Claims
- 1. A compound of the formula whereinA is C1-C6 alkyl; R0 is hydrogen; R1 is R2 is hydrogen or C1-C6 alkyl; R3, R4 and R5 are independently hydrogen or C1-C6 alkyl, said alkyl group optionally substituted with hydroxy, oxo or cyano; R6 is hydrogen or C1-C6 alkyl, said alkyl group optionally substituted with hydroxy, oxo or cyano; R7 is hydrogen; R8 is 7-azabicylco[2.2.1] heptane; R9 and R9a are independently C1-C6 alkyl; R10 and R10a are hydrogen; R13 is hydrogen or NHSO2(C1-C6 alkyl); R14 and R15 are hydrogen; X is C(O); or a pharmaceutically acceptable addition salt and/or hydrate thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof.
- 2. A pharmaceutical composition which comprises an effective amount of a compound as defined in claim 1 and a pharmaceutically acceptable carrier therefor.
- 3. A method for antagonizing gonadotropin-releasing hormone in a subject in need thereof which comprises administering to said subject an effective amount of a compound as defined in claim 1 to a subject suffering from a gonadotropin-releasing hormone derived disorder.
- 4. A method according to claim 3 wherein the gonadotropin-releasing hormone derived disorder is a sex-hormone related condition.
- 5. A method according to claim 4 wherein the sex hormone related condition is selected from the group consisting of endometriosis, polycystic ovarian disease, uterine fibroids and precocious puberty.
- 6. A pharmaceutical composition which comprises an inert carrier and an effective amount of a compound which stimulates the endogenous production or release of growth hormone in combination with a compound as defined in claim 1.
- 7. A pharmaceutical composition made by combining the compound of claim 1 and a pharmaceutically acceptable carrier therefor.
- 8. A process for making a pharmaceutical composition comprising combining a compound of claim 1 and a pharmaceutically acceptable carrier.
- 9. The compound according to claim 1 of the formula wherein X-R8 is as indicated in the table below: or a pharmaceutically acceptable addition salt and/or hydrate thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof.
- 10. A method according to claim 3 wherein the gonadotropin-releasing hormone derived disorder is a sex hormone dependent cancer, benign prostatic hypertropy or myoma of the uterus.
- 11. A method according to claim 10 wherein the sex hormone dependent cancer is selected from the group consisting of prostatic cancer, uterine cancer, breast cancer and pituitary gonadotrophe adenomas.
- 12. A method for preventing pregnancy in a subject in need thereof which comprises administering an effective amount of a compound as defined in claim 1.
- 13. A method for treating lupus erythematosis in a subject in need thereof which comprises administering to said subject an effective amount of a compound as defined in claim 1.
- 14. A method for treating irritable bowel syndrome in a subject in need thereof which comprises administering to said subject an effective amount of a compound as defined in claim 1.
- 15. A method for treating premenstrual syndrome in a subject in need thereof which comprises administering to said subject an effective amount of a compound as defined in claim 1.
- 16. A method for treating hirsutism in a subject in need thereof which comprises administering to said subject an effective amount of a compound as defined in claim 1.
- 17. A method for treating short stature or a growth hormone deficiency in a subject in need thereof which comprises administering to said subject an effective amount of a compound which stimulates the endogenous production or release of growth hormone and an effective amount of a compound as defined in claim 1.
- 18. A method for treating sleep disorders in a subject in need thereof which comprises administering to said subject an effective amount of a compound as defined in claim 1.
- 19. The method of claim 18 wherein the sleep disorder is sleep apnea.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9603344 |
Feb 1996 |
GB |
|
Parent Case Info
This application claims benefit of Provisional 06/008,631, filed Dec. 14, 1995, and continuation of Ser. No. 08/760,866, filed Dec. 5, 1996, now abandoned.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/US96/19767 |
|
WO |
00 |
6/1/1998 |
6/1/1998 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO97/21707 |
6/19/1997 |
WO |
A |
US Referenced Citations (7)
Foreign Referenced Citations (6)
Number |
Date |
Country |
0 219 292 A2 |
Apr 1987 |
EP |
0 679 642 A1 |
Nov 1995 |
EP |
WO9005721 |
May 1990 |
WO |
9510513 |
Apr 1995 |
WO |
WO9528405 |
Oct 1995 |
WO |
WO9529900 |
Nov 1995 |
WO |
Non-Patent Literature Citations (2)
Entry |
J. Med. Chem., vol. 32, No. 9, pp. 2036-2038 (1989), by Biswanath De, et al. |
CA 80:108368, FR 2181559, by Boch, et al. (No 8F. in Abstract, Need the Whole Document). |
Provisional Applications (1)
|
Number |
Date |
Country |
|
60/008631 |
Dec 1995 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
08/760866 |
Dec 1996 |
US |
Child |
09/077565 |
|
US |