| 摘要 |
Disclosed herein are compounds of the formula: A-N(R<1>)C(O)CH2CHR<2>C(O)-B wherein A is R<3>R<4>NC(O)CH2 wherein, for example, R<3> is hydrogen or alkyl and R<4> is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R<3> and R<4> together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R<1> is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R<2> is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure. |
