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1. 发明申请

WO2013024043A2 IN VIVO SCREENING MODELS FOR TREATMENT OF QC-RELATED DISORDERS 审中-公开
标题翻译：模型体内筛选相关的疾病治疗QC
公开(公告)号：WO2013024043A2
公开(公告)日：2013-02-21
申请号：PCT/EP2012/065724
申请日：2012-08-10
申请人： PROBIODRUG AG , GRAUBNER, Sigrid , JAGLA, Wolfgang , SCHILLING, Stephan , CYNIS, Holger , HOFFMANN, Torsten , WERMANN, Michael , SCHULZ, Katrin , BAEUSCHER, Christoph , KOHLMANN, Stefanie , DEMUTH, Hans-Ulrich
发明人： GRAUBNER, Sigrid , JAGLA, Wolfgang , SCHILLING, Stephan , CYNIS, Holger , HOFFMANN, Torsten , WERMANN, Michael , SCHULZ, Katrin , BAEUSCHER, Christoph , KOHLMANN, Stefanie , DEMUTH, Hans-Ulrich
IPC分类号： C07K14/47 , C12N9/10 , A01K67/027
CPC分类号： A01K67/0278 , A01K2217/052 , A01K2217/15 , A01K2217/206 , A01K2227/105 , A01K2267/0312 , C07K14/4711 , C12N9/104
摘要： The present invention provides a double transgenic non-human animal, in particular a transgenic mouse encoding Qpct proteins, which have been implicated in Qpct-related diseases, and Amyloid Precursor Protein (APP). The present invention additionally provides cells and cell lines comprising transgenes encoding for Qpct and APP. The present invention further provides methods and compositions for evaluating agents that affect Qpct, for use in compositions for the treatment of Qpct-related diseases.
摘要翻译：本发明涉及一种双转基因非人动物，特别是编码蛋白质的转基因小鼠QPCT已在与QPCT相关的疾病有牵连，和淀粉样前体蛋白（APP）。本发明还涉及细胞和细胞系，其包含编码QPCT和APP转基因。本发明还涉及一种用于评估影响QPCT对于用于组合物用于治疗与QPCT相关的疾病的治疗剂的方法和组合物。

2. 发明申请

WO2008087197A1 IN VIVO SCREENING MODELS FOR TREATMENT OF ALZHEIMER'S DISEASE AND OTHER QPCT-RELATED DISORDERS 审中-公开
标题翻译：用于治疗阿尔茨海默病和其他与QPCT有关的疾病的生殖器筛查模型
公开(公告)号：WO2008087197A1
公开(公告)日：2008-07-24
申请号：PCT/EP2008/050532
申请日：2008-01-18
申请人： PROBIODRUG AG , SCHILLING, Stephan , CYNIS, Holger , HOFFMANN, Torsten , DEMUTH, Hans-Ulrich , WERMANN, Michael , SCHULZ, Katrin
发明人： SCHILLING, Stephan , CYNIS, Holger , HOFFMANN, Torsten , DEMUTH, Hans-Ulrich , WERMANN, Michael , SCHULZ, Katrin
IPC分类号： C12N15/85
CPC分类号： C12N15/8509 , A01K67/0275 , A01K2217/052 , A01K2267/0312 , A01K2267/0318 , C12N9/104
摘要： The present invention provides a transgenic non-human animal, in particular a transgenic mouse encoding Qpct proteins, which have been implicated in Qpct-related diseases. The present invention additionally provides cells and cell lines comprising transgenes encoding for Qpct. The present invention further provides methods and compositions for evaluating agents that affect Qpct, for use in compositions for the treatment of Qpct-related diseases.
摘要翻译：本发明提供了转基因非人动物，特别是编码Qpct蛋白的转基因小鼠，其涉及Qpct相关疾病。本发明另外提供了包含编码Qpct的转基因的细胞和细胞系。本发明还提供了用于评估影响Qpct的药剂的方法和组合物，用于治疗Qpct相关疾病的组合物。

