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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。
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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。
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公开(公告)号：US20110262388A1
公开(公告)日：2011-10-27
申请号：US13091276
申请日：2011-04-21
申请人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
发明人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K38/20 , C07D405/14 , C07D409/14 , C07D417/14 , C07D401/14 , C07D409/12 , C07D417/12 , A61K31/4184 , A61K31/428 , A61K31/433 , A61K31/4709 , A61K39/395 , A61K31/4409 , A61K38/21 , A61P35/00 , A61P25/18 , A61P35/04 , A61P17/06 , A61P29/00 , A61P25/00 , A61P5/00 , A61P25/28 , A61P9/10 , A61P19/02 , A61P9/00 , A61P15/08 , A61P3/00 , C07D235/08
CPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
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公开(公告)号：US20110092501A1
公开(公告)日：2011-04-21
申请号：US12880369
申请日：2010-09-13
申请人： Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
发明人： Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
IPC分类号： A61K31/535 , C07D403/02 , A61K31/4184 , A61K31/454 , C07D401/02 , C07D413/14 , C07D471/04 , A61K31/437 , A61P35/00 , A61P29/00 , A61P25/00 , A61P35/04 , A61P3/00 , A61P5/00
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K45/06 , C07D235/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
摘要翻译： 本发明涉及式（I）的新型吡咯烷衍生物：其中R1，R2和R3如本文所定义，作为谷氨酰胺酰环化酶抑制剂（QC，EC 2.3.2.5）。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸（5-氧代 - 脯氨酰基，pGlu *）中的分子内环化，并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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公开(公告)号：US09181233B2
公开(公告)日：2015-11-10
申请号：US13040159
申请日：2011-03-03
IPC分类号： C07D235/04 , A61K31/4184 , C07D417/04 , C07D403/04 , C07D413/04
CPC分类号： C07D417/04 , A61K31/4184 , C07D235/04 , C07D403/04 , C07D413/04
摘要： The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
摘要翻译： 本发明涉及作为谷氨酰胺酰环化酶抑制剂的新型杂环衍生物（QC，EC 2.3.2.5）。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸（5-氧代 - 脯氨酰基，pGlu *）中的分子内环化，并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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公开(公告)号：US08541596B2
公开(公告)日：2013-09-24
申请号：US13091276
申请日：2011-04-21
申请人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
发明人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K31/4184 , C07D235/08
CPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
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公开(公告)号：US08486940B2
公开(公告)日：2013-07-16
申请号：US12880369
申请日：2010-09-13
申请人： Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
发明人： Ulrich Heiser , Daniel Ramsbeck , Robert Sommer , Antje Meyer , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
IPC分类号： A61K31/535 , A61K31/497 , A61K31/42 , A61K31/415 , A61K31/40 , C07D211/06 , C07D265/30 , C07D241/02 , C07D263/02 , C07D233/02
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5355 , A61K31/5377 , A61K45/06 , C07D235/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
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8.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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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。
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10.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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