伊加地平盐酸盐

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 伊加地平盐酸盐
• 英文名称: 5-O-[2,2-dimethyl-3-(4-prop-2-enylpiperazin-1-yl)propyl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;hydron;dichloride
• 化学式: C28H40Cl2N4O6
• 分子量: 599.5
• InChiKey: PJGTYHKZUAHNHC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.22
• 重原子数：
  40
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  117
• 氢给体数：
  3
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  3-(1-piperazinyl)-2,2-dimethylpropyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 以75的产率得到伊加地平盐酸盐
  参考文献：
  名称：

  1,4-dihydropyridine derivatives and pharmaceutical composition thereof

  摘要：

  通式为： ##STR1## 的1,4-二氢吡啶衍生物，其中X.sup.1和X.sup.2独立地表示氢、氟甲基、氟甲氧基、卤素、氰基或硝基；R.sup.1表示低级烷基；R.sup.2表示酰基、烷氧羰基、酰基烷基、N-烷基取代的氨基甲酰基烷基、烷氧基烷基、烷氧羰基烷基、酰氧基烷基、硝酸酯基烷基、氰基烷基、杂环基烷基、卤代烷基、烯基或炔基；A表示含有一个碳原子，与2个烷基连接的烷基，总共至少有5个碳原子的烷基；m表示整数1、2或3；以及其酸加成盐；制备方法；和含有这种化合物的药物组合物。这些化合物具有药理活性，特别是强大而持久的降压活性，冠状动脉扩张、脑血管扩张、周围血管扩张、肾血管扩张和抑制血小板聚集活性。

  公开号：

  US04937242A1

文献信息

• 1,4-Dihydropyridine derivatives and pharmaceutical composition thereof
  申请人：Kyoto Pharmaceutical Industries, Ltd.

  公开号：EP0289746A2

  公开（公告）日：1988-11-09

  1,4-Dihydropyridine derivatives of the general formula: wherein X' and X2 independently represent hydrogen, fluoromethyl, fluoromethoxy, halogen, cyano, or nitro: R1 represents a lower alkyl; R2 represents acyl, alkoxycarbonyl, acylalkyl, an N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, heterocycle-alkyl, haloalkyl, alkenyl, or alkynyl; A represents an alkylene comprising a carbon atom to which 2 alkyls are bonded and having in total at least 5 carbon atoms; m represents the integer 1, 2 or 3; acid addition salts thereof; a method of production thereof; and pharmaceutical compositions containing such compound(s). Such compounds have pharmacological activities, in particular potent and long lasting hypotensive activity. coronary vasodilatation, cerebral vasodilatation, peripheral vasodilatation, renal vasodilatation and platelet aggregation inhibitory activity.

  通式如下的 1，4-二氢吡啶衍生物 其中 X' 和 X2 独立地代表氢、氟甲基、氟甲氧基、卤素、氰基或硝基：R1 代表低级烷基；R2 代表酰基、烷氧羰基、酰基烷基、N-烷基取代的氨基甲酰基、烷氧基烷基、烷氧羰基烷基、酰氧基烷基、硝基烷基、氰基烷基、杂环烷基、卤代烷基、烯基或炔基；A 代表由一个碳原子组成的亚烷基，其中有 2 个烷基与之键合，且总共至少有 5 个碳原子；m 代表整数 1、2 或 3；其酸加成盐；其生产方法；以及含有此类化合物的药物组合物。 这类化合物具有药理活性，特别是强效持久的降血压活性、冠状动脉血管舒张活性、脑血管舒张活性、外周血管舒张活性、肾血管舒张活性和血小板聚集抑制活性。
• ANTI-INFLAMMATORY AGENTS AND INHIBITORS AGAINST INCREASE IN OCULAR TENSION CAUSED BY IRRADIATION WITH LASERS, CONTAINING 1,4-DIHYDROPYRIDINE DERIVATIVES
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1179345A1

  公开（公告）日：2002-02-13

  The present invention provides an anti-inflammatory medicament and an inhibitor of intraocular pressure rise due to laser irradiation, which contains 1,4-dihydropyridine derivative of the formula (I) wherein X1 and X2 are the same or different and each is hydrogen atom, fluoromethyl, fluoromethoxy, halogen, cyano or nitro, R1 is lower alkyl, R2 is acyl, alkoxycarbonyl, acylalkyl, N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, hetero ring-alkyl, haloalkyl, alkenyl or alkynyl, A is alkylene having a carbon atom bonded with two alkyls and 5 or more carbon atoms in total, and m is an integer of 1 to 3, or an acid addition salt thereof, as an active ingredient.

