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    • 4. 发明授权
    • Triazine derivatives, and pharmaceutical compositions comprising the same
    • 三嗪衍生物和包含其的药物组合物
    • US4616015A
    • 1986-10-07
    • US598685
    • 1984-04-10
    • Tsutomu TerajiYouichi ShiokawaKazuo OkumuraYoshinari Sato
    • Tsutomu TerajiYouichi ShiokawaKazuo OkumuraYoshinari Sato
    • A61K31/53A61K31/535A61P1/04A61P7/02A61P9/12C07D215/22C07D215/227C07D253/06C07D253/07C07D401/04C07D401/12C07D403/10C07D403/12C07D405/12C07D521/00
    • C07D215/227C07D231/12C07D233/56C07D249/08C07D253/06C07D253/07C07D401/04C07D401/12C07D403/10C07D403/12C07D405/12
    • New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is hydrogen; halogen or hydrazinocarbonyl(lower)alkyl;R.sup.2 is hydrazino;azido;halosulfonyl;mono- or di(lower)alkylamino;mono- or di-(lower alkynylamino;pyridylamino;lower alkylideneamino substituted by furyl pyridyl or aryl;mono- or di-(lower)alkylamino substituted by amino, carboxy, hydroxy, ureido, lower alkoxy, lower alkoxycarbonyl, lower alkoxy(lower)alkoxy, aryl, furyl, pyridyl, phthalimido, or succinimido;N-methyl(lower)alkanoylamino;N-containing, 5- or 6-membered heterocyclic group optionally substituted by oxo, lower alkyl and/or lower alkoxycalbonyl;lower alkoxy substituted by hydroxy and lower alkylamino; ora group of the formula ##STR2## in which R.sup.3 is hydrogen; lower alkyl or ar(lower)alkyl;R.sup.4 is pyridyl; aryl; styryl; alkynyl; lower alkoxycarbonyl; .alpha.-hydroxybenzyl; lower alkanoyl; carboxy; or lower alkyl substituted by halogen, amino, hydroxy, carboxy, lower alkanoyl, lower alkanoyloxy, lower alkoxycarbonyl, morpholino, lower alkoxycarbonylamino, 1-methyl-2-oxo-1,2,3,4-tetrahydroquinolyloxy, mono- or di(lower)alkylamino, piperazinyl being substituted with hydroxy(lower)alkyl or furoyl, or pyrrolidino;and pharmaceutically acceptable salt thereof, which are useful in the treatment of hypertension, thrombosis and ulcer in human beings and animals.
    • 由下式表示的新的三嗪衍生物:其中R1是氢; 卤素或肼基羰基(低级)烷基; R2是肼基; 叠氮 卤磺酰; 单或二(低级)烷基氨基; 羧基,羧基,羟基,脲基,低级烷氧基,低级烷氧基羰基,低级烷氧基(低级),低级烷基氨基,低级烷基氨基, 烷氧基,芳基,呋喃基,吡啶基,苯二甲酰亚氨基或琥珀酰亚胺基; N-甲基(低级)烷酰基氨基;任选被氧代,低级烷基和/或低级烷氧基羰基取代的含N,5或6元杂环基; 羟基和低级烷基氨基;或其中R 3为氢的式(Ia)基团;低级烷基或芳(低级)烷基; R 4为吡啶基;芳基;苯乙烯基;炔基;低级烷氧羰基;α-羟基苄基;低级烷酰基;羧基 或被卤素,氨基,羟基,羧基,低级烷酰基,低级烷酰氧基,低级烷氧基羰基,吗啉代,低级烷氧基羰基氨基,1-甲基-2-氧代-1,2,3,4-四氢喹啉氧基,一或二 (低级)烷基氨基,哌嗪基被羟基(低级)烷基取代 糠酰基或吡咯烷子基; 和其药学上可接受的盐,其可用于治疗人和动物中的高血压,血栓形成和溃疡。
    • 5. 发明授权
    • (+)-5-isopropyl 3-methyl 2-cyano-6 methyl-4-(3-nitrophenyl)-1,
4-dihydropyridine-3, 5-dicarboxylate
    • (+) - 5-异丙基3-甲基2-氰基-6-甲基-4-(3-硝基苯基)-1,4-二氢吡啶-3,5-二羧酸酯
    • US5508413A
    • 1996-04-16
    • US662507
    • 1991-03-22
    • Youichi ShiokawaKazuo Okumura
    • Youichi ShiokawaKazuo Okumura
    • C07D213/84C07D213/80
    • C07D213/84
    • This invention relates to novel (+)-5-isopropyl 3-methyl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.More particularly, it relates to novel (+)-5-isopropyl 3-methyl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, which has pharmacological activities such as hypotensive and vasodilating activities, to a pharmaceutical composition comprising the same and to a method for treating hypertension, cardiovascular diseases, and the like.Accordingly, one object of this invention is to provide novel (+)-5-isopropyl 3-methyl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, which is of use for treating hyperxtension, cardiovascular diseases, and the like.
    • 本发明涉及2-氰基-6-甲基-4-(3-硝基苯基)-1,4-二氢吡啶-3,5-二羧酸的新的(+) - 5-异丙基-3-甲酯。 更具体地说,它涉及2-(3-硝基苯基)-1,4-二氢吡啶-3,5-二羧酸的新的(+) - 5-异丙基3-氰基-6-甲基-4-(3-硝基苯基)-1,4-二氢吡啶-3,5-二羧酸酯,其药理活性如 作为降血压和血管舒张活性,涉及包含其的药物组合物和治疗高血压,心血管疾病等的方法。 因此,本发明的一个目的是提供新的(+) - 5-异丙基2-氰基-6-甲基-4-(3-硝基苯基)-1,4-二氢吡啶-3,5-二甲酸3-甲酯,其中 用于治疗高血压,心血管疾病等。