Patent · US Expired

Catechol derivatives

US5705703A · kind A · utility

21Cited by
7References
21Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJan 21, 1997
Grant dateJan 6, 1998
Priority date
Expiry dateJan 21, 2017

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D471/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.