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    • 3. 发明授权
    • 1,4-dihydropyridine-3,5-dicarboxylic acid ester derivatives and
pharmaceutical compositions
    • 1,4-二氢吡啶-3,5-二羧酸酯衍生物和药物组合物
    • US4618607A
    • 1986-10-21
    • US448576
    • 1982-12-10
    • Kazuhiko ArakiHideki AoJun InuiKenichi Aihara
    • Kazuhiko ArakiHideki AoJun InuiKenichi Aihara
    • C07D211/90C07D213/89C07D401/04C07D401/12C07D405/04C07D405/12C07D407/12C07D409/04C07D409/12C07D409/14C07D413/12C07D417/04C07D417/12C07D491/10A61K31/445A61K31/55C07D401/14
    • C07D213/89C07D211/90C07D401/04C07D401/12C07D405/04C07D405/12C07D409/04C07D409/12C07D409/14C07D413/12C07D417/04C07D417/12C07D491/10
    • 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives of the general formula: ##STR1## or acid addition salts thereof, wherein W is --CH.dbd. or --N.dbd.; Y is --CH.dbd.CH--, --O--, --S--, --CH.dbd.N(O)p-- (p is zero or 1) or --N(R)-- (R is hydrogen or lower alkyl); X.sup.1, X.sup.2 and X.sup.3 are the same or different, and are each hydrogen, halogen, nitro, trifluoromethyl, cyano or lower alkylthio; Z is aryl or 5- or 6-membered aromatic heterocyclic ring (which may have a substituent or two or three substituents which may be the same or different, and the substituent may be halogen, lower alkyl, lower alkoxy, lower alkanoylamino, cyano, nitro, lower alkylthio, trifluoromethyl, sulfamoyl, di-lower alkylsulfamoyl, amino or di-lower alkylamino); ##STR2## is 5- to 7-membered heterocyclic ring which may have nitrogen atom, oxygen atom, sulfur atom or unsaturated bond on the ring, and may be substituted by lower alkyl, lower alkoxycarbonyl, lower alkanoylamino, ethylenedioxy or --(CH.sub.2).sub.m --OR.sup.4 (R.sup.4 is hydrogen, lower alkyl or lower alkanoyl and m is 0, 1 or 2); R.sup.1 and R.sup.2 are the same or different, and are each lower alkyl; R.sup.3 is lower alkyl, aralkyl, heteroaralkyl; and n is an integer 1 to 5. Such compounds are useful as antihypertensive agents and as therapeutic agents for cardiac and cerebral circulation disorders.
    • 1,4-二氢吡啶-3,5-二羧酸酯衍生物或其酸加成盐,其中W是-CH =或-N =; Y是-CH = CH-,-O-,-S-,-CH = N(O)p - (p是0或1)或-N(R) - (R是氢或低级烷基) X1,X2和X3相同或不同,各自为氢,卤素,硝基,三氟甲基,氰基或低级烷硫基; Z是芳基或5-或6-元芳族杂环(其可以具有取代基或两个或三个可以相同或不同的取代基,并且取代基可以是卤素,低级烷基,低级烷氧基,低级烷酰基氨基,氰基, 硝基,低级烷硫基,三氟甲基,氨磺酰基,二低级烷基氨磺酰基,氨基或二低级烷基氨基)。 可以在环上具有氮原子,氧原子,硫原子或不饱和键的5-至7-元杂环,并且可被低级烷基,低级烷氧基羰基,低级烷酰基氨基,亚乙二氧基或 - (CH 2) m-OR4(R4是氢,低级烷基或低级烷酰基,m是0,1或2)。 R 1和R 2相同或不同,并且各自为低级烷基; R3是低级烷基,芳烷基,杂芳烷基; 并且n为1至5的整数。这些化合物可用作抗高血压剂和作为心脏和脑循环障碍的治疗剂。