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11. 发明授权

US08470781B2 Use of effectors of glutaminyl and glutamate cyclases 有权
标题翻译：使用谷氨酰胺和谷氨酸环化酶的效应物
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。

12. 发明申请

US20130052203A1 IN VIVO SCREENING MODELS FOR TREATMENT OF QC-RELATED DISORDERS 审中-公开
标题翻译：用于治疗与QC有关的疾病的生殖器筛查模型
公开(公告)号：US20130052203A1
公开(公告)日：2013-02-28
申请号：US13571947
申请日：2012-08-10
申请人： Sigrid Graubner , Wolfgang Jagla , Stephan Schilling , Holger Cynis , Hans-Ulrich Demuth , Torsten Hoffmann , Michael Wermann , Katrin Schulz , Christoph Baeuscher , Stefanie Kohlmann
发明人： Sigrid Graubner , Wolfgang Jagla , Stephan Schilling , Holger Cynis , Hans-Ulrich Demuth , Torsten Hoffmann , Michael Wermann , Katrin Schulz , Christoph Baeuscher , Stefanie Kohlmann
IPC分类号： A01K67/027 , A61K49/00 , C12N5/071 , C07K16/40 , A61K39/395 , A61P11/00 , A61P25/18 , A61P35/00 , A61P19/02 , A61P35/04 , A61P9/10 , A61P1/18 , A01K67/02 , A61P25/28
CPC分类号： A01K67/0278 , A01K2217/052 , A01K2217/15 , A01K2217/206 , A01K2227/105 , A01K2267/0312 , C07K14/4711 , C12N9/104
摘要： 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). Also provided are cells and cell lines comprising transgenes encoding for Qpct and APP. Also provided are methods and compositions for evaluating agents that affect Qpct, for use in compositions for the treatment of Qpct-related diseases.
摘要翻译：双重转基因非人动物，特别是编码Qpct蛋白的转基因小鼠，其涉及Qpct相关疾病，和淀粉样前体蛋白（APP）。还提供了包含编码Qpct和APP的转基因的细胞和细胞系。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。

13. 发明申请

US20110178055A1 DUAL NK1/NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：双NK1 / NK3受体拮抗剂
公开(公告)号：US20110178055A1
公开(公告)日：2011-07-21
申请号：US13076891
申请日：2011-03-31
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： A61K31/4427 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/551 , A61K31/5377 , A61P25/18
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译：本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。本发明还提供具有式I的新化合物和制备本发明化合物的方法。

14. 发明申请

US20110053954A1 METHOD OF TREATMENT AND/OR PREVENTION OF BRAIN, SPINAL OR NERVE INJURY 审中-公开
标题翻译：治疗和/或预防脑，脊髓或神经损伤的方法
公开(公告)号：US20110053954A1
公开(公告)日：2011-03-03
申请号：US12886691
申请日：2010-09-21
申请人： Torsten Hoffmann , Alan Nimmo , Andrew Sleight , Pierre Vankan , Robert Vink
发明人： Torsten Hoffmann , Alan Nimmo , Andrew Sleight , Pierre Vankan , Robert Vink
IPC分类号： A61K31/496 , A61P25/00
CPC分类号： A61K31/435
摘要： The invention relates to a method of treatment and/or prevention of brain, spinal or nerve injury comprising administration to a person in need of such treatment, of a therapeutically effective amount of an NK-1 receptor antagonist compound of the formula wherein the meanings of R, R1, R2, R2′, R3, and R4 are explained in the specification and the pharmaceutically acceptable acid addition salts and the prodrugs thereof either alone or in combination with a magnesium salt. Exemplified is the use of N-(3,5-bis-trifluoromethyl-benzyl)-N-methyl-6-(4-methyl-piperazin-1-yl)-4-o-tolyl-nicotinamide. The invention also relates to pharmaceutical composition comprising one or more such NK-1 receptor antagonists, optionally in combination with a magnesium salt, and a pharmaceutically acceptable excipient for the treatment and/or prevention of brain, spinal or nerve injury.
摘要翻译：本发明涉及一种治疗和/或预防脑，脊髓或神经损伤的方法，包括向需要这种治疗的人施用治疗有效量的下式的NK-1受体拮抗剂化合物，其中，说明书和其药学上可接受的酸加成盐及其前药单独或与镁盐组合说明了R，R 1，R 2，R 2'，R 3和R 4。举例说明了使用N-（3,5-双 - 三氟甲基 - 苄基）-N-甲基-6-（4-甲基 - 哌嗪-1-基）-4-邻甲苯基 - 烟酰胺。本发明还涉及包含一种或多种这样的NK-1受体拮抗剂，任选与镁盐组合的药物组合物和用于治疗和/或预防脑，脊髓或神经损伤的药学上可接受的赋形剂。

