Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2007-06-26
2007-06-26
McKane, Joseph K. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S427000
Reexamination Certificate
active
10514893
ABSTRACT:
The invention provides processes of preparing 3-substituted 1-(chloromethyl)- 1,2-dihydro-3H-[ring fused indol-5-yl(amine-derived)] compounds of formula (I) and its analogues, or a physiologically functional derivative thereof, (I), wherein A and B together may represent a fused optionally substituted benezene, naphthalene, pyridine, furan or a pyrrole ring, where the optional substituents are represented by Y; X is halogen or OSO2R, and W is selected from NO2, NHOH, N(R3)2NHR3, NHCO2R3, N(phthaloyl) or NH2, or W is further selected from the group (a), wherein J is selected from OH or H, and P is a group which is a substrate suitable for a nitroreductase or carboxypeptidase enzyme. The invention is also directed to the use of compounds of formula (I) prepared by the processes of the invention as cytotoxins for cancer therapy and as prodrugs for gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzyme-prodrug theraphy (ADEPT).
REFERENCES:
Atwell, G., et al; “Synthesis and Cytotoxicity of 5-Amino-1-(chloromethyl)-3-[(5,6,7-trimethoxyindol-2-yl)carbonyl]-1,2-dihydro-3H-benz[e]indole (Amino-seco-CNI-TMI) and Related 5-Alkylamino Analogues: New DNA Minor Groove Alkylating Agents”;J. Org. Chem.; vol. 63, pp. 9414-9420 (1998).
Tercel, M., et al; “Synthesis and Cytotoxicity of Amino-seco-DSA: An Amino Analogue of the DNA Alkylating Agent Duocarmycin SA”;J. Org. Chem.; vol. 64; pp. 5946-5953 (1999).
Atwell Graham John
Denny William Alexander
Jeffrey Scott Charles
Yang Shanjin
Auckland Uniservices Limited
McKane Joseph K.
Nixon & Vanderhye
Nolan Jason M.
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