公开(公告)号：US20020052351A1

公开(公告)日：2002-05-02

申请号：US09985679

申请日：2001-11-05

申请人： Glaxo Group Limited

发明人： Russell Michael Hagan ,  Keith Thomas Bunce

IPC分类号： A61K038/16 ,  A61K031/704 ,  A61K031/7048 ,  A61K031/7068 ,  A61K031/4375 ,  A61K031/573 ,  A61K033/24

CPC分类号： C07D487/08 ,  A61K31/44 ,  A61K31/445 ,  A61K31/57 ,  A61K45/06 ,  Y10S514/872 ,  A61K31/435 ,  A61K31/415 ,  A61K31/165 ,  A61K2300/00

摘要： The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. 1 wherein R represents the ring A 2 or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

摘要翻译： 本发明涉及速激肽拮抗剂（包括P物质拮抗剂和其他神经激肽拮抗剂）在治疗呕吐中的用途。 还描述了式（I）的新型速激肽拮抗剂，其制备方法，含有它们的药物组合物及其医疗用途。 其中R表示环A或2-吡啶基或2-吡啶基-N-氧化物; R 1选自卤素原子和C 1-4烷基，C 1-4烷氧基，三氟甲基和S（O）n C 1-4烷基; R 2和R 3可以相同或不同，各自独立地选自氢和卤素原子和C 1-4烷基，C 1-4烷氧基，三氟甲基和氰基; n表示0，1或2; 及其药学上可接受的盐和溶剂化物。