Biaryl-pyridoquinazolinone derivatives as anti-cancer agents

Details Biaryl-pyridoquinazolinone derivatives as anti-cancer agents Biaryl-pyridoquinazolinone derivatives as anti-cancer agents

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2272916

This invention provides a compound having formula (a) wherein: (A) n = 2-4; (B) R1 and R2 are the same or different and selected from the group consisting of H, (C1-C3)alkyl, -CH2CH2OH, -CH2CH2NH2, and -CH2CH2N(CH3)2 or R1 and R2 are alkyl moieties which may be taken together to form a 4- to 7-membered ring; (C) R3 is selected from H, -CH3, -CH2CH3, -CH2CH2NH2; (D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1- naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of -OR4, -NR5R6, (C1- C3)alkyl, -CF3, F, C1, Br, I, -NO2, -CN, -SO3H, -SO2NR5R6, -CO2H, -CO2R4, and phenyl; R4 is H or (C1-C4)alkyl; R5 and R6 are the same or different and are selected form H, or (C1-C4)alkyl, or R5 and R6 are alkyl groups which may be taken together to form a 4-7 membered ring; (E) W is selected from H, -OR4, - NR5R6, (C1-C3)alkyl, -CF3, F, C1, Br, I, -NO2, -CN, -SO2NR5R6, -CO2R4; or a pharmacologically acceptable salt thereof which is useful as an antineoplastic agent.

L'invention concerne les composés ayant la formule (a) et les sels de ces composés, acceptables sur le plan pharmaceutique. Dans cette formule, (A) n = 2 - 4; (B) R¿1? et R¿2? sont les mêmes ou différents et ils sont choisis dans le groupe constitué par H, (C¿1?-C¿3?)alkyle, -CH¿2?CH¿2?OH, -CH¿2?CH¿2?NH¿2? et -CH¿2?CH¿2?N(CH¿3?)¿2? ou R¿1? et R¿2? sont des groupes alkyle qui peuvent être réunis ensemble pour former un cycle à 4 - 7 éléments; (C) R¿3? est choisi parmi H, -CH¿3?, -CH¿2?CH¿3?, -CH¿2?CH¿2?NH¿2?; (D) X se trouve en position 2 ou 3 et il est choisi dans le groupe constitué par 2-naphtyle, 1-naphtyle, 1-phénanthrényle, 2-phénanthrényle, 3-phénanthrényle, 4-phénanthrényle, 9-phénanthrényle, phényle et phényle mono- ou pluri-substitué, les substituants étant choisis dans le groupe constitué par -OR¿4?, -NR¿5?R¿6?, (C¿1?-C¿3?)alkyle, -CF¿3?, F, Cl, Br, I, -NO¿2?, -CN, -SO¿3?H, -SO¿2?NR¿5?R¿6?, -CO¿2?H, -CO¿2?R¿4? et phényle; R¿4? est H ou (C¿1?-C¿4?)alkyle; R¿5? et R¿6? sont les mêmes ou différents et ils sont choisis parmi H, (C¿1?-C¿4?)alkyle ou R¿5? et R¿6? sont des groupes alkyle qui peuvent être réunis ensemble pour former un cycle à 4 - 7 éléments; (E) W est choisi parmi H, -OR¿4?, -NR¿5?R¿6?, (C¿1?-C¿3?)alkyle, -CF¿3?, F, Cl, Br, I, -NO¿2?, -CN, -SO¿2?NR¿5?R¿6?, -CO¿2?R¿4?. Ces composés sont utiles en tant qu'agents antinéoplasiques.

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