42 results about "Receptor antagonist activity" patented technology

This invention provides the compounds of formula (I): or its a pharmaceutically acceptable ester or amide of such compound, or a pharmaceutically acceptable salt thereof, wherein X1 is NH; R1, R2, R4 through R6 and R7 through R11 are all hydrogen; R3 is hydroxy; X2 and X3 are methylene; X4 is a bond; and X5 is a carbon atom, and the like. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

The invention relates to novel proteins with TNF-receptor antagonist activity and nucleic acids encoding these proteins. The invention further relates to TNF-receptor proteins with reduced immunogenicity and the use of these novel proteins in the treatment of TNF related disorders.

The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount.

This invention provides the compounds of formula (I):or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like;R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2.These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

The invention relates to a method of decreasing intestinal motility in a subject in need of treatment. The method comprises administering to the subject a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of decreasing intestinal motility in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone. In certain embodiments, the subject is a subject with a functional bowel disorder, such as IBS, functional abdominal bloating, or functional diarrhea.

A heteroaromatic methyl cyclic amine derivative represented by formula (IA) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of an orexin (OX) receptor antagonist activity.

Disintegrin variants and pharmaceutical uses thereof are disclosed. The disintegrin variant includes an isolated polypeptide that has integrin αvβ3 receptor-antagonist activity and substantially reduced integrin αllbβ3 and / or α5β1 receptor-blocking activity as compared to a wild-type disintegrin. The variant is encoded by a modified disintegrin nucleotide sequence that encodes a modified amino acid sequence, resulting in a polypeptide having substantially reduced affinity to integrin αllbβ3 and / or α5β1 as compared to a wild-type disintegrin. The variant is useful for treatment and / or prevention of αvβ3 integrin-associated diseases in a mammal, which include osteoporosis, bone tumor or cancer growth, angiogenesis-related tumor growth and metastasis, tumor metastasis in bone, malignancy-induced hypercalcemia, angiogenesis-related eye diseases, Paget's disease, rheumatic arthritis, and osteoarthritis. The angiogenesis-related eye diseases include age-related macular degeneration, diabetic retinopathy, corneal neovascularizing diseases, ischaemia-induced neovascularizing retinopathy, high myopia, and retinopathy of prematurity.

This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R<1> and R<2> independently represent hydrogen or the like; R<3> and R<4> independently represents hydrogen or the like; R<5> represents aryl or the like; -X-Y- represents -CH2O- or the like; and n represents 0, 1 or 2.These compounds have ORL1 -receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

The invention relates to compounds having the formula: (I) wherein Ar, r, n, X, R2, R2', R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and aprocess and intermediates for preparing such compounds.

The invention discloses a discovery and application of an acting target of hydroxyl cinnamamide compound separated from solanaceae plants, and particularly relates to a discovery of an acting target of hydroxyl cinnamamide compound N1, N8-bis (dihydrocaffeoyl) spermidine (BDCS for short) and application thereof in spasmolysis drug. Unmarked cell target pharmacology technology finds that the compound has high muscarine M receptor antagonistic activity, dose-effect relationship researches show that dose is dependently antagonistic to DMR response signals caused by acetylcholine and BDCS is a muscarine M receptor antagonist. BDCS and one or more than two of pharmaceutically-acceptable salts of BDCS are used as active ingredients of the muscarine M receptor antagonist. Current researches show that muscarine M receptor is related to diseases like spasm, analgesia, sedation and schizophrenia, so that an efficient novel ligand with the acting target being clear can be provided for related diseases.

A branched chain alkyl heteroaromatic ring derivative represented by formula (Ia) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of an orexin (OX) receptor antagonist activity.

Disclosed is a compound represented by general formula (I), which has EP1 receptor antagonist activity, or a pharmacologically acceptable salt thereof. (In general formula (I), A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents an optionally substituted phenyl group, an optionally substituted five-membered aromatic heterocyclic group, an optionally substituted six-membered aromatic heterocyclic group or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like.) The compound of general formula (I) is able to be used as an agent for treatment or prevention of LUTS, in particular symptoms of OABS.

Provided is a novel heterocyclic compound having an aryl hydrocarbon receptor antagonist activity and useful for the promotion of platelet production, the compound being represented by the general formula [I]: wherein ring A, ring B, R1, R2, R3, R4, n, and X are as defined above, or a salt thereof.

The invention relates to cyclopeptide derivatives with luteinizing hormone releasing hormone (LHRH) receptor antagonist activity shown in a general formula I in the specification, a preparation method thereof, pharmaceutical compositions containing the cyclopeptide derivatives and use of the cyclopeptide derivatives in treatment of prostatic cancer, endometrial cancer, ovarian cancer, breast cancer and other sex hormone-dependent diseases associated with reproduction, contraception and the like.

Compositions and methods for treatment of Parkinson's disease to reduce the negative side effects of the disease by administering a therapeutically effective diarylmethylpiperazine compound which exhibits delta opioid receptor agonist activity, and optionally, mu receptor antagonist activity.

A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.

Compositions and methods for treatment of Parkinson's disease to reduce the negative side effects of the disease by administering a therapeutically effective diarylmethylpiperazine compound which exhibits delta opioid receptor agonist activity, and optionally, mu receptor antagonist activity.

The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.