C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/5.06, 167/10
C07K 5/065 (2006.01) A61K 38/05 (2006.01) C07K 5/06 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2009982
72222-136 PHOSPHORUS CONTAINING RENIN INHIBITORS Abstract Phosphorus containing polypeptides of the formula below have a renin inhibiting activity and are useful as antihyper- tensive agents: Image Wherein R1 is (CH3O)2PO-, (CH2)2O2PO- or X-Y-, where X is mor- pholino, 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, 4- oxopiperidino, 4-oxocyclohexyl, alkoxy having one to five carbon atoms or 4-hydroxypiperidino and Y is CH2C=O or C=O; R2 is hy- drogen or methoxy; R3 is alkyl having one to four carbon atoms, methoxyalkyl said alkyl having one to three carbon atoms, methyl- thioalkyl said alkyl having one to three carbon atoms, hydroxy- methyl, imidazol-4-ylmethyl, methylsulfonylmethyl, methylsulfinyl- methyl 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.
Limited Pfizer
Smart & Biggar
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