Nitrogen mustard compounds and prodrugs therefor

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

2005-02-08

2005-02-08

Tsang, Cecilia J. (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

C514S533000, C558S047000, C558S048000, C562S565000, C562S126000

Reexamination Certificate

active

06852755

ABSTRACT:
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: R1and R2are independently —Cl, —Br, —I, —OSO2CH3, or —OSO2Ph; R1a, R2a, R1b, and R2bare independently —H, a C1-4alkyl group, or a C1-4haloalkyl group; R3is —F, —Cl, —Br, —I, —OCHF2, —C≡CH, —OCF3, —CH3, —CF3, —SF5, —SCF3, or —CF2CF3; R4is —H or as defined for R3−, R5is —H or —F; R7is —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.

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