C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 323/52 (2006.01) A61K 31/10 (2006.01) A61P 35/00 (2006.01) C07C 315/02 (2006.01) C07C 315/04 (2006.01) C07C 317/10 (2006.01) C07C 317/18 (2006.01) C07C 317/44 (2006.01) C07C 319/20 (2006.01) C07F 9/12 (2006.01)
Patent
CA 2406212
Styryl benzylsulfones of formula (I) are useful as antiproliferative agents, including, for example, anticancer agents. In said formula, (a) (i) at least three of R1, R2, R3, R4 and R5 are independently selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl, and the balance of said R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl; and (ii) R6, R7, R8, R9, and R10 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl; or (b) (i) at least three of R6, R7, R8, R9, and R10 are independently selected from the group consisting of halogen, C1-C6 alkyl, C1- C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl, and the balance of said R6, R7, R8, R9, and R10 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl; and (ii) R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 lakoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) and trifluoromethyl; or a pharmaceutically acceptable salt thereof.
Cette invention concerne des styryl benzylsulfones représentés par la formule I qui sont utiles comme agents antiprolifératifs, notamment comme agents anticancéreux. Dans cette formule: (a) (i) au moins trois de R¿1?, R¿2?, R¿3?, R¿4? et R¿5? sont pris indépendamment dans le groupe composé d'halogène, C1-C6 alkyle, C1-C6 alkoxy, nitro, cyano, carboxyle, hydroxyle, phosphonato, amino, sulfamyle, acétoxy, diméthylamino (C2-C6 alkoxy) et trifluorométhyle, et le restant desdits R¿1?, R¿2?, R¿3?, R¿4? and R¿5? est pris indépendamment dans le groupe comprenant hydrogène, halogène, C1-C6 alkoxy, nitro, cyano carboxyle, hydroxyle, phosphonato, amino sulfamyle, acétoxy, diméthylamino (C2-C6) alkoxy) and trifluorométhyle; et (ii) R¿6?, R¿7?, R¿8?, R¿9?, and R¿10? sont pris indépendamment dans le groupe composé d'hydrogène, halogène, C1-C6 alkyle, C1-C6 alkoxy, nitro, cyano, carboxyle, hydroxyle, phosphonato, amino, sulfamyle, acétoxy, diméthylamino (C2-C6 alkoxy) et trifluorométhyle; ou (b) (i) au moins trois de R¿6?, R¿7?, R¿8?, R¿9?, et R¿10? Sont pris indépendamment dans le groupe composé d'halogène, C1-C6 alkyle, C1-C6 alkoxy, nitro, cyano, carboxyle, hydroxyle, phosphonato, amino, sulfamyle, acétoxy, diméthylamino (C2-C6 alkoxy) and trifluorméthyle, et le restant desdits R¿6?, R¿7?, R¿8?, R¿9?, et R¿10? est pris indépendamment dans le groupe composé d'hydrogène, halogène, C1-C6 alkyle, C1-C6 alkoxy, nitro, cyano, carboxyle, hydroxyle, phosphonato, amino sulfamyle, acétoxy, diméthylamino (C2-C6 alkoxy) and trifluorométhyle; et (ii) R¿1?, R¿2?, R¿3?, R¿4? et R¿5? Sont pris indépendamment dans le groupe composé d'hydrogène, halogène, C1-C6 alkyle, nitro, cyano, carboxyle, hydroxyle, phosphonato, amino, sulfamyle, acétoxy, diméthylamino (C2-C6 alkoxy) et trifluorométhyle. L'invention concerne également un sel pharmaceutiquement acceptable de ces composés.
Reddy E. Premkumar
Reddy M. V. Ramana
Mccarthy Tetrault Llp
Temple University - Of The Commonwealth System Of Higher Educati
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