Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-06-20
1997-09-16
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544336, C07D24100, A61K 3154
Patent
active
056681372
ABSTRACT:
The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.
REFERENCES:
patent: 5270313 (1993-12-01), Burri et al.
patent: 5292740 (1994-03-01), Burri et al.
patent: 5397798 (1995-03-01), Fitch et al.
patent: 5420129 (1995-05-01), Breu et al.
patent: 5464853 (1995-11-01), Chan et al.
R.D. Desai et al., "Studies in Sulphonamides: Part II. Preparation of N.sup.1 -Heterocyclic Substituted Sulphonamides from Alpha-naphthylamine and Evaluation of their Antibacterial Properties", Jour. Indian Chem. Soc., pp. 115-118, vol. 46, No. 2, 1969.
R.D. Desai et al., "Studies in Sulphonamides: Part IV. Some N.sup.6 -Heterocyclic Sulphonamides from 2-Naphthylamine as possible Antibacterial Agents", J. Indian Chem. Soc., pp. 411-414, vol. 46, No. 5, 1969.
P. Mamalis et al., "142. Some Heterocyclic N-Oxides", J. Chem. Soc., pp. 703-705, 1950.
Chemical Abstracts, vol. 84, No. 15, 1976, 84:100672y.
Chemical Abstracts, vol. 100, No. 15, 1984, 100:131420t.
Chemical Abstracts, vol.. 106, No. 17, 1987, 106:133792p (corresponds to JP61257960).
Himel et al., "Fluorescent Analogs of Insecticides and Synergists. Synthesis and Reactions of Active-Site-Directed Fluorescent Probes", Journal Agr. Food Chem., vol. 19, No. 6, 1971, pp. 1175-1180.
Shigehara et al., "Preparation of Pyridine Derivatives and their Salts as Phospholipase A.sub.2 Inhibitors", Chemical Abstracts, vol. 122, No. 25, 1995, 122:314455g.
STN Printout identifying compounds disclosed in PCT 90-009787 and Japan 61-257960.
The Discovery of Sulfonamide Endothelin Antagonists and the Development of the Orally Active ET.sub.A antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesul fonamide, Journal of Medicinal Chemistry, Feb. 4, 1994, vol. 37, No. 3, pp. 329-331.
Identification of a New Class of ET.sub.A Selective Endothelin Antagonists by Pharmacophore Directed Screening, Biochemical and Biophysical Research Communications, May 30, 1994, vol. 201, No. 1, pp. 228-234.
Pharmacological Characterization of Bosentan, a New Potent Orally Active Nonpeptide Endothelin Receptor Antagonist, Journal Pharmacol. Exp. Therap., 1994, 270, 228-235.
Pages copied from a book of abstracts provided in an International Business Communications Conference entitled "Endothelin Inhibitors--Advances in Therapeutic Application and Development", Philadelphia, PA, Jun. 9-10, 1994, 33 pages.
Ballard Peter Grahame
Bradbury Robert Hugh
James Roger
Phillips Paul John
Bucknum Michael
Grumbling Matthew V.
Harris Robert J.
Higgins Patrick H.
Zeneca Ltd.
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