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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。

    ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS
    2.
    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。

    Quinoline Compounds
    3.
    发明申请
    Quinoline Compounds 审中-公开
    喹啉化合物

    公开(公告)号：US20090088441A1

    公开(公告)日：2009-04-02

    申请号：US12238982

    申请日：2008-09-26

    申请人： Leifeng Cheng ,  Michael Karle

    发明人： Leifeng Cheng ,  Michael Karle

    IPC分类号： A61K31/496 ,  C07D215/14 ,  C07D401/10 ,  A61K31/47

    CPC分类号： C07D215/18 ,  C07D215/38 ,  C07D215/54 ,  C07D401/06 ,  C07D401/12

    摘要： The present invention relates to novel compounds of the general formula (I) wherein R1, R4, R5 and X are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).

    摘要翻译： 本发明涉及通式（I）的新化合物，其中R 1，R 4，R 5和X如上定义，具有正变构GABA B受体（GBR）调节剂作用，制备所述化合物的方法及其用途， 任选地与GABAB激动剂组合，用于抑制短暂的食管下括约肌松弛，用于治疗胃食管反流疾病，以及治疗功能性胃肠道疾病和肠易激综合征（IBS）。

    Therapeutic Agents
    4.
    发明申请
    Therapeutic Agents 审中-公开
    治疗剂

    公开(公告)号：US20080319019A1

    公开(公告)日：2008-12-25

    申请号：US11793375

    申请日：2005-12-21

    申请人： Leifeng Cheng

    发明人： Leifeng Cheng

    IPC分类号： A61K31/4164 ,  A61P3/04 ,  A61P25/00 ,  C07D401/02 ,  A61K31/454 ,  C07D233/90

    CPC分类号： C07D233/84 ,  C07D233/90

    摘要： The present invention relates to certain 1,2-diarylimidazoles of formula I 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.

    摘要翻译： 本发明涉及式I的某些1,2-二芳基咪唑和制备这些化合物的方法，它们在治疗肥胖，精神和神经障碍中的用途，其治疗用途的方法和含有它们的药物组合物。

    Therapeutic Agents
    5.
    发明申请
    Therapeutic Agents 失效
    治疗剂

    公开(公告)号：US20080312269A1

    公开(公告)日：2008-12-18

    申请号：US11915643

    申请日：2006-10-05

    申请人： Leifeng Cheng

    发明人： Leifeng Cheng

    IPC分类号： A61K31/437 ,  C07D211/06 ,  A61K31/4545 ,  A61P25/00 ,  A61P1/00 ,  A61P11/00 ,  A61P3/04 ,  C07D471/02

    CPC分类号： C07D471/04 ,  C07D221/04

    摘要： The present invention relates to 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula (I) 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.

    摘要翻译： 本发明涉及式（I）的4,5,6,7-四氢吡咯并[3,2-c]吡啶-4-酮和4,5-二氢吡咯并[3,2-c]吡啶-4-酮化合物， 以及制备这些化合物的方法，它们在治疗肥胖，精神和神经障碍中的应用，其治疗用途的方法和含有它们的药物组合物。

    Therapeutic agents
    7.
    发明申请
    Therapeutic agents 审中-公开
    治疗剂

    公开(公告)号：US20070099923A1

    公开(公告)日：2007-05-03

    申请号：US10579830

    申请日：2004-11-24

    申请人： Leifeng Cheng

    发明人： Leifeng Cheng

    IPC分类号： A61K31/498 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts thereof, in which R1 and R2 independently represent phenyl, thienyl, pyridyl, C1-10alkyl, C1-10alkoxy or C3-15cycloalkyl; R3 represents a C1-15alkyl group, C3-15cycloalkyl, a phenylC1-4alkyl group, a heteroaryl group, a heteroarylC1-4alkyl group, or a group R4(CH2)n— in which R4 represents a saturated or partially unsaturated 5 to 8 membered heterocyclic group containing one or more heteroatoms selected from nitrogen, oxygen or sulphur and n is 0, 1, 2, 3 or 4; X and Y independently represent O or S; m and n independently represent 0 or 1; wherein each of R1, R2, R3 and R4 is optionally substituted by one, two or three groups represented by Z wherein Z represents a C1-6alkyl group optionally substituted by one or more fluoro, a C1-6alkoxy group optionally substituted by one or more fluoro, hydroxy, halo, trifluoromethylsulphonyl, benzyl, nitro, amino, mono or di C1-4alkylamino, mono or di C1-3alkylamido, C1-3alkylsulphonyl, C1-6alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkyl carbamoyl, sulphamoyl or acetyl 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.

    摘要翻译： 本发明涉及式（I）化合物; 其中R 1和R 2独立代表苯基，噻吩基，吡啶基，C 1-10烷基，C 1 -C 10烷基， C 1-10烷氧基或C 3-15环烷基; R 3表示C 1-15烷基，C 3-15环烷基，苯基C 1-4烷基， 烷基，杂芳基，杂芳基C 1-4烷基或基团R 4（CH 2）n， 其中R 4表示含有一个或多个选自氮，氧或硫的杂原子的饱和或部分不饱和的5至8元杂环基，n为0,1,2,3或 4; X和Y独立地表示O或S; m和n独立地表示0或1; 其中R 1，R 2，R 3和R 4中的每一个任选被一个，两个或者两个或者多个 由Z表示的三个基团，其中Z表示任选被一个或多个氟取代的C 1-6烷基，任选被一个或多个 氟，羟基，卤素，三氟甲基磺酰基，苄基，硝基，氨基，单或二C 1-4烷基氨基，单或二C 1-3烷基酰氨基， 1-3个烷基磺酰基，C 1-6烷氧基羰基，羧基，氰基，氨基甲酰基，一或二C 1-3烷基氨基甲酰基，氨磺酰基或乙酰基，以及 用于制备这些化合物，它们在治疗肥胖，精神和神经障碍中的用途，其治疗用途的方法和含有它们的药物组合物。

    THERAPEUTIC AGENTS
    8.
    发明申请
    THERAPEUTIC AGENTS 审中-公开
    治疗药剂

    公开(公告)号：US20100234439A1

    公开(公告)日：2010-09-16

    申请号：US12304052

    申请日：2007-06-18

    申请人： Leifeng Cheng

    发明人： Leifeng Cheng

    IPC分类号： A61K31/415 ,  C07D231/12 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/00 ,  A61P3/00

    CPC分类号： C07D231/14

    摘要： The present invention relates to a 1,5-diphenylpyrazole compound and its use in the treatment of obesity, psychiatric and neurological disorders, to methods for the its therapeutic use and to pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及1,5-二苯基吡唑化合物及其在治疗肥胖，精神病和神经障碍中的用途及其治疗用途的方法和含有它们的药物组合物。