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1.发明授权Use of dipeptidyl peptidase IV effectors for lowering the blood glucose level in mammals 有权使用二肽基肽酶IV效应物降低哺乳动物血糖水平公开(公告)号：US06303661B1
公开(公告)日：2001-10-16
申请号：US09155833
申请日：1998-10-06
申请人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert P. Pauly , Christopher H. S. McIntosh , Ray A. Pederson
发明人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert P. Pauly , Christopher H. S. McIntosh , Ray A. Pederson
IPC分类号： A61K3848
CPC分类号： A61K31/401 , A61K31/00 , A61K31/40 , A61K31/426
摘要： Novel therapeutic regimens are provided which comprise the administration of therapeutically effective amounts of an inhibitor to dipeptidyl peptidase (DP-IV) or enzymes of similar activity whereby their ability to degrade the incretins, GLP-1 and GIP, is reduced. As a result hyperglycemia, such as that accompanying food intake may be reduced due to improved insulin release. A preferred therapeutic regimen amongst a number of routes of administration and inhibitors that may be used comprises the oral administration of isoleucyl thiazolidine.
摘要翻译： 提供了新的治疗方案，其包括向二肽基肽酶（DP-IV）或类似活性的酶施用治疗有效量的抑制剂，由此降低肠降胰醇素GLP-1和GIP的降解能力。 因此，由于改善的胰岛素释放，可能会降低伴随食物摄入的高血糖症。 可以使用的许多给药途径和抑制剂中优选的治疗方案包括口服给予异亮氨酰基噻唑烷。
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2.发明申请Use of Dipeptidyl Peptidase IV Effectors for Normalizing the Blood Glucose Level in Mammals 审中-公开使用二肽基肽酶IV效应物来调节哺乳动物血糖水平公开(公告)号：US20130116290A1
公开(公告)日：2013-05-09
申请号：US13458484
申请日：2012-04-27
申请人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert P. Pauly , Christopher H.S. McIntosh , Ray A. Pederson
发明人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert P. Pauly , Christopher H.S. McIntosh , Ray A. Pederson
IPC分类号： A61K31/426
CPC分类号： A61K31/426 , A61K9/0019 , A61K9/0053 , A61K31/00 , A61K31/40 , A61K31/401
摘要： The present invention comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to lower elevated post-prandial and basal blood glucose levels in mammalian organisms. The invention further comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to increase the half-life of incretins in vivo.
摘要翻译： 本发明包括使用哺乳动物血液中二肽基肽酶（DP IV）的活性降低作用剂和DP IV类似酶活性降低哺乳动物生物体内升高的餐后和基础血糖水平。 本发明还包括在哺乳动物的血液中使用二肽基肽酶（DP IV）的活性降低效应物和DP IV-类似酶活性以增加体内胰岛素的半衰期。
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3.发明申请Use of dipeptidyl peptidase IV effectors for normalizing the blood glucose level in mammals 审中-公开使用二肽基肽酶IV效应物来标准化哺乳动物的血糖水平公开(公告)号：US20050107309A1
公开(公告)日：2005-05-19
申请号：US11022087
申请日：2004-12-22
申请人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert Pauly , Christopher McIntosh , Ray Pederson
发明人： Hans-Ulrich Demuth , Fred Rosche , Joem Schmidt , Robert Pauly , Christopher McIntosh , Ray Pederson
IPC分类号： C07D277/04 , A61K31/00 , A61K31/40 , A61K31/401 , A61K31/425 , A61K31/426 , A61K38/00 , A61K38/46 , A61K38/55 , A61K39/395 , A61K45/00 , A61P3/06 , A61P3/10 , A61P9/12 , A61P43/00 , C07D295/18 , A61K31/675 , A61K31/69 , A61K38/04
CPC分类号： A61K31/426 , A61K9/0019 , A61K9/0053 , A61K31/00 , A61K31/40 , A61K31/401
摘要： The present invention comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to lower elevated post-prandial and basal blood glucose levels in mammalian organisms. The invention further comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to increase the half-life of incretins in vivo.
