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11.发明授权公开(公告)号：US08945510B2
公开(公告)日：2015-02-03
申请号：US13479826
申请日：2012-05-24
IPC分类号： A61K51/04 , A61K31/415 , C07D403/10
CPC分类号： A61K51/0453 , C07B59/002
摘要： Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.
摘要翻译： 放射性标记的谷氨酰胺酶（QC）抑制剂作为成像剂，特别地但不排他地作为用于检测神经障碍的医学成像剂; 以及使用放射性标记的抑制剂的用于检测神经系统疾病的药物组合物，方法和试剂盒。
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公开(公告)号：US20120301398A1
公开(公告)日：2012-11-29
申请号：US13479826
申请日：2012-05-24
IPC分类号： C07D403/10 , G01N33/53 , A61K51/04
CPC分类号： A61K51/0453 , C07B59/002
摘要： Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.
摘要翻译： 放射性标记的谷氨酰胺酶（QC）抑制剂作为成像剂，特别地但不排他地作为用于检测神经障碍的医学成像剂; 以及使用放射性标记的抑制剂的用于检测神经系统疾病的药物组合物，方法和试剂盒。
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公开(公告)号：US09126987B2
公开(公告)日：2015-09-08
申请号：US11946101
申请日：2007-11-28
IPC分类号： C07D413/04
CPC分类号： C07D413/04
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; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.
摘要翻译： 本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，其中R 1表示杂芳基， - 碳环基 - 杂芳基， - 烯基杂芳基或 - 烷基杂芳基; R2代表烷基; 可任意被烷基取代的碳环基; 烯基; 炔基，条件是三键不与X相邻; - 烷基 - 芳基; - 烷基 - 杂芳基; - 烷基 - 杂环基，其中杂环基可以任选被烷基取代; - 烷基 - 碳环基，其中碳环基可以任选地被烷基取代; 芳基; 杂芳基; 或H; X表示S或NR 3; R 3表示H或C 1-4烷基。
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公开(公告)号：US08530670B2
公开(公告)日：2013-09-10
申请号：US13422619
申请日：2012-03-16
申请人： Ulrich Heiser , Daniel Ramsbeck
发明人： Ulrich Heiser , Daniel Ramsbeck
IPC分类号： A61K31/4184 , C07D401/14 , C07D403/04 , C07D413/14
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/4409 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K38/2026 , A61K38/21 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
摘要翻译： 式（I）的新型杂环衍生物：或其药学上可接受的盐，溶剂化物或多晶型物，包括其所有互变异构体和立体异构体，其中R a，n，R 1和R 2如本文所定义，作为谷氨酰胺酰环化酶抑制剂（QC，EC2.3 .2.5）。
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公开(公告)号：US20080214620A1
公开(公告)日：2008-09-04
申请号：US11946101
申请日：2007-11-28
IPC分类号： A61K31/4245 , C07D413/02 , C07D413/14 , A61P31/00 , A61P19/00 , A61P25/00 , A61K31/4439
CPC分类号： C07D413/04
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; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.
摘要翻译： 本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，其中R 1表示杂芳基，碳环基 - 杂芳基， - 烯基杂芳基或 - 烷基杂芳基; R 2表示烷基; 可任意被烷基取代的碳环基; 烯基; 炔基，条件是三键不与X相邻; - 烷基 - 芳基; - 烷基 - 杂芳基; - 烷基 - 杂环基，其中杂环基可以任选被烷基取代; - 烷基 - 碳环基，其中碳环基可以任选地被烷基取代; 芳基; 杂芳基; 或H; X表示S或NR 3; R 3表示H或C 1-4烷基。
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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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17.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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公开(公告)号：US06949515B2
公开(公告)日：2005-09-27
申请号：US10082001
申请日：2002-02-22
IPC分类号： A61K9/06 , A61K8/49 , A61K8/72 , A61K9/08 , A61K9/107 , A61K9/12 , A61K9/70 , A61K9/72 , A61K31/765 , A61K38/00 , A61K47/48 , A61P1/02 , A61P3/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07K5/037 , C07K5/06 , C07K5/072 , C07K5/083 , C07K5/113 , C07K7/06 , C07K7/08 , C08G65/329 , A61K31/33
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06104 , C07K5/0806 , C07K7/08 , C08G65/329
摘要： The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain; B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.
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19.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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20.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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