|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.|
|Inventor(s):||Bernauer; Karl (Oberwil, CH), Borgulya; Janos (Basel, CH), Bruderer; Hans (Biel-Benken, CH), Da Prada; Mose (Riehen, CH), Zurcher; Gerhard (Basel, CH)|
|Assignee:||Hoffman-La Roche Inc. (Nutley, NJ)|
|Patent Claim Types:|
see list of patent claims
|Country||Document Number||Publication Date|
|South Africa||8701564||Oct 28, 1987|
|United States||5236952||Aug 17, 1993|
|United States||5389653||Feb 14, 1995|
|United States||5633371||May 27, 1997|
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