公开(公告)号：US20130005988A1

公开(公告)日：2013-01-03

申请号：US13609553

申请日：2012-09-11

申请人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

发明人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

IPC分类号： C07D207/09 ,  C07D207/10

CPC分类号： C07D205/04 ,  C07D207/09

摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

公开(公告)号：US20120142665A1

公开(公告)日：2012-06-07

申请号：US13308588

申请日：2011-12-01

申请人： Alexander Flohr ,  Luca Gobbi ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Jens-Uwe Peters

发明人： Alexander Flohr ,  Luca Gobbi ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Jens-Uwe Peters

IPC分类号： A61K31/437 ,  A61P25/18 ,  A61K31/541 ,  A61K31/551 ,  C07D471/04 ,  A61K31/5377

CPC分类号： C07D471/04 ,  C07D519/00

摘要： The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.

摘要翻译： 本发明涉及式（I）的三唑并吡啶化合物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其生理上可接受的盐。 这些化合物抑制PDE10A，可用作药物。

公开(公告)号：US20120071506A1

公开(公告)日：2012-03-22

申请号：US13303465

申请日：2011-11-23

申请人： Guido Galley ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

发明人： Guido Galley ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

IPC分类号： A61K31/4709 ,  A61K31/4178 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D233/60 ,  C07D233/58 ,  C07D233/20 ,  A61P25/20 ,  C07D233/06 ,  C07D233/24 ,  C07D405/06 ,  C07D233/22 ,  A61P25/24 ,  A61P25/22 ,  A61P25/18 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P25/08 ,  A61P25/06 ,  A61P9/12 ,  A61P25/30 ,  A61P3/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P43/00 ,  A61P9/00 ,  A61K31/4164

CPC分类号： C07D233/56 ,  A61K31/4166 ,  A61K31/4174 ,  A61K31/4709 ,  C07D233/06 ,  C07D233/20 ,  C07D233/22 ,  C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04

摘要： The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms. The invention also relates to novel compounds of formula I, compositions containing them, and methods for their preparation.

摘要翻译： 本发明涉及一种治疗选自抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关障碍，精神病性精神分裂症，神经性疾病如帕金森病，神经变性疾病如阿尔茨海默病 ，癫痫，偏头痛，高血压，药物滥用和代谢紊乱，如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管 其包括向个体施用治疗有效量的式I化合物，其中R 1，R 2，Q，W，X，Y，m和n如说明书中所定义，以及它们的药学活性盐，外消旋混合物， 对映体，光学异构体和互变异构体。 本发明还涉及式I的新化合物，含有它们的组合物及其制备方法。

公开(公告)号：US20110294779A1

公开(公告)日：2011-12-01

申请号：US13151310

申请日：2011-06-02

申请人： DANIELA ALBERATI ,  RUBÉN ALVAREZ SÁNCHEZ ,  KONRAD BLEICHER ,  ALEXANDER FLOHR ,  KATRIN GROEBKE ZBINDEN ,  MATTHIAS KOERNER ,  BERND KUHN ,  JENS-UWE PETERS ,  MARKUS RUDOLPH

发明人： DANIELA ALBERATI ,  RUBÉN ALVAREZ SÁNCHEZ ,  KONRAD BLEICHER ,  ALEXANDER FLOHR ,  KATRIN GROEBKE ZBINDEN ,  MATTHIAS KOERNER ,  BERND KUHN ,  JENS-UWE PETERS ,  MARKUS RUDOLPH

IPC分类号： A61K31/437 ,  A61K31/5377 ,  C07D519/00 ,  A61K31/4985 ,  A61K31/553 ,  A61P25/22 ,  A61K31/541 ,  A61P25/18 ,  A61P25/28 ,  A61P25/24 ,  A61P25/30 ,  C07D471/04 ,  A61K31/496

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/553 ,  C07D487/04

摘要： The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.

