Estriol esters

• US 4,738,957 A
• Filed: 03/21/1986
• Issued: 04/19/1988
• Est. Priority Date: 03/21/1985
• Status: Expired due to Fees

• Current Assignee: Schering Ag (Merck & Co., Inc.)
• Original Assignee: Schering Ag (Merck & Co., Inc.)
• Inventors: Elger, Walter, Bittler, Dieter, Laurent, Henry, Beier, Sybille
• Primary Examiner(s): NOT, DEFINED
• Assistant Examiner(s): Lipovsky, Joseph A.
• Application Number:
  US06/842,691
• Time in Patent Office: 760 Days
• Field of Search: 260/397.5, 514/170, 514/182
• US Class Current: 514/182
• CPC Class Codes: C07J 1/0059 substituted in position 17 by a keto group
• CPC Class Codes: C07J 1/007 the substituent being an OH group free esterified or etherified

Abstract

Estriol esters of Formula I ##STR1## wherein R is, in each case, the residue of an aliphatic monocarboxylic acid of 3-10 carbon atoms,

surpass estriol in strength and duration of estrogen activity.

Claims

1. An estriol ester of the formula ##STR4## wherein R is, in each case, alkanoyl of 3-10 carbon atoms.

2. A compound of claim 1, wherein the R groups are identical.

3. 3,16α

-Dipropionyloxy-1,3,5(10)-estratrien-17β

-ol, a compound of claim 2.

4. 3,16α

-Dibutyryloxy-1,3,5(10)-estratrien-17β

-ol, a compound of claim 2.

5. 3,16α

-Divaleryloxy-1,3,5(10)-estratrien-17β

-ol, a compound of claim 2.

6. 3,16α

-Dihexanoyloxy-1,3,5(10)-estratrien-17β

-ol, a compound of claim 2.

7. 3,16α

-Didecanoyloxy-1,3,5(10)-estratrien-17β

-ol, a compound of claim 2.

8. A pharmaceutical composition comprising a compound of claim 1 and a carrier.

9. A pharmaceutical composition comprising 1-100 mg of a compound of claim 1 and a carrier.

10. A pharmaceutical composition of claim 8 adapted for parenteral administration.

11. A method of treating climacteric deficiency symptoms in a female comprising administering a compound of claim 1.

12. A method of claim 11, wherein the symptom is hot flashes, osteoporosis, or atrophy of skin or the genitals.

13. A method of claim 11, wherein the administration is parenterally.

14. A method of contraception comprising administering a compound of claim 1.

15. A method of treating a gynecological disorder comprising administering a compound of claim 1.

16. A method of claim 15, wherein the disorder is vaginal atrophy or praurosis vulvae.

17. A method of claim 15, wherein the administration is parenterally.

18. A method of treating a patient in need of estrogen comprising administering a compound of claim 1 in controlled release fashion whereby a depot estrogenic effect is achieved.