Claims
- 1. A compound having the following structure:
- 2. The compound of claim 1 wherein Q is a direct bond and having the following structure:
- 3. The compounds of claim 1 wherein Q is —(CR8aR8b)r-Z-(CR10aR10b)s—.
- 4. The compound of claim 3 wherein r is zero.
- 5. The compound of claim 3 wherein s is zero.
- 6. The compound of claim 3 wherein Z is carbonyl.
- 7. The compound of claim 2 wherein A is CR4, B is nitrogen and having the following structure:
- 8. The compound of claim 2 wherein A is CR4, B is CR5 and having the following structure:
- 9. The compound of claim 2 wherein A is N, B is CR5 and having the following structure:
- 10. The compound of claim 2 wherein A is N, B is N and having the following structure:
- 11. The compound of claim 1 wherein R6 is arylalkyl or substituted arylalkyl.
- 12. The compound of claim 11 wherein R6 is benzyl or substituted benzyl.
- 13. The compound of claim 1 wherein R7 is alkyl.
- 14. The compound of claim 13 wherein R7 is methyl.
- 15. The compound of claim 1 wherein R5 is hydrogen.
- 16. The compound of claim 1 wherein R5 is halogen, nitro or cyano.
- 17. The compound of claim 1 wherein R4 is alkyl or substituted alkyl.
- 18. The compound of claim 1 wherein R3a and R3b are both hydrogen.
- 19. The compound of claim 1 wherein m is 1.
- 20. The compound of claim 1 wherein R2 is alkyl.
- 21. The compound of claim 1 wherein R1 is arylalkyl, substituted arylalkyl, heteroarylalkyl or substituted heteroarylalkyl.
- 22. The compound of claim 21 wherein R1 is benzyl or substituted benzyl.
- 23. The compound of claim 21 wherein R1 is —CH2(heteroaryl) or —CH2CH2(heteroaryl).
- 24. The compound of claim 1 wherein R1 and R2 taken together with the nitrogen atom to which they are attached form a heterocycle ring or substituted heterocycle ring.
- 25. The compound of claim 1 wherein the compound is:
3-(N-Benzyl-N-methyl)aminomethyl-2-(tert-butyl)-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)imidazolo[1,2-a]pyrimid-4-one; 3-(N-(2-Pyridylmethyl))aminomethyl-2-(tert-butyl)-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)imidazolo[1,2-a]pyrimid-4-one; 3-(N-(2-Pyridylmethyl)-N-methyl)aminomethyl-2-(tert-butyl)-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)imidazolo[1,2-a]pyrimid-4-one; 3-[N-Methyl-N-(2-pyridylethyl)]aminomethyl-2-(tert-butyl)-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)imidazolo[1,2-a]pyrimid-4-one; 3-[N-(2-Furanmethyl)-N-methyl]aminomethyl-2-(tert-butyl)-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)imidazolo[1,2-a]pyrimid-4-one; 3-[N-Methyl-N-(2-pyridylethyl)]aminomethyl-2-(ethoxycarbonylmethyl)-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)imidazolo [1,2-a]pyrimid-4-one; 1-(N-Benzyl-N-methyl)aminomethyl-2-(tert-butyl)-4-(2-fluorobenzyl)-6-(3-phenylpropylaminocarbonyl)pyrrolo[1,2-a]pyrimid-7-one; 1-[(N-Methyl-N-(2-pyridylethyl)]aminomethyl-2-(tert-butyl)-4-(2-fluorobenzyl)-6-(3-phenylpropylaminocarbonyl)pyrrolo[1,2-a]pyrimid-7-one; 1-[(N-Methyl-N-(2-pyridylethyl)] aminomethyl-2-(tert-butyl)-4-(2-fluorobenzyl)-5-methyl-6-(3-methoxyphenyl)pyrrolo [1,2-a]pyrimid-7-one; 3-(N-Benzyl-N-methyl)aminomethyl-2-(t-butyl)-4-(2-fluorobenzyl)-5-methyl-6-(3-methoxyphenyl)imidazolo[3,4-a]pyrimid-7-one; 1-[N-Methyl-N-(2-pyridylethyl)]aminomethyl-4-(2-fluorobenzyl)-5-methyl-6-(3-methoxyphenyl)imidazolo [3,4-a]pyrimid-7-one; 1-[N-(2-Furanmethyl)-N-methyl]aminomethyl-4-(2-fluorobenzyl)-5-methyl-6-(3-methoxyphenyl)imidazolo[3,4-a]pyrimid-7-one; 3-(N-Benzyl-N-methyl)aminomethyl-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)-1,2,4-triazolo[4,3-a]pyrimid-4-one; 3-[N-Methyl-N-(2-pyridylethyl)]aminomethyl-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)-1,2,4-triazolo[4,3-a]pyrimid-4-one; 3-[N-(2-Furanmethyl)-N-methyl]aminomethyl-6-methyl-7-(2-fluorobenzyl)-5-(3-methoxyphenyl)-1,2,4-triazolo[4,3-a]pyrimid-4-one; 1-(N-Benzyl-N-methyl)aminomethyl-2-(1-methoxycarbonyl-1-methylethyl)-7-(2-fluorobenzyl)-6-methyl-5-(3-methoxyphenyl)imidazolo [1,2-a]pyrimid-4-one; or 1-[N-(2-Pyridylethyl)-N-methyl]aminomethyl-2-(1-methoxycarbonyl-1-methylethyl)-7-(2-fluorobenzyl)-6-methyl-5-(3-methoxyphenyl)imidazolo[1,2-a]pyrimid-4-one.
- 26. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier or diluent.
- 27. A method for antagonizing gonadotropin-releasing hormone in a subject in need thereof, comprising administering to the subject an effective amount of a compound of claim 1.
- 28. A method for treating an sex-hormone related condition of a subject in need thereof, comprising administering to the subject an effective amount of the pharmaceutical composition of claim 26.
- 29. The method of claim 28 wherein the sex-hormone related condition is cancer, benign prostatic hypertrophy or myoma of the uterus.
- 30. The method of claim 29 wherein the cancer is prostatic cancer, uterine cancer, breast cancer or pituitary gonadotroph adenomas.
- 31. The method of claim 28 wherein the sex-hormone related condition is endometriosis, polycystic ovarian disease, uterine fibroids or precocious puberty.
- 32. A method for preventing pregnancy of a subject in need thereof, comprising administering an effective amount of the pharmaceutical composition of claim 26.
- 33. A method for treating lupus erythematosis, irritable bowel syndrome, premenstrual syndrome, hirsutism, short stature or sleep disorders of a subject in need thereof, comprising administering to the subject an effective amount of the pharmaceutical composition of claim 26.
CROSS REFERENCE TO RELATED APPLICATION
[0001] This application is a divisional of U.S. application Ser. No. 09/688,774 filed Oct. 16, 2000, which claims the benefit of U.S. Provisional Application No. 60/304,171 filed Oct. 15, 1999.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60304171 |
Oct 1999 |
US |
Divisions (1)
|
Number |
Date |
Country |
Parent |
09688774 |
Oct 2000 |
US |
Child |
10353806 |
Jan 2003 |
US |