Naphthalene thromboxane synthetase inhibitors

Details Naphthalene thromboxane synthetase inhibitors Naphthalene thromboxane synthetase inhibitors

1984-10-22

1986-05-20

Fan, Jane T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514277, 514351, 514345, 514355, 514399, 546342, 546333, 546334, 546300, 546301, 546302, 546315, 548335, C07D21306, A61K 31435

Patent

active

045902003

ABSTRACT:
A novel series of carboxy-substituted naphthalenes and carboxy-substituted benzo-fused heterocycles, such as carboxy-substituted derivatives of indole, benzofuran and benzothiophene, has been prepared, including their pharmaceutically acceptable salts. These particular compounds are useful in therapy for the treatment of thrombosis, ischaemic heart disease, stroke, transient ischaemic attack, migraine, peripheral vascular disease, the vascular complications of diabetes and endotoxic shock. Preferred member compounds include 2-(1-imidazolylmethyl)-3-methylbenzo[b]thiophene-5-carboxylic acid and 3-methyl-2-(3-pyridylmethyl)benzo[b]thiophene-5-carboxylic acid, respectively. Methods for preparing these compounds from known starting materials are provided.

REFERENCES:
patent: 4179565 (1979-12-01), Jarque et al.
patent: 4217357 (1980-08-01), Cross et al.
patent: 4230714 (1980-10-01), Cross et al.
patent: 4273782 (1981-08-01), Cross et al.
patent: 4410539 (1983-10-01), Cross et al.
John G. Topliss, "Utilization of Operation Schemes for Analog Synthesis in Drug Design", Journal of Medicinal Chemistry, vol. 15, No. 10, p. 1006 (1972).

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