Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-04-16
1995-02-14
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514241, 514242, 514255, 514299, 514303, 514307, 514311, 514354, 514381, 514394, 514399, 514406, 514419, 544180, 544167, 544182, 544 52, 544163, 544406, 544 49, 544 8, 544105, 544 90, 544344, 546118, 546146, 546153, 546165, 546313, 546314, 546328, 548253, 5483355, 5483365, 5483741, A61K 3144, C07D21302
Patent
active
053896530
ABSTRACT:
Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.
Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
REFERENCES:
Chemical Abstracts, vol. 115, No. 5, Abstract 49134d, p. 790 Aug. 5, 1991, Bernauer et al.
Borgulya et al., Helv. Chim. Acta, vol. 72(5), pp. 952-968, 1989.
Bernauer Karl
Borgulya Janos
Bruderer Hans
Da Prada Mose
Zurcher Gerhard
Davis Zinna N.
Gould George M.
Hoffman-La Roche Inc.
Ivy C. Warren
Johnston George W.
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