| 摘要 |
The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia. Specifically, the invention provides fused azole derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin 1b receptor:; |
| 主权项 |
1. A fused azole derivative represented by Formula (I): [in Formula (I), R1 represents a C1-5 alkyl (the C1-5 alkyl is optionally substituted by one to three groups selected from the group consisting of hydroxy, halogen atoms, cyano, C3-7 cycloalkyl, and C1-5 alkoxy), C3-7 cycloalkyl, or 4- to 8-membered saturated heterocycle; R2 represents aryl or heteroaryl (the aryl and heteroaryl are optionally substituted by one or two groups selected from the group consisting of C1-5 alkoxy, C1-5 alkyl, halogen atoms, trifluoromethyl, trifluoromethoxy, cyano, hydroxy, difluoromethoxy, and C1-5 alkylsulfonyl); R3 represents either the following formula (II), (III) or (IIIa): X represents a single bond, an oxygen atom or phenylene (the phenylene is optionally substituted by a halogen atom); n represents an integer of 1 to 4; R4 and R5 which may be the same or different each represent a hydrogen atom, C1-5 alkyl (the C1-5 alkyl is optionally substituted by one to three groups selected from the group consisting of hydroxy, halogen atoms, cyano, C3-7 cycloalkyl, and C1-5 alkoxy), C3-7 cycloalkyl, or a 4- to 8-membered saturated or unsaturated heterocycle containing one or more nitrogen, oxygen or sulfur atoms in the ring (the 4- to 8-membered saturated or unsaturated heterocycle is optionally substituted by one or two groups selected from the group consisting of hydroxy, C1-5 alkyl, C1-5 alkoxy, halogen atoms, cyano, C2-5 alkanoyl, and trifluoromethyl), or R4 and R5, together with the adjoining nitrogen atom, may form a 4- to 8-membered saturated or unsaturated heterocycle optionally containing one or more nitrogen, oxygen or sulfur atoms in the ring in addition to the adjoining nitrogen atom (the 4- to 8-membered saturated or unsaturated heterocycle is optionally substituted by one or two groups selected from the group consisting of hydroxy, C1-5 alkyl (the C1-5 alkyl is optionally substituted by one or two hydroxyl groups), C1-5 alkoxy, halogen atoms, cyano, C2-5 alkanoyl, oxo, aminocarbonyl, mono-C1-5 alkylaminocarbonyl, di-C1-5 alkylaminocarbonyl, and trifluoromethyl, and the 4- to 8-membered saturated or unsaturated heterocycle optionally has a C1-5 alkylene group crosslinking two different carbon atoms in the ring), 2-oxa-6-azaspiro[3.3]hept-6-yl, or 2-oxa-7-azaspiro[3.5]non-7-yl; R6 represents C1-5 alkyl, C3-7 cycloalkyl, or a 4- to 8-membered saturated heterocycle; Y represents a nitrogen atom or the formula CH; when Y is a nitrogen atom, R7 represents C1-5 alkyl; when Y is the formula CH, R7 represents a 4- to 8-membered nitrogen-containing saturated heterocycle; n1 represents an integer of 1 or 2; ring A represents any one of the structures in the following formula group (IV)]or a pharmaceutically acceptable salt thereof. |
