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1.发明授权Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease 有权使用谷氨酰胺酰环化酶抑制剂治疗和预防疾病公开(公告)号：US07381537B2
公开(公告)日：2008-06-03
申请号：US10839017
申请日：2004-05-05
IPC分类号： C12Q1/34
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物，这种效应物的筛选方法，以及包含这些效果子的这种效应物和药物组合物的用途，用于治疗 可以通过调节QC活性来治疗。 优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。
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2.发明授权Method for prophylactic treatment of alzheimer's disease using inhibitors of glutaminyl cyclase and glutamate cyclases 有权使用谷氨酰胺环化酶和谷氨酸环化酶抑制剂预防性治疗阿尔茨海默病的方法公开(公告)号：US08809010B2
公开(公告)日：2014-08-19
申请号：US12506823
申请日：2009-07-21
申请人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： C12Q1/34
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： Provided herein are methods for treating and preventing neurodegenerative disease in a mammal by administering an inhibitor of glutaminyl cyclase (QC). Neurodegenerative diseases treatable or preventable according to methods described herein include mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia.
摘要翻译： 本文提供了通过施用谷氨酰胺环化酶（QC）抑制剂来治疗和预防哺乳动物中的神经变性疾病的方法。 根据本文描述的方法可治疗或可预防的神经变性疾病包括轻度认知障碍（MCI），阿尔茨海默病，唐氏综合征中的神经变性，家族性的痴呆和家族性丹麦痴呆。
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3.发明申请USE OF INHIBITORS OF GLUTAMINYL CYCLASE AND GLUTAMATE CYCLASE FOR TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES 有权谷氨酰胺环糊精和谷氨酸环化酶抑制剂用于治疗和预防神经病变性疾病的使用公开(公告)号：US20100040575A1
公开(公告)日：2010-02-18
申请号：US12506823
申请日：2009-07-21
申请人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/4164 , A61P25/00 , A61P25/28 , A61K31/4184 , A61K31/428 , A61K31/517 , A61K31/5415 , A61K39/395 , A61K38/21 , A61K45/00
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： Physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的生理底物，QC的新效应物，用于筛选此类效应物的方法，以及使用这些效应物和包含这些效应物的药物组合物用于治疗可通过调节 的QC活动。 优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。
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公开(公告)号：US20080153892A1
公开(公告)日：2008-06-26
申请号：US12046520
申请日：2008-03-12
IPC分类号： A61K31/415
CPC分类号： C07D207/08 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D207/10 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/24 , C07D231/04 , C07D231/06 , C07D233/02 , C07D233/06 , C07D233/28 , C07D233/42 , C07D233/54 , C07D249/04 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/04 , C07D263/04 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/185 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： Compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia
摘要翻译： 作为QC抑制剂的化合物，包括由通式1至9表示的化合物及其组合，用于治疗神经元疾病，特别是阿尔茨海默氏病，唐氏综合征，帕金森病，柯达亨廷顿病，致病精神病，精神分裂症，食物摄取受损 睡眠觉醒，能量代谢障碍的稳态调节，自主神经功能障碍，激素平衡受损，调节受损，体液，高血压，发烧，睡眠失调，厌食，焦虑相关障碍，包括抑郁症，癫痫发作，药物戒断和酒精中毒， 神经变性疾病包括认知功能障碍和痴呆
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公开(公告)号：US07371871B2
公开(公告)日：2008-05-13
申请号：US10838993
申请日：2004-05-05
IPC分类号： A61K31/4174 , C07D233/61
CPC分类号： C07D207/08 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D207/10 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/24 , C07D231/04 , C07D231/06 , C07D233/02 , C07D233/06 , C07D233/28 , C07D233/42 , C07D233/54 , C07D249/04 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/04 , C07D263/04 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/185 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
摘要翻译： 本发明涉及作为QC抑制剂的化合物，包括由通式1至9表示的化合物及其组合用于治疗神经元疾病，特别是阿尔茨海默氏病，唐氏综合征，帕金森病，柯达亨廷顿病，致病性精神病症状， 精神分裂症，食物摄取受损，睡眠觉醒，能量代谢的稳态调节受损，自主神经功能受损，激素平衡受损，调节受损，体液，高血压，发热，睡眠失调，厌食，焦虑相关障碍，包括癫痫发作， 药物戒断和酒精中毒，神经变性疾病，包括认知功能障碍和痴呆。