15. 发明申请

US20090183267A1 MOUSE MODELS CARRYING A KNOCK-OUT MUTATION OF THE QPCT-GENE 有权
标题翻译：携带QPCT基因的锁定突变的小鼠模型
公开(公告)号：US20090183267A1
公开(公告)日：2009-07-16
申请号：US12353463
申请日：2009-01-14
申请人： Stephan Schilling , Torsten Hoffmann , Hans-Ulrich Demuth
发明人： Stephan Schilling , Torsten Hoffmann , Hans-Ulrich Demuth
IPC分类号： G01N33/48 , A01K67/027 , C12Q1/68 , C12N5/10 , A61K38/16
CPC分类号： A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/03 , C12N9/104 , C12N15/8509 , C12N2800/30 , G01N2500/00 , G01N2800/2814
摘要： The present invention provides a knock-out non-human animal, in particular a mouse carrying a Qpct 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.
摘要翻译：本发明提供了敲除非人动物，特别是携带Qpct敲除突变的小鼠。本发明另外提供了用于评价影响Qpct的药剂的各种细胞和细胞系以及用于评估用于治疗Qpct相关疾病的组合物的方法和组合物。

16. 发明申请

US20090137806A1 DUAL NK1/NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：双NK1 / NK3受体拮抗剂
公开(公告)号：US20090137806A1
公开(公告)日：2009-05-28
申请号：US12361569
申请日：2009-01-29
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： C07D401/04 , C07D497/10
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译：本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。本发明还提供具有式I的新化合物和制备本发明化合物的方法。

17. 发明申请

US20080286810A1 Use of Inhibtors of Glutaminyl Cyclases for Treatment and Prevention of Disease 有权
标题翻译：谷氨酰胺酰化酶抑制剂用于治疗和预防疾病的应用
公开(公告)号：US20080286810A1
公开(公告)日：2008-11-20
申请号：US12101497
申请日：2008-04-11
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
IPC分类号： G01N33/53 , C12Q1/00
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： 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：哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新型生理底物，QC的新效应物，筛选此类效应物的方法，以及包含这些效应物的这种效应物和药物组合物的用途，用于治疗可由调节QC活性。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。

18. 发明申请

US20080267912A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：US20080267912A1
公开(公告)日：2008-10-30
申请号：US12105874
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
发明人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K38/20 , C07D233/54 , A61K31/4164 , A61K38/21 , A61P31/00 , A61P3/00 , A61P9/00 , A61P25/00 , A61P35/00 , A61K31/4178 , A61K39/395
CPC分类号： C07D233/61 , C07D233/64 , C07D235/06 , C07D405/12 , C07D417/12
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
摘要翻译：式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中：A表示和B，R 1，R R 3，R 4，R 4，R 5，R 6和Z 3，在整个说明书和权利要求书中都是定义的。

19. 发明申请

US20060293248A1 Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents 失效
公开(公告)号：US20060293248A1
公开(公告)日：2006-12-28
申请号：US11481349
申请日：2006-07-05
申请人： Stephen von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
发明人： Stephen von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
IPC分类号： A61K38/04 , A61K31/426 , A61K31/401
CPC分类号： A61K31/401 , A61K31/426 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/55
摘要： The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of metastasis and tumor colonization.

20. 发明授权

US07109347B2 Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents 失效
公开(公告)号：US07109347B2
公开(公告)日：2006-09-19
申请号：US11093991
申请日：2005-03-30
申请人： Stephan von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
发明人： Stephan von Hoersten , Hans-Ulrich Demuth , Torsten Hoffmann
IPC分类号： C07D277/04 , C07D277/16 , C07D277/18 , C07D207/00 , C07D295/00 , C07D291/00 , C07D291/02 , C07D291/04
CPC分类号： A61K31/401 , A61K31/426 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/55
摘要： The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of metastasis and tumor colonization.

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