申请人:Glaxo Group Limited
公开号:US20020052351A1
公开(公告)日:2002-05-02
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;
R
1
is selected from halogen atoms and C
1-4
alkyl, C
1-4
alkoxy, trifluoromethyl, and S(O)
n
C
1-4
alkyl groups;
R
2
and R
3
, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C
1-4
alkyl, C
1-4
alkoxy, trifluoromethyl and cyano groups;
n represents zero, 1 or 2;
and pharmaceutically acceptable salts and solvates thereof.
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)在治疗呃逆中的应用。本发明还描述了式(I)的新型速激肽拮抗剂、其制备工艺、含有它们的药物组合物及其医疗用途。
1
其中
R 代表环 A
2
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,各自独立地选自氢原子、卤素原子和 C
1-4
烷基,C
1-4
烷氧基、三氟甲基和氰基;
n 代表 0、1 或 2;
及其药学上可接受的盐类和溶剂。