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1.发明授权N-aryl-piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors 有权N-芳基 - 哌嗪衍生物及其作为mGluR5受体的正变构调节剂的用途公开(公告)号：US08822464B2
公开(公告)日：2014-09-02
申请号：US13684606
申请日：2012-11-26
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , C07D231/12 , C07D473/34 , C07D401/12 , C07D403/12 , C07D401/14 , C07D403/14 , A61K31/53 , C07D409/14 , C07D401/06 , C07D413/14
CPC分类号： C07D403/14 , C07D231/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/14 , C07D473/34
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作mGlu5受体活性的正变构调节剂，含有它们的药物组合物，以及将其用作用于治疗和/或预防与谷氨酸功能障碍相关的神经和精神障碍的药剂的方法，例如 精神分裂症或认知衰退如痴呆或认知障碍。 A，B，Ar，R 1，R 2，R 3具有说明书中给出的含义。
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公开(公告)号：US08741892B2
公开(公告)日：2014-06-03
申请号：US13689867
申请日：2012-11-30
申请人： Matthias Grauert , Daniel Bischoff , Georg Dahmann , Raimund Kuelzer , Klaus Rudolf , Bernd Wellenzohn
发明人： Matthias Grauert , Daniel Bischoff , Georg Dahmann , Raimund Kuelzer , Klaus Rudolf , Bernd Wellenzohn
IPC分类号： A01K43/00 , C07D223/16 , C07D513/00 , C07D487/00 , C07D401/00 , C07D413/00
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作mGlu5受体活性的正变构调节剂，含有它们的药物组合物，以及将其用作用于治疗和/或预防与谷氨酸功能障碍相关的神经和精神障碍的药剂的方法，例如 精神分裂症或认知衰退如痴呆或认知障碍。 A，B，X，R 1，R 2，R 3具有说明书中给出的含义。
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公开(公告)号：US08642774B2
公开(公告)日：2014-02-04
申请号：US13692019
申请日：2012-12-03
申请人： Matthias Grauert , Daniel Bischoff , Georg Dahmann , Raimund Kuelzer , Klaus Rudolf , Bernd Wellenzohn
发明人： Matthias Grauert , Daniel Bischoff , Georg Dahmann , Raimund Kuelzer , Klaus Rudolf , Bernd Wellenzohn
IPC分类号： C07D401/00 , C07D211/00 , C07D295/00 , C07D421/00 , C07D405/00 , C07D409/00 , C07D413/00 , C07D213/02 , C07D211/60
CPC分类号： C07D513/04 , C07D249/08 , C07D401/06 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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公开(公告)号：US08846948B2
公开(公告)日：2014-09-30
申请号：US13707715
申请日：2012-12-07
IPC分类号： C07D403/02 , C07D401/00 , C07D213/72 , A01N43/50 , A61K31/415 , C07D405/14 , C07D403/12 , C07D403/14 , C07D473/34 , C07D401/14 , C07D413/14 , C07D401/12
CPC分类号： C07D403/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D473/34
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作mGlu5受体活性的正变构调节剂，含有它们的药物组合物，以及将其用作用于治疗和/或预防与谷氨酸功能障碍相关的神经和精神障碍的药剂的方法，例如 精神分裂症或认知衰退如痴呆或认知障碍。 A，B，Ar，R 1，R 2，R 3，R 3a具有说明书中给出的含义。
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公开(公告)号：US08937176B2
公开(公告)日：2015-01-20
申请号：US13709319
申请日：2012-12-10
IPC分类号： C07D403/14 , C07D401/14 , C07D403/12 , C07D233/64 , C07D401/12
CPC分类号： C07D403/14 , C07D233/64 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作mGlu5受体活性的正变构调节剂，含有它们的药物组合物，以及将其用作用于治疗和/或预防与谷氨酸功能障碍相关的神经和精神障碍的药剂的方法，例如 精神分裂症或认知衰退如痴呆或认知障碍。 A，B，Ar，R 1，R 2，R 3具有说明书中给出的含义。
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公开(公告)号：US08889677B2
公开(公告)日：2014-11-18
申请号：US13739059
申请日：2013-01-11
IPC分类号： A61K31/496 , A61K31/506 , A61K31/52 , A61K31/53 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D473/34 , C07D249/08
CPC分类号： C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作mGlu5受体活性的正变构调节剂，含有它们的药物组合物，以及将其用作用于治疗和/或预防与谷氨酸功能障碍相关的神经和精神障碍的药剂的方法，例如 精神分裂症或认知衰退如痴呆或认知障碍。 A，B，Ar，R 1，R 2，R 3具有说明书中给出的含义。
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公开(公告)号：US08796467B2
