Renin inhibitors
AssigneeAbbott Laboratories
InventorsSaul H. Rosenberg, Jon F. Denissen
Life of this patent
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Abstract
A renin inhibiting compound of the formula: ##STR1## wherein R.sub.1 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; R.sub.2 is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl; R.sub.3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH.sub.3 S-- or CH.sub.3 SCH.sub.2 --; R.sub.4 is isobutyl or cyclopropyl; R.sub.5 is hydrogen or loweralkyl; and X is CH.sub.2 or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that when X is NH and R.sub.3 is 2-amino-4-thiazolyl, then R.sub.4 is cyclopropyl.
Claims15
A compound of formula:
- ##STR9## wherein R.sub.1 is 4-morpholinyl or 4-thiomorpholinyl;
- R.sub.2 is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;
- R.sub.3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH.sub.3 S-- or CH.sub.3 SCH.sub.2 ;
- R.sub.4 is isobutyl or cyclopropyl;
- R.sub.5 is hydrogen or loweralkyl;
- and
- X is CH.sub.2 ;
- or a pharmaceutically acceptable salt, ester or prodrug thereof.
A compound of the formula:
- ##STR10## wherein R.sub.1 is 4-morpholinyl or 4-thiomorpholinyl;
- R.sub.2 is benzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;
- R.sub.3 is 4-thiazolyl or 2-amino-4-thiazolyl;
- R.sub.4 is isobutyl or cyclopropyl;
- and
- R.sub.5 is hydrogen or loweralkyl;
- or a pharmaceutically acceptable salt, ester or prodrug thereof.
A compound selected from the group consisting of:
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-(5-Thiazolyl)Ala Amide of (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane;
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-(2-Thiazolyl)Ala Amide of (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane;
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-)2-aminothiazol-4-yl) Ala Amide of
- (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane;
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-(4-thiazolyl)Ala Amide of (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane;
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-(5-Thiazolyl)Ala Amide of (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-4-(cyclopropyl)butane;
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-(2-Thiazolyl)Ala Amide of (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-4-(cyclopropyl)butane;
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-(2-aminothiazol-4-yl) Ala Amide of (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-4-(cyclopropyl)butane;
- and
- (2S)-2-Benzyl-3-(morpholin-4-ylsulfonyl)propionyl-(L)-(4-thiazolyl)Ala Amide of (2S,3R,4S)-2-Amino-1-cyclohexyl-3,4-dihydroxy-4-(cyclopropyl)butane;
- or a pharmaceutically acceptable salt, ester or prodrug thereof.
Dependencies are inferred from the claim text.