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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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42.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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44.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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公开(公告)号：US07608577B2
公开(公告)日：2009-10-27
申请号：US10216305
申请日：2002-08-09
CPC分类号： C07K7/06 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The present invention relates to compounds of the general formula 1 and pharmaceutically acceptable salts thereof, to the use of the compounds for the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidosis, diabetes mellitus, diabetic neuropathy and nephropathy and of sequelae caused by diabetes mellitus in mammals.
摘要翻译： 本发明涉及通式1的化合物及其药学上可接受的盐，该化合物用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸中毒，糖尿病，糖尿病性神经病变和肾病以及由 哺乳动物糖尿病。
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公开(公告)号：US20060194852A1
公开(公告)日：2006-08-31
申请号：US11369606
申请日：2006-03-07
IPC分类号： A61K31/426 , A61K31/401 , C07D277/56
CPC分类号： C07D277/24
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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公开(公告)号：US20050058635A1
公开(公告)日：2005-03-17
申请号：US10839017
申请日：2004-05-05
IPC分类号： A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4745 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561 , A61K38/48
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： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing 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，这种效应物的筛选方法，以及包含这些效果子的这种效应物和药物组合物的用途，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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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。
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公开(公告)号：US07335645B2
公开(公告)日：2008-02-26
申请号：US11069926
申请日：2005-03-01
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。
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公开(公告)号：US07060719B2
公开(公告)日：2006-06-13
申请号：US10779158
申请日：2004-02-13
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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