Estrogenic compounds and pharmaceutical formulations comprising the same

• US 7,989,436 B2
• Filed: 05/27/2010
• Issued: 08/02/2011
• Est. Priority Date: 07/23/2003
• Status: Expired due to Fees

• Current Assignee: Duramed Pharmaceuticals Incorporated
• Original Assignee: Duramed Pharmaceuticals Incorporated
• Inventors: Hill, Edward N., Whittle, Robert R., Sancilio, Frederick D.
• Primary Examiner(s): Badio; Barbara P
• Application Number:
  US12/788,450
• Publication Number:
  US 20100234330A1
• Time in Patent Office: 432 Days
• Field of Search: 514/171, 552/615
• US Class Current: 514/171
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: C07J 1/00 Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
• CPC Class Codes: C07J 17/00 Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton cardanolide, bufanolide C07J19/00

Abstract

Novel estrogenic compounds of Formula I are provided.

wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R₁ is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R₁ does not exist; R₂ is lower alkyl; R₃ may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R₄ through R₁₃ may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower alkyl, lower alkoxy, halogen, and carbonyl groups and R₁₄ is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R₁ is hydroxy, the hydroxy or ester substituent may have either an α or a β orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.

Claims

1. A topical pharmaceutical formulation comprising:

(a) a compound represented by the following Formula;

2. The topical pharmaceutical formulation of claim 1, wherein the formulation is a vaginal cream.

3. The topical pharmaceutical formulation of claim 1, wherein the formulation is a gel.

4. The topical pharmaceutical formulation of claim 1, wherein the formulation is a suppository.

5. The topical pharmaceutical formulation of claim 1, wherein the formulation is a transdermal patch.

6. A topical pharmaceutical formulation comprising:

(a) a compound represented by the following Formula;

7. The topical pharmaceutical formulation of claim 6, wherein the formulation is a vaginal cream.

8. The topical pharmaceutical formulation of claim 6, wherein the formulation is a gel.

9. The topical pharmaceutical formulation of claim 6, wherein the formulation is a suppository.

10. The topical pharmaceutical formulation of claim 6, wherein the formulation is a transdermal patch.