New imidazo[4,5-c]pyridine derivatives, processes for their preparation and pharmaceutical formulations containing such compounds
申请人:MERCK PATENT GmbH
公开号:EP0079083A1
公开(公告)日:1983-05-18
Compounds of formula (I'), and compositions containing them:
(wherein n is 1, 2 or 3, each R1 independently represents a halogen atom; a hydroxy, carboxyl or C1-4 alkyl group, a C2-4 alkenyloxy, phenyl or phenyl-C1-4 alkoxy group which may be optionally substituted by one or more halogen atoms; an .amino, mono- or dialkyl-amino, morpholino or piperazino group; a group of formula -S(O)xRa where x is 0, 1 or 2 and Ra is a C1-4 alkyl group; or a C1-4 alkoxy group which may be optionally substituted by one or more radicals selected from hydroxy, C1-4 alkoxy, amino, mono- or di- C1-4 alkylamino, (phenyl- C1-4 alkyl)amino, N,N-C1-4alkyl(phenyl-C1-4alkyl)-amino and N,N-(C1-4alkoxyphenyl-C1-4alkyl)C1-4 alkyl-amino; n is 1, 2 or 3; m is 0 or 1;
R2 represents a C1-4 alkyl group in the 1- or 3-position of the imidazo ring;
R3 represents a hydrogen or halogen (fluorine, chlorine, bromine or iodine) atom, or a hydroxy, amino or C1-4 alkyl or alkoxy group; and physiologically acceptable acid addition salts thereof and N-oxides of such compounds and salts. Formula (1') includes the alternative tautomeric form. The compounds and compositions are useful for treatment of the human or animal body by therapy, particularly for use in the treatment or prophylaxis of heart failure and myocardial insufficiency.
式(I')化合物及含有它们的组合物:
(其中 n 为 1、2 或 3,每个 R1 独立地代表卤素原子;羟基、羧基或 C1-4 烷基、C2-4 烯氧基、苯基或苯基-C1-4 烷氧基,可任选被一个或多个卤素原子取代;.氨基、单或二烷基氨基、吗啉基或哌嗪基;式 -S(O)xRa 的基团,其中 x 为 0、1 或 2,Ra 为 C1-4 烷基;或 C1-4 烷氧基,可任选被一个或多个基团取代,这些基团选自羟基、C1-4 烷氧基、氨基、单-或二-C1-4 烷基氨基、(苯基-C1-4 烷基)氨基、N,N-C1-4 烷基(苯基-C1-4 烷基)氨基和 N,N-(C1-4 烷氧基苯基-C1-4 烷基)C1-4 烷基氨基;n 为 1、2 或 3;m 为 0 或 1;
R2 代表咪唑环 1 位或 3 位上的 C1-4 烷基;
R3 代表氢原子或卤素(氟、氯、溴或碘)原子,或羟基、氨基或 C1-4 烷基或 烷氧基;及其生理上可接受的酸加成盐和此类化合物和盐的 N-氧化物。式(1')包括另一种同分异构形式。这些化合物和组合物可用于人体或动物机体的治疗,特别是用于治疗或预防心力衰竭和心肌功能不全。