Organic compounds -- part of the class 532-570 series – Organic compounds – Oxygen containing
Patent
1997-01-21
1998-01-06
Davis, Zinna Northington
Organic compounds -- part of the class 532-570 series
Organic compounds
Oxygen containing
558414, 558415, 558416, 562465, 562473, 564170, C07C25549, C07C20520
Patent
active
057057036
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.
REFERENCES:
patent: 2199389 (1940-05-01), Britton et al.
patent: 3985783 (1976-10-01), Johnson et al.
patent: 4124726 (1978-11-01), Hamazaki et al.
patent: 4332820 (1982-06-01), Markley
patent: 4622066 (1986-11-01), Kitahara et al.
patent: 4801616 (1989-01-01), Gapinski
patent: 4963590 (1990-10-01), Backstrom et al.
J. Pharmacol Exp. Ther. vol. 174, pp. 83-93 (1970).
Biochem. Pharmacol. vol. 28, pp. 1221-1225 (1979).
Arch. Pharmacol. vol. 320, pp. 34-37 (1982).
J. Med. Chem. vol. 25, pp. 258-263 (1982).
J. Med. Chem. vol. 25, pp. 321-323 (1982).
Registry Handbook 1965-1971 pp. 1066R.
Function & Regulation of Monoamine Enzymes, Basic & Clinical Aspects, MacMillan Publishers, pp. 657-664 (1981).
Chemical Abstracts 92, 146461x (1980).
Chemical Abstracts 98, 50111f (1983) & J. Antibiot. 35(10) pp. 1361-1366 (1982).
Miyamoto et al., Chem. Abstr. vol. 99 # 121998; (1983).
CA 95:135254t (1981).
Chem. Abstracts vol. 115, No. 5, Abstr. 49134d p. 190 Aug. 5, 1991, Bernauer, et al.
Borgulya et al., Helv. Chim. Acta. vol. 72(5) pp. 952-68 (1989).
Backstrom, Chemical Abstracts vol. 109, No. 15, Abstract 12857OX, Oct. 10, 1988, p. 646.
Bernauer Karl
Borgulya Janos
Bruderer Hans
Da Prada Mose
Zurcher Gerhard
Ciambrone Coletti Ellen
Davis Zinna Northington
Hoffmann-La Roche Inc.
Johnston George W.
Silverman Robert A.
LandOfFree
Catechol derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Catechol derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Catechol derivatives will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2330414