Renin inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 417/12 (2006.01) A61K 31/395 (2006.01) A61K 38/05 (2006.01) C07D 277/28 (2006.01) C07D 295/26 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2041825

-142- RENIN INHIBITORS ABSTRACT OF THE DISCLOSURE A renin inhibiting compound of the formula: Image wherein R1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4- homopiperazinyl; R2 is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2- naphthylmethyl; R3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH3S- or CH3SCH2-; R4 is isobutyl or cyclopropyl; R5 is hydrogen or loweralkyl; and X is CH2 or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that when X is NH and R3 is 2-amino-4-thiazolyl, then R4 is cyclopropyl.

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