3,4-methylenedioxy-substituted chalcones as therapeutic agents

Details 3,4-methylenedioxy-substituted chalcones as therapeutic agents 3,4-methylenedioxy-substituted chalcones as therapeutic agents

C - Chemistry, Metallurgy

07

D

C07D 317/54 (2006.01) A61K 31/357 (2006.01) A61K 31/36 (2006.01) A61K 47/48 (2006.01) A61P 11/06 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 35/00 (2006.01) C07C 43/205 (2006.01) C07C 43/215 (2006.01) C07F 9/655 (2006.01) C12Q 1/26 (2006.01) G01N 33/574 (2006.01)

Patent

CA 2462276

The present invention pertains to the use of a compound for the manufacture of a medicament for use in the treatment of a proliferative condition, wherein the compounds have the following formula (1): wherein: each of RB2, RB3, RB4, and RB5 is independently -H, -OH, or -OMe; each of R1 and R2 is independently: -H, optionally substituted C1-4alkyl, or optionally substituted C5-20aryl; RA3 is -H, -OH, -OC(=O)RE, -OS(=O)2OH, or -OP(=O)(OH)2; RE is: -H, optionally substituted C1-6alkyl, optionally substituted C3-20heterocyclyl, or optionally substituted C5-20aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

La présente invention concerne l'utilisation d'un composé pour la fabrication d'un médicament destiné au traitement d'un état prolifératif, ou un sel pharmaceutiquement acceptable, un solvate, un amide, un ester, un éther, une forme chimiquement protégée ou un promédicament de ce composé, ledit composé est représenté par la formule (I) dans laquelle : R<SP>B2</SP>, R<SP>B3</SP>, R<SP>B4</SP> et R<SP>B5</SP> sont chacun indépendamment -H, -OH, ou OMe; R?1¿ et R?2¿ sont chacun indépendamment -H, alkyleC¿1-4? éventuellement substitué ou aryleC¿5-20? éventuellement substitué ; R<SP>A3</SP> représente -H, -OH, -OC(=O)R<SP>E</SP>, -OS(=O)¿2?OH ou -OP(=O)(OH)¿2? ; R<SP>E</SP> représente H, alkyleC¿1-6? éventuellement substitué, hétérocyclyleC¿3-20? éventuellement substitué ou aryleC¿5-20? éventuellement substitué . Cette invention concerne également de tels composés, des compositions pharmaceutiques renfermant ces composés et l'utilisation de ces composés et de ces compositions, aussi bien in vitro qu'in vivo, pour le diagnostic et le traitement, notamment, d'états prolifératifs tels que le cancer et d'états inflammatoires.

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