发明名称 Spiro azetidine isoxazole derivatives and their use as SSTR antagonists
摘要 Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.;
申请公布号 US9605000(B2) 申请公布日期 2017.03.28
申请号 US201414775265 申请日期 2014.03.13
申请人 Takeda Pharmaceutical Company Limited 发明人 Kasai Shizuo;Ogino Masaki;Mizojiri Ryo;Yamasaki Takeshi;Hirose Hideki;Takakura Nobuyuki;Yamashita Tohru;Morimoto Sachie;Nakahata Takashi;Kina Asato
分类号 C07D498/10;A61P3/00;A61K31/424 主分类号 C07D498/10
代理机构 Foley & Lardner LLP 代理人 Foley & Lardner LLP
主权项 1. A compound represented by the following formula: wherein ring P is pyrrolidine, piperidine, cyclohexane or bicyclo[2.2.2]octane, each of which is optionally substituted with a C1-6 alkyl group optionally substituted with an C6-14 aryl group, an C1-6 alkoxy group, or a hydroxyl group, ring Q is benzene optionally substituted with 1 to 4 substituents selected from the following (a) to (j): (a) a halogen atom;(b) a C3-10 cycloalkyl group optionally substituted with 1 to 3 substituents selected from a halogen atom, an C1-6 alkoxy group, a hydroxyl group, and an C1-6 alkyl group;(c) a C1-6 alkoxy group optionally substituted with 1 to 3 substituents selected from a halogen atom, an optionally halogenated C3-10 cycloalkyl group, an C1-6 alkoxy group, a C6-14 aryl group, a 5- to 14-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents selected from a C1-6 alkyl group and a C6-14 aryl group, and an C1-6 alkylsulfonyl group;(d) a 3- to 8-membered monocyclic non-aromatic heterocyclic group optionally substituted with 1 to 3 substituents selected from a halogen atom, and a halogenated C1-6 alkyl group;(e) a C6-14 aryl group optionally substituted with 1 to 3 substituents selected from a halogen atom, an C1-6 alkyl group, a halogenated C1-6 alkyl group, an amino group optionally substituted with 1 or 2 C1-6 alkyl group, a cyano group, an C1-6 alkylsulfonyl group; an C1-6 alkoxy group optionally substituted with a C6-14 aryl group or a halogen atom, and a C3-6 cycloalkyl group;(f) a C1-6 alkyl group optionally substituted with 1 to 3 substituents selected from a halogen atom, an optionally halogenated C3-10 cycloalkyl group, and an C1-6 alkoxy group;(g) a C6-14 aryloxy group optionally substituted with 1 to 3 substituents selected from a halogen atom;(h) a 5- to 6-membered monocyclic aromatic heterocyclic group optionally substituted with 1 to 3 substituents selected from an optionally halogenated C1-6 alkyl group, a halogen atom; and(i) a C3-10 cycloalkyloxy group,(j) a C3-10 cycloalkenyl group, or 5- to 14-membered heterocycle optionally substituted with 1 to 4 substituents selected from the following (k) to (s): (k) a halogen atom,(l) a C1-6 alkyl group,(m) a C3-10 cycloalkyl group,(n) a C1-6 alkoxy group optionally substituted with 1 to 3 substituents selected from a halogen atom, a C6-14 aryl group,(o) a 5- to 6-membered monocyclic aromatic heterocyclic group,(p) a C6-14 aryl group optionally substituted with 1 to 3 substituents selected from a halogen atom,(q) a C7-16 aralkyl group,(r) an amino group optionally substituted with 1 to 2 substituents selected from an C6-14 aryl group,(s) a hydroxyl group optionally substituted with a halogenated C6-14 aryl group, R1 is CO2H, CO2CH3, or CO2CH2CH3, R2 and R3 are each independently a hydrogen atom, a halogen atom or a C1-6 alkyl group, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently a hydrogen atom or a methyl group, and n is 0 to 2 or a salt thereof.
地址 Osaka JP
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