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    • 1. 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。
    • 4. 发明专利
    • ANÁLOGOS DE ISOXAZOL-3(2H)-ONA COMO AGENTES TERAPÉUTICOS
    • CO6440580A2
    • 2012-05-15
    • CO11132448
    • 2011-10-06
    • ASTRAZENECA AB
    • BOSTROM JONASCHENG LEIFENGFEX TOMASKARLE MICHAELPETTERSEN DANIELSCHELL PETER
    • A61K31/4523A61P7/04C07D413/04
    • Un compuesto de Fórmula Io una sal farmacéuticamente aceptable de este, donde R1 y R2 son independientemente hidrógeno, deuterio, arilo, heteroarilo, alquilo C1-C8, y están opcionalmente sustituidos con uno o más sustituyentes que son independientemente R3,R3 es un arilo, heteroarilo, uno o más átomos de flúor, un alquilo C1-C6 que contiene uno o más átomos de flúor, un alquilo C1-C6 que contiene uno o más átomos de deuterio, un alquilo C1-C6 que contiene hidroxi, estando el arilo y el heteroarilo opcionalmente sustituidos con uno o más halógenos, un alcoxi fluorado, un alquilo fluorado, un sulfonilo, uno o más átomos de deuterio, un alquilo C1-C6, un alcoxi C1-C6, un nitrilo,o R3 es un alquilo C1-C6 opcionalmente sustituido con uno o más de los siguientes grupos: COOR4, OCOR4, CONR5R6, NRSCOR6, OR4;donde R4 es un alquilo C1-C10 opcionalmente sustituido con uno o más átomos de flúor, deuterio, alcoxi, carboxilato de arilo, carboxilato de alquilo;R5 y R6 se seleccionan independientemente entre hidrógeno, alquilo o pueden formar conjuntamente un anillo de carbono de 4-8 miembros;o R1 y R2 forman un anillo de carbono de 3-10 miembros que comprende opcionalmente O o N y está opcionalmente sustituido con un alquilo o arilo C1-C10, heteroarilo opcionalmente sustituido con R3.
    • 8. 发明专利
    • PYRAZOLE DERIVATIVES AS CBL MODULATORS
    • CA2615588A1
    • 2007-01-25
    • CA2615588
    • 2006-07-17
    • ASTRAZENECA AB
    • SCHELL PETERJONFORSEN MARIACHENG LEIFENG
    • C07D401/12A61P3/04A61P25/18A61P25/28C07D231/14
    • The present invention relates to compounds of formula (I) wherein R1 represents a group R5O- in which R5 represents a C3-7alkyl group substituted by one or more fluoro or R5 represents a C3-7alkylsulphonyl group which is optionally substituted by one or more fluoro; R2 represents a C1-4alkyl group, hydroxy, fluoro, chloro or cyano wherein each R2 is independently selected when n is >1; R3 represents a) cyclohexyl optionally substituted by one or more of the following: hydroxy, fluoro, amino, mono or diC1-3alkylamino, carboxy or a C1-4alkoxycarbonyl group b) piperidino substituted by one or more hydroxy c) unsubstituted piperidino but only when one of the following applies: R4 represents cyano or R1 represents 3-fluoropropylsulphonyloxy or R1 represents 3,3,3-trifluoropropoxy or R1 represents 3-fluoropropoxy or R2 is methyl d) phenyl substituted by one or more of the following: hydroxy, halo or a C1-4alkyl group e) pyridyl substituted by a C1-4alkyl group or f) a C4- 9alkyl group; R4 represents cyano or methyl; and n is 1, 2 or 3 and pharmaceutically acceptable salts thereof and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    • 9. 发明专利
    • Pyrazole derivatives as CB1 modulators
    • AU2006271499A1
    • 2007-01-25
    • AU2006271499
    • 2006-07-17
    • ASTRAZENECA AB
    • CHENG LEIFENGSCHELL PETERJONFORSEN MARIA
    • C07D401/12A61P3/04A61P25/18A61P25/28C07D231/14
    • The present invention relates to compounds of formula I wherein R 1 represents a group R 5 O- in which R 5 represents a C 3-7 alkyl group substituted by one or more fluoro or R 5 represents a C 3-7 alkylsulphonyl group which is optionally substituted by one or more fluoro; R 2 represents a C 1-4 alkyl group, hydroxy, fluoro, chloro or cyano wherein each R 2 is independently selected when n is >1; R 3 represents a) cyclohexyl optionally substituted by one or more of the following: hydroxy, fluoro, amino, mono or diC 1-3 alkylamino, carboxy or a C 1-4 alkoxycarbonyl group b) piperidino substituted by one or more hydroxy c) unsubstituted piperidino but only when one of the following applies: R 4 represents cyano or R 1 represents 3-fluoropropylsulphonyloxy or R 1 represents 3,3,3-trifluoropropoxy or R 1 represents 3-fluoropropoxy or R 2 is methyl d) phenyl substituted by one or more of the following: hydroxy, halo or a C 1-4 alkyl group e) pyridyl substituted by a C 1-4 alkyl group or f) a C 4-9 alkyl group; R 4 represents cyano or methyl; and n is 1, 2 or 3 and pharmaceutically acceptable salts thereof and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.