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公开(公告)号：US20100152193A1
公开(公告)日：2010-06-17
申请号：US12626982
申请日：2009-11-30
申请人： Daniela Alberati , Luca Gobbi , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Mark Rogers-Evans , Markus Rudolph
发明人： Daniela Alberati , Luca Gobbi , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Mark Rogers-Evans , Markus Rudolph
IPC分类号： A61K31/501 , C07D403/04 , A61P25/18
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14
摘要： The present invention is concerned with novel pyridazinones 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 and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of CNS disorders.
摘要翻译： 本发明涉及式（I）的新的哒嗪酮，其中R1，R2，R3和R4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CNS疾病。
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公开(公告)号：US09187455B2
公开(公告)日：2015-11-17
申请号：US12705988
申请日：2010-02-16
申请人： Daniela Alberati , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez Sarmiento , Mark Rogers-Evans , Markus Rudolph
发明人： Daniela Alberati , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez Sarmiento , Mark Rogers-Evans , Markus Rudolph
IPC分类号： A61K31/501 , C07D237/04 , C07D403/14
CPC分类号： C07D403/14
摘要： The present invention is concerned with novel pyridazinone derivatives 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 and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
摘要翻译： 本发明涉及式（I）的新的哒嗪酮衍生物，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和酯。 这些化合物抑制PDE10A，可用作药物。
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公开(公告)号：US08178538B2
公开(公告)日：2012-05-15
申请号：US12626982
申请日：2009-11-30
申请人： Daniela Alberati , Luca Gobbi , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Mark Rogers-Evans , Markus Rudolph
发明人： Daniela Alberati , Luca Gobbi , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Mark Rogers-Evans , Markus Rudolph
IPC分类号： A61K31/501 , C07D403/04
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14
摘要： The present invention is concerned with novel pyridazinones 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 and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of CNS disorders.
摘要翻译： 本发明涉及式（I）的新的哒嗪酮，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和酯。 这些化合物抑制PDE10A，可用于治疗CNS疾病。
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公开(公告)号：US20100216793A1
公开(公告)日：2010-08-26
申请号：US12705988
申请日：2010-02-16
申请人： Daniela Alberati , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rose Maria Rodriguez Sarmiento , Mark Rogers-Evans , Markus Rudolph
发明人： Daniela Alberati , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rose Maria Rodriguez Sarmiento , Mark Rogers-Evans , Markus Rudolph
IPC分类号： A61K31/501 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/5377
CPC分类号： C07D403/14
摘要： The present invention is concerned with novel pyridazinone derivatives 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 and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
摘要翻译： 本发明涉及式（I）的新的哒嗪酮衍生物，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和酯。 这些化合物抑制PDE10A，可用作药物。
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公开(公告)号：US20110071128A1
公开(公告)日：2011-03-24
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： A61K31/553 , C07D471/04 , C07D487/04 , C07D491/107 , A61K31/437 , A61K31/5377 , A61K31/5025 , A61K31/496 , 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。
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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。
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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。
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公开(公告)号：US20120035156A1
公开(公告)日：2012-02-09
申请号：US13195045
申请日：2011-08-01
IPC分类号： A61K31/496 , A61P25/18 , A61K31/554 , A61K31/55 , A61K31/551
CPC分类号： A61K31/495 , A61K31/497 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a pharmaceutical combination of a glycine transporter inhibitor (GlyT1) and an atypical antipsychotic drug which may be used for the treatment of positive and negative symptoms of schizophrenia.
摘要翻译： 本发明涉及可用于治疗精神分裂症的阳性和阴性症状的甘氨酸转运蛋白抑制剂（GlyT1）和非典型抗精神病药物的药物组合。
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公开(公告)号：US20100111862A1
公开(公告)日：2010-05-06
申请号：US12607111
申请日：2009-10-28
IPC分类号： A61K51/04 , C07D209/02 , A61P25/18
CPC分类号： C07D405/10
摘要： The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. whereinR1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; andR2 is a radiolabelled group CH3, wherein the radionuclide is 3H or 11C. The radiolabelled compounds of formula I may be used as PET (Positron Emission Tomography) radiotracer for the labelling and diagnostic molecular imaging of the glycine 1 transporter functionality.
摘要翻译： 本发明涉及用于甘氨酸1转运蛋白（GlyT1）的式I的新型放射性标记抑制剂，其可用于甘氨酸1转运蛋白官能度的标记和诊断成像。 其中R1是异丙氧基或2,2,2-三氟-1-甲基 - 乙氧基; 并且R 2是放射性标记的基团CH 3，其中放射性核素是3H或11C。 放射性标记的式I化合物可用作PET（正电子发射断层扫描）放射性示踪剂，用于甘氨酸1转运蛋白功能的标记和诊断分子成像。
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公开(公告)号：US08153679B2
公开(公告)日：2012-04-10
申请号：US12607111
申请日：2009-10-28
申请人： Daniela Alberati , Edilio Maurizio Borroni , Thomas Hartung , Roger David Norcross , Emmanuel Pinard
发明人： Daniela Alberati , Edilio Maurizio Borroni , Thomas Hartung , Roger David Norcross , Emmanuel Pinard
IPC分类号： A61K31/4035 , C07D209/44 , C07D405/04
CPC分类号： C07D405/10
摘要： The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. wherein R1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; and R2 is a radiolabelled group CH3, wherein the radionuclide is 3H or 11C. The radiolabelled compounds of formula I may be used as PET (Positron Emission Tomography) radiotracer for the labelling and diagnostic molecular imaging of the glycine 1 transporter functionality.
摘要翻译： 本发明涉及用于甘氨酸1转运蛋白（GlyT1）的式I的新型放射性标记抑制剂，其可用于甘氨酸1转运蛋白官能度的标记和诊断成像。 其中R1是异丙氧基或2,2,2-三氟-1-甲基 - 乙氧基; 并且R 2是放射性标记的基团CH 3，其中放射性核素是3H或11C。 放射性标记的式I化合物可用作PET（正电子发射断层扫描）放射性示踪剂，用于甘氨酸1转运蛋白功能的标记和诊断分子成像。
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