Indol-3-YL-2-oxoacetamide compounds and methods of use thereof

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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C514S310000, C514S313000, C514S323000, C514S363000, C514S367000, C514S370000, C514S371000, C514S372000, C514S380000, C514S397000, C514S419000, C546S143000, C546S162000, C546S201000, C548S139000, C548S159000, C548S195000, C548S212000, C548S245000, C548S246000, C548S312100, C548S454000, C548S493000

Reexamination Certificate

active

06903104

ABSTRACT:
The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula.In this formula, each R1is independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R5; or when taken together with R2and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R2is independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R5; or when taken together with R1and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R3is independently C3-C10 cycloalkyl, C4-C10 cycloalkenyl, isoxazolyl, furanyl, thiophenyl, thiazolyl, imidazolyl, pyridyl, or heterocyclyl, each being optionally substituted with 1-4 independent R5. Each R4is independently H, NO2, halo, CN, R7, OR7, CO2R7, SR7, NR7R7, C(O)R7, C(O)NR7R7, OC(O)R7, S(O)2R7, S(O)2NR7R7, NR7C(O)NR7R7, NR7C(O)R7, NR7(COOR7), NR7S(O)2NR7R7, NR7S(O)2R7, or S(O)2OR7.

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