  本发明提供了一种抗炎药物和激光照射引起的眼压升高的抑制剂，它含有式(I)的1,4-二氢吡啶衍生物 A是一个碳原子上键有两个烷基且总共有 5 个或更多碳原子的亚烷基，m 是 1 至 3 的整数、 或其酸加成盐作为活性成分。
• INHIBITORS FOR OPTIC HYPOFUNCTION CAUSED BY OPTIC NERVE CELL INJURY INDUCED BY FACTORS OTHER THAN OPTIC CIRCULATORY DISORDER
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1181934A1

  公开（公告）日：2002-02-27

  The present invention relates to an inhibitor of a visual function disturbance caused by an ophthalmic nerve cell disorder due to a factor other than an ophthalmic circulatory disorder, which contains, as an active ingredient, a 1,4-dihydropyridine derivative of the formula (I) wherein X1 and X2 are the same or different and each is hydrogen atom, fluoromethyl, fluoromethoxy, halogen, cyano or nitro, R1 is lower alkyl, R2 is acyl, alkoxycarbonyl, acylalkyl, N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, hetero ring-alkyl, haloalkyl, alkenyl or alkynyl, A is alkylene having 5 or more carbon atoms in total including a carbon atom bonded to two alkyls, and m is an integer of 1 to 3, or an acid addition salt thereof.

  本发明涉及一种眼神经细胞失调引起的视觉功能障碍的抑制剂，其活性成分为式(I)的1,4-二氢吡啶衍生物。 其中 X1 和 X2 相同或不同，且各自为氢原子、氟甲基、氟甲氧基、卤素、氰基或硝基，R1 为低级烷基，R2 为酰基、烷氧基羰基、酰基烷基、N-烷基取代的氨基甲酰基、烷氧基烷基、烷氧基羰基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、酰氧基烷基、A 是总共具有 5 个或更多碳原子的亚烷基，包括与两个烷基键合的碳原子，m 是 1 至 3 的整数，或其酸加成盐。
• Agents for treating intraocular inflammation caused by irradiation with lasers, containing 1,4-dihydropyridine derivatives
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1915996A1

  公开（公告）日：2008-04-30

  The present invention provides a 1,4-dihydropyridine derivative of the formula (I) wherein X1 and X2 are the same or different and each is hydrogen atom, fluoromethyl, fluoromethoxy, halogen, cyano or nitro, R1 is lower alkyl, R2 is acyl, alkoxycarbonyl, acylalkyl, N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, hetero ring-alkyl, haloalkyl, alkenyl or alkynyl, A is alkylene having a carbon atom bonded with two alkyls and 5 or more carbon atoms in total, and m is an integer of 1 to 3, or an acid addition salt thereof, and a medicament containing said compound of formula (I) as an active ingredient for topically treating intraocular inflammation caused by laser irradiation.

  本发明提供了一种式 (I) 的 1,4-二氢吡啶衍生物 其中 X1 和 X2 相同或不同，且各自为氢原子、氟甲基、氟甲氧基、卤素、氰基或硝基，R1 为低级烷基，R2 为酰基、烷氧基羰基、酰基烷基、N-烷基取代的氨基甲酰基、烷氧基烷基、烷氧基羰基、酰氧基烷基、硝基烷基、氰基烷基、杂环烷基、A是一个碳原子上键有两个烷基且总共有 5 个或更多碳原子的亚烷基，m 是 1 至 3 的整数、 或其酸加成盐，以及一种含有所述式（I）化合物作为活性成分的药物，用于局部治疗由激光照射引起的眼内炎症。
• DRUGS FOR AMELIORATING OCULAR CIRCULATORY DISORDERS
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP0968716B1

  公开（公告）日：2008-12-31