申请人:SMITH KLINE & FRENCH LABORATORIES
LIMITED
公开号:EP0089765A2
公开(公告)日:1983-09-28
1. A compound of formula (1):-
and pharmaceutically acceptable salts thereof, where
R1 and R2 are the same or different and are C1-6 alkyl or with the nitrogen atom to which they are attached form a pyrrolidino or piperidino group;
R3 is C1-4 alkylene;
R4 is hydrogen, C1-6 alkyl, hydroxy-C2-4alkyl; optionally substituted phenyl or phenyl (C1-6 alkyl) (the substituents being one or more C1-6 alkyl, or C1-6 alkoxy groups or halogen atoms);
R5 and RS are the same or different and are hydrogen, C1-6 alkyl, hydroxy C1-6 alkyl, C1-6 alkoxy-C1-6alkyl, C2-8 alkenyl, C2.6 alkynyl, optionally substituted phenyl or phenyl (C1-6 alkyl), (the substituents being one or more C1-6 alkyl or C1-6 alkoxy groups or halogen atoms or a methylenedioxo group), or optionally substituted furanyl- or thienyl- or pyridyl(C1-6 alkyl) (the substituents being one or more C1-6 alkyl or C1-6 alkoxy groups); or taken together represent a C4-6 alkylene group, or taken together represent a group of formula (2):-
where R7 is phenyl or pyridyl and R8 is hydrogen or C1-6 alkyl. where R1 to R4 are as defined with reference to formula (1) with an amine of formula (19):-
and optionally converting a compound of formula (1) produced by any one of steps (a) to (f) into a salt.
1.式 (1) 的化合物
及其药学上可接受的盐类,其中
R1 和 R2 相同或不同,且为 C1-6 烷基或与所连接的氮原子形成吡咯烷基或哌啶基;
R3 是 C1-4 亚烷基
R4是氢、C1-6烷基、羟基-C2-4烷基、任选取代的苯基或苯基(C1-6烷基)(取代基是一个或多个C1-6烷基或C1-6烷氧基或卤素原子);
R5 和 RS 相同或不同,并且是氢、C1-6 烷基、羟基 C1-6烷基、C1-6 烷氧基-C1-6烷基、C2-8 烯基、C2.6炔基、任选取代的苯基或苯基(C1-6 烷基)(取代基为一个或多个 C1-6 烷基或 C1-6 烷氧基或卤原子或亚甲基二氧基),或任选取代的呋喃基或噻吩基或吡啶基(C1-6 烷基)(取代基为一个或多个 C1-6 烷基或 C1-6 烷氧基);或合起来代表一个 C4-6 亚烷基,或合起来代表一个式(2)的基团:- R7 是苯基或吡啶基(C1-6 烷基)。
其中 R7 是苯基或吡啶基,R8 是氢或 C1-6 烷基。 其中 R1 至 R4 如参照式(1)所定义,加入式(19)的胺:- R1 至 R4 如参照式(1)所定义。
以及任选地将步骤(a)至(f)中任一步制得的式(1)化合物转化为盐。