N-(2-Substituted-1-oxoalkyl)-2,3-dihydro-1H-indole-2-carboxylic acid derivatives

阅读量:

15

申请(专利)号:

US19810284433

申请日期:

1981-07-20

公开/公告号:

US4350633A

公开/公告日期:

1982-09-21

申请(专利权)人:

AMERICAN HOME PRODUCTS CORPORATION

发明人:

Dong H. KimRonald J. McCaully

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被引量:

13

摘要:

Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substituted on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3- phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;< P>R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is ##STR2## wherein: L is O, NR. sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.13 or S;R.sub.11 and R.sub.12 are, independently, hydrogen, alkyl, aralkylor aryl;R.sub.13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3;R. sub.20 is hydrogen or aryl; andR.sub.21 is hydroxy or lower alkoxy; or pharmaceutically acceptable salts thereof.< P>Claimed compounds are intermediates of the formula: ##STR3## wherein R.sub.13 is hydrogen or lower alkyl; R.sub.14 is R.sub.5 or OZ, where R. sub.5 is hydroxy, amino, or lower alkoxy, and Z is a carboxylic acid protecting group.

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