Composition

• US 7,335,650 B2
• Filed: 04/10/2002
• Issued: 02/26/2008
• Est. Priority Date: 01/14/2000
• Status: Expired due to Fees

• Current Assignee: Schering Ag (Merck & Co., Inc.), Sterix Limited
• Original Assignee: Schering Ag (Merck & Co., Inc.), Sterix Limited
• Inventors: Reed, Michael John, Roddersen, Gudrun, Proske, Heinrich-Thomas, Potter, Barry Victor Lloyd, Elger, Walter
• Primary Examiner(s): HUI, SAN MING R
• Application Number:
  US10/120,275
• Publication Number:
  US 20020193444A1
• Time in Patent Office: 2,148 Days
• Field of Search: 514/182, 514/170, 514/180, 514/711, 514/181
• US Class Current: 514/181
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/566 having an oxo group in position 17, e.g. estrone
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone

Abstract

There is provided a pharmaceutical composition comprising (i) a compound of the formula

wherein: X is a hydrocarbyl ring having at least 4 atoms in the ring; K is a hydrocarbyl group; Rs is a sulphamate group; (ii) optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant, wherein the compound is present in an amount to provide a dosage of no greater than 200 μg/day.

Claims

1. A method for oral contraception in a human patient in need thereof comprising administering to said patient a compound of Formula (I):

3. The method according to any one of claims 1-2, wherein the administering of the compound is at a dosage of from 10 to 200 μ

g/day.

4. The method according to any one of claims 1-2, wherein the administering of the compound is at a dosage of from 50 to 200 μ

g/day.

5. The method according to any one of claims 1-2, wherein the administering of the compound is at a dosage of from 20 to 50 μ

g/day.

6. The method according to any one of claims 1-2, wherein the compound has Formula II

7. The method according to any one of claims 1-2, wherein the the steroidal ring is optionally substituted with halo groups R_h1 and R_h2;

and at least one of R_h1 and R_h2 is present.

8. The method according to claim 7, wherein R_h1 is present at position 2 of the steroidal ring.

9. The method according to claim 7 or 8, wherein R_h2 is at position 4 of the steroidal ring.

10. The method according to any one of claims 1-2, wherein the compound comprises two sulphamate groups.

11. The method according to any one of claims 1-2, wherein the compound of Formula I is selected from the group consisting of oestrone, oestradiol, oestratriol, epi-estriol.

12. The method according to any one of claims 1-2, wherein the steroidal ring of the compound of Formula I comprises one or more substituents selected from the group consisting of hydroxy, alkyl, alkoxy, alkinyl, and halogen.

13. The method according to any one of claims 1-2, wherein the steroidal ring of the compound of Formula I comprises one or more substituents selected from the group consisting of hydroxy, (C₁-C₆)alkyl, (C₁-C₆)alkoxy, alkinyl and halogen.

14. The method according to any one of claims 1-2, wherein R₁ and R₂ together represent alkylene.

15. The method according to any one of claims 1-2, wherein the sulphamate compound contains one or two N-alkyl, N-alkenyl, N-cycloalkyl, N-acyl, or N-aryl substituents.

16. The method according to any one of claims 1-2, wherein R₁ and R₂ are each independently selected from lower alkyl groups containing from 1 to 5 carbon atoms.

17. The method according to any one of claims 1-2, wherein R₁ and R₂ are each independently methyl, ethyl, or propyl.

18. The method according to any one of claims 1-2, wherein R₁ and R2 are both methyl.

19. The method according to any one of claims 1-2, wherein R₁ and R₂ together represent alkylene comprising 4 to 6 carbon atoms.

2. A method for hormone replacement therapy in a human patient in need thereof comprising administering to said patient a compound of Formula (I):