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Claims for Patent: RE38506

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Claims for Patent: RE38506

Title: Potent inducers of terminal differentiation and methods of use thereof
Abstract:The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition and a therapeutically acceptable amount of the compound above.
Inventor(s): Breslow; Ronald (Englewood, NJ), Marks; Paul A. (Bridgewater, CT), Rifkind; Richard A. (New York, NY), Jursic; Branko (New Orleans, LA)
Assignee: Sloan-Kettering Institute for Cancer Research (New York, NY) The Trustees of Columbia University in the City of New York (New York, NY)
Application Number:10/004,411
Patent Claims: 1. A compound having the structure: ##STR108##

wherein .[.each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when.]. R.sub.1 and R.sub.2 are the same.[., each is.]. .Iadd.and are .Iaddend.a substituted or unsubstituted .[.cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or.]. thiazoleamino group; .[.when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, or alkyloxy group;.]. and n is an integer from about 4 to about 8.

2. A compound of .[.claim 1.]. having the structure: ##STR109##

wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group; R.sub.2 is a hydroxylamino.[., hydroxyl, amino, alkylamino, or alkyloxy.]. group; .[.and.]. n is an integer from .[.about 4.]. .Iadd.5 .Iaddend.to .[.about 8.]. .Iadd.7; and R.sub.3 --N--R.sub.4 and R.sub.2 are different..Iaddend.

3. A compound of claim 2, wherein .[.R.sub.2 is a hydroxylamino, hydroxyl, amino, methylamino, or methoxy group and.]. n is 6.

4. A compound of claim 3, wherein R.sub.4 is a hydrogen atom and R.sub.3 is a substituted or unsubstituted phenyl group.

5. A compound of claim 4, wherein the phenyl group is substituted with a methyl, cyano, nitro, trifluoromethyl, amino, aminocarbonyl, metylcyano, chloro, fluoro, bromo, iodo, 2,3-difluoro, 2,4-difluoro, 2,5-difluoro, 3,4-difluoro, 3,5-difluoro, 2,6-difluoro, 1,2,3-trifluoro, 2,3,6-trifluoro, 2,4,6-trifluoro, 3,4,5-trifluoro, 2,3,5,6-tetrafluoro, 2,3,4,5,6-pentafluoro, azido, hexyl, t-butyl, phenyl, carboxyl, hydroxyl, .[.methyoxy.]. .Iadd.methoxy.Iaddend., phenyloxy, benzyloxy, phenylaminooxy, phenylaminocarbonyl, .[.methyoxycarbonyl.]. .Iadd.methoxycarbonyl.Iaddend., methylaminocarbonyl, dimethylamino, dimethylaminocarbonyl, or hydroxylaminocarbonyl group.

6. A compound of claim 3, wherein R.sub.4 is a hydrogen atom and R.sub.3 is a cyclohexyl group.

7. A compound of claim 3, wherein R.sub.4 is a hydrogen atom and R.sub.3 is a .[.methyoxy.]. .Iadd.methoxy .Iaddend.group.

8. A compound of claim 3, wherein R.sub.3 and R.sub.4 bond together to form a piperidine group..[.

9. A compound of claim 3, wherein R.sub.4 is a hydrogen atom and R.sub.3 is a hydroxyl group..].

10. A compound of claim 3, wherein R.sub.4 is a hydrogen atom and R.sub.3 is a benzyloxy group.

11. A compound of claim .[.3.]. .Iadd.2.Iaddend., wherein R.sub.4 is a hydrogen atom and R.sub.3 is a .[..delta.-pyridine.]. .Iadd..gamma.-pyridine .Iaddend.group.

12. A compound of claim .[.3.]. .Iadd.2.Iaddend., wherein R.sub.4 is a hydrogen atom and R.sub.3 is a .beta.-pyridine group.

13. A compound of claim .[.3.]. .Iadd.2.Iaddend., wherein R.sub.4 is a hydrogen atom and R.sub.3 is a .alpha.-pyridine group.

14. A compound of claim 3, wherein R.sub.3 and R.sub.4 are both methyl groups.

15. A compound of claim 3, wherein R.sub.4 is a methyl group and R.sub.3 is a phenyl group.

16. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of the compound of claim 2.

17. A pharmaceutical composition of claim 16 in combination with an antitumor agent..Iadd.

18. A compound having the structure: ##STR110##

wherein n is an integer selected from the group consisting of 5, 6, 7 and 8..Iaddend..Iadd.

19. A pharmaceutical composition comprising a therapeutically effective amount of a compound having the structure: ##STR111##

wherein n is an integer selected from the group consisting of 5, 6, 7 and 8: and a pharmaceutically acceptable carrier..Iaddend..Iadd.

20. A compound having the structure: ##STR112##

.Iaddend..Iadd.

21. A pharmaceutical composition comprising a therapeutically effective amount of a compound having the structure: ##STR113##

and a pharmaceutically acceptable carrier..Iaddend..Iadd.

22. A compound having the structure: ##STR114##

.Iaddend..Iadd.

23. A pharmaceutical composition comprising a compound having the structure: ##STR115##

and a pharmaceutically acceptable carrier..Iaddend..Iadd.

24. A compound having the structure: ##STR116##

wherein R.sub.3 is hydrogen and R.sub.4 cycloalkyl, aryl, aryloxy, arylalkloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group; R.sub.2 is a hydroxylamino group; and n is an integer selected from the group consisting of 5, 6, 7 and 8..Iaddend.
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