Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1994-12-22
1996-12-10
Springer, David B.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
546 24, 548119, 548121, 548112, 514 82, 514 89, A61K 31675, C07F 958, C07F 96524, C07F 9653
Patent
active
055831230
ABSTRACT:
The present invention relates to the phosphono-alkylamino-substituted tetrazole derivatives of formula I ##STR1## and tautomers thereof wherein R.sub.1 is (carbocyclic or heterocyclic) aryl-C.sub.1 -C.sub.4 -alkyl; X is phenylene, phenylene substituted by lower alkoxy, lower-alkyl, halogen or trifluoromethyl or X.sub.1 is ethynylene; R.sub.2 is carbocyclic or heterocyclic aryl; pharmaceutically acceptable mono- or di-ester derivatives thereof in which one or both of the acidic hydroxy groups of the phosphono functional group are esterified in form of a pharmaceutically acceptable mono- or di-ester, and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of endothelin-converting enzyme by administration of said compounds to mammals in need of such treatment.
REFERENCES:
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patent: 5250522 (1993-10-01), DeLombaert
patent: 5273990 (1993-12-01), DeLombaert
Trapani et al., J. Cardiovasc. Pharmacol. 1995, vol. 26, (Suppl. 3), pp. 569-571.
FASB Journal, Abstracts, Endothelin/Endothelin Receptors, Mar. 15, 1994.
Research Communications in Chemical Pathology and Pharmacology, vol. 52, No. 1, Apr. 1986.
Biochemical & Biophysical Research Communications, vol. 204, No. 1, 1994.
Bioorganic & Medicinal Chemistry Letters, vol. No. 10, pp. 1257-1262, 1994.
Ciba-Geigy Corporation
Gruenfeld Norbert
Springer David B.
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