Novel prodrugs of estradiol

• US 20070015741A1
• Filed: 07/03/2006
• Published: 01/18/2007
• Est. Priority Date: 07/12/2005
• Status: Abandoned Application

• Current Assignee: Warner Chilcott Company LLC (Abbvie Incorporated)
• Original Assignee: Warner Chilcott Company LLC (Abbvie Incorporated)
• Inventors: McIlroy, James, King, John, Keown, James, Armstrong, William, Gilligan, Claire
• Application Number:
  US11/478,584
• Publication Number:
  US 20070015741A1
• Time in Patent Office: Days
• US Class Current: 514/176
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: C07J 1/007 the substituent being an OH group free esterified or etherified
• CPC Class Codes: C07J 41/0072 the A ring of the steroid being aromatic
• CPC Class Codes: C07J 43/00 Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
• CPC Class Codes: C07J 43/003 not condensed

Abstract

The present invention is a prodrug derivative of estradiol according to Formula I:

Claims

1. A prodrug derivative of estradiol having the following formula:

2. The prodrug of claim 1, wherein X is

4. A method of providing contraception comprising the step of:

administering to a patient in need thereof, an effective amount of said prodrug derivative of estradiol of claim 1, for an effective period of time.

5. A method of providing hormone treatment therapy to a patient in need thereof, comprising the step of:

administering to said patient in need thereof, an effective amount of said prodrug derivative of estradiol of claim 1, for an effective period of time.

3. A pharmaceutical dosage unit comprising:

(a) a prodrug derivative of estradiol having the following formula;

and enantiomers and pharmaceutically acceptable salts thereof, wherein X is selected from the group consisting of

and

(b) one or more pharmaceutically acceptable excipients.