专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

12. 发明授权

US4894460A Basic esters exhibiting an antagonistic activity to calcium, process for the preparation thereof and pharmaceutical compositions therefrom 失效
标题翻译：对钙具有拮抗作用的碱性酯，其制备方法和药物组合物
公开(公告)号：US4894460A
公开(公告)日：1990-01-16
申请号：US563008
申请日：1983-12-19
申请人： Silvia Z. Tricerri , Cesare Casagrande , Franco de Marchi , Massimo Nicola
发明人： Silvia Z. Tricerri , Cesare Casagrande , Franco de Marchi , Massimo Nicola
IPC分类号： C07D211/90 , C07D295/088 , C07D401/12 , C07D417/12
CPC分类号： C07D295/088 , C07D211/90 , C07D401/12 , C07D417/12
摘要： Basic esters of 1,4-dihydropyridine-3,5-dicarboxylic acid of formula (I) ##STR1## are described, in which R.sup.1 is a linear or branched alkyl radical containing 1-5 carbon atoms which is unsubstituted or substituted by an alkoxy group; R.sup.2 is phenyl or a nitro phenyl radical; R.sup.3 is phenyl, phenyl substituted by one to three radicals selected from (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, fluoro, chloro, bromo, nitro, cyano, COOR in which R is alkyl of 1 to 4, trifluo carbon atoms, romethyl, hydroxy, amino, mono- or di-alkylamino, mono- or di-acylamino, mercapto, S(O).sub.n -alkyl with n=0, 1 or 2, (C.sub.1-5)acyl, carbamoyl, ureido or R.sup.3 is a 5 or 6 membered heteroaryl monocyclic radical which contains one or more heteroatoms which are N, O or S such as unsubstituted pyridyl, pyrazinyl, pyrimidyl, furyl, imidazolyl, thienyl, thiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl or mono-, di- or tri-substituted with alkyl, alkoxy, halogen or trifluoromethyl; X is a linear or branched alkylen radical containing between 2 and 5 carbon atoms which is unsubstituted or substituted by an alkoxy group and their racemates, enantiomers and diastereoisomers and addition salts thereof with a pharmaceutically acceptable acid. The novel compounds exhibit calcium antagonistic activity.
摘要翻译：描述了式（I）的1,4-二氢吡啶-3,5-二羧酸的碱性酯，其中R 1是含有1-5个碳原子的直链或支链烷基，其是未取代或取代的通过烷氧基; R2是苯基或硝基苯基; R3是苯基，被1-3个选自（C1-4）烷基，（C1-4）烷氧基，氟，氯，溴，硝基，氰基，COOR的基团取代的苯基，其中R是1-4的烷基，三氟碳单或二烷基氨基，单 - 或二 - 酰氨基，巯基，具有n = 0,1或2，（C 1-5）酰基，氨基甲酰基，脲基的S（O）n-烷基或R 3是含有一个或多个N，O或S的杂原子的5或6元杂芳基单环基团，例如未取代的吡啶基，吡嗪基，嘧啶基，呋喃基，咪唑基，噻吩基，噻唑基，1,2,3-三唑基，1 ，2,4-三唑基或被烷基，烷氧基，卤素或三氟甲基单，二或三取代; X是含有2至5个碳原子的直链或支链亚烷基，其未被取代或被烷氧基及其外消旋物，对映异构体和非对映异构体及其药学上可接受的酸的加成盐取代。新化合物表现出钙拮抗作用。

IPRDB

热门服务

关于我们

友情链接

联系方式