Steroid sulphatase inhibitors

Details Steroid sulphatase inhibitors Steroid sulphatase inhibitors

1998-07-08

2000-01-04

Cook, Rebecca

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514178, 514601, 514603, 514604, A61K 31165

Patent

active

060110244

ABSTRACT:
A method of inhibiting steroid sulphatase activity in a subject in need of same is described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37.degree. C. it would provide a K.sub.m value of less than 50 .mu.M.

REFERENCES:
patent: 4937237 (1990-06-01), Holt et al.
patent: 5281587 (1994-01-01), Reed
patent: 5344827 (1994-09-01), Reed
patent: 5604215 (1997-02-01), Reed et al.
patent: 5616574 (1997-04-01), Reed et al.
patent: 5677292 (1997-10-01), Li et al.
"Animal Experimental Contribution to the Development of Estrogenic Substances" (hereinafter "the Stolzer Dissertation"), Dissertation for award of Doctor of Science degree at the Mathematic-Naturwissenschaftlichh-Technischen Faculty of Friedrich-Schiller-University Jena, Jul. 1989.
Erythrocytes as a drug carrier--Investigations with selected estrogens for loading following oral administration, Natural Science Faculty, Science Council, Martin-Luther Universitat Halle-Wittenberg, Germany, Aug. 1989, Claussen.
WPI AN 90-377906, Y. Lo et al, 1990.
"Tierexperimenteller Beitrag zur Entwicklung Estrogener Wirkstoffe," Dissertation sur Erlangung des akademischen Grades eines Doktors der Wissenschaften an der Mathematisch-Naturwissenschaftlich-Technischen Fakultat des Wissenschaftlichen Rates der Friedrich-Schiller-Universitat Jena, Wolfgang Stolzner, Jena, Germany, Aug. 1988.
"Erythrozyten als Arzneimitteltrager--Untersuchungen mit ausgewahlten Estrogenen zur Beladung nach oraler Gabe," Dissertation B sur Erlangung des akademischen Grades eines Doktors der Wissenschaften, Der Fakultat fur Naturwissenschaftlichen Rates der Martin-Luther-Universitat Halle-Wittenberg, Claus Claussen, Jena, Germany, Aug. 1989.
Schwarz et al., Pharmazie, vol. 30 (1975), pp. 17-21.
Howarth et al., J. Med. Chem., vol. 37 (1994), pp. 219-221.
Townsley et al., Research Steroids, vol. 5 (1973), pp. 73-78.
Zeitschrift Fur Chemie, vol. 14, No. 1, 1974, pp. 219-221.

Affiliated with

Also associated with

Rating

Steroid sulphatase inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Steroid sulphatase inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Steroid sulphatase inhibitors will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1072772