发明名称 Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing Trk
摘要 The present invention relates to a compound of following formula (I) or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.;
申请公布号 US9428510(B2) 申请公布日期 2016.08.30
申请号 US201314417532 申请日期 2013.07.29
申请人 PIERRE FABRE MEDICAMENT 发明人 Kruczynski Anna;Creancier Laurent;Kaloun El Bachir;Bedjeguelal Karim;Rabot Rémi
分类号 C07D487/04;A61K31/437;A61K31/496;A61K31/4985;A61K31/5025;A61K31/519;C07D471/04;A61K45/06 主分类号 C07D487/04
代理机构 Birch, Stewart, Kolasch & Birch, LLP 代理人 Birch, Stewart, Kolasch & Birch, LLP
主权项 1. A method for treating a cancer associated with the overexpression of at least one Trk protein comprising the administration to a person in need thereof of an effective dose of a compound of following general formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, wherein: Y1 and Y4 each represent, independently of each other, a CH group or a nitrogen atom on the condition that at least one of Y1 and Y4 represent a nitrogen atom,Y2 represents a C—X—Ar group,Y3 represents a C—W group,Ar represents an aryl or heteroaryl group optionally substituted by one or more groups selected from a halogen atom, (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)haloalkoxy, (C1-C6)halothioalkoxy, CN, NO2, OR11, SR12, NR13R14, CO2R15, CONR16R17, SO2R18, SO2NR19R20, COR21, NR22COR23, NR24SO2R25, and R26NR27R28 and/or optionally fused to a heterocycle,X represents a divalent group selected from O, S, S(O), S(O)2, NR4, S(NR4), S(O)(NR4), S(O)2(NR4), NR4S, NR4S(O), NR4S(O)2, CH2, CH2S, CH2S(O), CH2S(O)2, SCH2, S(O)CH2, S(O)2CH2, CH2CH2, CH═CH, CH2O, OCH2, NR4CH2, and CH2NR4,W represents an R5, SR5, OR5 or NR5R6 group,U represents a CH2 or NH group, one or more hydrogen atoms which may be replaced by a (C1-C6)alkyl group,V represents C(O), C(S) or CH2,n represents 0 or 1,R1 represents a hydrogen atom, or an OR7 or NR7R8 group,R2 represents a hydrogen atom, an optionally substituted heterocycle, NO2, OR9 or NR9R10,R3, R4, R11 to R25 and R27 to R28 each represent, independently of each other, a hydrogen atom or a (C1-C6)alkyl group,R5 and R6 each represent, independently of each other, a hydrogen atom or a (C1-C6)alkyl, optionally substituted aryl or optionally substituted benzyl group,R7, R8, R9 and R10 each represent, independently of each other, a hydrogen atom or an optionally substituted (C1-C6)alkyl or (C3-C12)cycloalkyl group or an optionally substituted heterocycle, andR26 represents a (C1-C6)alkyl group.
地址 Boulogne-Billancourt FR