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    • 2. 发明申请
    • ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS
    • ISOXAZOL-3(2H) - 作为治疗剂的模拟物
    • WO2010117323A8
    • 2010-11-18
    • PCT/SE2010050375
    • 2010-04-06
    • ASTRAZENECA ABBOSTROEM JONASCHENG LEIFENGFEX TOMASKARLE MICHAELPETTERSEN DANIELSCHELL PETER
    • BOSTROEM JONASCHENG LEIFENGFEX TOMASKARLE MICHAELPETTERSEN DANIELSCHELL PETER
    • C07D413/04A61K31/4523A61P7/04
    • C07D413/04
    • Formula I 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.
    • 式I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, OCOR4,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。