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1. 发明申请

US20060234940A1 Secondary binding site of dipeptidyl peptidase IV (DP IV) 有权
标题翻译：二肽基肽酶IV（DP IV）的二级结合位点
公开(公告)号：US20060234940A1
公开(公告)日：2006-10-19
申请号：US11478217
申请日：2006-06-29
申请人： Kerstin Kuhn-Wache , Joachim Bar , Hans-Ulrich Demuth , Torsten Hofmann , Ulrich Heiser , Wolfgang Brandt
发明人： Kerstin Kuhn-Wache , Joachim Bar , Hans-Ulrich Demuth , Torsten Hofmann , Ulrich Heiser , Wolfgang Brandt
IPC分类号： A61K38/10 , A61K38/08 , A61K38/06 , A61K38/05
CPC分类号： A61K31/401 , A61K38/00 , C07K7/06 , C12Q1/37 , G01N2500/04
摘要： The present application relates to the secondary binding site of dipeptidyl peptidase IV, its relationship amongst substrates and to the modulation of substrate specificity of dipeptidyl peptidase IV (DP IV, synonym: DPP IV, CD26, EC 3.4.14.5). The application relates further to compounds that bind to the secondary binding site of DP IV and their use to modulate the substrate specificity of DP IV; methods of treatment of various DP IV mediated disorders; and screening methods for the identification of secondary binding sites on DP IV and DP IV-like enzymes.
摘要翻译：本申请涉及二肽基肽酶IV的二级结合位点，其与底物之间的关系以及二肽基肽酶IV（DP IV，同义词：DPP IV，CD26，EC 3.4.14.5）的底物特异性的调节。本申请还涉及结合DP IV的二级结合位点的化合物及其用于调节DP IV的底物特异性的用途; 各种DP IV介导的病症的治疗方法; 以及用于鉴定DP IV和DP IV样酶的二级结合位点的筛选方法。

2. 发明申请

US20050176622A1 Secondary binding site of dipeptidyl peptidase IV (DPIV) 审中-公开
标题翻译：二肽基肽酶IV（DPIV）的二级结合位点
公开(公告)号：US20050176622A1
公开(公告)日：2005-08-11
申请号：US10667200
申请日：2003-09-18
申请人： Kerstin Kuhn-Wache , Joachim Bar , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
发明人： Kerstin Kuhn-Wache , Joachim Bar , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
IPC分类号： A61K31/155 , A61K31/175 , A61K31/401 , A61K31/455 , A61K31/704 , A61K38/00 , A61K38/08 , A61K38/22 , A61K38/28 , A61P3/00 , C07K7/06 , C12Q1/37
CPC分类号： A61K31/401 , A61K38/00 , C07K7/06 , C12Q1/37 , G01N2500/04
摘要： The present application relates to the secondary binding site of dipeptidyl peptidase IV, its relationship amongst substrates and to the modulation of substrate specificity of dipeptidyl peptidase IV (DP IV, synonym: DPP IV, CD26, EC 3.4.14.5). The application relates further to compounds that bind to the secondary binding site of DP IV and their use to modulate the substrate specificity of DP IV; methods of treatment of various DP IV mediated disorders; and screening methods for the identification of secondary binding sites on DP IV and DP IV-like enzymes.
摘要翻译：本申请涉及二肽基肽酶IV的二级结合位点，其与底物之间的关系以及二肽基肽酶IV（DP IV，同义词：DPP IV，CD26，EC 3.4.14.5）的底物特异性的调节。本申请还涉及结合DP IV的二级结合位点的化合物及其用于调节DP IV的底物特异性的用途; 各种DP IV介导的病症的治疗方法; 以及用于鉴定DP IV和DP IV样酶的二级结合位点的筛选方法。

3. 发明授权

US07816325B2 Secondary binding site of dipeptidyl peptidase IV (DP IV) 有权
标题翻译：二肽基肽酶IV（DP IV）的二级结合位点
公开(公告)号：US07816325B2
公开(公告)日：2010-10-19
申请号：US11478217
申请日：2006-06-29
申请人： Kerstin Kühn-Wache , Joachim Bär , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
发明人： Kerstin Kühn-Wache , Joachim Bär , Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser , Wolfgang Brandt
IPC分类号： A61K38/08 , A61K39/395
CPC分类号： A61K31/401 , A61K38/00 , C07K7/06 , C12Q1/37 , G01N2500/04
摘要： The present application relates to the secondary binding site of dipeptidyl peptidase IV, its relationship amongst substrates and to the modulation of substrate specificity of dipeptidyl peptidase IV (DP IV, synonym: DPP IV, CD26, EC 3.4.14.5). The application relates further to compounds that bind to the secondary binding site of DP IV and their use to modulate the substrate specificity of DP IV; methods of treatment of various DP IV mediated disorders; and screening methods for the identification of secondary binding sites on DP IV and DP IV-like enzymes.
摘要翻译：本申请涉及二肽基肽酶IV的二级结合位点，其与底物之间的关系以及二肽基肽酶IV（DP IV，同义词：DPP IV，CD26，EC 3.4.14.5）的底物特异性的调节。本申请还涉及结合DP IV的二级结合位点的化合物及其用于调节DP IV的底物特异性的用途; 各种DP IV介导的病症的治疗方法; 以及用于鉴定DP IV和DP IV样酶的二级结合位点的筛选方法。

