Enzyme activated self-immolative n-substituted nitrogen...

Details Enzyme activated self-immolative n-substituted nitrogen... Enzyme activated self-immolative n-substituted nitrogen...

2007-06-26

2007-06-26

Barts, Samuel A (Department: 1621)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

C560S133000, C560S021000

Reexamination Certificate

active

10526173

ABSTRACT:
This invention pertains to certain enzyme (CPG2) activated self-immolative nitrogen mustard prodrugs, which are useful in enzyme prodrug therapy (EPT), such as ADEPT and GDEPT, for the treatment of proliferative conditions, such as cancer, and which have the following formula:wherein: RNis independently C1-7alkyl; X1is independently —I, —Br, or —Cl; X2is independently —I, —Br, or —Cl; the group —N(CH2CH2X1)(CH2CH2X2) is independently attached at the 2-position or at the 4-position; each RGis independently —H or an ester substituent; n is independently an integer from 0 to 4; each RP, if present, is independently a phenyl substituent; m is independently an integer from 0 to 4; each RM, if present, is independently a mustard substituent; and pharmaceutically acceptable salts, solvates, amides, and esters thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds; such compounds and compositions for use in methods of treatment of the human or animal body by therapy; the use of such compounds and compositions for the manufacture of medicaments for the treatment of proliferative conditions; and the like.

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