首页> 外国专利> The combination of Enalapril or a pharmaceutically acceptable salt thereof equivalent to 20 mg of enalapril maleate and 6 mg of thiazide hydrochloride in particular the combination of 20 mg of enalapril maleate and 6 mg of hydrochlorothiazide

The combination of Enalapril or a pharmaceutically acceptable salt thereof equivalent to 20 mg of enalapril maleate and 6 mg of thiazide hydrochloride in particular the combination of 20 mg of enalapril maleate and 6 mg of hydrochlorothiazide

机译:相当于20 mg马来酸依那普利和6 mg盐酸噻嗪的依那普利或其药学上可接受的盐的组合,尤其是20 mg马来酸依那普利和6 mg氢氯噻嗪的组合

摘要

Carboxyalkyl dipeptide derivatives and related compounds which are useful as antihypertensives, and having the formulae: CHEM wherein R1 and R6 are the same or different and are hydroxy, alkoxy, alkenoxy, dialkylamino alkoxy, acylamino alkoxy, acyloxy alkoxy, aryloxy, alkyloxy, substituted aryloxy or substituted aralkoxy wherein the substituent is methyl, halo, or methoxy, amino, alkylamino, dialkylamino, aralkylamino or hydroxyamino; R min is hydrogen, alkyl of from 1 to 20 carbon atoms, including branched, cyclic and unsaturated alkyl groups; substituted alkyl wherein the substituent is halo, hydroxy, alkoxy, aryloxy amino, alkylamino, dialkylamino, acylamino, arylamino, guanidino, imidazolyl, indolyl, mercapto, alkylthio, arylthio, carboxy, carboxamido, carbalkoxy, phenyl, substituted phenyl wherein the substituent is alkyl, alkoxy or halo; aralkyl or heteroaralkyl, aralkenyl or heteroaralkenyi, substituted aralkyl, substituted heteroaralkyl, substituted aralkenyl or substituted hetereoaralkenyl, wherein the substituent is halo or dihalo, alkyl, hydroxy, alkoxy, amino, aminomethyl, acylamino, dialkylamino, alkylamino, carboxyl, haloalkyl, cyano or sulfonamido, aralkyl or hetereoaralkyl substituted on the alkyl portion by amino or acylamino; R2 and R7 are hydrogen or alkyl; R3 is hydrogen, alkyl, phenylalkyl, aminomethylphenylalkyl, hydroxyphenylalkyl, hydroxyalkyl, acetylaminoalkyl, acylaminoalkyl, acylaminoalkyl aminoalkyl, dimethylaminoalkyl, haloalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl and alkylthioalkyl; R4 is hydrogen or alkyl; R5 is hydrogen, alkyl, phenyl, phenylalkyl, hydroxyphenylalkyl, hydroxyalkyl, aminoalkryl, guanidinoalkyl, imidazoylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl; R4 and R5 may be connected together to form an alkylene bridge of from 2 to 4 carbon atoms, an alkylene bridge of from 2 to 3 carbon atoms and one sulphur atom, an alkylene bridge of from 3 to 4 carbon atoms containing a double bond or an alkylene bridge as above, substituted with hydroxy, alkoxy or alkyl and the pharmaceutically acceptable salts thereof.
机译:用作抗高血压药并且具有下式的羧烷基二肽衍生物和相关化合物:其中R 1和R 6相同或不同,并且是羟基,烷氧基,烯氧基,二烷基氨基烷氧基,酰基氨基烷氧基,酰氧基烷氧基,芳氧基,烷氧基,取代的芳氧基或取代的芳烷氧基,其中取代基为甲基,卤素或甲氧基,氨基,烷基氨基,二烷基氨基,芳烷基氨基或羟基氨基; R min是氢,具有1至20个碳原子的烷基,包括支链,环状和不饱和烷基;其中取代基为卤素,羟基,烷氧基,芳氧基氨基,烷基氨基,二烷基氨基,酰基氨基,芳基氨基,胍基,咪唑基,吲哚基,巯基,烷硫基,芳硫基,羧基,羧酰胺基,羧烷氧基,苯基,取代苯基的取代烷基,烷氧基或卤素;芳烷基或杂芳烷基,芳烯基或杂芳烯基,取代的芳烷基,取代的杂芳烷基,取代的芳烯基或取代的杂芳烯基,其中取代基是卤素或二卤素,烷基,羟基,烷氧基,氨基,氨基甲基,酰基氨基,二烷基氨基,烷基氨基,羧基,卤代烷基,氰基或磺酰胺基,芳烷基或杂芳烷基在烷基部分上被氨基或酰基氨基取代; R 2和R 7为氢或烷基; R 3为氢,烷基,苯基烷基,氨基甲基苯基烷基,羟基苯基烷基,羟基烷基,乙酰氨基烷基,酰基氨基烷基,酰基氨基烷基氨基烷基,二甲基氨基烷基,卤代烷基,胍基烷基,咪唑基烷基,吲哚基烷基,巯基烷基和烷硫基烷基; R 4为氢或烷基; R 5为氢,烷基,苯基,苯基烷基,羟基苯基烷基,羟基烷基,氨基烷基,胍基烷基,咪唑基烷基,吲哚基烷基,巯基烷基或烷硫基烷基; R 4和R 5可以连接在一起以形成2-4个碳原子的亚烷基桥,2-3个碳原子和一个硫原子的亚烷基桥,3-4个碳原子的亚烷基桥。含有被羟基,烷氧基或烷基取代的上述双键或亚烷基桥的原子及其可药用盐。

著录项

  • 公开/公告号LU90173I2

    专利类型

  • 公开/公告日1998-01-27

    原文格式PDF

  • 申请/专利权人 MERCK & CO. INC.;

    申请/专利号LU19970090173C

  • 发明设计人

    申请日1997-11-19

  • 分类号C07C103/52;A61K37/02;

  • 国家 LU

  • 入库时间 2022-08-22 02:57:32

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