Method for the regioselective preparation of substituted...

Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system

Reexamination Certificate

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C560S019000, C560S045000, C558S418000

Reexamination Certificate

active

07365197

ABSTRACT:
This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.

REFERENCES:
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patent: 2002/0091273 (2002-07-01), Berger et al.
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patent: 97/13760 (1997-04-01), None
patent: 97/49688 (1997-12-01), None
patent: WO-A-98 43960 (1998-10-01), None
patent: 00/68201 (2000-11-01), None
patent: WO-A-01 47892 (2001-07-01), None
Kobayashi, et al., New General Synthesis of tert-Butyl 3-Amino-2-naphthalenecarboxylates by an Electrocyclic Reaction of o-Quinonedimethides generated from tert-Butyl (Z)-3-Amino-3-(bicycle[4.2.0]octa-1,3,5-trien-7-yl)prop-2-enoates, J. Chem. Soc., Chem. Commun., 780-81 (1992).
Rewcastle et al., “Tyrosine Kinase Inhibitors. 9. Synthesis and Evaluation of Fused Tricyclic Quinazoline Analogues as ATP Site Inhibitors of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor,” J. Med. Chem. 39:918-928 (1996).

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