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US 4,904,660 AGranted
Histidine derivatives as superior renin inhibitors
AssigneeYamanouchi Pharmaceutical Co., Ltd.
InventorsKohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
Life of this patent
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Abstract
Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.
Claims10
A compound of the formula (I) ##STR206## wherein R.sub.1 is a lower alkoxycarbonyl group, a lower alkoxycarbonylamino group, a group of the formula:
- --(CH.sub.2).sub.n --A--R.sup.a wherein n is an integer of 1 or 2;
- A is a single bond, a lower alkylene group which may be substituted by a hydroxy group (s), or a carbonyl group, R.sup.a is a cyano group, a lower alkyl group, a lower alkynyl group, a cycloalkyl, a cylcoalkylidene group, a hydrocarbyl aryl group, an aryloxy group which may be substituted by at least one halogen atom, or a 5 or 6 membered heterocyclic ring group wherein the heteroatoms are at least one of oxygen, nitrogen and sulfur, which groups may be substituted by at least on amino group, or a group of the formula:
- --CONH--B--R.sup.b wherein B is a single bond, or a lower alkylene;
- R.sup.b is a hydroxyl group, an aryl group, or a heterocyclic group;
- R.sub.2 is a phenyl group or a naphthyl group;
- R.sub.3 is a lower alkyl group, cyclohexyl group, or a phenyl group;
- R.sub.4 is a nitromethyl group, a group of the formula:
- --COOR.sup.c wherein R.sup.c is a lower alkyl group;
- or a group of the formula:
- ##STR207## wherein n is zero or an integer of 1 or 2;
- R.sup.d is a 5 or6 membered heterocyclic ring group wherein the heteroatoms are at least one of oxygen, nitrogen and sulfur which groups may be substituted by at least one lower alkyl group, a carbamoyl-lower-alkyl group (s), or a hydroxy-lower-alkyl group;
- and R.sup.5 is a hydrogen atom or a lower alkyl group.
9 more elements
Dependencies are inferred from the claim text.