Ethanolamine derivatives, process for their preparation and pharmaceutical compositions containing them
申请人:BEECHAM GROUP PLC
公开号:EP0091749A2
公开(公告)日:1983-10-19
AA compound of formula (I):
or a salt thereof, wherein;
R1 is hydrogen, halogen or trifluoromethyl.
R2 is hydrogen or halogen,
R3 is hydrogen or methyl,
R4 is hydrogen or methyl,
R6 is hydrogen, C1-10 straight or branched alkyl or optionally substituted benzyl,
R6 is hydrogen, C1-10 straight or branched alkyl, or optionally substituted benzyl,
or R6 and R6 taken together with the attached nitrogen atom represent a heterocyclic ring,
R7 is hydrogen or halogen, and
n is 1 or 2;
are useful in the treatment of obesity and/or diabetes.
Anti-hypertensive compounds of formula (I):
wherein
one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl or by C2-7 alkanoyl;
one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl, or R3 and R4 together with the carbon atom to which they are attached are C3-6 spiroalkyl;
R5 is hydrogen, C1-3 alkyl or C1-8 acyl; and
n is 1 or 2; the lactam group being trans to the OR5 group; or, when the other of R, and R2 is amino, a pharmaceutically acceptable salt thereof.
式 (I) 的 AA 化合物:
或其盐,其中
R1 是氢、卤素或三氟甲基。
R2 是氢或卤素、
R3 是氢或甲基
R4 是氢或甲基
R6 是氢、C1-10 直链或支链烷基或任选取代的苄基、
R6 是氢、C1-10 直链或支链烷基或任选取代的苄基、
或 R6 和 R6 连同所附的氮原子代表杂环、
R7 是氢或卤素,以及
n 为 1 或 2;
可用于治疗肥胖症和/或糖尿病。
式(I)的抗高血压化合物:
其中
R1 和 R2 中的一个是硝基、氰基或 C1-3 烷基羰基,另一个是甲氧基或可选被一个或两个 C1-6 烷基或 C2-7 烷酰基取代的氨基;
R3 和 R4 中的一个是氢或 C1-4 烷基,另一个是 C1-4 烷基,或 R3 和 R4 与它们所连接的碳原子一起是 C3-6 螺烷基;
R5 是氢、C1-3 烷基或 C1-8 丙烯酸基;以及
n为1或2;内酰胺基团反式为OR5基团;或者,当R和R2中的另一个为氨基时,为其药学上可接受的盐。