Nitrogen mustard compounds and prodrugs therefor

Details Nitrogen mustard compounds and prodrugs therefor Nitrogen mustard compounds and prodrugs therefor

C - Chemistry, Metallurgy

07

C

C07C 237/36 (2006.01) A61K 31/223 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01) C07C 229/60 (2006.01)

Patent

CA 2364622

This invention pertains to nitrogen mustard compounds (Formula (II)) and prodrugs therefor (Formula (I)), methods for their preparation, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in therapy and treatment, for example, of cancer, wherein: R1 and R2 are independently -Cl, -Br, -I, - OSO2CH3, or -OSO2Ph; R1a, R2a, R1b, and R2b are independently -H, a C1-4alkyl group, or a C1-4haloalkyl group; R3 is -F, -Cl, -Br, -I, -OCHF2, -C~CH, -OCF3, -CH3, -CF3, -SF5, -SCF3, or -CF2CF3; R4 is -H or as defined for R3; R5 is -H or -F; R7 is -H, -C(CH3)3, or -CH2-CH=CH2; Z is -CH2-T-W; T is -CH2-, -O-, -S- , -(S=O)-, or -(SO2)-; W is one of: (1) -COOH; (2) -(C=O)OR8; (3) -(C=O)NR9R9; (4) -SO2NHR10; (5) -SO2OR11; (6) -PO3R11R11; (7) a tetrazol-5-yl group; (8) - CONH-SO2R12; and, (9) -M-Het.

Cette invention concerne des composés azotés de moutarde (formule (II)) et leurs promédicaments (formule (I)), leurs procédés de préparation, des compositions pharmaceutiques contenant lesdits composés, et l'utilisation de ces composés et compositions, à la fois in vitro et in vivo, en thérapie et en traitement du cancer par exemple. Dans les formules (I) et (II) : R?1¿ et R?2¿ représentent respectivement -Cl, -Br, -I, -OSO¿2?CH¿3?, ou -OSO¿2?Ph; R?1a¿, R?2a¿, R?1b¿, et R?2b¿ représentent respectivement -H, un groupe alkyle C¿1-4?, ou un groupe haloalkyle C¿1-4?; R?3¿ représente -F, -Cl, -Br, -I, -OCHF¿2?, -C~CH, -OCF¿3?, -CH¿3?, -CF¿3?, -SF¿5?, -SCF¿3?, ou -CF¿2?CF¿3?; R?4¿ représente -H ou est tel que définit pour R?3¿; R?5¿ représente -H ou -F; R?7¿ représente -H, -C(CH¿3?)¿3?, ou -CH¿2?-CH=CH¿2?; Z représente -CH¿2?-T-W; T représente -CH¿2?-, -O-, -S-, -(S=O)-, ou -(SO¿2?)-; W représente: (1) -COOH; (2) -(C=O)OR?8¿; (3) -(C=O)NR?9¿R?9¿; (4) -SO¿2?NHR?10¿; (5) -SO¿2?OR?11¿; (6) -PO¿3?R?11¿R?11¿; (7) un groupe tétrazol-5-yle; (8) -CONH-SO¿2?R?12¿; et, (9) -M-Het.

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