Antitumoral ecteinascidin derivatives

Details Antitumoral ecteinascidin derivatives Antitumoral ecteinascidin derivatives

2007-04-10

2007-04-10

Wilson, James O. (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C514S250000

Reexamination Certificate

active

10240963

ABSTRACT:
This invention relates to compounds of the formula:wherein:the substituent groups defined by R1, R2are each independently selected of H, C(═O)R′, C1–C18alkyl, C2–C18alkenyl, C2–C18alkynyl, or aryl;each of the R′ groups is independently selected from the group consisting of H; OH; NO2; NH2; SH; CN; halogen; ═O; C(═O)H; C(═O)CH3; CO2H; or C1–C18alkyl, C2–C18alkenyl, C2–C18alkynyl, or aryl, each of which, independently, may be substituted with one or more substituents selected from the group consisting of halogen, cyano, hydroxy, nitro, azido; alkanoyl, carboxamido, alkyl, alkenyl, alkynyl, aryloxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, aminoalkyl, carbocylic aryl having 6 or more carbons, and aralkyl;X2is OX1or N(X1)2wherein each X1is independently H, C(═O)R′ where R′ is as defined, C1–C18alkyl, C2–C18alkenyl, C2–C18alkynyl, aryl, alkoxy, heterocyclyl, or two X1groups together form a cyclic substituent on the nitrogen atom, or X1is SO2CH3when X2is OX1, or N(X1)2is NHCOalkylCOOH, Nilbiotin, NH(aa)ywhere aa is amino acid acyl andy is 1, 2 or 3 optionally with a amide terminal group, protected NHCOCH(NH2)CH2SH, NHCOalkenylaryl substituted with CF3, or m-methoxycarbonylbenzoylNH; wherein N(X1)2is not NH2;X3is selected of OR1where R1is as defined, CN, (═O), or H;X4is—H or C1–C18alkyl; andX5is selected of H, or R1where R1is as defined; provided that the compound is not ecteinascidin 583 or 597, which are useful for treating tumors.

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