申请人:Synthelabo
公开号:US04382938A1
公开(公告)日:1983-05-10
Imidazo[1,2-a] pyridines of the formula: ##STR1## and their acid addition salts in which Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a naphthyl radical or a radical ##STR2## in which each of X.sub.1 and X.sub.2 independently of one another is a hydrogen or halogen atom, a C.sub.1-4 alkoxy radical, a C.sub.1-6 alkyl radical or CF.sub.3, CH.sub.3 S--, CH.sub.3 SO.sub.2 --, --NO.sub.2, --NH.sub.2 or --NHCOCH.sub.3, and each of R.sub.1 and R.sub.2 independently of one another represents a hydrogen atom, a straight or branched C.sub.1-5 alkyl radical which is unsubstituted or substituted by one or more halogen atoms or hydroxyl, --N(C.sub.1-4 alkyl).sub.2, carbamoyl or C.sub.1-4 alkoxy radicals, allyl, propargyl, a C.sub.3-6 cycloalkyl radical, benzyl, or phenyl, not both R.sub.1 and R.sub.2 being hydrogen, or --NR.sub.1 R.sub.2 represents a heterocyclic ring containing from 3 to 6 carbon atoms, or a heterocyclic ring of the formula ##STR3## in which X is O, S, CHOR' or >N--R, R' being hydrogen or benzyl and R being hydrogen, a C.sub.1-4 alkyl radical, or phenyl which is unsubstituted or substituted by methoxy or a halogen atom, which may be made from the corresponding acids, have valuable pharmacological properties, especially anxiolytic, anti-anoxic, sleep-inducing, hypnotic and anticonvulsant properties.
式子:##STR1##中的咪唑并[1,2-a]吡啶及其酸加成盐,其中Y代表氢或卤素原子或C.sub.1-4烷基基团,Z代表萘基团或基团##STR2##其中X.sub.1和X.sub.2各自独立地是氢或卤素原子、C.sub.1-4烷氧基、C.sub.1-6烷基或CF.sub.3、CH.sub.3S--、CH.sub.3SO.sub.2--、--NO.sub.2、--NH.sub.2或--NHCOCH.sub.3,R.sub.1和R.sub.2各自独立地代表氢原子、未取代或取代一个或多个卤素原子或羟基的直链或支链C.sub.1-5烷基、--N(C.sub.1-4烷基).sub.2、氨基甲酰基或C.sub.1-4烷氧基基团、烯丙基、丙炔基、C.sub.3-6环烷基、苄基或苯基,其中R.sub.1和R.sub.2不都是氢,或--NR.sub.1 R.sub.2代表含有3至6个碳原子的杂环或公式##STR3##中的杂环,其中X为O、S、CHOR'或>N--R,R'为氢或苄基,R为氢、C.sub.1-4烷基或苯基,未取代或取代一个甲氧基或卤素原子的苯基,可以从相应的酸制备而成,具有有价值的药理学特性,特别是抗焦虑、抗缺氧、催眠、催眠和抗癫痫特性。