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1. 发明申请

WO2010092342A1 ORGANOSILICON COMPOUNDS AND THEIR USE AS THE MODULATORS OF THE TRPV1 RECEPTOR 审中-公开
标题翻译：有机硅化合物及其作为TRPV1受体调节剂的用途
公开(公告)号：WO2010092342A1
公开(公告)日：2010-08-19
申请号：PCT/GB2010/000246
申请日：2010-02-10
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , AYSCOUGH, Andrew Paul , SHOWELL, Graham Andrew , TEALL, Martin Richard , TEMPLE, Hannah Elizabeth , AHMED, Saleh
发明人： AYSCOUGH, Andrew Paul , SHOWELL, Graham Andrew , TEALL, Martin Richard , TEMPLE, Hannah Elizabeth , AHMED, Saleh
IPC分类号： C07F7/08 , A61K31/695
CPC分类号： C07F7/0814
摘要： A compound having the Formula (1): wherein: X 1 , X 2 , X 3 and X 4 independently represent CH or N; R 1 , R 2 and R 3 independently represent C 1-6 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalky IC 1-6 alkyl, each of which groups may be optionally substituted with one or more substituents independently selected from halogen and haloC 1-6 alkyl; R 4 , R 5 , R 6 , R 7 , R 8 and R 9 independently represent H, C 1-6 alkyl, C 3-8 cycloalkyl or -Q I -OR 14 , or R 4 and R 9 may join to form a bridging C 1-6 alkylene chain; R 10 represents aryl or heteroaryl, each of which may be optionally substituted by one or more substituents, independently selected from halogen, C 1-6 alkyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, haloC 1-6 alkoxy, cyano, -Q 2 -CO 2 R 12 , -Q 2 -COR 12 , -Q 2 -CONR 12 R 13 , -Q 2 -OR 12 , -Q 2 -NR 12 Rn, -Q 2 -NR 12 SO 2 R 13 , -Q 2 - NR 12 COR 13 , -Q 2 -SO 2 NR 12 R 13 , -Q 2 -S(O) m R 12 , -Y-aryl, -Y-heteroaryl, -Y-C 3-8 cycloalkyl and -Y-heterocyclyl; Q 1 and Q 2 independently represent a covalent bond, C 1-6 alkylene, or 1-6 alkylene substituted with hydroxy; R 12 and R 13 independently represent a H atom, or a C 1-6 alkyl or C 3-8 cycloalkyl group, in which each group may be optionally substituted with one or more C 1-6 alkoxy; or when R 12 and R 13 are attached to the same nitrogen atom they may join to form a nitrogen containing heterocyclyl ring, which may be optionally substituted with one or more substituents independently selected from C 1-6 alkyl and C 1-6 alkoxy; R 14 represents a H atom, or a C 1-6 alkyl or C 3-8 cycloalkyl group, in which each group may be optionally substituted with one or more C 1-6 alkoxy; Y represents a covalent bond, C 1-6 alkylene, or -O-. m represents 0, 1 or 2; R 11 , which is optionally present and may be attached to any available carbon atom X 1 to X 4 instead of H, represents halogen, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, cyano or C 1-6 alkyl which may be optionally substituted with one or more substituents independently selected from halogen, haloC1-6 alkyl and OR 16 ; q represents 0, 1 or 2; W represents -(CH 2 ) n -, which may be optionally substituted with one or more substituents independently selected from C 1-6 alkyl, C 3-8 cycloalkyl and -Q 3 -OR 15 ; n represents 1 or 2; Q 3 represents a covalent bond or C1-6 alkylene; R 15 represents H, C 1-6 alkyl, or C 3-8 cycloalkyl; R 16 is as defined for R 14 ; or a pharmaceutically acceptable salt or ester thereof. Uses of the compounds as modulators of the TrpVl receptor are also disclosed.
摘要翻译：具有式（1）的化合物：其中：X 1，X 2，X 3和X 4独立地表示CH或N; R 1，R 2和R 3独立地表示C 1-6烷基，C 3-8环烷基或C 3-8环烷基IC 1-6烷基，其各自可以任选地被一个或多个独立地选自卤素和卤代C 1-6烷基的取代基取代; R 4，R 5，R 6，R 7，R 8和R 9独立地表示H，C 1-6烷基，C 3-8环烷基或-QI-OR 14，或者R 4和R 9可以连接形成桥连C 1-6亚烷基链; R 10表示芳基或杂芳基，其各自可以任选被一个或多个独立地选自卤素，C 1-6烷基，卤代C 1-6烷基，羟基C 1-6烷基，卤代C 1-6烷氧基，氰基，-Q 2 -CO 2 R 12， -Q2-COR12，-Q2-CONR12R13，-Q2-OR12，-Q2-NR12Rn，-Q2-NR12SO2R13，-Q2- NR12COR13，-Q2-SO2NR12R13，-Q2-S（O）mR12，-Y-芳基， Y-杂芳基，-Y-C 3-8环烷基和-Y-杂环基; Q1和Q2独立地表示共价键，C1-6亚烷基或被羟基取代的1-6个亚烷基; R 12和R 13独立地表示H原子或C 1-6烷基或C 3-8环烷基，其中每个基团可以任选被一个或多个C 1-6烷氧基取代; 或当R 12和R 13连接到相同的氮原子上时，它们可以连接形成含氮杂环基环，其可任选地被一个或多个独立地选自C 1-6烷基和C 1-6烷氧基的取代基取代; R 14表示H原子或C 1-6烷基或C 3-8环烷基，其中各基团可任选被一个或多个C 1-6烷氧基取代; Y表示共价键，C 1-6亚烷基或-O-。 m表示0,1或2; 任选存在并且可以连接到任何可用的碳原子X 1至X 4而不是H的R 11表示卤素，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，氰基或C 1-6烷基，其可任选被一个或更多取代基，其独立地选自卤素，卤代C 1-6烷基和OR 16; q表示0,1或2; W表示 - （CH 2）n - ，其可任选被一个或多个独立地选自C 1-6烷基，C 3-8环烷基和-Q 3 -OR 15的取代基取代; n表示1或2; Q3表示共价键或C 1-6亚烷基; R 15表示H，C 1-6烷基或C 3-8环烷基; R16如R14所定义; 或其药学上可接受的盐或酯。还公开了化合物作为TrpV1受体的调节剂的用途。

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