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1. 发明申请

US20050209159A1 Effectors of dipeptidyl peptidase IV for topical use 失效
标题翻译：二肽基肽酶IV用于局部使用的作用
公开(公告)号：US20050209159A1
公开(公告)日：2005-09-22
申请号：US11069926
申请日：2005-03-01
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
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 , A61K38/10 , A61K38/08
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.
摘要翻译：本发明涉及用于局部影响以下通式的二肽基肽酶的活性的化合物：其中A是在侧链中具有至少一个官能团的氨基酸; B是与A的侧链官能团共价结合的化合物，选自（a）链长达20个氨基酸的寡肽，（b）由多达6个氨基酸组成的甘氨酸均聚物甘氨酸单体，和（c）摩尔质量高达20 000g / mol的聚乙二醇; 和C是选自噻唑烷，吡咯烷，氰基吡咯烷，羟脯氨酸，脱氢脯氨酸或哌啶的酰胺键合的基团。本发明进一步涉及所述化合物在局部免疫学过程（趋化性，炎性过程，自身免疫性疾病）中的靶向干预的用途，以及与之相关的病理生理和生理过程的有效和靶向治疗（牛皮癣，牙周炎，关节炎，过敏，炎症），特别是。

2. 发明授权

US06949515B2 Effectors of dipeptidyl peptidase IV for topical use 失效
公开(公告)号：US06949515B2
公开(公告)日：2005-09-27
申请号：US10082001
申请日：2002-02-22
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
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.

3. 发明授权

US07335645B2 Effectors of dipeptidyl peptidase IV for topical use 失效
标题翻译：二肽基肽酶IV用于局部使用的作用
公开(公告)号：US07335645B2
公开(公告)日：2008-02-26
申请号：US11069926
申请日：2005-03-01
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Dagmar Schlenzig , Ulrich Heiser
IPC分类号： A61K38/00 , 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.
摘要翻译：本发明涉及用于局部影响以下通式的二肽基肽酶的活性的化合物：其中A是在侧链中具有至少一个官能团的氨基酸; B是与A的侧链官能团共价结合的化合物，选自（a）链长达20个氨基酸的寡肽，（b）由多达6个氨基酸组成的甘氨酸均聚物甘氨酸单体，和（c）摩尔质量高达20 000g / mol的聚乙二醇; 和C是选自噻唑烷，吡咯烷，氰基吡咯烷，羟脯氨酸，脱氢脯氨酸或哌啶的酰胺键合的基团。本发明进一步涉及所述化合物在局部免疫学过程（趋化性，炎性过程，自身免疫性疾病）中的靶向干预的用途，以及与之相关的病理生理和生理过程的有效和靶向治疗（牛皮癣，牙周炎，关节炎，过敏，炎症），特别是。

4. 发明授权

US07166579B2 Prodrugs of DP IV-inhibitors 有权
标题翻译： DP IV抑制剂的前药
公开(公告)号：US07166579B2
公开(公告)日：2007-01-23
申请号：US10735582
申请日：2003-12-11
申请人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
发明人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
IPC分类号： A61K38/05 , A61K38/04
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06173 , C07K5/0806 , C07K5/0808 , C07K5/0823
摘要： Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.
摘要翻译：丝氨酸肽酶二肽基肽酶IV的不稳定抑制剂的前药化合物用于治疗各种疾病，特别是代谢紊乱。前药化合物可用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病变和肾病。

5. 发明授权

US07084120B2 Prodrugs of DP IV-inhibitors 失效
标题翻译： DP IV抑制剂的前药
公开(公告)号：US07084120B2
公开(公告)日：2006-08-01
申请号：US09745776
申请日：2000-12-22
申请人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
发明人： Hans-Ulrich Demuth , Dagmar Schlenzig , Torsten Hoffmann , Susanne Manhart
IPC分类号： A61K38/05 , C07K5/078
CPC分类号： C07K5/06165 , A61K38/00 , C07K5/06173 , C07K5/0806 , C07K5/0808 , C07K5/0823
摘要： Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.
摘要翻译：丝氨酸肽酶二肽基肽酶IV的不稳定抑制剂的前药化合物用于治疗各种疾病，特别是代谢紊乱。前药化合物可用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病变和肾病。

6. 发明授权

US08470781B2 Use of effectors of glutaminyl and glutamate cyclases 有权
标题翻译：使用谷氨酰胺和谷氨酸环化酶的效应物
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。

7. 发明申请

US20080286810A1 Use of Inhibtors of Glutaminyl Cyclases for Treatment and Prevention of Disease 有权
标题翻译：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
IPC分类号： G01N33/53 , C12Q1/00
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。

8. 发明授权

US09181233B2 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：US09181233B2
公开(公告)日：2015-11-10
申请号：US13040159
申请日：2011-03-03
申请人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
发明人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme , Hans-Ulrich Demuth
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。

9. 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。

10. 发明授权

US08685664B2 Use of inhibtors of glutaminyl cyclases for treatment and prevention of disease 有权
标题翻译：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
IPC分类号： C12Q1/48 , C12Q1/00 , C12N9/10 , C07H21/04 , A61K38/00
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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