Claims
- 1. An N-(tetrahydropyran-4-yloxy-alkanoyl)-staurosporin derivative of formula I ##STR7## wherein the depicted configurations are intended to illustrate only the relative stereochemistry, whereas the absolute stereochemistry corresponds to that of staurosporin, and wherein
- R.sub.1 is hydrogen, hydroxy, lower alkoxy or oxo,
- R.sub.2 is hydrogen or C.sub.1-4 alkyl and
- R.sub.3 is hydrogen or C.sub.1-4 alkyl.
- 2. A compound according to claim 1 of formula I, wherein R.sub.3 is hydrogen.
- 3. A compound according to claim 1 of formula I, wherein R.sub.1 is hydrogen, hydroxy or oxo, R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen or C.sub.1-4 alkyl.
- 4. A compound according to claim 1 of formula I, wherein R.sub.1 is hydrogen or oxo, R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen.
- 5. A compound according to claim 1 of formula I, wherein R.sub.1 is hydrogen or oxo, R.sub.2 is hydrogen or methyl and R.sub.3 is hydrogen.
- 6. A compound according to claim 1 of formula I that has the (D)-configuration at the C-R.sub.2 atom when R.sub.2 is different from R.sub.3.
- 7. N-[O -(tetrahydropyran-4-yl)-D-lactoyl]-staurosporin according to claim 1.
- 8. N-[2-(tetrahydropyran-4-yloxy)-acetyl]-staurosporin according to claim 1.
- 9. A compound according to claim 1 of the formula I selected from N-[O-(tetrahydropyran-4-yl)-D-lactoyl]-7-oxo-staurosporin, N-[O-(tetrahydropyran-4-yl)-L-lactoyl]-staurosporin, N- [O-(tetrahydropyran-4-yloxy)-acetyl]-7-oxo-staurosporin, N-[2-(tetrahydropyran-4-yloxy)-acetyl]-7-hydroxy-staurosporin, and N -[2-methyl-2-(tetrahydropyran-4-yloxy) -propionyl]- staurosporin.
- 10. A pharmaceutical composition for administration to a warm-blooded animal comprising a compound of formula I according to claim 1 in an amount of from about 1 mg to about 1500 mg/day/70 kg of warm-blooded animal in 1-3 divided doses.
- 11. A pharmaceutical composition for the treatment of protein kinase C dependent proliferative disorders comprising an amount effective in inhibiting protein kinase C of a compound of formula I according to claim 1 together with a pharmaceutical carrier.
- 12. A pharmaceutical composition for the treatment of platelet-derived growth factor kinase dependent proliferative disorders comprising an amount effective in inhibiting platelet-derived growth factor kinase of a compound of formula I according to claim 1 together with a pharmaceutical carrier.
- 13. A method of treating protein kinase C dependent proliferative disorders in a warm-blooded animal requiring such treatment which comprises administering to said animal a dose effective in inhibiting protein kinase C of a compound of formula I according to claim 1.
- 14. A method of treating platelet-derived growth factor kinase dependent proliferative disorders in a warm-blooded animal requiring such treatment which comprises administering to such animal a dose that is effective in inhibiting platelet-derived growth factor kinase of a compound of formula I according to claim 1.
Priority Claims (2)
Number |
Date |
Country |
Kind |
1406/93 |
May 1993 |
CHX |
|
335/94 |
Feb 1994 |
CHX |
|
Parent Case Info
This is a divisional of Ser. No. 234,763, filed Apr. 28, 1994, now U.S. Pat. No. 5,382,675.
US Referenced Citations (8)
Foreign Referenced Citations (4)
Number |
Date |
Country |
0383919 |
Aug 1990 |
EPX |
0532178 |
Mar 1993 |
EPX |
0575955 |
Dec 1993 |
EPX |
9109034 |
Jun 1991 |
WOX |
Divisions (1)
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Number |
Date |
Country |
Parent |
234763 |
Apr 1994 |
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