C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/211, 260/245
C07D 253/10 (2006.01) A61K 31/53 (2006.01) C07D 403/02 (2006.01)
Patent
CA 2001903
A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. Novel compounds of a novel method for preparing the 1,2,4- benzotriazine oxides is also disclosed. Novel compounds of the formula Image wherein X is OH, alkoxy (1-4C), NHR or NRR where each R is independently an alkyl of 1-4 carbon atoms, or aryl of 1-4 carbon atoms, or where the two R groups are alkyls linked together to form a pyrrolidino or piperidino ring or linked through an oxygen to form a morpholino ring, and the R groups may be further substituted with OH, NH2, alkyl (1-4C) secondary amino, dialkyl (1-4C) tertiary amino, pyrrolidino, piperidino, alkoxy (1-4C), or halogen substitutents; n is 1; and Y1 is H and Y2 is nitro; or a pharmacologically acceptable salt thereof are also disclosed. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.
Brown Martin J.
Grange Edward W.
Lee William W.
Martinez Abelardo P.
Pollart Daniel J.
Gowling Lafleur Henderson Llp
Sri International
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