首页> 外国专利> New 1-(imino or amino)methyl-2-hydroxymethylene indolizine derivs. - and their prepn. from 1-formyl cpds. useful as cardio:property and CNS protectants e.g. against post-traumatic shock

New 1-(imino or amino)methyl-2-hydroxymethylene indolizine derivs. - and their prepn. from 1-formyl cpds. useful as cardio:property and CNS protectants e.g. against post-traumatic shock

机译：新的1-（亚氨基或氨基）甲基-2-羟基亚甲基吲哚嗪衍生物。 -和他们的准备。来自1-甲酰基cpds。可用作心脏：财产和中枢神经系统保护剂，例如防止创伤后休克

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1-(Imino or amino)methyl -2-hydroxymethylene -indolizine derivs. (I) and their addn. salts are new. In (I), A = -CH=NR3 or -CH2NR3R4; B plus vicinal C atoms = gp. (i)-(v); X = S or NR5; Y = S, O or NR6; R1, R2 = H, 1-4C alkoxy, mercapto, methylmercapto or amino or R1+R2 = -O-(CH2)n-O- where n = 1 or 2; R3 = H, a satd. 1-12C aliphatic, unsatd. 2-12C aliphatic or 3-6C cyclic hydrocarbon gp. opt. substd. by hydroxy, methoxy, amino, 1-5C alkylamino, di(1-5C alkyl)amino, 3-6C cycloalkyl, opt. substd. phenyl or a 5- or 6-membered satd. or unsatd. heterocyclic gp. contg. 1 or 2 N, S and/or O atoms and opt. substd. by 1-3C alkyl; or phenyl opt. substd. by hydroxy, methoxy or halogen; R4 = H, 1-4C alkylcarbonyl or 1-4C alkyl; R5, R6 = H, methyl or benzyl; R8 = H, 1-3C alkyl, 3-6C cycloalkyl or methylmercapto. USE/ADVANTAGE - Cpds. (I) are cardioprotectives, e.g. against angina pectoris, cardiac infarct and cardiac fibrillation, and CNS protectants, e.g. against post-traumatic shock and alcohol-induced disorders. Cpds. (I) can be administered enterally or parenterally, with oral dosages being e.g. 2-20 mg/kg 1-3 times daily. In the hypoxia tolerance test cpds. (I) showed pronounced CNS protection at a dosage of 5 mg/kg p.o. and were superior to diltiazem, verapamil and nifedipine.

机译：1-（氨基或氨基）甲基-2-羟基亚甲基-吲哚嗪衍生物。（I）及其地址。盐是新的。在（I）中，A ＝ -CH ＝ NR 3或-CH 2 NR 3 R 4; B加邻近的C原子= gp。（i）-（v）; X = S或NR5; Y = S，O或NR6; R1，R2 ＝ H，1-4C烷氧基，巯基，甲基巯基或氨基或R1 + R2 ＝ -O-（CH2）n-O-，其中n ＝ 1或2; R3 = H，饱和1-12C脂肪族，未饱和。 2-12C脂族或3-6C环状烃gp。选择。取代羟基，甲氧基，氨基，1-5C烷基氨基，二（1-5C烷基）氨基，3-6C环烷基取代苯基或5或6元饱和还是不满意杂环续1或2个N，S和/或O原子并选择。取代1-3C烷基;或苯基选择。取代通过羟基，甲氧基或卤素; R4 ＝ H，1-4C烷基羰基或1-4C烷基; R5，R6 ＝ H，甲基或苄基; R 8 ＝ H，1-3C烷基，3-6C环烷基或甲基巯基。使用/优势-Cpds。（I）是心脏保护剂，例如预防心绞痛，心肌梗塞和心脏颤动，以及中枢神经系统保护剂，例如防止创伤后休克和酒精引起的疾病。 Cpds。（I）可以肠内或肠胃外给药，口服剂量例如为。每天2-3次，每次2-20 mg / kg。在缺氧耐受性试验中使用cpds。（I）在剂量为5 mg / kg p.o时显示出明显的中枢神经保护作用。并且优于地尔硫卓，维拉帕米和硝苯地平。

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公开/公告号DE3918519A1

专利类型
公开/公告日1990-12-13

原文格式PDF
申请/专利权人 BOEHRINGER INGELHEIM KG 6507 INGELHEIM DE;
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申请/专利号DE19893918519
发明设计人 LOESEL WALTER DIPL.-CHEM. DR. 6535 GAU-ALGESHEIM DE;ROOS OTTO DIPL.-CHEM. DR. 6501 SCHWABENHEIM DE;ARNDTS DIETRICH DR. 6531 APPENHEIM DE;SPECK GEORG DIPL.-CHEM. DR. 6507 INGELHEIM DE;STRELLER ILSE DR. 6534 STROMBERG DE;
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申请日1989-06-07
分类号C07D471/04;C07D491/12;C07D471/14;C07D495/14;C07D491/147;A61K31/40;
国家 DE
入库时间 2022-08-22 05:49:37

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