Claims
- 1. A compound of the formula ##STR100## or pharmaceutically acceptable salts thereof, wherein X and Y are independently .dbd.O, .dbd.NH, (H,H) or (H,OH);
- R.sub.1 and R.sub.2, are independently --H, --OH, --Cl, --F, --OCH.sub.3, or --CH.sub.3 ;
- Z is O, S, SO, or SO.sub.2 ;
- n is 1 or 2;
- m is 0, 1, 2 or 3;
- R.sub.4 and R.sub.5 are the same or different and each independently is selected from the group consisting of H, --(CH.sub.2).sub.p OH, --(CH.sub.2).sub.q NH.sub.2, --(CH.sub.2).sub.r NHCH.sub.3, --(CH.sub.2).sub.s N (CH.sub.3).sub.2, --(CH.sub.2).sub.t OCH.sub.3, --(CH.sub.2).sub.u CO.sub.2 CH.sub.3, --CH.sub.2 CO.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CO.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CO.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CO.sub.2 tert-Bu., --CH.sub.2 CO.sub.2 tert-Bu., --CH.sub.2 CH.sub.2 CO.sub.2 t Bu., and --(CH.sub.2).sub.v CO.sub.2 H --(CH.sub.2).sub.w CONH.sub.2 ;
- R.sub.6 is --C.sub.1 -C.sub.4 alkyl;
- p, q, r, s, t, u, v and w are each independently 1 or 2;
- with the proviso that when Z is N--R.sub.3, O, ##STR101## S, or SO, R.sub.4 and R.sub.5 are both H.
- 2. A compound according to claim 1, wherein Z is N--R.sub.3.
- 3. A compound according to claim 2, wherein R.sub.3 is --(CH.sub.2).sub.n CO.sub.2 H, --(CH.sub.2).sub.2 OH, --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2, --CH.sub.2 CH.sub.2 SH, --CH.sub.2 CH.sub.2 SCH.sub.3, --CH.sub.2 CO.sub.2 CH.sub.3, --CH.sub.2 CO.sub.2 CH.sub.2 CH.sub.3, or --CH.sub.2 CN.
- 4. A compound according to claim 2, wherein R.sub.3 is --H, --OH or --CH.sub.3.
- 5. A compound according to claim 2, wherein R.sub.3 is --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2.
- 6. A compound according to claim 2, wherein X and Y are both O and R.sub.3 is --CH.sub.2 CH.sub.2 OH.
- 7. A compound according to claim 1, wherein Z is S, wherein only one of X and Y is O.
- 8. A compound according to claim 1, wherein Z is SO.
- 9. A compound according to claim 1, wherein Z is SO.sub.2.
- 10. A compound according to claim 1, wherein Z is O.
- 11. A compound according to claim 1, wherein X and Y are both O.
- 12. A compound according to claim 1, wherein R.sub.1 and R.sub.2 are both H.
- 13. A compound according to claim 1, wherein Z is SO.sub.2 and R.sub.4 and R.sub.5 are both H.
- 14. A compound according to claim 1, selected from the group consisting of ##STR102## or a pharmaceutically acceptable salt thereof.
- 15. The compound according to claim 1 ##STR103## or a pharmaceutically acceptable salt thereof.
- 16. A pharmaceutical composition comprising a therapeutically effective amount of a compound as defined in claim 1 in combination with a pharmaceutically acceptable carrier.
- 17. A method for treating a tumor wherein said tumor is treatable by a compound according to claim 1 which inhibits protein kinase C, which comprises administering an antitumor effective amount of said compound to a mammal in need thereof.
Parent Case Info
This application is a 371 of PCT/US93/08276 Sep. 9, 1993, which is a CIP of U.S. application Ser. No. 07/951,052 filed Sep. 25, 1992, now abandoned.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/US93/08276 |
9/9/1993 |
|
|
3/10/1995 |
3/10/1995 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO94/07895 |
4/14/1994 |
|
|
Foreign Referenced Citations (2)
Number |
Date |
Country |
0410389 |
Mar 1991 |
EPX |
0508792 |
Apr 1992 |
EPX |
Non-Patent Literature Citations (4)
Entry |
Liebigs Annalen Derchemie, No. 6, 1976 Weinhem pp. 1090-1102. |
Fabre et al. Biorganic letters, vol. 2, No. 4, pp. 449-452, 1992. |
5th Symposium Blackbury VA, Oct. 2, 1992. |
Weinreb et al, Heterocycles, vol. 21, No. 1, 1984 pp. 309-316, 324. |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
951052 |
Sep 1992 |
|