公开(公告)号：US08017604B2

公开(公告)日：2011-09-13

申请号：US12886657

申请日：2010-09-21

申请人： Daniela Alberati ,  Rubén Alvarez Sánchez ,  Konrad Bleicher ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

发明人： Daniela Alberati ,  Rubén Alvarez Sánchez ,  Konrad Bleicher ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

IPC分类号： A61K31/535 ,  A61K31/44 ,  A01N43/42 ,  C07D491/02 ,  C07D498/02 ,  C07D413/00

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/553 ,  C07D487/04

摘要： The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.

摘要翻译： 本发明涉及式（I）的新咪唑并吡啶衍生物，其中R 1，R 2，R 3，R 4，R 5和A如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。 这些化合物抑制PDE10A，可用于治疗各种疾病，包括中枢神经系统疾病如阿尔茨海默病，帕金森病和精神分裂症。

公开(公告)号：US07902238B2

公开(公告)日：2011-03-08

申请号：US12028028

申请日：2008-02-08

申请人： Guido Galley ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

发明人： Guido Galley ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

IPC分类号： A61K31/42 ,  C07D263/28

CPC分类号： C07D263/28 ,  C07D413/06

摘要： The invention relates to compounds of formula wherein R1, R2, and R3 are as defined herein and to a pharmaceutically suitable acid addition salts thereof for the treatment of CNS disorders.

摘要翻译： 本发明涉及下式的化合物，其中R 1，R 2和R 3如本文所定义，及其药学上合适的酸加成盐，用于治疗CNS病症。

公开(公告)号：US08772510B2

公开(公告)日：2014-07-08

申请号：US13598848

申请日：2012-08-30

申请人： Stephan Bachmann ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

发明人： Stephan Bachmann ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

IPC分类号： C07D249/04 ,  C07D233/54 ,  C07D231/10 ,  C07D207/30

CPC分类号： C07D471/04 ,  C07D231/14 ,  C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.

摘要翻译： 本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 5，W，X，X 1，Y，Y 1，Z和Z 1如说明书和权利要求书中所定义，以及生理上可接受的盐 其中。 这些化合物抑制PDE10A，可用于治疗CNS疾病如精神分裂症，阿尔茨海默病和帕金森病。

公开(公告)号：US08703768B2

公开(公告)日：2014-04-22

申请号：US13151301

申请日：2011-06-02

申请人： Konrad Bleicher ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Felix Gruber ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Rosa Maria Rodriguez-Sarmiento

发明人： Konrad Bleicher ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Felix Gruber ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Rosa Maria Rodriguez-Sarmiento

IPC分类号： C07D239/42 ,  A01N43/54 ,  A61K31/5355 ,  C07D403/14 ,  A61K31/497 ,  A61P25/18

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.

摘要翻译： 本发明涉及式（I）的新型含氮杂芳基化合物，其中A1，A2，R1，R2，R3，R4，R5和R6如说明书和权利要求书中所定义，以及生理上可接受的盐和 的酯。 这些化合物抑制PDE10A，可用作治疗剂。

公开(公告)号：US08357712B2

公开(公告)日：2013-01-22

申请号：US13033645

申请日：2011-02-24

申请人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross

发明人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross

IPC分类号： A61K31/421 ,  C07D263/08

摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

公开(公告)号：US08263584B2

公开(公告)日：2012-09-11

申请号：US13151310

申请日：2011-06-02

申请人： Daniela Alberati ,  Ruben Alvarez Sanchez ,  Konrad Bleicher ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

发明人： Daniela Alberati ,  Ruben Alvarez Sanchez ,  Konrad Bleicher ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

IPC分类号： A61K31/437 ,  A61K31/5377 ,  A61K31/4985 ,  A61K31/553 ,  A61K31/541 ,  C07D519/00 ,  C07D471/04 ,  A61P25/22 ,  A61P25/18

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/553 ,  C07D487/04

摘要： The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.

摘要翻译： 本发明涉及式（I）的新咪唑并吡啶衍生物，其中R 1，R 2，R 3，R 4，R 5和A如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。 这些化合物抑制PDE10A，可用于治疗各种疾病，包括中枢神经系统疾病如阿尔茨海默病，帕金森病和精神分裂症。