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Details for Patent: 5,476,875

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Summary for Patent: 5,476,875

Title: Catechol derivatives
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)
Application Number:08/327,160
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent PDF download available with subscription

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Foreign Priority and PCT Information for Patent: 5,476,875

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Switzerland980/86Mar 11, 1986
Switzerland62/87Jan 09, 1987

International Patent Family for Patent: 5,476,875

Country Document Number Publication Date Supplementary Protection Certificate SPC Country SPC Expiration
South Korea930001337Feb 26, 1993
European Patent Office0237929Sep 23, 1987C970041Netherlands<disabled>
Hong Kong165896Sep 13, 1996
Norway165959Jan 28, 1991
European Patent Office0237929Sep 23, 198797C0112Belgium<disabled>
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Preferred citation:

Friedman, Y. Location of pharmaceutical innovation: 2000–2009 Nature Reviews Drug Discovery 9, 835–836 (2010).

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