Aromatically substituted .omega.-amino-alkanoic acid amides and

Details Aromatically substituted .omega.-amino-alkanoic acid amides and Aromatically substituted .omega.-amino-alkanoic acid amides and

1995-12-06

1997-06-24

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514617, 544 581, 544 86, 544131, 544165, 544386, 544400, 546225, 546227, 546233, 546316, 546323, 548253, 548492, 548568, 554 37, A61K 31165, A61K 31535, C07C23722, C07D295145

Patent

active

056417780

ABSTRACT:
Compounds of formula I ##STR1## wherein R.sub.1 is a 2-R.sub.A -3-R.sub.B -phenyl radical, a 2-R.sub.A -4-R.sub.C -phenyl radical, a 2-R.sub.A -pyridin-3-yl radical, a 3-R.sub.A -pyridin-2-yl radical or a 1-R.sub.D -indol-3-yl radical, wherein one of the radicals R.sub.A and R.sub.B is an aliphatic or heterocycloaliphatic-aliphatic radical or free or aliphatically, araliphatically or heteroaraliphatically etherified hydroxy and the other is hydrogen, an aliphatic radical or free or esterified or amidated carboxy, R.sub.C is hydrogen, an aliphatic radical, free or aliphatically, araliphatically, heteroaraliphatically or heteroarylaliphatically etherified hydroxy or an unsubstituted or heteroaliphatically substituted amino group, and R.sub.D is an aliphatic, araliphatic or heteroaliphatic radical, one of the radicals X.sub.1 and X.sub.2 is carbonyl and the other is methylene, R.sub.2 is an aliphatic radical, R.sub.3 is unsubstituted or aliphatically substituted amino, R.sub.4 is an aliphatic or araliphatic radical, and R.sub.5 is an aliphatic or cycloaliphatic-aliphatic radical or an optionally hydrogenated and/or oxo-substituted heteroaryl radical or an optionally hydrogenated and/or oxo-substituted heteroaryl or heteroaliphatyl radical bonded via a carbon atom, and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive active ingredients of medicaments.

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Plummer, Mark et al. Biorganic & Medicinal Chemistry Letters, vol. 3, No. 10 pp. 2119-2124, 1993.
Hanessdan, Stephen et al. Biorganic & Medicinal Chemistry Letters, vol. 4, No. 14, pp. 1697-1702, 1994.
Bradbury, Robert et al. Tetrahedron Letters, vol. 30, No. 29 pp. 3845-3848, 1989.
Prasad et al. Tetrahedron Letters, vol. 31, No. 13, pp. 1803-1806, 1990.
Hadrami et al. Tetrahedron Letters, vol. 32, No. 32, pp. 3985-3988, 1991.
Bradbury, Robert et al. J. Med. Chem. vol. 33, pp. 2335-2342, 1990.
Fray, Andrew et al. J. Org. Chem. vol. 51, pp. 4828-4833, 1986.

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