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Generated: August 18, 2017

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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 Claims: 1. A method of treating parkinsonism which comprises administering to a host requiring such treatment an effective amount of a pharmaceutical composition comprising L-dopa, a peripheral decarboxylic inhibitor, a compound of the formula ##STR25## wherein Ra is nitro or cyano, Rb is hydrogen or halogen, Rc is --CO--R.sup.1 wherein R.sup.1 is a phenyl group optionally mono- or disubstituted by halogen, cyano, hydroxy or lower alkyl or an ester or ether derivative thereof which is hydrolyzable under physiological conditions or a pharmaceutically acceptable salt thereof, and a therapeutically inert carrier material.

2. A method of treating parkinsonism, according to claim 1, wherein the compound is 3,4-dihydroxy-5-nitrobenzophenone.

3. A method of treating parkinsonism, according to claim 1, wherein the compound is 2'-fluoro-3,4-dihydroxy-5-nitrobenzophenone.

4. A method of treating parkinsonism according to claim 1, wherein the compound is 3,4-dihydroxy-4'-methyl-5-nitrobenzophenone.

5. A method of treating Parkinson's Disease which comprises administering to a host requiring such treatment an effective amount of a pharmaceutical composition comprising L-dopa, a peripheral decarboxylase inhibitor, a compound of the formula ##STR26## wherein Ra is nitro or cyano, Rb is hydrogen or halogen, Rc is CO--R.sup.1 wherein R.sup.1 is a phenyl group optically mono- or disubstituted by halogen, cyano, hydroxy or lower alkyl or an ester or ether derivative thereof which is hydrolyzable under physiological conditions or a pharmaceutically acceptable salt thereof, and a therapeutically inert carrier material.

6. A method of treating parkinsonism according to claim 5, wherein the compound is 3,4-dihydroxy-4'-methyl-5-nitrobenzophenone.

7. A method of treating Parkinson's disease, according to claim 6, wherein the compound is 3,4-dihydroxy-5-nitrobenzophenone.

8. A method of treating Parkinson's disease, according to claim 6, wherein the compound is 2'-fluoro-3,4-dihydroxy-5-nitrobenzophenone.
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