Claims
- 1. A compound having the structural formula ##STR38## wherein X is CH.sub.3, CH.sub.3 CH.sub.2, CH.sub.3 CH.sub.2 CH.sub.2 or ClCh.sub.2 ;
- Y-Z is ##STR39## R.sub.6 is H or CH.sub.3 when Y-Z is CH.dbd.C or H when Y-Z is other than CH.dbd.C;
- R.sub.10 is H or CH.sub.3 ;
- R.sub.17.alpha. taken alone is H, C.sub.3, CH.sub.2 CH.sub.3, CH.tbd.CH.sub.2, C.tbd.CH or C.tbd.CBr;
- R.sub.17.beta. taken alone is OH, OCOCHCl.sub.2, OCOCF.sub.3, OCH.sub.3, OCH.sub.2 SCH.sub.3,
- OCH.sub.2 SOCH.sub.3, OCH.sub.2 SO.sub.2 CH.sub.3 or ##STR40## and R.sub.17.alpha. taken together with R.sub.17.beta. is OCh.sub.2 CH.sub.2 O.
- 2. A compound according to claim 1 wherein X is CH.sub.3 Y-Z is ##STR41## R.sub.6 is H, R.sub.10 is CH.sub.3, R.sub.17.alpha. is CH.sub.3 or C.tbd.CH and R.sub.17.beta. is OH.
- 3. (5.alpha.,17.alpha.)-1'-(Methylsulfonyl)-1'H-pregn-20-yno[3,2-c]pyrazol-17-ol according to claim 2.
- 4. (5.alpha.,17.beta.)-17-Methyl-1'-(methylsulfonyl)-1'H-androstano[3,2-c]pyrazol-17-ol according to claim 2.
- 5. (17.beta.)-4,17-Dimethyl-1'-(methylsulfonyl)-1'H-androst-4-eno[3,2-c]pyrazol-17-ol according to claim 2.
- 6. (17.alpha.)-4-Methyl-1'-(methylsulfonyl)-1H-pregn-4-en-20-yno[3,2-c]pyrazol-17-ol according to claim 2.
- 7. The process of preparing a compound according to claim 1 which comprises sulfonylating the corresponding compound having the structural formula ##STR42## with the corresponding compound having the structural formula
- XSO.sub.2 Q
- wherein Q is Cl, Br or OSO.sub.2 X.
- 8. The process according to claim 7 wherein X is CH.sub.3, Y-Z is ##STR43## R.sub.6 is H, R.sub.10 is CH.sub.3, R.sub.17.alpha. is CH.sub.3 or CH.tbd.CH and R.sub.17.beta. is OH.
- 9. The process of preparing a compound according to claim 1 which comprises condensing the corresponding compound having the structural formula ##STR44## with the corresponding compound having the structural formula
- XSO.sub.2 NHNH.sub.2
- wherein R' is CH.sub.3 or CH.sub.3 CH.sub.2.
- 10. The process according to claim 9 wherein X is CH.sub.3, Y-Z is ##STR45## R.sub.6 is H, R.sub.10 is CH.sub.3, R.sub.17.alpha. is CH.sub.3 or C.tbd.CH and R.sub.17.beta. is OH.
- 11. The process according to claim 10 wherein R' is CH.sub.3 CH.sub.2.
- 12. The process of preparing a compound according to claim 1 which comprises condensing the corresponding compound having the structural formula ##STR46## with the corresponding compound having the structural formula
- XSO.sub.2 NHNH.sub.2
- wherein R' is CH.sub.3, CH.sub.3 CH.sub.2 or C.sub.6 H.sub.5.
- 13. The process according to claim 12 wherein X is CH.sub.3, Y-Z is ##STR47## R.sub.6 is H, R.sub.10 is CH.sub.3, R.sub.17.alpha. is CH.sub.3 or C.tbd.CH and R.sub.17.beta. is OH.
- 14. The process according to claim 13 wherein Y-Z is ##STR48## R.sub.17.alpha. is C.tbd.CH and R' is C.sub.6 H.sub.5.
- 15. The process for effecting an antiandrogenic response in a mammal which comprises administering to the mammal an antiandrogenically effective amount of a compound according to claim 1.
- 16. The process according to claim 15 wherein X is CH.sub.3, Y-Z is ##STR49## R.sub.6 is H, R.sub.10 is CH.sub.3, R.sub.17.alpha. is CH.sub.3 or C.tbd.CH and R.sub.17.beta. is OH.
- 17. A composition which comprises an antiandrogenically effective concentration of a compound according to claim 1 and a pharmaceutically acceptable vehicle.
- 18. A composition according to claim 17 wherein X is CH.sub.3, Y-Z is ##STR50## R.sub.6 is H, R.sub.10 is CH.sub.3, R.sub.17.alpha. is CH.sub.3 or C.dbd.CH and R.sub.17.beta. is OH.
- 19. 4-Methyl-1'-(methylsulfonyl)-1'H-androst-4-eno[3,2-c]pyrazol-17-one.
CROSS-REFERENCE TO RELATED APPLICATION
This application is a continuation-in-part of our copending application Ser. No. 748,378 filed June 24, 1985, now abandoned.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
3704295 |
Clinton |
Nov 1972 |
|
4297350 |
Bahcock et al. |
Oct 1981 |
|
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
748378 |
Jun 1985 |
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