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公开(公告)号：US08962860B2
公开(公告)日：2015-02-24
申请号：US12554611
申请日：2009-09-04
申请人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
发明人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
IPC分类号： C07D403/04 , C07D403/06 , C07D417/04 , C07D471/04 , C07D405/14 , C07D417/14
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.
摘要翻译： 通式（I）的化合物：其中R1，R2，R3，R4，X和Y如本文所定义，是谷氨酰胺酰环化酶的抑制剂，因此可用于治疗可通过调节谷氨酰胺酰环化酶活性治疗的病症。
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公开(公告)号：US20100119475A1
公开(公告)日：2010-05-13
申请号：US12554611
申请日：2009-09-04
申请人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
发明人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
IPC分类号： A61K31/4184 , C07D417/14 , C07D403/10 , C07D405/14 , C07D471/04 , A61K31/433 , A61K31/4439 , A61K39/395 , A61K38/20 , A61K38/21 , A61P35/00 , A61P3/00 , A61P25/00
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.
摘要翻译： 通式（I）的化合物：其中R1，R2，R3，R4，X和Y如本文所定义，是谷氨酰胺酰环化酶的抑制剂，因此可用于治疗可通过调节谷氨酰胺酰环化酶活性治疗的病症。
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3.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：US08269019B2
公开(公告)日：2012-09-18
申请号：US13044678
申请日：2011-03-10
IPC分类号： A61K31/4184 , C07D235/06 , C07D401/14
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14
摘要： Novel heterocyclic derivatives 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.
摘要翻译： 新型杂环衍生物作为谷氨酰胺酰环化酶的抑制剂（QC，EC 2.3.2.5）。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸（5-氧代 - 脯氨酰基，pGlu *）中的分子内环化，并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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公开(公告)号：US20110224254A1
公开(公告)日：2011-09-15
申请号：US13044678
申请日：2011-03-10
IPC分类号： A61K31/4709 , C07D403/10 , A61K31/4184 , C07D401/14 , A61K31/454 , A61P35/00 , A61P7/00 , A61P5/00 , A61P25/28 , A61P1/04
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14
摘要： Novel heterocyclic derivatives 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.
摘要翻译： 新型杂环衍生物作为谷氨酰胺酰环化酶的抑制剂（QC，EC 2.3.2.5）。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸（5-氧代 - 脯氨酰基，pGlu *）中的分子内环化，并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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7.发明授权Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase IV inhibitors 失效环丙基稠合吡咯烷衍生物作为二肽基肽酶IV抑制剂公开(公告)号：US07625939B2
公开(公告)日：2009-12-01
申请号：US12120595
申请日：2008-05-14
IPC分类号： A61K31/40 , C07D209/00
CPC分类号： C07F5/025
摘要： The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.
摘要翻译： 本发明涉及用于治疗和/或预防包括癌症和肿瘤在内的哺乳动物疾病，转移和肿瘤定植的式（1）的DP IV抑制剂; 和代谢疾病。
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公开(公告)号：US08420828B2
公开(公告)日：2013-04-16
申请号：US13547501
申请日：2012-07-12
IPC分类号： A61K31/4184 , C07D403/04
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14
摘要： Novel heterocyclic derivatives 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.
摘要翻译： 新型杂环衍生物作为谷氨酰胺酰环化酶的抑制剂（QC，EC 2.3.2.5）。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸（5-氧代 - 脯氨酰基，pGlu *）中的分子内环化，并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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公开(公告)号：US20120283259A1
公开(公告)日：2012-11-08
申请号：US13547501
申请日：2012-07-12
IPC分类号： C07D403/10 , C07D413/14 , A61K31/5377 , C07D401/14 , A61P1/18 , A61K31/4709 , A61P25/28 , A61P25/00 , A61P19/02 , A61P9/10 , A61K31/4184 , A61K31/454
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14
摘要： Novel heterocyclic derivatives 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.
摘要翻译： 新型杂环衍生物作为谷氨酰胺酰环化酶的抑制剂（QC，EC 2.3.2.5）。 QC在氨释放下催化N-末端谷氨酰胺残基在焦谷氨酸（5-氧代 - 脯氨酰基，pGlu *）中的分子内环化，并且在释放水下将N-末端谷氨酸残基分子内环化成焦谷氨酸。
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10.发明申请CYCLOPROPYL-FUSED PYRROLIDINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE IV INHIBITORS 失效作为DIPEPTIDYL PEPTIDASE IV抑制剂的环丙基 - 氟化吡咯烷衍生物公开(公告)号：US20080293618A1
公开(公告)日：2008-11-27
申请号：US12120595
申请日：2008-05-14
IPC分类号： A61K31/403 , C07D209/52 , A61K31/69 , A61K31/7088 , A61P3/00 , A61P35/00 , A61K38/28 , C07F5/02
CPC分类号： C07F5/025
摘要： The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.
摘要翻译： 本发明涉及用于治疗和/或预防包括癌症和肿瘤在内的哺乳动物疾病，转移和肿瘤定植的式（1）的DP IV抑制剂; 和代谢疾病。
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