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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：US20060100253A1
公开(公告)日：2006-05-11
申请号：US11290735
申请日：2005-11-30
申请人： Andre Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
发明人： Andre Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
IPC分类号： A61K31/427 , C07D417/14
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的脯氨酰内肽酶的新型抑制剂<？in-line-formula description =“In-line Formulas”end =“lead”→> W-KCONH-X-CON-Y-CO-Z ）<？in-line-formula description =“In-line Formulas”end =“tail”？>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：US20100099721A1
公开(公告)日：2010-04-22
申请号：US12646111
申请日：2009-12-23
申请人： André J. Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
发明人： André J. Niestroj , Ulrich Heiser , Ingo Schulz , Jens-Ulrich Rahfeld , Joachim Baer , Hans-Ulrich Demuth
IPC分类号： A61K31/428 , A61K31/426 , A61K31/4025 , A61P25/00 , A61P9/10 , A61P7/00
CPC分类号： A61K31/4025 , A61K31/426 , A61K31/428 , A61K45/06 , A61K2300/00
摘要： 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： 式1中的脯氨酰内肽酶的抑制剂W-KCONH-X-CON-Y-CO-Z（1）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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4.发明授权Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions 有权使用isoQC抑制剂治疗和预防炎性疾病或病症公开(公告)号：US08889709B2
公开(公告)日：2014-11-18
申请号：US12554584
申请日：2009-09-04
申请人： Hans-Ulrich Demuth , Stephan Schilling , Michael Wermann , Holger Cynis , Astrid Kehlen , Daniel Friedrich , Torsten Hoffmann , Kathrin Gans , Jens-Ulrich Rahfeld , Ulrich Heiser , Michael Almstetter , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Thormann , Andreas Treml
发明人： Hans-Ulrich Demuth , Stephan Schilling , Michael Wermann , Holger Cynis , Astrid Kehlen , Daniel Friedrich , Torsten Hoffmann , Kathrin Gans , Jens-Ulrich Rahfeld , Ulrich Heiser , Michael Almstetter , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Thormann , Andreas Treml
IPC分类号： A01N43/42 , C12N9/00 , C12N9/10 , C12N1/20 , C12N15/00 , C07H21/04 , C07D417/12 , C07D405/12 , C07D233/61 , C07D409/12 , C07D403/12 , C07D413/12 , C07D403/06 , C07D401/12 , C07D233/54 , C07D235/06
CPC分类号： C07D233/54 , C07D233/61 , C07D235/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C12N9/104
摘要： The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinizing polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.
摘要翻译： 本发明一般涉及谷氨酰胺肽环转移酶样蛋白（QPCTL）的抑制剂及其用于治疗和/或预防炎性疾病或病症的用途，所述炎性疾病或病症选自（a）慢性和急性 炎症，例如 类风湿关节炎，动脉粥样硬化，再狭窄，胰腺炎; （b）其他炎性疾病，例如 艾滋病，睾丸炎，结节性硬化症，吉兰巴利综合征，慢性炎性脱髓鞘性多发性神经系统疾病和多发性硬化; （c）神经炎症; 和（d）神经变性疾病，例如 轻度认知障碍（MCI），阿尔茨海默氏症，唐氏综合征神经变性，家族性英国痴呆和家族性丹麦痴呆，可能由神经炎症引起。
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公开(公告)号：US20100125086A1
公开(公告)日：2010-05-20
申请号：US12554584
申请日：2009-09-04
申请人： Hans-Ulrich Demuth , Stephan Schilling , Michael Wermann , Holger Cynis , Astrid Kehlen , Daniel Friedrich , Torsten Hoffmann , Kathrin Gans , Jens-Ulrich Rahfeld , Ulrich Heiser , Michael Almstetter , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Thormann , Andreas Tremel
发明人： Hans-Ulrich Demuth , Stephan Schilling , Michael Wermann , Holger Cynis , Astrid Kehlen , Daniel Friedrich , Torsten Hoffmann , Kathrin Gans , Jens-Ulrich Rahfeld , Ulrich Heiser , Michael Almstetter , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Thormann , Andreas Tremel
IPC分类号： A61K31/4178 , C12Q1/25 , A61K31/437 , A61K31/433 , A61K31/4184 , A61P29/00
CPC分类号： C07D233/54 , C07D233/61 , C07D235/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C12N9/104
摘要： The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.
