摘要:
Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating diseases associated with a nociceptin receptor. (I) [in the formula, A1, A2 and A3 independently represent a carbon atom or a nitrogen atom, and one or two of A1, A2 and A3 represent a carbon atom; R1 represents a lower alkyl group or the like; R2 represents a phenyl group which may be substituted with a halogen atom or the like; R3 represents a hydrogen atom, a lower alkyl group or the like; and R4 represents a lower alkyl group or the like.]
摘要翻译:公开了由下式(I)表示的芳基取代的含氮杂环化合物或其药学上可接受的盐。 该化合物用作伤害感受肽受体拮抗剂,可用作治疗与伤害感受肽受体相关疾病的药剂。 (I)[式中,A1,A2和A3独立地表示碳原子或氮原子,A1,A2和A3中的一个或二个表示碳原子; R1表示低级烷基等; R 2表示可以被卤素原子等取代的苯基; R3表示氢原子,低级烷基等; R4表示低级烷基等。]
摘要:
Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating diseases associated with a nociceptin receptor. (I) [in the formula, A1, A2 and A3 independently represent a carbon atom or a nitrogen atom, and one or two of A1, A2 and A3 represent a carbon atom; R1 represents a lower alkyl group or the like; R2 represents a phenyl group which may be substituted with a halogen atom or the like; R3 represents a hydrogen atom, a lower alkyl group or the like; and R4 represents a lower alkyl group or the like.]
摘要翻译:公开了由下式(I)表示的芳基取代的含氮杂环化合物或其药学上可接受的盐。 该化合物用作伤害感受肽受体拮抗剂,可用作治疗与伤害感受肽受体相关疾病的药剂。 (I)[式中,A1,A2和A3独立地表示碳原子或氮原子,A1,A2和A3中的一个或二个表示碳原子; R1表示低级烷基等; R 2表示可以被卤素原子等取代的苯基; R3表示氢原子,低级烷基等; R4表示低级烷基等。]
摘要:
The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] [in which A1, A2, A3, A4 and A5 stand for optionally halogen-substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like]or salts thereof These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.
摘要翻译:本发明涉及由通式[I]表示的4-氧代咪唑烷-2-螺哌啶衍生物[其中A 1,A 2,A 3, 任选地,卤素取代的次甲基或氮原子的烷基,亚氨基, R 1和R 2代表低级烷基等; R 3代表氢或低级烷基; R 4和R 5代表氢,或任选被羟基取代的低级烷基等)或其盐这些化合物作为伤害感受肽受体激动剂起作用,并且是 可用作止痛剂,缓解药物对麻醉止痛药的缓解,依赖麻醉止痛药缓解,镇痛增强剂,抗胆碱药物,改善脑功能的药物,精神分裂症治疗药物,治疗退行性神经退行性疾病药物,抗焦虑剂或抗抑郁药物及对尿崩症的治疗 多尿 等等。
摘要:
The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] [in which A1, A2, A3, A4 and A5 stand for optionally halogen-substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like]or salts thereof. These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.
摘要:
The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.
摘要:
It is intended to provide a method for evaluating a compound which regulates eating or body weight characterized by comprising the steps of introducing a BARLP gene and preparing a cell expressing BARLP; bringing a test compound into contact with the cell; and detecting a specific binding of the test compound to the BARLP and a method for evaluating a compound further comprising the step of evaluating a test compound using a nonhuman genetically-engineered animal in which the BARLP gene is inactivated. According to this invention, knowledge about a relationship between BARLP and biological functions is obtained and a method for evaluating a compound targeting BARLP and a BARLP ligand obtained by the evaluation can be provided.
摘要:
A nucleic acid having a base sequence of SEQ ID NO. 1; a protein having an amino acid sequence of SEQ ID NO. 2; a recombinant vector comprising a gene constituted of the above nucleic acid; and a transformant cell comprising the recombinant vector. By the use of these, it is feasible to provide ORL1 gene of non-human primates, etc. and to perform assessment, screening, etc. of compounds acting on the ORL1.
摘要翻译:具有SEQ ID NO:1的碱基序列的核酸。 1; 具有SEQ ID NO:1的氨基酸序列的蛋白质。 2; 包含由上述核酸构成的基因的重组载体; 和包含重组载体的转化体细胞。 通过使用这些,可以提供非人灵长类动物的ORL1基因等,并对作用于ORL1的化合物进行评估,筛选等。
摘要:
The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.
摘要:
The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.
摘要:
A keyword acquiring unit transmits a keyword acquisition request to a first server serving as a keyword providing service, and receives a keyword from the first server. An information acquiring unit transmits an acquisition request of information related to the keyword to a second server serving as an information providing service, and receives the information from the second server. A cover unit presents information acquired by the information acquiring unit to a user. An input unit receives selection of at least one of information presented by the cover unit. A service acquiring unit transmits a search request based on the keyword related to information selected at the input unit to a third server serving as a search service, and acquires a search result from the third server. A socket unit presents the search result to the user.