Potent inducers of terminal differentiation and methods of use thereof

a terminal differentiation and potent technology, applied in the field of terminal differentiation potent inducers, can solve the problems of limited potent efficacy of hmba, and the inability of symmetrical dimers such as hmba and related compounds to be the best cytodifferentiating agents, and achieve the effect of inhibiting their proliferation
USRE38506E1Inactive Publication Date: 2004-04-20SLOAN KETTERING INST FOR CANCER RES +1

Patent Information

Authority / Receiving Office
US ยท United States
Current Assignee / Owner
SLOAN KETTERING INST FOR CANCER RES
Publication Date
2004-04-20
Estimated Expiration
Not applicable ยท inactive patent

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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.
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Description

BACKGROUND OF THE INVENTIONThroughout this application various publications are referenced by arabic numerals within parentheses. Full citations for these publications may be found at the end of the specification immediately preceding the claims. The disclosures of these publications in their entireties are hereby incorporated by reference into this application in order to more fully describe the state of the art to which this invention pertains.Cancer is a disorder in which a population of cells has become, in varying degrees, unresponsive to the control mechanisms which normally govern proliferation and differentiation. For many years there have been two principal strategies for chemotherapeutic treatment of cancer: a) blocking hormone-dependent tumor cell proliferation by interference with the production of peripheral action of sex hormones; and b) killing cancer cells directly by exposing them to cytotoxic substances, which injure both neoplastic and normal cell populations.Rela...

Claims

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