4-(1h-2-methylimidazo 4,5-c pyridinylmethyl)phenyl...

Details 4-(1h-2-methylimidazo 4,5-c pyridinylmethyl)phenyl... 4-(1h-2-methylimidazo 4,5-c pyridinylmethyl)phenyl...

A - Human Necessities

61

K

A61K 31/44 (2006.01) A61K 31/415 (2006.01)

Patent

CA 2176124

Compounds of formula (II), wherein R1 represents hydrogen, -C1-C6 alkyl, -C2- C6 alkenyl, -C2-C6 alkynyl, -COC1-C6 alkyl, -CO2C1-C6 alkyl, -(COC1-C6 alkyl)phenyl, -(CO2C1-C6 alkyl)phenyl, -(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)SC1-C6 alkyl, -(C1-C6 alkyl)CO2C1-C6 alkyl, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl or a group -D wherein D represents a group (A) wherein n is an integer from 0 to 3, and each of R3 and R4 is independently hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, halogen, -CN, -CO2H, -CO2C1-C6 alkyl, - CONH2, -CONHC1-C6 alkyl, -CONH(C1-C6 alkyl) 2, -CHO, -CH2OH, -CF3, -OC1-C6 alkyl, -SC1-C6 alkyl, -SOC1-C6 alkyl, -SO2C1-C6 alkyl, -NH2 or -NHCOMe; R2 represents hydrogen, halogen, -C1-C6 alkyl optionally substituted by one or more halogen atoms, -C2-C6 alkenyl, -C2-C6 alkynyl, -(C1-C6 alkyl)CO2C1-C6 alkyl, -(C1-C6 alkyl)SC1-C6 alkyl, -(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)N(C1-C6 alkyl)2, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl, -(C1-C6 alkyl)C3-C8 cycloalkyl, -(C1-C6 alkyl)C4-C8 cycloalkenyl, -(C1-C6 alkyl)OC3-C8 cycloalkyl,-(C1-C6 alkyl)OC4-C8 cycloalkenyl, -(C1-C6 alkyl)SC3-C8 cycloalkyl, -(C1-C6 alkyl)SC4-C8 cycloalkenyl, a side chain of a naturally occurring amino acid, a group -D as defined above or a -(C1-C6 alkyl)OD group wherein D is as defined above; or a pharmaceutically or veterinarily acceptable salt thereof, are PAF inhibitors.

L'invention se rapporte à des composés de la formule (II) ainsi qu'à leurs sels acceptables sur les plans pharmacologiques et vétérinaires, qui sont des inhibiteurs du facteur d'activation plaquettaire (PAF). Dans cette formule, R?1¿ représente hydrogène, alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?, alcynyle C¿2?-C¿6?, alkyle COC¿1?-C¿6?, alkyle CO¿2?C¿1?-C¿6?, (alkyle COC¿1?-C¿6?)phenyle, (alkyle CO¿2?C¿1?-C¿6?)phényle, (alkyle C¿1?-C¿6?)alkyle OC¿1?-C¿6?, (alkyle C¿1?-C¿6?)alkyle SC¿1?-C¿6?, (alkyle C¿1?-C¿6?)alkyle CO¿2?CO¿1?-C¿6?, cycloalkyle C¿3?-C¿8?, cycloalcényle C¿4?-C¿8? ou un groupe D dans lequel D représente un groupe de la formule (A) dans laquelle n est un nombre entier compris entre 0 et 3, et chacun des R?3¿ et R?4¿ est indépendamment hydrogène, alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?, alcynyle C¿2?-C¿6?, halogène, CN, CO¿2?H, alkyle CO¿2?C¿1?-C¿6?, CONH¿2?, alkyle CONHC¿1?-C¿6?, (alkyle C¿1?-C¿6?)¿2? CONH, CHO, CH¿2?OH, CF¿3?, alkyle OC¿1?-C¿6?, alkyle SC¿1?-C¿6?, alkyle SOC¿1?-C¿6?, alkyle SO¿2?C¿1?-C¿6?, NH¿2? ou NHCOMe; R?2¿ représente hydrogène, halogène, alkyle C¿1?-C¿6? facultativement substitué par un ou plusieurs atomes d'halogène, alcényle C¿2?-C¿6?, alcynyle C¿2?-C¿6?, (alkyle C¿1?-C¿6?)alkyle CO¿2?C¿1?-C¿6?, (alkyle C¿1?-C¿6?)alkyle SC¿1?-C¿6? (alkyle C¿1?-C¿6?)alkyle OC¿1?-C¿6?, (alkyle C¿1?-C¿6?)N(alkyle C¿1?-C¿6?)¿2?, cycloalkyle C¿3?-C¿8?, cycloalcényle C¿4?-C¿8?, (alkyle C¿1?-C¿6?)cycloalkyle C¿3?-C¿8?, (alkyle C¿1?-C¿6?)cycloalcényle C¿4?-C¿8?, (alkyle C¿1?-C¿6?)cycloalkyle OC¿3?-C¿8?, (alkyle C¿1?-C¿6?)cycloalcényle OC¿4?-C¿8?, (alkyle C¿1?-C¿6?)cycloalkyle SC¿3?-C¿8?, (alkyle C¿1?-C¿6?)cycloalcényle SC¿4?-C¿8?, une chaîne latérale d'un aminoacide survenant naturellement, un groupe D tel que défini ci-dessus ou un groupe (alkyle C¿1?-C¿6?)OD dans lequel D est tel que défini ci-dessus.

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