Compositions inhibiting estrogen sulfotransferase activity

Information

  • Patent Grant
  • 4810700
  • Patent Number
    4,810,700
  • Date Filed
    Wednesday, May 18, 1983
    41 years ago
  • Date Issued
    Tuesday, March 7, 1989
    35 years ago
Abstract
An estrogen sulfotransferase inhibitor composition comprises a compound of the formula ##STR1## wherein R.sub.1 is F, Br, NO.sub.2, or H; R.sub.2 is F, Br, NO.sub.2, NH.sub.2, or H; R is H or alkyl of 1-4 carbon atoms; R.sub.3 is O or H.sub.2 ; and R.sub.4 is H.sub.2, O, or .alpha.-H, .beta.-OH; R.sub.5 is H.sub.2, .alpha.-H and .beta.-OH or B-H and .alpha.-OH in admixture with a pharmaceutically acceptable carrier with the proviso that R.sub.1, R.sub.2 and R.sub.3 cannot all be hydrogen and one of R.sub.1 and R.sub.2 is F.
Description
Claims
  • 1. A unit dosage pharmaceutical composition for the prevention of implanation of a blastocyst in the epithelial uterine lining of a female mammal and possessing a total per unit dosage of an accurate predetermined amount of an estrogen sulfotransferase inhibiting compound such that said dosage is administered daily for from 3 to 9 days in quantities each day of from 0.1 to 500 mg of the compound, wherein the compound is 4-fluoroestrone-3-methyl ether.
  • 2. A method of treating a female mammal to prevent implanation of a blastocyst which method comprises administering an effective dosage of an estrogen sulfotransferase inhibiting compound wherein the compound is 4-fluoroestrone-3-methyl ether.
CROSS REFERENCE TO RELATED APPLICATION

This is a continuation of application Ser. No. 355,806 filed Mar. 8, 1982 now abandoned, which is a continuation-in-part of copending application Ser. No. 952,592, filed Oct. 18, 1978, now U.S. Pat. No. 4,340,602.

Government Interests

This invention described herein was made in the course of work under a Public Health Service Grant No. HD 14775-01 from the Department of Health, Education and Welfare.

Non-Patent Literature Citations (1)
Entry
Utne et al., "Journal of Organic Chemistry", Jun. (1968), pp. 2469-2473.
Continuations (1)
Number Date Country
Parent 355806 Mar 1982
Continuation in Parts (1)
Number Date Country
Parent 952592 Oct 1978