发明名称 6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof
摘要 The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I):; Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.
申请公布号 US8846676(B2) 申请公布日期 2014.09.30
申请号 US201213617678 申请日期 2012.09.14
申请人 Sanofi 发明人 Almario Garcia Antonio;Barrague Mathieu;Burnier Philippe;Enguehard-Gueiffier Cecile;Gao Zhongli;George Pascal;Gueiffier Alain;Li Adrien Tak;Peuch Frederic;Vaz Roy;Zhao Qiuxia
分类号 A01N43/58;A01N43/60;A61K31/50;A61K31/495;C07D487/04 主分类号 A01N43/58
代理机构 Scully, Scott, Murphy & Presser, P.C. 代理人 Scully, Scott, Murphy & Presser, P.C.
主权项 1. A process for preparing a compound of formula (I),or salt thereof, which comprises reacting a compound of formula (IIa):with an amine of formula (IIIa):in a polar solvent wherein X6 is a leaving group; R2 represents an aryl group optionally substituted with one or more substituents selected from the group consisting of halogen atoms, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylthio, C1-6 fluoroalkyl, C1-6-fluoroalkyloxy and —CN; R3 represents a hydrogen atom, C1-3 alkyl, —NR4R5, hydroxyl or C1-4 alkyloxy; A represents a group C1-7-alkylene optionally substituted with one or two groups Ra; B represents a group C1-7-alkylene optionally substituted with a group Rb; L represents either a nitrogen atom substituted with a group Rc or Rd, or a carbon atom substituted with a group Re1 and a group Rd or two groups Re2; the carbon atoms of A and B being optionally substituted with one or more groups Rf, which may be identical to or different than each other; Ra, Rb and Rc are defined such that: two groups Ra may together form a group C1-6-alkylene; Ra and Rb may together form a bond or a group C1-6-alkylene; Ra and Rc may together form a bond or a group C1-6-alkylene; Rb and Rc may together form a bond or a group C1-6-alkylene; Rd represents a group selected from the group consisting of a hydrogen atom and the groups C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl, C1-6-alkyl, C1-6-alkylthio, C1-6-alkyl, C1-6-alkyloxy, C1-6-alkyl, C1-6-fluoroalkyl, benzyl, C1-6-acyl and hydroxy-C1-6-alkyl; Re1 represents a group —NR4R5 or a cyclic monoamine optionally comprising an oxygen atom, the cyclic monoamine being optionally substituted with one or more substituents selected from the group consisting of a fluorine atom and the groups C1-6-alkyl, C1-6-alkyloxy and hydroxyl; two groups Re2 form, with the carbon atom that bears them, a cyclic monoamine optionally comprising an oxygen atom, this cyclic monoamine being optionally substituted with one or more groups Rf, which may be identical to or different than each other; Rf represents a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, hydroxy-C1-6-alkyl, C1-6-fluoroalkyl or benzyl; R4 and R5 represent, independently of each other, a hydrogen atom or a group C1-4 alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-6-alkyl; and R7 and R8 represent, independently of each other, a hydrogen atom or a group C1-6-alkyl.
地址 Paris FR