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| 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 Claim Types: see list of patent claims | Compound; Composition; |
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | Type | RLD | Patent No. | Product | Substance | Delist_Flag | Patent Expiration | Patented / Exclusive Use | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Merck | ZOLINZA | vorinostat | CAPSULE; ORAL | 021991 | Oct 6, 2006 | RX | Yes | RE38506 | Y | Y | <disabled> | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| WIPO (PCT) | 9307148 | Apr 15, 1993 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| WIPO (PCT) | 9531977 | Nov 30, 1995 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| United States | 5369108 | Nov 29, 1994 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| United States | 5700811 | Dec 23, 1997 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The preview shows a limited data set. Complete access is available with a Subscription | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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