| 摘要 |
72222-136 PHOSPHORUS CONTAINING RENIN INHIBITORS Phosphorus containing polypeptides of the formula below have a renin inhibiting activity and are useful as antihypertensive agents: Wherein R1 is (CH3O)2PO-, (CH2)2O2PO- or X-Y-, where X is morpholino, N-methylpiperazino, piperidino, pyrrolidin-1-yl, pyrrolyl, 3-oxopyrrolidin-1-yl, imidazolyl, cis-4-hydroxycyclo-hexyl, trans-4-hydroxycyclohexyl, acetylalkyl having three to six carbon atoms, alkyl having one to three carbon atoms, 4oxopiperidino, 4-oxocyclohexyl, alkoxy having one to five carbon atoms or 4-hydroxypiperidino and Y is CH2C=O or C=O; R2 is hydrogen or methoxy; R3 is alkyl having one to four carbon atoms, methoxyalkyl said alkyl having one to three carbon atoms, methylthioalkyl said alkyl having one to three carbon atoms, hydroxymethyl, imidazol-4-ylmethyl, methylsulfonylmethyl, methylsulfinylmethyl or carbamylethyl; R4 and R5 when considered separately are each alkyl having one to three carbon atoms, benzyl, alkoxy having one to four carbon atoms, dimethylamino or hydroxy; and R4 and R5 when taken together are alkylene having four to six carbon atoms, alkylenedioxy having three to four carbon atoms or mono- or dimethylalkylenedioxy having four to six carbon atoms.
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