摘要翻译： 本发明一般涉及谷氨酰胺肽环转移酶样蛋白（QPCTL）的抑制剂及其用于治疗和/或预防炎性疾病或病症的用途，所述炎性疾病或病症选自（a）慢性和急性 炎症，例如 类风湿关节炎，动脉粥样硬化，再狭窄，胰腺炎; （b）其他炎性疾病，例如 神经性疼痛，移植物排斥/移植物衰竭/移植物血管病变，HIV感染/艾滋病，睾丸炎，结节性硬化症，吉兰巴利综合征，慢性炎症性脱髓鞘性多发性神经病和多发性硬化症; （c）神经炎症; 和（d）神经变性疾病，例如 轻度认知障碍（MCI），阿尔茨海默氏症，唐氏综合征神经变性，家族性英国痴呆和家族性丹麦痴呆，可能由神经炎症引起。
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公开(公告)号：US07279550B2
公开(公告)日：2007-10-09
申请号：US10485723
申请日：2002-07-23
IPC分类号： C07K5/023 , C07F9/28 , C07C229/26
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0806
摘要： Presented are compounds represented by the following general formulas (I) and (II), for inhibiting cysteine protease legumain for modulating associated disease states in subjects
摘要翻译： 提出的是由以下通式（I）和（II）表示的化合物，用于抑制半胱氨酸蛋白酶调节因子用于调节受试者的相关疾病状态
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公开(公告)号：US20100159032A1
公开(公告)日：2010-06-24
申请号：US12630760
申请日：2009-12-03
申请人： Ingo Schulz , Stephan Schilling , Hans-Ulrich Demuth , Ulrich Heiser , Andre Johannes Niestroj , Steffen Rossner
发明人： Ingo Schulz , Stephan Schilling , Hans-Ulrich Demuth , Ulrich Heiser , Andre Johannes Niestroj , Steffen Rossner
IPC分类号： A61K33/14 , A61K31/335 , A61K38/05 , A61K31/16 , A61K31/27 , A61P25/28 , A61P25/16 , A61P25/18 , A61P3/04 , A61P25/20 , A61P3/00 , A61P5/00 , A61P9/12 , A61P29/00 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/30 , A61P25/32 , A61K31/4985
CPC分类号： A61K31/00 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K38/04 , A61K2300/00
摘要： The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, LiCl, inhibitors of DP IV/DP IV-like enzymes, NPY-receptor ligands, NPY agonists, NPY antagonists, ACE-inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases and inhibitors of neutral endopeptidase, to a mammal in need thereof.
摘要翻译： 本发明提供在哺乳动物例如人中治疗神经元疾病的方法，该方法包括施用有效的，无毒的和药学上可接受量的至少一种QC抑制剂，任选地与至少一种 选自PEP抑制剂，LiCl，DP IV / DP IV类酶的抑制剂，NPY受体配体，NPY激动剂，NPY拮抗剂，ACE抑制剂，PIMT增强剂，β分泌酶抑制剂，抑制剂 γ-分泌酶和中性肽链内切酶抑制剂。
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公开(公告)号：US20050171112A1
公开(公告)日：2005-08-04
申请号：US11002169
申请日：2004-12-02
申请人： Ingo Schulz , Stephan Schilling , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth , Steffen Rossner
发明人： Ingo Schulz , Stephan Schilling , Andre Niestroj , Ulrich Heiser , Hans-Ulrich Demuth , Steffen Rossner
IPC分类号： A61K31/00 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K38/04
CPC分类号： A61K31/00 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/473 , A61K31/498 , A61K38/04 , A61K2300/00
摘要： The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, LiCl, inhibitors of DP IV/DP IV-like enzymes, NPY-receptor ligands, NPY agonists, NPY antagonists, ACE-inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases and inhibitors of neutral endopeptidase, to a mammal in need thereof.
摘要翻译： 本发明提供在哺乳动物例如人中治疗神经元疾病的方法，该方法包括施用有效的，无毒的和药学上可接受量的至少一种QC抑制剂，任选地与至少一种 选自PEP抑制剂，LiCl，DP IV / DP IV类酶的抑制剂，NPY受体配体，NPY激动剂，NPY拮抗剂，ACE抑制剂，PIMT增强剂，β分泌酶抑制剂，抑制剂 γ-分泌酶和中性肽链内切酶抑制剂。
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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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公开(公告)号：US07592467B2
公开(公告)日：2009-09-22
申请号：US11400582
申请日：2006-04-07
IPC分类号： C07D333/12 , C07D333/22 , C07D307/46 , A61K31/341 , A61K31/381
CPC分类号： C07D409/12 , C07D307/46 , C07D333/22 , C07D333/56
摘要： The present invention relates to novel inhibitors of prolyl endopeptidase of formula (1) wherein I, A, 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）的脯氨酰内肽酶的新型抑制剂，其中I，A，X，Y和Z在说明书中具体规定。 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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