公开(公告)号：US5763458A

公开(公告)日：1998-06-09

申请号：US456168

申请日：1995-05-31

申请人： Robin Douglas Clark ,  Richard Malcolm Eglen ,  John Otis Gardner ,  Alam Jahangir ,  Aaron Bayne Miller

发明人： Robin Douglas Clark ,  Richard Malcolm Eglen ,  John Otis Gardner ,  Alam Jahangir ,  Aaron Bayne Miller

IPC分类号： C07D295/10 ,  A61K31/136 ,  A61K31/335 ,  A61K31/357 ,  A61K31/36 ,  A61K31/40 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/443 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61P1/00 ,  A61P9/00 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P43/00 ,  C07C225/22 ,  C07C239/16 ,  C07C259/10 ,  C07D207/09 ,  C07D211/14 ,  C07D211/20 ,  C07D211/32 ,  C07D211/34 ,  C07D211/46 ,  C07D211/58 ,  C07D211/62 ,  C07D213/46 ,  C07D295/03 ,  C07D295/108 ,  C07D317/58 ,  C07D317/66 ,  C07D319/18 ,  C07D405/06 ,  C07D487/08

CPC分类号： C07D295/108 ,  C07C225/22 ,  C07C259/10 ,  C07D211/32 ,  C07D211/34 ,  C07D211/46 ,  C07D211/58 ,  C07D211/62 ,  C07D317/66 ,  C07D319/18

摘要： The present invention relates to novel 5-HT.sub.4 receptor ligands which are 1-(5-halo-4-aminophenyl) (C.sub.2-6)alkan-1-one derivatives in which the 5-halo-4-aminophenyl group is substituted at its 2-position with (C.sub.1-4)alkyloxy or phenyl(C.sub.1-4)alkyloxy and optionally substituted at its 3-position with (C.sub.1-4)alkyloxy or substituted at its 2- and 3-positions together with methylenedioxy or ethylenedioxy and the highest numbered carbon of the (C.sub.2-6)alkan-1-one is substituted with di(C.sub.1-4)alkylamino, morpholin-1-yl or pyrrolidin-1-yl or optionally substituted piperidin-1-yl, piperidin-4-yl, azacyclohept-1-yl, azabicyclo�2.2.1!hept-3-yl, azabicylo�2.2.2!oct-3-yl or azabicylo�3.2.2!non-3-yl; and the pharmaceutically acceptable salts, individual isomers and mixtures of isomers and methods of using and making such derivatives.

摘要翻译： 本发明涉及5-（5-卤代-4-氨基苯基）（C 2-6）烷-1-酮衍生物的新型5-HT 4受体配体，其中5-卤代-4-氨基苯基在其 （C 1-4）烷氧基或苯基（C 1-4）烷氧基，并且其3-位上任选被（C 1-4）烷氧基取代或在其2-和3-位与亚甲二氧基或亚乙二氧基取代， （C2-6）烷基-1-酮的最高编号的碳被二（C 1-4）烷基氨基，吗啉-1-基或吡咯烷-1-基或任选取代的哌啶-1-基，哌啶-4-基， 氮杂环庚烯-1-基，氮杂双环[2.2.1]庚-3-基，氮杂双环[2.2.2]辛-3-基或氮杂双环[3.2.2]壬-3-基; 和其药学上可接受的盐，各异构体和异构体的混合物以及使用和制备这些衍生物的方法。