公开(公告)号：US08211882B2

公开(公告)日：2012-07-03

申请号：US12381086

申请日：2009-03-06

申请人： Richard Delarey Wood ,  William J Welsh ,  Sean Ekins ,  Ni Ai

发明人： Richard Delarey Wood ,  William J Welsh ,  Sean Ekins ,  Ni Ai

IPC分类号： A01N43/00 ,  A61K31/33

CPC分类号： C07C235/56 ,  C07C235/64 ,  C07C255/58 ,  C07C271/02 ,  C07C271/44 ,  C07C271/56 ,  C07D207/16 ,  C07D277/46 ,  C07D277/58 ,  C07D317/34

摘要： The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds. Diseases and disorders contemplated include, inter alia, diseases and disorders of the central nervous system, the peripheral nervous system, the gastrointestinal system, the circulatory system, skin, retina, brain, heart, and lungs.

摘要翻译： 本发明公开了使用确定类型的苯甲酰胺化合物调节I组mGluR的活性的方法。 在一个实施方案中，提供调节mGluR1活性的方法。 在另一个实施方案中，提供调节mGluR5活性的方法。 在另一个实施方案中，提供了同时调节mGluR1和mGluR5的活性的方法。 本发明还提供了使用一种或多种属于所定义类型的苯甲酰胺化合物的化合物来治疗全部或部分由I组mGluR介导的疾病或病症的方法。 本发明还提供了使用一种或多种属于所定类化合物的化合物来预防全部或部分由I组mGluR介导的疾病或病症的方法。 预期的疾病和障碍尤其包括中枢神经系统，周围神经系统，胃肠系统，循环系统，皮肤，视网膜，脑，心脏和肺的疾病和病症。

公开(公告)号：US07989487B2

公开(公告)日：2011-08-02

申请号：US12307565

申请日：2007-07-06

申请人： William J. Welsh ,  Nina Ching Y. Wang ,  Ni Ai

发明人： William J. Welsh ,  Nina Ching Y. Wang ,  Ni Ai

IPC分类号： A61K31/40 ,  A61K31/12

CPC分类号： A61K31/4035 ,  A61K31/122 ,  A61K2300/00

摘要： A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C═O)(C1-7)alkyl; Ra is (C1-7)alkyl or (C═O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.

摘要翻译： 一种通过向有需要的患者施用有效量的式I，II化合物或其组合来预防，诊断或治疗由雌激素受体介导的病症的方法，其中R1，R3，R4和R5 独立地选自H，OH和ORa; R2选自H，OH和（C = O）（C 1-7）烷基; R a为（C 1-7）烷基或（C = O）（C 1-7）烷基; 或选自所述化合物的N-氧化物衍生物，前药衍生物，保护的衍生物，异构体和异构体混合物的化合物的衍生物; 或化合物或其衍生物的药学上可接受的盐或溶剂化物。 还提供了式I和II的化合物及其药物组合物。

公开(公告)号：US20090239919A1

公开(公告)日：2009-09-24

申请号：US12381086

申请日：2009-03-06

申请人： Richard Delarey Wood ,  William J. Welsh ,  Sean Ekins ,  Ni Ai

发明人： Richard Delarey Wood ,  William J. Welsh ,  Sean Ekins ,  Ni Ai

IPC分类号： A61K31/166 ,  C07C233/66 ,  C07D207/12 ,  A61K31/426 ,  A61K31/40 ,  A61P1/00 ,  A61P25/00

CPC分类号： C07C235/56 ,  C07C235/64 ,  C07C255/58 ,  C07C271/02 ,  C07C271/44 ,  C07C271/56 ,  C07D207/16 ,  C07D277/46 ,  C07D277/58 ,  C07D317/34

摘要： The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds. Diseases and disorders contemplated include, inter alia, diseases and disorders of the central nervous system, the peripheral nervous system, the gastrointestinal system, the circulatory system, skin, retina, brain, heart, and lungs.

