公开(公告)号：EP1809606A1

公开(公告)日：2007-07-25

申请号：EP05802078.5

申请日：2005-11-10

申请人： SmithKline Beecham Corporation

发明人： BRADLEY, Daniel Marcus, GlaxoSmithKline ,  PORTER, Roderick Alan, GlaxoSmithKline ,  SMITH, Paul William, GlaxoSmithKline ,  STEAD, Rachel Elizabeth Anne, GlaxoSmithKline ,  VONG, Antonio Kuok Keong, GlaxoSmithKline

IPC分类号： C07D215/52 ,  A61K31/47 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D409/04 ,  C07D215/52

摘要： The invention also relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl or cyclohexyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; R2 is C1-6alkyl or C3-6cycloalkyl; n is 1 or 2; R3 is hydrogen, C1-6alkyl or C3-6cycloalkyl; X is -(C=O)- or -SO2-; R4 is C1-6alkyl, C1-6haloalkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6haloalkoxy, amino, monoC1-6alkylamino or diC1-6alkylamino, or R4 is heterocyclyl or carbocyclyl, either of which is optionally substituted independently by one or more halogen, C1-6alkyl, C1-6haloalkyl, C1-6alkoxy or C1-6haloalkoxy; R5 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms; and y is 0, 1 or 2; wherein when y is 1 or 2, Y is a halogen atom, and wherein when y is 2 the halogen atoms may be the same or different. Also disclosed are use of the compounds in treating diseases and conditions mediated by activation of the NK3 receptor, compositions containing the derivatives and processes for their preparation.

摘要翻译： 本发明还涉及式（I）化合物，其药学上可接受的盐，溶剂合物或前药：其中R 1为苯基或环己基，其任一个任选被1,2或3个卤原子取代，所述卤原子可以相同 或不同; R2是C1-6烷基或C3-6环烷基; n是1或2; R3是氢，C1-6烷基或C3-6环烷基; X是 - （C = O） - 或-SO 2 - ; R 4是C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6卤代烷氧基，氨基，单C 1-6烷基氨基或二C 1-6烷基氨基，或者R 4是杂环基或碳环基， 或更多卤素，C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基或C 1-6卤代烷氧基; R5为苯基或噻吩基，其任一个任选被1,2或3个卤素原子取代; y是0,1或2; 其中当y是1或2时，Y是卤素原子，并且其中当y是2时，卤素原子可以相同或不同。 还公开了所述化合物在治疗由NK3受体活化介导的疾病和病症中的用途，含有所述衍生物的组合物及其制备方法。