4-(c2-6alkoxy)-substituted chalcones as therapeutic agents

Details 4-(c2-6alkoxy)-substituted chalcones as therapeutic agents 4-(c2-6alkoxy)-substituted chalcones as therapeutic agents

C - Chemistry, Metallurgy

07

C

C07C 49/84 (2006.01) A61K 31/12 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07C 45/29 (2006.01) C07C 45/71 (2006.01) C07C 45/74 (2006.01)

Patent

CA 2462228

The present invention pertains to compounds of the following formula: (1) wherein: RALK is primary or secondary aliphatic saturated C2-6alkyl; 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 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 des composés de formule (1) dans laquelle: R¿ALK? est alkyle en C¿2-6? saturé aliphatique primaire ou secondaire; chacun des radicaux R¿B2?, R¿B3?, R¿B4?, et R¿B5? est indépendamment -H, -OH, ou OMe; chacun des radicaux R¿1? et R¿2? est indépendamment -H, alkyle en C¿1-4? éventuellement substitué, ou aryle en C¿5-20? éventuellement substitué; R¿A3? est -H, -OH, -OC(=O)R¿E?, -OS(=O)¿2?OH, ou -OP(=O)(OH)¿2?; R¿E? est H, alkyle en C¿2-6 ?éventuellement substitué, hétérocyclyle en C¿3-20? éventuellement substitué, ou aryle en C¿5-20? éventuellement substitué; ou un sel pharmaceutiquement acceptable, solvate, amide, ester, éther, forme chimiquement protégée ou promédicament correspondant. L'invention a également pour objet des compositions pharmaceutiques comprenant lesdits composés, et l'utilisation de ces composés et compositions, à la fois in vitro et in vivo, pour le diagnostique et le traitement par exemple des états pathologiques prolifératifs tels que le cancer, et les états pathologiques inflammatoires.

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