摘要翻译： 本发明包括使用哺乳动物血液中二肽基肽酶（DP IV）的活性降低作用剂和DP IV类似酶活性降低哺乳动物生物体内升高的餐后和基础血糖水平。 本发明还包括在哺乳动物的血液中使用二肽基肽酶（DP IV）的活性降低效应物和DP IV-类似酶活性以增加体内胰岛素的半衰期。
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4.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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公开(公告)号：US20140255414A1
公开(公告)日：2014-09-11
申请号：US14280919
申请日：2014-05-19
申请人： Martin Kleinschmidt , Stephan Schilling , Jens-Ulrich Rahfeld , Kristin Ebermann , Hans-Ulrich Demuth
发明人： Martin Kleinschmidt , Stephan Schilling , Jens-Ulrich Rahfeld , Kristin Ebermann , Hans-Ulrich Demuth
CPC分类号： C07K16/18 , A61K39/3955 , A61K2039/505 , C07K2317/24 , C07K2317/56 , C07K2317/92 , G01N33/6896 , G01N2333/4709 , G01N2800/2821
摘要： Novel diagnostic assays for the diagnosis of amyloidosis, in particular Alzheimer's disease, and related aspects. In particular, monoclonal antibodies and an antibody assay are provided.
摘要翻译： 用于诊断淀粉样变性，特别是阿尔茨海默病的新型诊断测定法和相关方面。 特别地，提供单克隆抗体和抗体测定。
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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：US20120070444A1
公开(公告)日：2012-03-22
申请号：US13225033
申请日：2011-09-02
申请人： Sigrid Graubner , Reinhard Sedlmeier , Andreas Becker , Stephan Schilling , Holger Cynis , Hans-Ulrich Demuth
发明人： Sigrid Graubner , Reinhard Sedlmeier , Andreas Becker , Stephan Schilling , Holger Cynis , Hans-Ulrich Demuth
IPC分类号： A61K38/45 , C07K16/00 , A61K49/00 , A01K67/027 , A61P1/04 , A61P25/00 , A61P25/28 , A61P35/00 , A61P31/04 , A61P25/18 , A61P15/00 , A61P29/00 , A61P35/04 , A61P17/06 , A61P11/00 , A61P1/16 , A61P3/00 , A61P5/00 , C12N5/10
CPC分类号： A01K67/0278 , A01K67/0275 , A01K2217/052 , A01K2217/15 , A01K2217/206 , A01K2227/105 , A01K2267/0312 , A01K2267/0318 , C12N9/104 , C12N15/8509 , C12Y203/02005 , G01N33/5088 , G01N2333/9108 , G01N2500/10
摘要： A transgenic non-human animal for overexpressing isoQC, comprising cells containing a DNA transgene encoding human isoQC, characterized in that said human isoQC comprises the amino acid sequence of SEQ ID NO: 1 or an amino acid sequence having at least 75% sequence identity to the amino acid sequence of SEQ ID NO: 1 or a fragment or derivative of the amino acid sequence of SEQ ID NO: 1. Additionally disclosed is a method of screening for biologically active agents that inhibit or promote isoQC.
摘要翻译： 一种用于过表达isoQC的转基因非人动物，其包含含有编码人isoQC的DNA转基因的细胞，其特征在于所述人isoQC包含SEQ ID NO：1的氨基酸序列或与SEQ ID NO：1的氨基酸序列具有至少75％ SEQ ID NO：1的氨基酸序列或SEQ ID NO：1的氨基酸序列的片段或衍生物。另外公开了筛选抑制或促进isoQC的生物活性剂的方法。
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公开(公告)号：US20110091910A1
公开(公告)日：2011-04-21
申请号：US12884403
申请日：2010-09-17
IPC分类号： G01N33/566
CPC分类号： G01N33/6896 , G01N2333/4709 , G01N2800/2821
摘要： A novel method for detection of Aβ peptides, in particular in plasma, and to the use of Aβ peptides for diagnosis of Alzheimer's disease.
摘要翻译： 一种新的A＆Bgr检测方法 肽，特别是血浆中的肽，以及使用A＆bgr; 用于诊断阿尔茨海默氏病的肽。
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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。
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公开(公告)号：US20100009337A1
公开(公告)日：2010-01-14
申请号：US12497082
申请日：2009-07-02
IPC分类号： C12Q1/00
CPC分类号： C12N9/104 , C07D233/54 , C07D233/61 , C07D235/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Novel glutaminyl-peptide cyclotransferase-like proteins (QPCTLs), which are isoenzymes of glutaminyl cyclase (QC, EC 2.3.2.5), and to isolated nucleic acids coding for these isoenzymes, all of which are useful for the discovery of new therapeutic agents, for measuring cyclase activity, and for determining the inhibitory activity of compounds against these glutaminyl cyclase isoenzymes.
摘要翻译： 作为谷氨酰胺环化酶同功酶（QC，EC 2.3.2.5）的新型谷氨酰胺肽 - 转移酶样蛋白（QPCTL），以及编码这些同工酶的分离的核酸，所有这些都可用于发现新的治疗剂， 用于测定环化酶活性，以及测定化合物对这些谷氨酰胺环化酶同工酶的抑制活性。
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