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    Isoxazol-3(2H)-one analogs as therapeutic agents
    1.
    发明授权
    Isoxazol-3(2H)-one analogs as therapeutic agents 有权
    异恶唑-3（2H） - 酮类似物作为治疗剂

    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。

    5, 6-diaryl-pyrazine-2-amide derivatives as CB1 antagonists
    2.
    发明授权
    5, 6-diaryl-pyrazine-2-amide derivatives as CB1 antagonists 失效

    公开(公告)号：US07342019B2

    公开(公告)日：2008-03-11

    申请号：US10499054

    申请日：2002-12-18

    申请人： Anna Ingrid Kristina Berggren ,  Stig Jonas Boström ,  Stig Thomas Elebring ,  Peter Greasley ,  Emma Terricabras ,  Johan Michael Wilstermann

    发明人： Anna Ingrid Kristina Berggren ,  Stig Jonas Boström ,  Stig Thomas Elebring ,  Peter Greasley ,  Emma Terricabras ,  Johan Michael Wilstermann

    IPC分类号： A61K31/4965 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00

    CPC分类号： C07D241/24

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substituted (amino)C1-4alkyl-group; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group —(CH2)t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R1 represents H and R2 is as defined above; or R1 and R2 together with the nitrogen atom to which they are attached represent a saturated optionally substituted 5 to 8 membered heterocyclic group as defined above; X is CO or SO2; Y is absent or represents NH optionally substitututed by a C1-3alkyl group; R3 and R4 independently represent phenyl, thienyl or pyridyl substituted by Z; Z represents a C1-3alkyl group, a C1-3alkoxy group, hydroxy, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, trifluoromethylsulphonyl, nitro, amino, mono or di C1-3alkylamino, mono or di C1-3alkylamido, C1-3alkylsulphonyl, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkyl carbamoyl, sulphamoyl and acetyl; and R5 is H, a C1-3alkyl group, a C1-3alkoxymethyl group, trifluoromethyl, a hydroxyC1-3alkyl group, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula —CONHNRaRb; with the provisos; 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.

    ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS
    5.
    发明申请
    ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS 有权
    ISOXAZOL-3（2H） - 作为治疗剂的模拟物

    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。