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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。
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公开(公告)号：US08623866B2
公开(公告)日：2014-01-07
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
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.
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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。
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公开(公告)号：US08470820B2
公开(公告)日：2013-06-25
申请号：US13005572
申请日：2011-01-13
申请人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Eric Vieira
发明人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Eric Vieira
IPC分类号： A61K31/535 , A61K31/4965 , C07D239/42 , C07D403/14 , C07D413/12 , C07D239/02
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y 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 medicaments.
摘要翻译： 本发明涉及式（I）的新型含氮杂芳基衍生物，其中R1，R2，R3，R4，R5，A1，A2和Y如说明书和权利要求书中所定义，以及生理上可接受的盐 及其酯。 这些化合物抑制PDE10A，可用作药物。
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公开(公告)号：US20110306589A1
公开(公告)日：2011-12-15
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： A61K31/506 , C07D403/14 , C07D413/14 , A61K31/5377 , C07D491/107 , C07D417/14 , C07D403/12 , C07D405/14 , C07D409/14 , A61P25/00 , A61P25/22 , A61P25/18 , A61P25/30 , A61P25/16 , A61P25/14 , A61P25/28 , A61P29/00 , C07D401/14
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。
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公开(公告)号：US20110183979A1
公开(公告)日：2011-07-28
申请号：US13005572
申请日：2011-01-13
申请人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Eric Vieira
发明人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Eric Vieira
IPC分类号： A61K31/506 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/497 , A61P25/18 , A61P25/22 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/24 , A61P7/00 , A61P35/00 , A61P3/10
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y 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 medicaments.
摘要翻译： 本发明涉及式（I）的新型含氮杂芳基衍生物，其中R1，R2，R3，R4，R5，A1，A2和Y如说明书和权利要求书中所定义，以及生理上可接受的盐 及其酯。 这些化合物抑制PDE10A，并可用作药物。
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公开(公告)号：US08349824B2
公开(公告)日：2013-01-08
申请号：US13308588
申请日：2011-12-01
IPC分类号： A61K31/397 , A61K31/55 , A61K31/541 , A61K31/5355 , A61K31/437 , C07D243/00 , C07D279/10 , C07D413/14 , C07D471/04
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。
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公开(公告)号：US20120142665A1
公开(公告)日：2012-06-07
申请号：US13308588
申请日：2011-12-01
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。
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公开(公告)号：US07989657B2
公开(公告)日：2011-08-02
申请号：US12477525
申请日：2009-06-03
申请人： Henrietta Dehmlow , Uwe Grether , Nicole A Kratochwil , Robert Narquizian , Constantinos Panousis , Jens-Uwe Peters
发明人： Henrietta Dehmlow , Uwe Grether , Nicole A Kratochwil , Robert Narquizian , Constantinos Panousis , Jens-Uwe Peters
IPC分类号： C07C235/00 , C07C229/56
CPC分类号： C07D215/26 , C07C235/56 , C07C255/54 , C07C317/22 , C07D213/643 , C07D213/65 , C07D249/08
摘要： The invention is concerned with novel anthranilic acid derivatives of formula (I) wherein R1 to R14, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.
摘要翻译： 本发明涉及式（I）的新型邻氨基苯甲酸衍生物，其中R 1至R 14，m和n如说明书和权利要求书中所定义，以及其生理学上可接受的盐和酯。 这些化合物是HM74A激动剂，可用作药物。
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公开(公告)号：US20110178055A1
公开(公告)日：2011-07-21
申请号：US13076891
申请日：2011-03-31
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： A61K31/4427 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/551 , A61K31/5377 , A61P25/18
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译： 本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。 特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。 本发明还提供具有式I的新化合物和制备本发明化合物的方法。
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