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公开(公告)号：US07053055B2
公开(公告)日：2006-05-30
申请号：US09745883
申请日：2000-12-21
CPC分类号： C07K5/0808 , A61K38/00
摘要： Novel compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The 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的不稳定抑制剂的新型化合物用于治疗各种疾病，特别是代谢紊乱。 该化合物可用于治疗葡萄糖耐量异常，葡萄糖尿，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病和肾病。
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2.发明授权Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis 失效二肽基肽酶IV抑制剂在多发性硬化症的治疗中的应用公开(公告)号：US07368421B2
公开(公告)日：2008-05-06
申请号：US10126374
申请日：2002-04-19
IPC分类号： A61K38/00 , A61K38/02 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08 , C07K2/00 , C07K7/04 , C07K5/02 , C07K5/08 , C07K5/10
CPC分类号： C07K7/06 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D277/04 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The present invention provides a new use of DP IV-inhibitors. The compounds of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in treating conditions mediated by DP IV or DP IV-like enzymes, such as immune, autoimmune or central nervous system disorder selected from the group consisting of strokes, tumors, ischemia, Parkinson's disease and migraines. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of multiple sclerosis.
摘要翻译： 本发明提供DPIV-抑制剂的新用途。 本发明的化合物及其相应的药学上可接受的酸加成盐形式可用于治疗由DP IV或DP IV样酶介导的病症，例如免疫，自身免疫或中枢神经系统疾病，其选自中风 ，肿瘤，局部缺血，帕金森病和偏头痛。 在更优选的实施方案中，本发明的化合物可用于治疗多发性硬化。
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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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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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5.发明授权公开(公告)号：US07368576B2
公开(公告)日：2008-05-06
申请号：US11481349
申请日：2006-07-05
IPC分类号： C07D277/04 , C07D277/16 , C07D277/18 , C07D291/02 , C07D291/04
CPC分类号： A61K31/401 , A61K31/426 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/55
摘要： The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of metastasis and tumor colonization.
摘要翻译： 本发明提供本发明的DPIV-抑制剂及其相应的药学上可接受的酸加成盐形式的新用途，用于治疗由DPIV或DPIV样酶如癌和肿瘤介导的病症。 在更优选的实施方案中，本发明的化合物可用于治疗转移和肿瘤定植。
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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：US07166579B2
公开(公告)日：2007-01-23
申请号：US10735582
申请日：2003-12-11
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。
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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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公开(公告)号：US20050014946A1
公开(公告)日：2005-01-20
申请号：US10914261
申请日：2004-08-09
IPC分类号： A61K31/4439 , A61K31/4709 , A61K31/675 , C07D211/82 , C07D217/12 , C07F9/28
CPC分类号： A61K31/4439 , A61K31/4709 , A61K31/675 , C07D211/82 , C07D217/12 , C07F9/28
摘要： The present invention relates to compounds of the general formula I B—(CH—R1)n—C(═X2)-D (I) and pharmaceutically acceptable salts thereof including stereoisomers, 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I B-（CH-R 1）n C（= X 2）-D（I）的化合物及其药学上可接受的盐，包括立体异构体，用于 治疗糖耐量异常，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哺乳动物糖尿病引起的后遗症。
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10.发明授权Raising blood sugar level in hypoglycemic mammals by administering inhibitors of dipeptidyl peptidase IV 有权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
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。
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