公开(公告)号：US08415378B2

公开(公告)日：2013-04-09

申请号：US12755010

申请日：2010-04-06

申请人： Jonas Boström ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

发明人： Jonas Boström ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

IPC分类号： A01N43/40 ,  A01N43/80 ,  A61K31/445 ,  A61K31/42 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00 ,  C07D261/00 ,  C07D307/02 ,  C07D315/00 ,  C07D407/00

CPC分类号： C07D413/04

摘要： or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.

摘要翻译： 或其药学上合适的盐，其中R 1和R 2独立地是氢，氘，芳基，杂芳基，任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基，R 3是芳基，杂芳基，氟（ 含有一个或多个氟的C 1 -C 6烷基，含有一个或多个氘的C 1 -C 6烷基，含羟基的C 1 -C 6烷基，任选被一个或多个卤素取代的芳基和杂芳基，氟化烷氧基， 氟化烷基，磺酰基，一个或多个氘，C 1-6烷基，C 1-6烷氧基，腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基：COOR 4，OCOR 4， CONR5R6，NR5COR6，OR4; 其中，R4为任选被一个或多个氟，氘，烷氧基，芳基羧酸酯，羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢，烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环，任选被R 3取代的杂芳基。

公开(公告)号：US20100261755A1

公开(公告)日：2010-10-14

申请号：US12755010

申请日：2010-04-06

申请人： Jonas BOSTRÖM ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

发明人： Jonas BOSTRÖM ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

IPC分类号： A61K31/454 ,  C07D401/04 ,  A61P1/16 ,  A61P9/10 ,  A61P7/04

CPC分类号： C07D413/04

摘要： or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.

摘要翻译： 或其药学上合适的盐，其中R 1和R 2独立地是氢，氘，芳基，杂芳基，任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基，R 3是芳基，杂芳基，氟（ 含有一个或多个氟的C 1 -C 6烷基，含有一个或多个氘的C 1 -C 6烷基，含羟基的C 1 -C 6烷基，任选被一个或多个卤素取代的芳基和杂芳基，氟化烷氧基， 氟化烷基，磺酰基，一个或多个氘，C 1-6烷基，C 1-6烷氧基，腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基：COOR 4，OCOR 4， CONR5R6，NR5COR6，OR4; 其中，R4为任选被一个或多个氟，氘，烷氧基，芳基羧酸酯，羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢，烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环，任选被R 3取代的杂芳基。