| 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, and so forth. Specifically, the invention provides azole derivatives represented by general formula (I), or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin (AVP) V1b receptor:; |
| 主权项 |
1. An azole derivative represented by Formula (I): [in Formula (I), R1 represents 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 4- to 8-membered saturated heterocycle; R2 represents a hydrogen atom or C1-5 alkyl; R3 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); 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, 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, trifluoromethyl, amino, mono-C1-5 alkylamino, di-C1-5 alkylamino and C2-5 alkanoylamino, 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) or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; the optionally substituted azole ring which is represented by the following formula (α): has any one of the structures in the following formula group (II): where Ry represents a hydrogen atom or C1-5 alkyl; X1 and X2 are such that i) when X1 is a single bond or the formula —CO—, X2 represents —C1-5 alkylene- or —O—C1-5 alkylene-; and ii) when X1 is the formula —CONRx1—, X2 represents a single bond; Rx1 represents a hydrogen atom or C1-5 alkyl; and the ring A represents a benzene ring, a 6-membered aromatic heterocycle (the benzene ring and the 6-membered aromatic heterocycle are optionally substituted by one or two groups selected from the group consisting of halogen atoms and C1-5 alkoxy), a 4- to 8-membered saturated or partially unsaturated heterocycle containing one or two nitrogen atoms (the 4- to 8-membered saturated or unsaturated heterocycle is optionally substituted by one oxo) or C3-7 cycloalkane] or a pharmaceutically acceptable salt of the azole derivative. |
