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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：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.
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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：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：US20050070539A1
公开(公告)日：2005-03-31
申请号：US10933103
申请日：2004-09-02
申请人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Nettekoven , Roger Norcross , Emmanuel Pinard , Henri Stadler
发明人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Nettekoven , Roger Norcross , Emmanuel Pinard , Henri Stadler
IPC分类号： A61K31/495 , A61K31/496 , A61P25/28 , C07D207/08 , C07D207/12 , C07D207/20 , C07D211/42 , C07D231/12 , C07D233/54 , C07D237/20 , C07D249/08 , C07D257/04 , C07D295/192 , C07D307/14 , C07D309/14 , C07D43/02 , A61K31/501 , A61K31/506 , A61K31/53
CPC分类号： C07D295/192 , A61K31/495 , A61K31/496 , C07D207/08 , C07D207/12 , C07D207/20 , C07D211/42 , C07D231/12 , C07D233/54 , C07D237/20 , C07D249/08 , C07D257/04 , C07D307/14 , C07D309/14
摘要： A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译： 式的化合物，其中取代基如治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆和其他认知过程受损的其他疾病（如注意力缺陷障碍或阿尔茨海默病）的治疗方法所述。
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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：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：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：US20050210540A1
公开(公告)日：2005-09-22
申请号：US11080962
申请日：2005-03-15
IPC分类号： A01K67/027 , C07K14/47 , C12N5/06 , C12N5/10 , C12N15/09 , C12N15/12 , C12N15/63 , C12N15/85 , C12Q1/00 , C12Q1/02 , G01N33/15 , G01N33/50
CPC分类号： C07K14/47 , A01K67/0275 , A01K2217/05 , A01K2227/105 , A01K2267/0356 , C12N15/8509 , C12N2830/008
摘要： The present invention provides genetic constructs and methods for producing transgenic non-human animals comprising within their genome transgenic DNA encoding GLYT1. These transgenic animals could be further used to generate transgenic animals which produce more active GLYT1. Also provided are transgenic animals producing more GLYT1 protein, as well as the methods of producing same. The invention also relates to the use of these animals as a model for analyzing the effects of depressing synaptic NMDA receptor function and studying the ability of compounds to reduce symptoms of psychotic behavior.
摘要翻译： 本发明提供用于产生转基因非人动物的遗传构建体和方法，其在其基因组中包含编码GLYT1的转基因DNA。 这些转基因动物可以进一步用于产生产生更活性的GLYT1的转基因动物。 还提供了产生更多GLYT1蛋白质的转基因动物以及其生产方法。 本发明还涉及这些动物作为分析抑制突触NMDA受体功能的作用并研究化合物降低精神病性症状的能力的模型。
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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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