Catechol derivatives

Details Catechol derivatives Catechol derivatives

1991-04-16

1993-08-17

Reamer, James H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514523, 514525, 514676, 568306, 558415, A61K 31275

Patent

active

052369528

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-adensoylmethionine 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, extraneuornal 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 (1982-11-01), 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.
Miyamoto et al., Chemical Abstracts, vol. 99, 121998 (1983).
Chemical Abstracts, vol. 95, 135254t (1981).
Nikadejvic et al., Catechol-O-Methyl Transferase II. A New Class of Inhibitors of Catechol-O-Methyl Transferase, J. Pharmacol. Exp. Ther. 174, 83-93 (1970).
Fahn et al., Effect of Catechol-O-Methyl Transferase Inhibitor, U-0521 with Levodopa Administration, Biochem Pharmacol. 28, 1221-1225 (1979).
Reches et al., Catechol-O-Methyl Transferase Inhibition by U-0521 Increases Striatal Utilization of Levdopa, Arch. Pharmacol. 320, 34-37 (1982).
Borchardt et al., Catechol-O-Methyl Transferase, J. Med. Chem. 25, 258-263 (1982).
Borchardt and Huber, Catechol-O-Methyl Transferase, J. Med. Chem. 25,321-323 (1982).
Borchardt and Huber, Function and Regulation of Monoamine Enzymes, Basic and Clinical Aspects, ed. E. Usdin, N. Weinder and M. B. H. Youdim, MacMillin Publishers, 1981, 657-664.
Chemical Abstracts 92, 146461x (1980).
Chemical Abstracts, 98,50111f (1983).
Traxler and Ghisalba, A Genetic Approach to the Biosynthesis of the Rifamycin-Chromophore in Nocardia Mediterranei, J. Antibiotics 35 (10), 1361-6 (1982).
Chemical Abstracts Service, Registry Handbook 1965-1971, p. 10666R.

Affiliated with

Also associated with

Rating

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.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2244019