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A process for the preparation of dihidrapiridinas antisquemicos useful as antihypertensive agents and anti-.

机译:一种用于抗高血压的双歧吡啶二酸的制备方法,其用作抗高血压药和抗高血压药。

摘要

1,4-dihydropyridine derivatives of the formula (I): CHEM and pharmaceutically acceptable salts; wherein R is aryl or heteroaryl; R1 and R2 are each independently C1-C4 alkyl or 2-methoxy-ethyl; Y is -(CH2)n-, -CH2CH(CH3)- or -CH2C(CH3)2-; X is a group of the formula: CHEM wherein R3 is H, het, -(CH2)n-het, -NH-het, -NH-(CH2)n-het, -O-het, -O-(CH2)n-het, -(CH2)n-OH, -NR6R7, -(CH2)nNR6R7 or -NH- -(CH2)pNR6R7; R4 is H, C1-C4 alkyl, -(CH2)pNR6R7, -(CH2)p-OH or -(CH2)n-het; and R5 is H, C1-C4 alkyl or phenyl; wherein R6 and R7 are each independently H or C1-C4 alkyl or the two groups R6 and R7 are taken together with the nitrogen atom to which they are attached to form a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C1-C4 alkyl)piperazinyl group; n is 1-4 and p is 2-4; with the proviso that when R4 is H or C1-C4 alkyl, R3 is not H or -NR6R7. These compounds are useful as anti-ischaemic and anti-hypertensive agents.
机译:式(I)的1,4-二氢吡啶衍生物:和药学上可接受的盐;其中R是芳基或杂芳基; R 1和R 2各自独立地为碳数1〜4的烷基或2-甲氧基乙基。 Y为-(CH 2)n-,-CH 2 CH(CH 3)-或-CH 2 C(CH 3)2-; X是下式的基团:其中R 3为H,het,-(CH 2)n-het,-NH-het,-NH-(CH 2)n-het,-O-het,- O-(CH2)n-het,-(CH2)n-OH,-NR 6 R 7,-(CH2)nNR 6 R 7或-NH--(CH2)pNR <6 > R <7>; R 4为H,C 1 -C 4烷基,-(CH 2)pNR 6 R 7,-(CH 2)p-OH或-(CH 2)n -het; R 5为H,C 1 -C 4烷基或苯基。其中R 6和R 7各自独立地为H或C 1 -C 4烷基,或两个基团R 6和R 7与它们所连接的氮原子一起形成吡咯烷基,哌啶子基,吗啉代,哌嗪基或N-(C1-C4烷基)哌嗪基; n为1-4,p为2-4;前提是当R 4是H或C 1 -C 4烷基时,R 3不是H或-NR 6 R 7。这些化合物可用作抗缺血和抗高血压药。

著录项

  • 公开/公告号ES551012A0

    专利类型

  • 公开/公告日1988-02-16

    原文格式PDF

  • 申请/专利权人 PFIZER CORPORATION;

    申请/专利号ES19860551012

  • 发明设计人

    申请日1986-01-17

  • 分类号C07D211/84;A61K31/44;

  • 国家 ES

  • 入库时间 2022-08-22 06:57:23

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