Novel potent inducers of terminal differentiation and...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 259/06 (2006.01) A61K 31/16 (2006.01) A61K 31/195 (2006.01) A61K 31/275 (2006.01) A61K 31/395 (2006.01) C07C 233/04 (2006.01) C07C 233/06 (2006.01) C07C 233/07 (2006.01) C07C 233/15 (2006.01) C07C 233/25 (2006.01) C07C 233/36 (2006.01) C07C 233/43 (2006.01) C07C 233/54 (2006.01) C07C 233/92 (2006.01) C07C 235/74 (2006.01) C07C 237/42 (2006.01) C07C 255/42 (2006.01) C07C 255/60 (2006.01) C07C 255/64 (2006.01) C07C 259/10 (2006.01) C07C 275/28 (2006.01) C07C 275/40 (2006.01) C07C 323/42 (2006.01) C07D 21

Patent

CA 2190765

The present invention provides the compound having structure (I), wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiazoleamino group; when R1 and R2 are different, R1 = R3-N-R4, wherein each of R3 and R4 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 R3 and R4 bond together to form a piperidine group and R2 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 comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.

La présente invention concerne un composé présentant la structure (I), dans laquelle: R¿1? et R¿2? sont indépendamment identiques ou différents; quand R¿1? et R¿2? sont identiques, il représentent chacun un groupe arylamino, cycloalkylamino, pyridinamino, pipéridino, 9-purine-6-amine, ou thiazolamino substitué ou non substitué; quand R¿1? et R¿2? sont différents, R¿1? représente R¿3?-N-R¿4?, où R¿3? et R¿4? sont indépendamment identiques ou différents et représentent un atome d'hydrogène, un groupe hydroxyle, un groupe alkyle, alcényle, cycloalkyle, aryle, alkyloxy, aryloxy, arylalkyloxy ou pyridine substitué ou non substitué, ramifié ou non ramifié, ou bien R¿3? et R¿4? sont liés pour former un groupe pipéridine, et R¿2? représente un groupe hydroxylamino, hydroxyle, amino, alkylamino, dialkylamino ou alkyloxy; et n représente un nombre entier compris entre environ 4 et environ 8. La présente invention concerne également un procédé permettant d'induire de façon sélective la différenciation terminale de cellules néoplasiques et d'ainsi inhiber la prolifération de telles cellules. En outre, la présente invention concerne un procédé permettant de traiter un patient présentant une tumeur caractérisée par la prolifération de cellules néoplasiques. Enfin, la présente invention concerne une composition pharmaceutique comprenant un excipient pharmaceutiquement acceptable et une dose thérapeutiquement acceptable du composé décrit ci-dessus.

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