| 摘要 |
Mercapto-acylamino acids of the formula: <CHEM> wherein n is 0-4; R is <CHEM> R1 is 1-3 substituents selected from the group consisting of hydrogen, halogeno, lower alkyl, cyclolower alkyl, lower alkoxy, hydroxy, aryl, aryloxy, cyano, aminomethyl, carboxy, lower alkoxy carbonyl and carbamyl; R2 is hydrogen, R11- @- or R11- @-OCH2-, wherein R11 is lower alkyl, aryl or arylmethyl; R<3> is -OR12, <CHEM> R4, R5, R6, R7, R8, R9 and R10 are independently lower alkyl, aryl lower alkyl, (cyclolower alkyl) lower alkyl, substituted aryl lower alkyl or substituted (cyclolower alkyl) lower alkyl, wherein in the substituents on the aryl and cyclolower alkyl portions are 1-3 substituents selected from the group consisting of lower alkyl, hydroxy, halogeno, lower alkoxy and amino, or R4 and R5 are alkyl and together with the sulfur and carbon atoms to which they are attached form a 5-7 membered ring; R12 and R13 are independently hydrogen, lower alkyl or substituted lower alkyl wherein the substituents are selected from the group consisting of 1 or 2 hydroxy groups, 1 or 2 lower alkoxy groups, lower alkoxy lower alkoxy, halogeno, halogeno lower alkoxy, amino, mono- or di-lower alkylamino, aryl, substituted aryl wherein the substituents on aryl are 1-3 substituents selected from the group consisting of lower alkyl, hydroxy, halogeno, lower alkoxy and amino, and a 5-6 membered saturated ring comprising 1-2 oxygen atoms as ring members wherein the ring carbon atoms can be substituted with 0-2 lower alkyl substituents; or R12 and R13 together with the nitrogen to which they are attached complete a 5-7 membered ring, wherein one of the 4-6 ring members comprising R12 and R13 may be a nitrogen atom, an alkyl-substituted nitrogen atom or an oxygen atom, and wherein the ring may be substituted on the ring carbon atoms with substituents chosen from alkyl and hydroxy groups; R14 is hydrogen, alkyl, carboxyalkyl, mercaptoalkyl, alkylthioalkyl, aminoalkyl, hydroxyalkyl, phenylalkyl, hydroxyphenylalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl or carbamoylalkyl; the pharmaceutically acceptable salts thereof and their combinations with atrial natriuretic factors or angiotensin converting enzyme inhibitors are disclosed. Such preparations are useful for treating hypertension and congestive heart failure.
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