Organic compounds -- part of the class 532-570 series – Organic compounds – Chalcogen in the nitrogen containing substituent
Patent
1995-09-15
1997-05-27
Davis, Zinna Northington
Organic compounds -- part of the class 532-570 series
Organic compounds
Chalcogen in the nitrogen containing substituent
544 8, 544 50, 544 51, 544 90, 544180, 544182, 544215, 544336, 544344, 544353, 546118, 546139, 546152, 546176, 546329, 546330, 548131, 548143, 548151, 548153, 548202, 548203, 548205, 548235, 548252, 548254, 5483097, 5483361, 5483411, 5483751, 548503, 549 13, 549407, C07D21302, C07D49802
Patent
active
056333714
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.
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Bernauer Karl
Borgulya Janos
Bruderer Hans
Da Prada Mos e
Z urcher Gerhard
Ciambrone Coletti Ellen
Davis Zinna Northington
Hoffmann-La Roche Inc.
Johnston George W.
Silverman Robert A.
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