摘要翻译： 本发明公开了使用确定类型的苯甲酰胺化合物调节I组mGluR的活性的方法。 在一个实施方案中，提供调节mGluR1活性的方法。 在另一个实施方案中，提供调节mGluR5活性的方法。 在另一个实施方案中，提供了同时调节mGluR1和mGluR5的活性的方法。 本发明还提供了使用一种或多种属于所定义类型的苯甲酰胺化合物的化合物来治疗全部或部分由I组mGluR介导的疾病或病症的方法。 本发明还提供了使用一种或多种属于所定类化合物的化合物来预防全部或部分由I组mGluR介导的疾病或病症的方法。 预期的疾病和障碍尤其包括中枢神经系统，周围神经系统，胃肠系统，循环系统，皮肤，视网膜，脑，心脏和肺的疾病和病症。

公开(公告)号：US08455537B2

公开(公告)日：2013-06-04

申请号：US13165431

申请日：2011-06-21

申请人： William J. Welsh ,  Ching Y. Wang ,  Ni Ai

发明人： William J. Welsh ,  Ching Y. Wang ,  Ni Ai

IPC分类号： A61K31/40 ,  A61K31/12 ,  C07C253/00 ,  C07D209/48

CPC分类号： A61K31/4035 ,  A61K31/122 ,  A61K2300/00

摘要： A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C═O) (C1-7)alkyl; Ra is (C1-7)alkyl or (C═O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.

摘要翻译： 一种通过向有需要的患者施用有效量的式I，II化合物或其组合来预防，诊断或治疗由雌激素受体介导的病症的方法，其中R1，R3，R4和R5 独立地选自H，OH和ORa; R 2选自H，OH和（C = O）（C 1-7）烷基; R a为（C 1-7）烷基或（C = O）（C 1-7）烷基; 或选自所述化合物的N-氧化物衍生物，前药衍生物，保护的衍生物，异构体和异构体混合物的化合物的衍生物; 或化合物或其衍生物的药学上可接受的盐或溶剂化物。 还提供了式I和II的化合物及其药物组合物。

公开(公告)号：US20110319465A1

公开(公告)日：2011-12-29

申请号：US13165431

申请日：2011-06-21

申请人： William Welsh ,  Ching Y. Wang ,  Ni Ai

发明人： William Welsh ,  Ching Y. Wang ,  Ni Ai

IPC分类号： A61K31/4035 ,  C07D209/48 ,  A61K31/122 ,  A61P19/10 ,  A61P9/10 ,  G01N33/566 ,  A61P43/00 ,  A61P13/08 ,  A61P7/00 ,  A61P15/00 ,  A61P17/00 ,  A61P25/28 ,  C07C49/753 ,  A61P35/00

CPC分类号： A61K31/4035 ,  A61K31/122 ,  A61K2300/00

摘要： A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C═O) (C1-7)alkyl; Ra is (C1-7)alkyl or (C═O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.

摘要翻译： 一种通过向有需要的患者施用有效量的式I，II化合物或其组合来预防，诊断或治疗由雌激素受体介导的病症的方法，其中R1，R3，R4和R5 独立地选自H，OH和ORa; R2选自H，OH和（C = O）（C 1-7）烷基; R a为（C 1-7）烷基或（C = O）（C 1-7）烷基; 或选自所述化合物的N-氧化物衍生物，前药衍生物，保护的衍生物，异构体和异构体混合物的化合物的衍生物; 或化合物或其衍生物的药学上可接受的盐或溶剂化物。 还提供了式I和II的化合物及其药物组合物。

公开(公告)号：US20100152271A1

公开(公告)日：2010-06-17

申请号：US12307565

申请日：2007-07-06

申请人： William J. Welsh ,  Nina Ching Y. Wang ,  Ni Ai

发明人： William J. Welsh ,  Nina Ching Y. Wang ,  Ni Ai

IPC分类号： A61K31/4035 ,  A61K31/122 ,  A61P19/10 ,  A61P9/10 ,  A61P35/00 ,  A61P25/28 ,  A61P3/00 ,  C07C49/175 ,  C07D209/48 ,  G01N33/53

CPC分类号： A61K31/4035 ,  A61K31/122 ,  A61K2300/00

摘要： A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C═O)(C1-7)alkyl; Ra is (C1-7)alkyl or (C═O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.

摘要翻译： 一种通过向有需要的患者施用有效量的式I，II化合物或其组合来预防，诊断或治疗由雌激素受体介导的病症的方法，其中R1，R3，R4和R5 独立地选自H，OH和ORa; R2选自H，OH和（C = O）（C 1-7）烷基; R a为（C 1-7）烷基或（C = O）（C 1-7）烷基; 或选自所述化合物的N-氧化物衍生物，前药衍生物，保护的衍生物，异构体和异构体混合物的化合物的衍生物; 或化合物或其衍生物的药学上可接受的盐或溶剂化物。 还提供式I和II的化合物及其药物组合物。