Composition

• US 20020193444A1
• Filed: 04/10/2002
• Published: 12/19/2002
• Est. Priority Date: 01/14/2000
• Status: Active Grant

• Current Assignee: Barry Victor Lloyd Potter, Gudrun Reddersen, Heinrich-Thomas Proske, Michael John Reed, Walter Elger
• Original Assignee: Barry Victor Lloyd Potter, Gudrun Reddersen, Heinrich-Thomas Proske, Michael John Reed, Walter Elger
• Inventors: Reed, Michael John, Potter, Barry Victor Lloyd, Elger, Walter, Reddersen, Gudrun, Proske, Heinrich-Thomas
• Granted Patent: US 7,335,650 B2
• Time in Patent Office: Days
• US Class Current: 514/601
• 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 pharmaceutical composition comprising

(i) a compound of Formula (I)

 

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 μ

g/day

2. A pharmaceutical composition according to claim 1 wherein the compound is present in an amount to provide a dosage of from 10 to 200 μ

g/day.

3. A pharmaceutical composition according to claim 1 or 2 wherein the compound is present in an amount to provide a dosage of from 50 to 200 μ

g/day.

4. A pharmaceutical composition according to claim 1 or 2 wherein the compound is present in an amount to provide a dosage of from 20 to 50 μ

g/day.

5. A pharmaceutical composition according to claim 1 wherein the compound is present in an amount no greater than 200 μ

g/dose.

6. A pharmaceutical composition according to claim 1 wherein the compound is present in an amount no greater than 1 mg/dose.

7. A pharmaceutical composition according to claim 1 wherein the compound is present in an amount no greater than 4 mg/dose.

8. A pharmaceutical composition according to any one of the preceding claims wherein X in combination with K mimics a steroidal structure.

9. A pharmaceutical composition according to any one of the preceding claims wherein K is a cyclic group.

10. A pharmaceutical composition according to any one of the preceding claims wherein X is a six-membered ring.

11. A pharmaceutical composition according to any one of the preceding claims wherein the ring X has six carbon atoms in the ring.

12. A pharmaceutical composition according to any one of the preceding claims wherein the compound is of Formula II

13. A pharmaceutical composition according to any one of the preceding claims wherein X in combination with K is a steroidal ring structure.

14. A pharmaceutical composition according to any one of the preceding claims wherein group K and ring X are a steroid ring structure or a substituted derivative thereof.

15. A pharmaceutical composition according to claim 14 wherein the Rs group is at position 3 of the ring X

16. A pharmaceutical composition according to any one of the preceding claims wherein Rs is a sulphamate group.

17. A pharmaceutical composition according to any one of the preceding claims wherein the compound is of Formula III

18. A pharmaceutical composition according to claim 17 wherein Rh1 is at position 2 of the ring X.

19. A pharmaceutical composition according to claim 17 or 18 wherein Rh2 is at position 4 of the ring X.

20. A pharmaceutical composition according to claim 1 wherein the compound of Formula I is selected from compounds

21. A composition according to any one of the preceding claims for use in medicine.

22. Use of a composition according to any one of claims 1 to 20 in the manufacture of a medicament for use in oral contraception.

23. Use of a composition according to any one of claims 1 to 20 in the manufacture of a medicament for use in hormone replacement therapy.

24. Use of a composition according to any one of claims 1 to 20 in the manufacture of a medicament for bone protecting hormone replacement therapy without endometrial stimulation

25. Use of a composition according to any one of claims 1 to 20 in the manufacture of a medicament for use in the therapy of a condition or disease associated with STS.

26. Use of a composition according to any one of claims 1 to 20 in the manufacture of a medicament for use in the therapy of a condition or disease associated with adverse STS levels.