公开(公告)日：2014-08-05
申请号：US13707718
申请日：2012-12-07
申请人： Klaus Rudolf , Daniel Bischoff , Georg Dahmann , Matthias Grauert , Raimund Kuelzer , Bernd Wellenzohn
发明人： Klaus Rudolf , Daniel Bischoff , Georg Dahmann , Matthias Grauert , Raimund Kuelzer , Bernd Wellenzohn
IPC分类号： C07D403/02 , C07D401/00 , A01N43/50 , C07D498/04 , C07D403/06 , C07D401/14 , C07D513/04
CPC分类号： C07D513/04 , C07D401/14 , C07D403/06 , C07D498/04
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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8.发明授权Substituted imidazole compounds useful as positive allosteric modulators of mGlu5 receptor activity 有权用作mGlu5受体活性的正变构调节剂的取代的咪唑化合物公开(公告)号：US08716277B2
公开(公告)日：2014-05-06
申请号：US13709330
申请日：2012-12-10
申请人： Klaus Rudolf , Daniel Bischoff , Georg Dahmann , Matthias Grauert , Raimund Kuelzer , Bernd Wellenzohn
发明人： Klaus Rudolf , Daniel Bischoff , Georg Dahmann , Matthias Grauert , Raimund Kuelzer , Bernd Wellenzohn
IPC分类号： C07D513/04 , C07D498/04 , C07D413/14 , C07D403/06 , C07D413/12 , C07D233/64 , A61K31/424 , A61K31/429 , A61K31/437 , A61K31/496 , A61K31/55
CPC分类号： C07D513/04 , C07D233/64 , C07D403/06 , C07D413/12 , C07D413/14 , C07D498/04
摘要： This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作mGlu5受体活性的正变构调节剂，含有它们的药物组合物，以及将其用作用于治疗和/或预防与谷氨酸功能障碍相关的神经和精神障碍的药剂的方法，例如 精神分裂症或认知衰退如痴呆或认知障碍。 A，B，X，R 1，R 2，R 3具有说明书中给出的含义。
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公开(公告)号：US08674113B2
公开(公告)日：2014-03-18
申请号：US13314561
申请日：2011-12-08
申请人： Henning Priepke , Henri Doods , Alexander Heim-Riether , Raimund Kuelzer , Roland Pfau , Klaus Rudolf , Dirk Stenkamp
发明人： Henning Priepke , Henri Doods , Alexander Heim-Riether , Raimund Kuelzer , Roland Pfau , Klaus Rudolf , Dirk Stenkamp
IPC分类号： A61K31/4184 , A61K31/5377 , A61K31/4545 , A61K31/4995 , C07D235/30 , C07D401/12 , C07D403/12 , C07D513/04 , C07D413/12 , C07D417/12
CPC分类号： C07D235/30 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/04 , C07D491/08 , C07D491/10 , C07D498/08 , C07D513/04
摘要： This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作微粒体前列腺素E2合酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为用于治疗和/或预防炎性疾病及相关病症的药物的用途。 A，L，M，W，R 1，R 2，R 3，R 4，R 6，R 7，R 9，R a，R b具有说明书中给出的含义。
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![3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents](/abs-image/US/2014/06/24/US08759537B2/abs.jpg.150x150.jpg)
10.发明授权3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents 有权3H-咪唑并[4,5-C]吡啶-6-甲酰胺作为抗炎剂公开(公告)号：US08759537B2
公开(公告)日：2014-06-24
申请号：US13211470
申请日：2011-08-17
申请人： Henning Priepke , Henri Doods , Raimund Kuelzer , Roland Pfau , Dirk Stenkamp , Benjamin Pelcman , Robert Roenn
发明人： Henning Priepke , Henri Doods , Raimund Kuelzer , Roland Pfau , Dirk Stenkamp , Benjamin Pelcman , Robert Roenn
IPC分类号： A61K31/427 , A61K31/428 , A61K31/422 , A61K31/4439 , C07D401/12 , C07D403/12 , C07D413/12 , C07D235/30 , C07D417/12
CPC分类号： C07D235/30 , C07C211/29 , C07C211/52 , C07C233/36 , C07C233/62 , C07C271/20 , C07C331/28 , C07C2601/02 , C07D277/56 , C07D277/82 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.
摘要翻译： 本发明涉及式I化合物，其用作微粒体前列腺素E2合酶-1（mPGES-1）的抑制剂，含有它们的药物组合物及其作为用于治疗和/或预防炎性疾病及相关病症的药物的用途。 A，M，W，R 1，R 2，R 6，R 7，R 8具有说明书中给出的含义。
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