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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.发明授权公开(公告)号：US07732162B2
公开(公告)日：2010-06-08
申请号：US11685881
申请日：2007-03-14
申请人： Torsten Hoffman , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffman , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： C12Q1/34
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
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 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： 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，用于筛选此类效应物的方法，以及使用这些效应物和包含这些效应物的药物组合物，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：US08338120B2
公开(公告)日：2012-12-25
申请号：US12039066
申请日：2008-02-28
IPC分类号： C12Q1/34
CPC分类号： A61K31/4178 , A61K31/4184 , C07D231/12 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04
摘要： Provided herein are methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis and pancreatitis.
摘要翻译： 本文提供了通过施用谷氨酰胺肽环转移酶的抑制剂来治疗和/或预防炎性疾病或病症的方法。 通过本文公开的方法治疗或预防的炎性疾病或病症包括轻度认知障碍（MCI），类风湿性关节炎，动脉粥样硬化，再狭窄和胰腺炎。
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5.发明申请METHODS OF TREATING OR PREVENTING AN INFLAMMATORY DISEASE OR CONDITION USING GLUTAMINYL CYCLASE INHIBITORS 审中-公开使用谷氨酰胺环化酶抑制剂治疗或预防炎性疾病或病症的方法公开(公告)号：US20120184518A1
公开(公告)日：2012-07-19
申请号：US13354971
申请日：2012-01-20
IPC分类号： A61K31/56 , G01N33/566 , A61K31/5415 , A61K31/5377 , A61K31/517 , A61K31/454 , A61K31/428 , A61K31/422 , A61K31/4184 , A61K31/4164 , C07D417/12 , C07D413/02 , C07D403/06 , C07D401/02 , C07D235/04 , C07D233/54 , A61P29/00 , A61P19/02 , A61P9/10 , A61P1/18 , A61P25/16 , A61P25/24 , A61P25/18 , A61P25/00 , C07D405/12 , G01N33/567
CPC分类号： C07D231/12 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/517 , A61K31/5415 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04
摘要： Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.
摘要翻译： 通过施用谷氨酰胺肽转移酶抑制剂来治疗和/或预防炎性疾病或病症的方法。 通过本文公开的方法治疗或预防的炎性疾病或病症包括轻度认知障碍（MCI），类风湿性关节炎，动脉粥样硬化，再狭窄，胰腺炎，败血症和peritonitus。 进一步提供了各自的诊断方法，测定和试剂盒。
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公开(公告)号：US20120165393A1
公开(公告)日：2012-06-28
申请号：US13326433
申请日：2011-12-15
申请人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffman , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
发明人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffman , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
CPC分类号： A61K47/48261 , A61K47/549 , A61K47/64 , A61K47/6415 , C12N15/111 , C12N2310/14 , C12N2310/351 , C12N2310/3515 , C12N2320/32
摘要： The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.
摘要翻译： 本发明涉及用于将体内RNA干扰（RNAi）多核苷酸靶向递送至肝细胞的组合物。 靶向的RNAi多核苷酸与共靶向的蜂毒肽递送肽一起施用。 递送肽提供膜穿透功能，用于将RNAi多核苷酸从细胞外部移动到细胞内。 可逆修饰提供对递送肽的生理反应性。
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