3. 发明申请

WO2010026209A1 Use of isoQC inhibitors 审中-公开
标题翻译：使用isoQC抑制剂
公开(公告)号：WO2010026209A1
公开(公告)日：2010-03-11
申请号：PCT/EP2009/061440
申请日：2009-09-04
申请人： PROBIODRUG AG , DEMUTH, Hans-Ulrich , CYNIS, Holger , GANS, Kathrin , HOFFMANN, Torsten , KEHLEN, Astrid , RAHFELD, Jens-Ulrich , SCHILLING, Stephan , HEISER, Ulrich , WERMANN, Michael , FRIEDRICH, Daniel , GAERTNER, Ulf-Torsten , HAMANN, Antje , SOMMER, Robert , ALMSTETTER, Michael , TREML, Andreas , THORMANN, Michael
发明人： DEMUTH, Hans-Ulrich , CYNIS, Holger , GANS, Kathrin , HOFFMANN, Torsten , KEHLEN, Astrid , RAHFELD, Jens-Ulrich , SCHILLING, Stephan , HEISER, Ulrich , WERMANN, Michael , FRIEDRICH, Daniel , GAERTNER, Ulf-Torsten , HAMANN, Antje , SOMMER, Robert , ALMSTETTER, Michael , TREML, Andreas , THORMANN, Michael
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/433 , A61K31/437 , A61P29/00
CPC分类号： A61K31/4178 , A61K31/4184 , A61K31/433 , A61K31/437 , A61K45/06 , A61K2300/00
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 disorderselected 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-Barr 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转氨酶样蛋白（QPCTL）的抑制剂及其用于治疗和/或预防由慢性和急性炎症组成的组中选择的炎性疾病或病症的用途，例如类风湿性关节炎，动脉粥样硬化，再狭窄，胰腺炎等。神经性疼痛，移植物排斥反应/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，吉兰巴尔综合征，慢性炎症性脱髓鞘性多发性神经病和多发性硬化，神经炎症和神经退行性疾病。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。

4. 发明申请

WO2008104580A1 NEW USE OF GLUTAMINYL CYCLASE INHIBITORS 审中-公开
标题翻译：谷氨酰胺环化酶抑制剂的新用途
公开(公告)号：WO2008104580A1
公开(公告)日：2008-09-04
申请号：PCT/EP2008/052411
申请日：2008-02-28
申请人： PROBIODRUG AG , SCHILLING, Stephan , CYNIS, Holger , HOFFMANN, Torsten , DEMUTH, Hans-Ulrich
发明人： SCHILLING, Stephan , CYNIS, Holger , HOFFMANN, Torsten , DEMUTH, Hans-Ulrich
IPC分类号： A61K31/4164 , C07D233/54 , C07D235/06 , C07D403/12 , C07D405/12 , C07D417/12 , A61P25/28
CPC分类号： A61K31/4164 , C07D233/54 , C07D233/61 , C07D235/06 , C07D403/06 , C07D417/12
摘要： The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase, and use thereof for the treatment and/or prevention of a disease or disorder selected from the group consisting of inflammatory diseases selected from a. neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, Familial Danish Dementia, multiple sclerosis, b. chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, c. fibrosis, e.g. lung fibrosis, liver fibrosis, renal fibrosis, d. cancer, e.g. cancer/hemangioendothelioma proliferation, gastric carcinomas, e. metabolic diseases, e.g. hypertension, f. and other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis. Further, the invention relates to a respective diagnostic method, assay and kit.
摘要翻译：本发明一般涉及谷氨酰胺肽环转移酶的抑制剂及其用于治疗和/或预防选自以下的炎性疾病的疾病或病症的用途。神经变性疾病，例如轻度认知障碍（MCI），阿尔茨海默病，唐氏综合征神经变性，家族性英国痴呆，家族性丹麦痴呆，多发性硬化，b。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，c。纤维化，例如肺纤维化，肝纤维化，肾纤维化，d。癌症，例如癌症/血管内皮瘤增生，胃癌，e。代谢疾病，例如高血压，f。和其它炎性疾病，例如神经性疼痛，移植排斥/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。此外，本发明涉及相应的诊断方法，测定和试剂盒。

5. 发明申请

WO2005039548A2 USE OF EFFECTORS OF GLUTAMINYL AND GLUTAMATE CYCLASES 审中-公开
标题翻译：使用谷氨酰胺和谷氨酸周期的影响
公开(公告)号：WO2005039548A2
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011630
申请日：2004-10-15
申请人： PROBIODRUG AG , SCHILLING, Stephan , HOFFMANN, Torsten , NIESTROJ, André, Johannes , DEMUTH, Hans-Ulrich , HEISER, Ulrich
发明人： SCHILLING, Stephan , HOFFMANN, Torsten , NIESTROJ, André, Johannes , DEMUTH, Hans-Ulrich , HEISER, Ulrich
IPC分类号： A61K31/00
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。

6. 发明申请

WO2009090190A9 MOUSE MODELS CARRYING A KNOCK-OUT MUTATION OF THE GLUTAMINYL CYCLASE GENE 审中-公开
公开(公告)号：WO2009090190A9
公开(公告)日：2009-07-23
申请号：PCT/EP2009/050387
申请日：2009-01-14
申请人： PROBIODRUG AG , DEMUTH, Hans-Ulrich , HOFFMANN, Torsten , SCHILLING, Stephan
发明人： DEMUTH, Hans-Ulrich , HOFFMANN, Torsten , SCHILLING, Stephan
IPC分类号： C12N15/54 , C12N9/10 , C12N5/10 , A01K67/027 , A61K35/00 , G01N33/50
摘要： The present invention provides a knock-out non-human animal, in particular a mouse carrying a glutaminyl cyclase (EC 2.3.2.5) knock-out mutation. The present invention additionally provides the respective cells and cell lines and methods and compositions for evaluating agents that affect Qpct, for use in compositions for the treatment of Qpct-related diseases.

