Renin-inhibiting amino acid derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514332, 514333, 514334, 514335, 514337, 514338, 514340, 514342, 514343, 514346, 514347, 514348, 514349, 514350, 514351, 514352, 514354, 514355, 514356, 514357, 546146, 546147, 546256, 546257, 546258, 546261, 546270, 546274, 546278, 546291, 546292, 546293, 546294, 546296, 546297, 546298, 546299, 546300, 546304, 546307, 546308, 546309, 546310, 546311, 546312, 546330, 546331, 546334, 546335, 546336, 546337, A61K 3144, A61K 3147, C07D40104, C07D40106, C07D21182, C07D21184, C07D21186

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052043576

ABSTRACT:
The invention relates to compounds of the formula I ##STR1## in which A represents a substituted thio-, sulfinyl- or sulfonyl-alkanoyl radical or a four- to eleven-membered heterocycle, B is an amino acid residue, R.sup.1 denotes hydrogen (substituted) alkyl, (substituted)cycloalkyl or aryl, R.sup.2 represents hydrogen, (substituted)alkyl or aryl, R.sup.3 denotes a radical of the formula --(CH.sub.2).sub.q --(X).sub.r --(CH.sub.2).sub.s --R.sup.6 with X denoting CF.sub.2, CO or CHR.sup.8, R.sup.6 denoting a (substituted)heteroaromatic, R.sup.8 denoting alkyl, alkoxy, alkylthio, alkylamino, hydroxyl, azide or halogen, q and s denoting 1 to 4, and r denoting 0 or 1, and R.sup.9 is hydrogen, (substituted)alkyl, alkanoyl, cycloalkanoyl, (substituted) aroyl or (substituted)aryl, and to the salts thereof. In addition, processes for the preparation of these compounds, and the use thereof as renin inhibitors are described.

REFERENCES:
Burger, A. Medicinal Chemistry, 2nd Ed. pp. 565-601 (1960).
Haber et al.; J. of Cardiovascular Pharm. pp. 554-558 (1987).
Denkewalter et al. Progress in Drug. Research, pp. 510-512 (1966).
Bolis et al. Renin Inhibitors, J. Medicinal Chemistry, vol. 30, No. 10, pp. 1729-1737 (1987).
Plattner et al.; J. Medicinal Chem. vol. 31, No. 12, pp. 2277-2288 (1988).
Browne et al. Chem. Abstracts vol. 111; 58354v (1989).

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