use

Particles comprising an opioid receptor antagonist as well as methods of their use and methods of their preparation are provided herein. Such particles may be used for treating and preventing opioid-induced side effects in patients, and may be provided to chronic opioid users as well.
Owner:UNIVERSITY OF CHICAGO

Methods for decreasing detrusor muscle overactivity

InactiveUS20050239890A1Limited efficacyReduce patient complianceBiocideOrganic active ingredientsDiseaseGabapentin
A method is provided for using α2δ subunit calcium channel modulators or other compounds that interact with the α2δ calcium channel subunit in combination with one or more compounds with smooth muscle modulatory effects to treat and / or alleviate the symptoms associated with painful and non-painful lower urinary tract disorders in normal and spinal cord injured patients. According to the present invention, α2δ subunit calcium channel modulators include GABA analogs, e.g., gabapentin and pregabalin, fused bicyclic or tricyclic amino acid analogs of gabapentin, and amino acid compounds. Compounds with smooth muscle modulatory effects include antimuscarinics, β3 adrenergic agonists, spasmolytics, neurokinin receptor antagonists, bradykinin receptor antagonists, and nitric oxide donors.
Owner:DYNOGEN PHARM INC
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