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6.发明授权公开(公告)号：US07732162B2
公开(公告)日：2010-06-08
申请号：US11685881
申请日：2007-03-14
申请人： Torsten Hoffman , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffman , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： C12Q1/34
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物，用于筛选此类效应物的方法，以及使用这些效应物和包含这些效应物的药物组合物，用于治疗 可以通过调节QC活性来治疗。 优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。
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公开(公告)号：US20090149394A1
公开(公告)日：2009-06-11
申请号：US12182113
申请日：2008-07-29
申请人： Stephan Schilling , Torsten Hoffmann , Andre Johannes Niestroj , Hans-Ulrich Demuth , Ulrich Heiser
发明人： Stephan Schilling , Torsten Hoffmann , Andre Johannes Niestroj , Hans-Ulrich Demuth , Ulrich Heiser
IPC分类号： A61K38/06 , A61K31/131 , A61K31/095 , A61K31/426 , A61K31/40 , A61P25/00 , A61K31/4439 , A61K31/472 , A61K38/05
CPC分类号： A61K31/00 , A61K31/13 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K38/06 , A61K38/07 , A61K38/08
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of diseases that can be treated by modulation of QC-activity, e.g. diseases selected from the group consisting of duodenal cancer with or w/o Heliobacter pylori infections, colorectal cancer, Zolliger-Ellison syndrome, Familial British Dementia and Familial Danish Dementia.
摘要翻译： 本发明提供了哺乳动物谷氨酰胺酰化环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物以及包含这些效应物的这些效应物和药物组合物的用途，用于治疗可以通过调节QC- 活动，例如 选自由具有或不具有幽门螺旋杆菌感染的十二指肠癌，结肠直肠癌，佐立格 - 埃利森综合征，家族性英国痴呆和家族性丹麦痴呆组成的组的疾病。
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公开(公告)号：US08470781B2
公开(公告)日：2013-06-25
申请号：US12182113
申请日：2008-07-29
申请人： Stephan Schilling , Torsten Hoffmann , Andre Johannes Niestroj , Hans-Ulrich Demuth , Ulrich Heiser
发明人： Stephan Schilling , Torsten Hoffmann , Andre Johannes Niestroj , Hans-Ulrich Demuth , Ulrich Heiser
IPC分类号： C07K5/06
CPC分类号： A61K31/00 , A61K31/13 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K38/06 , A61K38/07 , A61K38/08
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of diseases that can be treated by modulation of QC-activity, e.g. diseases selected from the group consisting of duodenal cancer with or w/o Heliobacter pylori infections, colorectal cancer, Zolliger-Ellison syndrome, Familial British Dementia and Familial Danish Dementia.
摘要翻译： 本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物以及包含这些效应物的这些效应物和药物组合物的用途，用于治疗可通过调节QC- 活动，例如 选自由具有或不具有幽门螺旋杆菌感染的十二指肠癌，结肠直肠癌，佐立格 - 埃利森综合征，家族性英国痴呆和家族性丹麦痴呆组成的组的疾病。
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9.发明申请Use of Inhibtors of Glutaminyl Cyclases for Treatment and Prevention of Disease 有权谷氨酰胺酰化酶抑制剂用于治疗和预防疾病的应用公开(公告)号：US20080286810A1
公开(公告)日：2008-11-20
申请号：US12101497
申请日：2008-04-11
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： Novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新型生理底物，QC的新效应物，筛选此类效应物的方法，以及包含这些效应物的这种效应物和药物组合物的用途，用于治疗可由 调节QC活性。 优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。
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10.发明授权Use of inhibtors of glutaminyl cyclases for treatment and prevention of disease 有权使用谷氨酰胺环化酶抑制剂治疗和预防疾病公开(公告)号：US08685664B2
公开(公告)日：2014-04-01
申请号：US12101497
申请日：2008-04-11
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： Novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新型生理底物，QC的新效应物，筛选此类效应物的方法，以及包含这些效应物的这种效应物和药物组合物的用途，用于治疗可由 调节QC活性。 优选的组合物还包含用于治疗或减轻可通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV类似酶的抑制剂。
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