4. 发明授权

US06319893B1 Raising blood sugar level in hypoglycemic mammals by administering inhibitors of dipeptidyl peptidase IV 有权
标题翻译：通过施用二肽基肽酶IV抑制剂提高低血糖哺乳动物血糖水平
公开(公告)号：US06319893B1
公开(公告)日：2001-11-20
申请号：US09365404
申请日：1999-08-02
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Kerstin Kuhn-Wache , Fred Rosche
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Kerstin Kuhn-Wache , Fred Rosche
IPC分类号： A01N3718
CPC分类号： A61K38/26
摘要： A method of raising the blood sugar level in a mammal having hypoglycemia is described. The method reduces degradation of glucagon by administering to the mammal a therapeutically effective amount of an inhibitor of dipeptidyl peptidase IV and physiologically acceptable adjuvants and/or excipients.
摘要翻译：描述了一种提高低血糖哺乳动物血糖水平的方法。该方法通过向哺乳动物施用治疗有效量的二肽基肽酶IV抑制剂和生理上可接受的佐剂和/或赋形剂来降低胰高血糖素的降解。

5. 发明授权

US08486940B2 Inhibitors 有权
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.

6. 发明授权

US07667044B2 Compounds for the treatment of neurological disorders 失效
标题翻译：用于治疗神经障碍的化合物
公开(公告)号：US07667044B2
公开(公告)日：2010-02-23
申请号：US11290735
申请日：2005-11-30
申请人： André Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
发明人： André Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
IPC分类号： C07D277/00 , C07D207/00 , C07D295/00 , C07D409/00 , C07D411/00 , A01N43/78 , A01N43/36 , A61K31/425 , A61K31/40
CPC分类号： C07D417/06 , C07D417/14
摘要： The present invention relates to novel inhibitors of prolyl endopeptidase of formula 1 W—KCONH—X—CON—Y—CO—Z (1) wherein K, W, X, Y and Z are specified in the description. The compounds are useful for the treatment of diseases such as mild cognitive impairment (MCI), Alzheimer's disease, Down Syndrome, Parkinson disease and Chorea Huntington.
摘要翻译：本发明涉及式1的W-KCONH-X-CON-Y-CO-Z（1）的脯氨酰内肽酶的新型抑制剂，其中K，W，X，Y和Z在说明书中规定。该化合物可用于治疗诸如轻度认知障碍（MCI），阿尔茨海默病，唐氏综合症，帕金森病和霍乱金淋巴瘤等疾病。

7. 发明申请

US20090149394A1 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：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。

8. 发明申请

US20080153892A1 Inhibitors of Glutaminyl Cyclase 有权
标题翻译：谷氨酰胺酰化酶抑制剂
公开(公告)号：US20080153892A1
公开(公告)日：2008-06-26
申请号：US12046520
申请日：2008-03-12
申请人： Stephan Schilling , Andre J. Niestroj , Ulrich Heiser , Mirko Buchholz , Hans-Ulrich Demuth
发明人： Stephan Schilling , Andre J. Niestroj , Ulrich Heiser , Mirko Buchholz , Hans-Ulrich Demuth
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

9. 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。

10. 发明授权

US07060719B2 Glutaminyl based DPIV inhibitors 有权
标题翻译：基于谷氨酰胺基的DPIV抑制剂
公开(公告)号：US07060719B2
公开(公告)日：2006-06-13
申请号：US10779158
申请日：2004-02-13
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
IPC分类号： A61K31/425 , A61K31/40 , C07D277/04 , C07D207/00
CPC分类号： C07D277/04 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D295/185 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K7/06
摘要： The present invention provides compounds of the formula: wherein X=CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
摘要翻译：本发明提供下式的化合物：其中X = CH 2或S或其药学上可接受的盐可用于治疗由DPIV或DPIV样酶如关节炎，肥胖，免疫和自身免疫介导的病症疾病，同种异体移植，癌症，神经元疾病和皮肤疾病。

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