公开(公告)号：US20050176791A1

公开(公告)日：2005-08-11

申请号：US10640476

申请日：2003-08-14

申请人： Alexander Oxford ,  Richard Borman ,  Robert Coleman ,  Kenneth Clark ,  George Hynd ,  Janet Archer ,  Amanda Aley ,  Neil Harris ,  Andrew Goulter

发明人： Alexander Oxford ,  Richard Borman ,  Robert Coleman ,  Kenneth Clark ,  George Hynd ,  Janet Archer ,  Amanda Aley ,  Neil Harris ,  Andrew Goulter

IPC分类号： A61K31/421 ,  A61P9/04 ,  C07D263/48 ,  C07D413/04

CPC分类号： C07D263/48 ,  A61K31/421 ,  C07D413/04

摘要： The present invention relates to compounds which include compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, and phenyl-C1-4 alkyl; and the other of R1 and R4 is an optionally substituted C9-14 aryl group; R2 and R3 are either: (i) independently selected from H, R, R′, SO2R, C(═O)R, (CH2)nNR5R6, where n is from 1 to 4 and R5 and R6 are independently selected from H and R, where R is optionally substituted C1-4 alkyl, and R′ is optionally substituted phenyl-C1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C5-7 heterocyclic group. The compounds are useful in the treatment of conditions including conditions which can be alleviated by antagonism of a 5-HT2B receptor such as GI disorders and congestive heart failure.

摘要翻译： 本发明涉及包括式I化合物或其药学上可接受的盐的化合物，其中R 1和R 4中的一个选自由以下组成的组： H和任选取代的C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1〜 4烷基和苯基-C 1-4烷基; R 1和R 4中的另一个是任选取代的C 9-14芳基; R 2和R 3是：（i）独立地选自H，R，R'，SO 2 R，C（-O ）R，（CH 2）2 NR 6，其中n为1至4，R H和R 6独立地选自H和R，其中R是任选取代的C 1-4烷基，R'任选被取代 苯基-C 1-4烷基，或（ii）与它们所连接的氮原子一起形成任选取代的C 5-7杂环基。 所述化合物可用于治疗包括可通过拮抗5-HT 2B受体如GI病症和充血性心力衰竭而缓解的病症的病症。