C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/675 (2006.01) C07F 9/6561 (2006.01)
Patent
CA 2168659
The present invention relates to compounds useful as tyrosine kinase inhibitors, having general formula (I) wherein one of the groups X1, X2, X3, X4 is N and the others are CH; R is a group of formula (a), (b), (c) or (d) each of R1 and R3 independently is hydrogen, amino, carboxy, cyano, -SO3R4. - SO2NHR5. (1), -COOR6, -CONH(CH2)oPh, -CONHCH2(CHOH)nCH2OH, (2), -N(CH2CH2OH)2, -NHCH2(CHOH)nCH2OH, -NHCONH2, -NHC(NH2)=NH, -NHCO(CHOH)nCH2OH, (3), -NHSO2R7, - OCH2(CHOH)nCH2OH, -OOC(CHOH)nCH2OH, -OPO(OH)2, -OCH2SO2NH2, -CH2NH2, - C(NH2)=NH, -CH2NHC(NH2)=NH, (4), -CH2OH, -CH2OOC(CHOH)nC2OH, -CH2OPO(OH)2, - PO(OH)2; R2 is H, C1-C6 alkyl, C2-C6 alkanoyl, -CH2OH, -CH2CH2CONH2, -SO2Me, - COCH2SO2NH2; R4 is H, -CH2(CHOH)nCH2OH, C1-C6 alkyl; R5 is H, C1-C6 alkyl, - CH2(CHOH)nCH2OH, -(CH2)mNMe2; R6 is C1-C6 alkyl, unsubstituted or substituted by phenyl, -CH2(CHOH)nCH2OH; R7 is Me, -C6H4Me; Z is CH2, O, NH, NCH2CH2OH; n is 0 or 1; m is 2 or 3; o is 0, 1, 2 or 3; p is 1, 2 or 3; provided that when R is (a), (b), or (c) then R1 is not H and when R is (d) then one of R1 and R3 is not H; and the pharmaceutically acceptable salts thereof.
La présente invention se rapporte à des composés utilisés comme inhibiteurs de la tyrosine kinase et ayant la formule générale (I) dans laquelle un des groupes X?1¿, X?2¿, X?3¿, X?4¿ représente n et les autres CH; R représente un groupe de la formule (a), (b), (c) ou (d), chaque R?1¿ et R?3¿ représentant indépendamment hydrogène, amino, carboxy, cyano, -SO¿3?R?4¿. -SO¿2?NHR?5¿. (1), -COOR?6¿, -CONH(CH¿2?)¿o?Ph, -CONHCH¿2?(CHOH)¿n?CH¿2?OH, (2), -N(CH¿2?CH¿2?OH)¿2?, -NHCH¿2?(CHOH)¿n?CH¿2?OH, -NHCONH¿2?, -NHC(NH¿2?)=NH, -NHCO(CHOH)¿n?CH¿2?OH, (3), -NHSO¿2?R?7¿, -OHC¿2?(CHOH)¿n?CH¿2?OH, -OOC(CHOH)¿n?CH¿2?OH, -OPO(OH)¿2?, -OCH¿2?SO¿2?NH¿2?, -CH¿2?NH¿2?, -C(NH¿2?)=NH, -CH¿2?NHC(NH¿2?)=NH, (4), -CH¿2?OH, -CH¿2?OOC(CHOH)¿n?C¿2?OH, -CH¿2?OPO(OH)¿2?, -PO(OH)¿2?; R?2¿ représente H, alkyle C¿1?-C¿6?, alcanoyle C¿2?-C¿6?, -CH¿2?OH, -CH¿2?CH¿2?CONH¿2?, -SO¿2?Me, -COCH¿2?SO¿2?NH¿2?; R?4¿ représente H, -CH¿2?(CHOH)¿n?CH¿2?OH, alkyle C¿1?-C¿6?; R?5¿ représente H, alkyle C¿1?-C¿6?, -CH¿2?(CHOH)¿n?CH¿2?OH, -(CH¿2?)¿m?NMe¿2?; R?6¿ représente alkyle C¿1?-C¿6?, non substitué ou substitué par phényle, -CH¿2?(CHOH)¿n?CH¿2?OH; R?7¿ représente Me, -C6H¿4?Me; Z représente CH¿2?, O, NH, NCH¿2?CH¿2?OH; n vaut 0 ou 1; m vaut 2 ou 3; o vaut 0, 1, 2 ou 3; p vaut 1, 2 ou 3; à condition que, lorsque R représente (a), (b) ou (c), R?1¿ ne repésente donc pas H et lorsque R représente (d), un des R?1¿ ou R?3¿ ne représente pas H; et l'invention se rapporte également aux sels pharmaceutiquement acceptables de ces composés.
Ballinari Dario
Brasca Maria Gabriella
Buzzetti Franco
Longo Antonio
Pharmacia S.p.a.
Smart & Biggar
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