7. 发明申请

WO2004098625A3 MEDICAL USE OF INHIBITORS OF GLUTAMINYL AND GLUTAMATE CYCLASES 审中-公开
公开(公告)号：WO2004098625A3
公开(公告)日：2004-11-18
申请号：PCT/EP2004/004778
申请日：2004-05-05
申请人： PROBIODRUG AG , DEMUTH, Hans-Ulrich , HOFFMANN, Torsten , NIESTROJ, André, J. , SCHILLING, Stephan , HEISER, Ulrich
发明人： DEMUTH, Hans-Ulrich , HOFFMANN, Torsten , NIESTROJ, André, J. , SCHILLING, Stephan , HEISER, Ulrich
IPC分类号： A61K31/00
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 screeing 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.

8. 发明申请

WO2011029920A1 HETEROCYLCIC DERIVATIVES AS INHIBITORS OF GLUTAMINYL CYCLASE 审中-公开
标题翻译：作为谷氨酰胺环化酶抑制剂的杂环衍生物
公开(公告)号：WO2011029920A1
公开(公告)日：2011-03-17
申请号：PCT/EP2010/063341
申请日：2010-09-13
申请人： PROBIODRUG AG , HEISER, Ulrich , SOMMER, Robert , RAMSBECK, Daniel , MEYER, Antje , HOFFMANN, Torsten , BOEHME, Livia , DEMUTH, Hans-Ulrich
发明人： HEISER, Ulrich , SOMMER, Robert , RAMSBECK, Daniel , MEYER, Antje , HOFFMANN, Torsten , BOEHME, Livia , DEMUTH, Hans-Ulrich
IPC分类号： A61P25/00 , A61P25/28 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , A61K31/437 , A61K31/4184
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 R 1 , R 2 and R 3 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.
摘要翻译：本发明涉及式（I）的新型吡咯烷衍生物，其中R1，R2和R3如本文所定义，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。

9. 发明申请

WO2004099134A2 GLUTAMINYL BASED DP IV-INHIBITORS 审中-公开
标题翻译：基于谷氨酰胺的DP IV抑制剂
公开(公告)号：WO2004099134A2
公开(公告)日：2004-11-18
申请号：PCT/EP2004/004774
申请日：2004-05-05
申请人： PROSIDION LTD. , DEMUTH, Hans-Ulrich , HOFFMANN, Matthias , HOFFMANN, Torsten , NIESTROJ, André, J. , SCHILLING, Stephan , HEISER, Ulrich
发明人： DEMUTH, Hans-Ulrich , HOFFMANN, Matthias , HOFFMANN, Torsten , NIESTROJ, André, J. , SCHILLING, Stephan , HEISER, Ulrich
IPC分类号： C07D207/00
CPC分类号： C07D207/08 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D205/04 , C07D207/10 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/24 , C07D231/04 , C07D231/06 , C07D233/02 , C07D233/06 , C07D233/28 , C07D233/42 , C07D233/54 , C07D249/04 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/04 , C07D263/04 , C07D263/06 , C07D277/04 , C07D277/06 , C07D295/185 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07F9/5726 , C07F9/597 , C07F9/65066 , C07F9/6561
摘要： The present invention relates dipeptidyl peptidase IV inhibition and, more particularly, relates to glutaminyl derivatives, wherein the glutamin residue is bound in a peptide manner to a moiety which imitates the amino acid residue prolin, especially to a nitrogen containing moiety, pharmaceutical compositions containing said compounds, and the use of said compounds in inhibiting dipeptidyl peptidase IV and dipeptidyl peptidase IV -like enzyme activity.
摘要翻译：本发明涉及二肽基肽酶IV抑制，更具体地，涉及谷氨酰胺基衍生物，其中谷氨酰胺残基以肽的方式结合到模拟氨基酸残基脯氨酸，特别是含氮部分的部分，含有所述化合物，以及所述化合物在抑制二肽基肽酶IV和二肽基肽酶IV样酶活性中的用途。

10. 发明申请

WO2011107530A3 INHIBITORS OF GLUTAMINYL CYCLASE 审中-公开
公开(公告)号：WO2011107530A3
公开(公告)日：2011-09-09
申请号：PCT/EP2011/053154
申请日：2011-03-03
申请人： PROBIODRUG AG , HEISER, Ulrich , RAMSBECK, Daniel , HOFFMANN, Torsten , BOEHME, Livia , DEMUTH, Hans-Ulrich
发明人： HEISER, Ulrich , RAMSBECK, Daniel , HOFFMANN, Torsten , BOEHME, Livia , DEMUTH, Hans-Ulrich
IPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： The invention relates to 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.

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