Substituted 2-arylbenzazole compounds and their use as...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S375000, C548S179000, C548S217000

Reexamination Certificate

active

06858633

ABSTRACT:
Substituted 2-phenylbenzazole compounds of formula (I) wherein X represents S or O and Q represents a direct bond, —CH2— or —CH═Ch—, exhibt selective antiproliferactive activity in respect of mammalian tumour cells. At least in preferred enbodiments the benzene ring of the benzazole nucleus has a halogen substituent, preferably flourine, and the 2-phenyl group has a 4′-amino substituent which may be conjugated with an amino acid to provide a water soluble amino acid amide prodrug or salt thereof.

REFERENCES:
patent: 3257204 (1966-06-01), Sus et al.
patent: 3401048 (1968-09-01), Okubo et al.
patent: 2333378 (1975-01-01), None
patent: 11060573 (1999-03-01), None
patent: WO 9506469 (1995-03-01), None
patent: WO 9626932 (1996-09-01), None
Hauser, Hermann, “2-Aminophenyl benzothiazoles”Chemical Abstracts22:9 (May 10, 1928) 1590 (Abstract); andHelv. Chim. ACTA11 (1928) 198-209 (article).
Hutchinson et al., “The regiospecific synthesis of 5- and 7-monosubstituted and 5,6-disubstituted 2-arylbenzothiazoles ”Tetrahedron Letters41 (2000) 425-428.

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