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1. 发明申请

US20080267912A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：US20080267912A1
公开(公告)日：2008-10-30
申请号：US12105874
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
发明人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K38/20 , C07D233/54 , A61K31/4164 , A61K38/21 , A61P31/00 , A61P3/00 , A61P9/00 , A61P25/00 , A61P35/00 , A61K31/4178 , A61K39/395
CPC分类号： C07D233/61 , C07D233/64 , C07D235/06 , C07D405/12 , C07D417/12
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
摘要翻译：式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中：A表示和B，R 1，R R 3，R 4，R 4，R 5，R 6和Z 3，在整个说明书和权利要求书中都是定义的。

2. 发明授权

US08227498B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08227498B2
公开(公告)日：2012-07-24
申请号：US12105874
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
发明人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K31/417 , C07D233/64 , C07D235/06
CPC分类号： C07D233/61 , C07D233/64 , C07D235/06 , C07D405/12 , C07D417/12
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
摘要翻译：式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中：A表示和B，R1，R2，R3，R4，R5，R6 和Z如在说明书和权利要求书中所定义。

3. 发明授权

US08809010B2 Method for prophylactic treatment of alzheimer's disease using inhibitors of glutaminyl cyclase and glutamate cyclases 有权
标题翻译：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。

4. 发明申请

US20070191366A1 USE OF EFFECTORS OF GLUTAMINYL AND GLUTAMATE CYCLASES 有权
标题翻译：使用谷氨酰胺和谷氨酸周期的影响
公开(公告)号：US20070191366A1
公开(公告)日：2007-08-16
申请号：US11685881
申请日：2007-03-14
申请人： Torsten Hoffmann , Stephan Schilling , Andre Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffmann , Stephan Schilling , Andre Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/5377 , A61K31/517 , A61K31/454 , A61K31/4439 , A61K31/4184 , A61K31/4178
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。

5. 发明申请

US20100040575A1 USE OF INHIBITORS OF GLUTAMINYL CYCLASE AND GLUTAMATE CYCLASE FOR TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES 有权
标题翻译：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。

6. 发明授权

US09656991B2 Inhibitors of glutaminyl cyclase 有权
公开(公告)号：US09656991B2
公开(公告)日：2017-05-23
申请号：US12105703
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , André J. Niestroj , Robert Sommer
发明人： Mirko Buchholz , Ulrich Heiser , André J. Niestroj , Robert Sommer
IPC分类号： C07D233/64 , C07D233/61 , C07D235/06 , C07D401/12 , C07D417/12 , C07D409/12 , C07D413/12 , C07D405/12
CPC分类号： C07D401/12 , C07D233/64 , C07D235/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.

7. 发明授权

US08188094B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08188094B2
公开(公告)日：2012-05-29
申请号：US12105832
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Robert Sommer
发明人： Mirko Buchholz , Ulrich Heiser , Robert Sommer
IPC分类号： A61K31/506 , A61K31/4178 , C07D403/06
CPC分类号： C07D403/12 , C07D401/14 , C07D405/14
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined throughout the description and the claims.
摘要翻译：式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中：A表示和B，R1，R2，R3，R4，R5，R6 R7，Y和Z如在说明书和权利要求书中所定义。

8. 发明授权

US07897633B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US07897633B2
公开(公告)日：2011-03-01
申请号：US11923307
申请日：2007-10-24
申请人： Stephan Schilling , Mirko Buchholz , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
发明人： Stephan Schilling , Mirko Buchholz , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
IPC分类号： A61K31/417 , A61K31/4164 , C07D233/61
CPC分类号： A61K31/4164 , C07D233/54 , C07D235/06 , C07D403/12 , C07D405/12 , C07D417/12
摘要： The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea 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：本发明涉及谷氨酰胺酰基环化酶的新型抑制剂及其组合，用于治疗神经元疾病，特别是阿尔茨海默病，唐氏综合征，帕金森病，霍乱金淋巴瘤，致病精神病，精神分裂症，食物摄入受损，睡眠觉醒，内稳态调节障碍能量代谢受损，自主神经功能障碍，体内受损的调节，体液，高血压，发热，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，神经变性障碍，包括认知功能障碍和痴呆。

9. 发明授权

US07741354B2 Inhibitors of glutaminyl cyclase 有权
公开(公告)号：US07741354B2
公开(公告)日：2010-06-22
申请号：US11937159
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/41 , C07D257/00
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, —C(O)O-alkyl and —C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)O-alkyl and —C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R2 together with R4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, amino, halogen, haloalkyl, hydroxyl, -alkoxy, -thioalkyl, —C(O)OH and —C(O)O-alkyl; alkenyl; -alkyl-aryl; -alkyl(aryl)2, -alkyl(heteroaryl)2, -alkyl(aryl)(heteroaryl), -alkyl-heteroaryl; -alkyl-heterocyclyl which heterocyclyl group may optionally be substituted by one or more groups selected from alkyl, hydroxy and oxo ; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-aryl; -aryl-O-aryl, -heteroaryl-heteroaryl; -aryl; heteroaryl; heterocyclyl; -aryl-alkyl-aryl; -aryl-O-alkyl-aryl; -alkyl-C(O)—NH-alkyl-aryl; -alkyl-C(O)—NH-alkyl-heteroaryl; -alkyl-C(O)—NH-alkyl-heterocyclyl; -alkyl-C(O)—(N-piperidinyl) or -alkyl-C(O)—(N-pyrrolidinyl) in which piperidinyl or pyrrolidinyl may optionally be fused to optionally substituted phenyl. R4 represents H or alkyl.

10. 发明申请

US20090018087A1 Novel Inhibitors of Glutaminyl Cyclase 有权
标题翻译：新型抑制谷氨酰胺环化酶
公开(公告)号：US20090018087A1
公开(公告)日：2009-01-15
申请号：US11923307
申请日：2007-10-24
申请人： Stephan Schilling , Mirko Buchholz , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
发明人： Stephan Schilling , Mirko Buchholz , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth
IPC分类号： A61K38/05 , C07D233/61 , A61K31/4164 , A61K31/5377 , A61P25/16 , A61P25/30 , A61P25/28 , C07D413/12 , C07D417/12 , A61K31/423
CPC分类号： A61K31/4164 , C07D233/54 , C07D235/06 , C07D403/12 , C07D405/12 , C07D417/12
摘要： The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea 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：本发明涉及谷氨酰胺酰基环化酶的新型抑制剂及其组合，用于治疗神经元疾病，特别是阿尔茨海默病，唐氏综合征，帕金森病，霍乱金淋巴瘤，致病精神病，精神分裂症，食物摄入受损，睡眠觉醒，内稳态调节障碍能量代谢受损，自主神经功能障碍，体内受损的调节，体液，高血压，发热，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，神经变性障碍，包括认知功能障碍和痴呆。

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