公开(公告)号：US20110312934A1

公开(公告)日：2011-12-22

申请号：US13058665

申请日：2009-08-12

申请人： Antonio Almario Garcia ,  Philippe Burnier ,  Sylvain Cote-Des Combes ,  Jean-François Gibert ,  Christophe Pacaud ,  Frédéric Puech ,  Yulin Chiang ,  Larry Davis ,  Zhongli Gao ,  Qiuxia Zhao

发明人： Antonio Almario Garcia ,  Philippe Burnier ,  Sylvain Cote-Des Combes ,  Jean-François Gibert ,  Christophe Pacaud ,  Frédéric Puech ,  Yulin Chiang ,  Larry Davis ,  Zhongli Gao ,  Qiuxia Zhao

IPC分类号： A61K31/551 ,  C07D498/10 ,  C07D471/08 ,  A61P25/30 ,  A61K31/5386 ,  A61P35/00 ,  A61P25/00 ,  C07D487/04 ,  A61K31/5025

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R2 is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-4-alkyl, C1-4-alkyloxy-C-M-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl>C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-alkyl, C1-4-fluoroalkyl group; R3 is a hydrogen atom or a substituent selected from halogen atoms and the C1-3 alkyl, —NR4R5, hydroxyl or C1-4 alkyloxy groups; A is a C1-7-alkylene group optionally substituted by one or two Ra groups; B is a C1-7-alkylene group optionally substituted by one or two Rb groups; L is either a nitrogen atom optionally substituted by an Rc or Rd group or a carbon atom substituted by an Re1 group and an Rd group or by two Re2 groups; Rd is a group selected from a hydrogen atom or a 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, hydroxy-C1-6-alkyl group; Rf is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl, C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-allyl, C1-6-fluoroalkyl or benzyl group. The invention also relates to a method for preparing same and to the therapeutic application thereof.

摘要翻译： 本发明涉及通式（I）的2-烷基-6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物，其中：R2是C1-6烷基，C3 7-环烷基，C 3-7 - 环烷基-C 1-4 - 烷基，C 1-4 - 烷氧基-C1-烷基，C 3-7 - 环烷氧基-C 1-4 - 烷基，C 3-7 - 环烷基-C 1-4 - 烷氧基 C 1-4烷基，羟基-C 1-6 - 烷基，C 1-4 - 氟代烷基; R3是氢原子或选自卤素原子和C1-3烷基，-NR4R5，羟基或C1-4烷氧基的取代基; A是任选被一个或两个R a基团取代的C 1-7 - 亚烷基; B是任选被一个或两个Rb基团取代的C 1-7 - 亚烷基; L是任选被Rc或Rd基团取代的氮原子或被Re 1基团和Rd基团取代的碳原子或两个Re 2基团; Rd是选自氢原子或C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 - 环烷基-C 1-6 - 烷基，C 1-6 - 烷硫基-C 1-6 - 烷基，C 1-6 - 烷氧基-C 1-6 - 烷基，C 1-6 - 氟代烷基，羟基-C 1-6 - 烷基; R f是C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 - 环烷基-C 1-6 - 烷基，C 1-6 - 烷氧基-C 1-6 - 烷基，C 3-7 - 环烷氧基-C 1-4 - 烷基 C 3-7 - 环烷基-C 1-4 - 烷氧基-C 1-4 - 烷基，羟基-C 1-6 - 烯丙基，C 1-6 - 氟烷基或苄基。 本发明还涉及其制备方法及其治疗应用。

公开(公告)号：US20120010208A1

公开(公告)日：2012-01-12

申请号：US13128998

申请日：2009-11-30

申请人： Christophe Pacaud ,  Frederic Puech

发明人： Christophe Pacaud ,  Frederic Puech

IPC分类号： A61K31/5025 ,  A61P25/30 ,  A61P25/24 ,  A61P25/22 ,  C07D519/00 ,  A61P25/00

CPC分类号： C07D519/00 ,  C07D401/12

摘要： The invention relates to 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to the general formula (I) in which R2 represents an aryl group optionally substituted with one or more halogen atoms or C1-6-alkyl, C1-6-alkyloxy, C1-6-alkylthio, C1-6-fluoroalkyl, C1-6-fluoroalkyloxy and —CN groups or R2 represents a group chosen from C1-6-alkyl, C1-6-fluoroalkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-6-alkyl groups; A represents a C1-7-alkylene group; B represents a C1-7-alkylene group; L represents either a nitrogen atom optionally substituted with an Rc or Rd group, or a carbon atom substituted with an Re1 group and an Rd group or two Re2 groups; the carbon atoms of A and of B being optionally substituted with one or more Rf groups, which may be identical to or different from one another. Preparation process and therapeutic use.

摘要翻译： 本发明涉及对应于通式（I）的6-环氨基-3-（1H-吡咯并[2,3-b]吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物，其中R 2表示 任选被一个或多个卤素原子或C 1-6 - 烷基，C 1-6 - 烷氧基，C 1-6 - 烷硫基，C 1-6 - 氟烷基，C 1-6 - 氟烷氧基和-CN基团取代的芳基，或者R 2表示选自 C 1-6 - 烷基，C 1-6 - 氟烷基，C 3-7 - 环烷基或C 3-7 - 环烷基-C 1-6 - 烷基; A表示C 1-7 - 亚烷基; B表示C 1-7 - 亚烷基; L表示任选被Rc或Rd基团取代的氮原子或被Re 1基团和Rd基团或两个Re 2基团取代的碳原子; A和B的碳原子任选被一个或多个可以彼此相同或不同的R f基团取代。 制备过程和治疗用途。

公开(公告)号：US08546395B2

公开(公告)日：2013-10-01

申请号：US13128998

申请日：2009-11-30

申请人： Christophe Pacaud ,  Frederic Puech

发明人： Christophe Pacaud ,  Frederic Puech

IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D487/00

CPC分类号： C07D519/00 ,  C07D401/12

摘要： The invention relates to 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to the general formula (I) in which R2 represents an aryl group optionally substituted with one or more halogen atoms or C1-6-alkyl, C1-6-alkyloxy, C1-6-alkylthio, C1-6-fluoroalkyl, C1-6-fluoroalkyloxy and —CN groups or R2 represents a group chosen from C1-6-alkyl, C1-6-fluoroalkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-6-alkyl groups; A represents a C1-7-alkylene group; B represents a C1-7-alkylene group; L represents either a nitrogen atom optionally substituted with an Rc or Rd group, or a carbon atom substituted with an Re1 group and an Rd group or two Re2 groups; the carbon atoms of A and of B being optionally substituted with one or more Rf groups, which may be identical to or different from one another. Preparation process and therapeutic use.

摘要翻译： 本发明涉及对应于通式（I）的6-环氨基-3-（1H-吡咯并[2,3-b]吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物，其中R 2表示 任选被一个或多个卤素原子或C 1-6 - 烷基，C 1-6 - 烷氧基，C 1-6 - 烷硫基，C 1-6 - 氟烷基，C 1-6 - 氟烷氧基和-CN基团取代的芳基，或者R 2表示选自 C 1-6 - 烷基，C 1-6 - 氟烷基，C 3-7 - 环烷基或C 3-7 - 环烷基-C 1-6 - 烷基; A表示C 1-7 - 亚烷基; B表示C 1-7 - 亚烷基; L表示任选被Rc或Rd基团取代的氮原子或被Re 1基团和Rd基团或两个Re 2基团取代的碳原子; A和B的碳原子任选被一个或多个可以彼此相同或不同的R f基团取代。 制备过程和治疗用途。