National Health Research Institutes

Wen-Tai Li

Chiung-Tong Chen

Der-Ren Hwang

Chu-Chung Lin

Shu-Jen Chen

Ming-Chu Hsu

Shin-Ru Shih

Kak-Shan Shia

Jyh-Haur Chern

Chung-Ming Chang

This invention relates to treating cancer or an angiogenesis-related disease using a compound of formula 1: wherein R, R, R, R, and n are defined herein.

Methods of 1H-indol-3-yl-2-oxoacetamide compounds

The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.

Imidazolamino compounds

A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1: wherein R, R, R, R, and n are as defined herein.

Use of 1H-indol-3-yl-2-oxoacetamide compounds

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 Ris independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R; or when taken together with Rand 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 R. Each Ris independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R; or when taken together with Rand 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 R. Each Ris independently C3-C10 cycloalkyl, C4-C10 cycloalkenyl, isoxazolyl, furanyl, thiophenyl, thiazolyl, imidazolyl, pyridyl, or heterocyclyl, each being optionally substituted with 1-4 independent R. Each Ris independently H, NO, halo, CN, R, OR, COR, SR, NRR, C(O)R, C(O)NRR, OC(O)R, S(O)R, S(O)NRR, NRC(O)NRR, NRC(O)R, NR(COOR), NRS(O)NRR, NRS(O)R, or S(O)OR.

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

Imidazolidinone compounds

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Taipei, Taiwan

Wen-Tai Li