Claims
- 1. A compound of the Formula 1:
- 2. The compound according to claim 1, wherein R5 is a disubstituted benzene ring containing the substituents X and Y as shown below:
- 3. The compound according to claim 1, wherein R5 is a five membered ring with the structure:
- 3. The compound according to claim 1, wherein R5 is a six membered ring with the structure shown below:
- 4. The compound according to claim 1, which is selected from the group consisting of:
i) 5-(3-Nitro-phenyl)-1,3-dihydro-indol-2-one; ii) 3-methyl-5-(3-nitrophenyl)-1,3-dihydro-indol-2-one; iii) 5-(3-Methoxy-phenyl)-3,3-dimethyl-1,3-dihydro-indol-2-one; iv) 5-(3-Chloro-phenyl)-3,3-dimethyl-1,3-dihydro-indol-2-one; v) 3,3-Dimethyl-5-(3-nitro-phenyl)-1,3-dihydro-indol-2-one; vi) 5-(3-Chloro-phenyl)-3-ethyl-1,3-dihydro-indol-2-one; vii) 5-(3-Chloro-phenyl)-3,3-diethyl-1,3-dihydro-indol-2-one; viii) 5-(3-Chloro-phenyl)-3-methoxy-3-methyl-1,3-dihydro-indol-2-one; ix) 5-(3-Chloro-phenyl)-3-methoxy-3-prop-1-ynyl-1,3-dihydro-indol-2-one; and x) 5-(3-Chloro-phenyl)-1,3-dihydro-indol-2-one; or a pharmaceutically acceptable salt thereof.
- 5. The compound according to claim 1, which is selected from the group consisting of:
i) 5-(3-Chloro-4-fluoro-phenyl)-3,3-dimethyl-1,3-dihydro-indol-2-one; ii) 3-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-benzonitrile; iii) 5-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-4-methyl thiophene-2-carbonitrile; iv) 5-(3-Chloro-5-fluoro-phenyl)-3,3-dimethyl-1,3-dihydro-indol-2-one; v) 5-(3-Fluoro-5-nitro-phenyl)-3,3-dimethyl-1,3-dihydro-indol-2-one; vi) 4-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-furan-2-carbonitrile; vii) 5-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-furan-2-carbonitrile; viii) 3-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-5-fluoro-benzonitrile; ix) 2-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-2-nitro-pyrrole; x) 5-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-thiophene-2-carbonitrile; xi) 3-(3,3-Dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-2-fluoro-benzonitrile; and xii) 3,3-Dimethyl-5-(5-nitro-thiophene-2-yl)-1,3-dihydro-indol-2-one; or a pharmaceutically acceptable salt thereof.
- 6. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.
- 7. A method of inducing contraception in a mammal, the method comprising administering to a mammal in need thereof a pharmaceutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.
- 8. A method of treating or preventing benign or malignant neoplastic disease, the method comprising administering to a mammal in need thereof a pharmaceutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.
- 9. The method of claim 8, wherein the benign or malignant neoplastic disease is selected from the group consisting of uterine myometrial fibroids, endometriosis, benign prostatic hypertrophy; carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, pituitary, meningioma and other hormone-dependent tumors.
- 10. A compound of the Formula 1:
- 11. A pharmaceutical composition comprising a compound of claim 10, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.
- 12. A method of inducing contraception in a mammal, the method comprising administering to a mammal in need thereof a pharmaceutically effective amount of a compound of claim 10, or a pharmaceutically acceptable salt thereof.
- 13. A method of treating or preventing benign or malignant neoplastic disease, the method comprising administering to a mammal in need thereof a pharmaceutically effective amount of a compound of claim 10, or a pharmaceutically acceptable salt thereof.
- 14. The method of claim 12, wherein the benign or malignant neoplastic disease is selected from the group consisting of uterine myometrial fibroids, endometriosis, benign prostatic hypertrophy; carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, pituitary, meningioma and other hormone-dependent tumors.
- 15. A method of hormone replacement therapy, the method comprising administering to a mammal in need thereof a pharmaceutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.
- 16. A method of hormone replacement therapy, the method comprising administering to a mammal in need thereof a pharmaceutically effective amount of a compound of claim 10, or a pharmaceutically acceptable salt thereof.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a divisional of U.S. patent application Ser. No. 10/014,173, filed Dec. 11, 2001, which is a divisional of U.S. patent application Ser. No. 09/552,632, filed Apr. 19, 2000, now U.S. Pat. No. 6,391,807, which claims the benefit of the priority of U.S. patent application Ser. No. 60/183,058, filed May 4, 1999, now abandoned.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60183058 |
May 1999 |
US |
Divisions (2)
|
Number |
Date |
Country |
Parent |
10014173 |
Dec 2001 |
US |
Child |
10456892 |
Jun 2003 |
US |
Parent |
09405629 |
Sep 1999 |
US |
Child |
10014173 |
Dec 2001 |
US |