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1. 发明申请

WO2008065141A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 审中-公开
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：WO2008065141A1
公开(公告)日：2008-06-05
申请号：PCT/EP2007/062953
申请日：2007-11-28
申请人： PROBIODRUG AG , BUCHHOLZ, Mirko , NIESTROJ, André, J. , HEISER, Ulrich , RAMSBECK, Daniel , SCHILLING, Stephan
发明人： BUCHHOLZ, Mirko , NIESTROJ, André, J. , HEISER, Ulrich , RAMSBECK, Daniel , SCHILLING, Stephan
IPC分类号： C07D413/04 , A61K31/4184 , A61K31/4245
CPC分类号： C07D413/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, Formula (I) wherein R 1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R 2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR 3 ; R 3 represents H or C 1-4 alkyl.
摘要翻译：本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，式（I）其中R 1表示杂芳基， - 碳环基 - 杂芳基， - 烯基杂芳基或 - 烷基杂芳基; R 2表示烷基; 可任意被烷基取代的碳环基; 烯基; 炔基，条件是三键不与X相邻; 烷基 - 芳基; 烷基 - 杂芳基; - 烷基 - 杂环基，其中杂环基可以任选被烷基取代; - 烷基 - 碳环基，其中碳环基可以任选地被烷基取代; 芳基; 杂; 或H; X表示S或NR 3; R 3表示H或C 1-4烷基。

2. 发明申请

WO2008110523A1 IMIDAZO [1,5-A] PYRIDINE 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咪唑并[1,5-A]吡啶衍生物
公开(公告)号：WO2008110523A1
公开(公告)日：2008-09-18
申请号：PCT/EP2008/052799
申请日：2008-03-10
申请人： PROBIODRUG AG , BUCHHOLZ, Mirko , HEISER, Ulrich , NIESTROJ, André J. , RAMSBECK, Daniel
发明人： BUCHHOLZ, Mirko , HEISER, Ulrich , NIESTROJ, André J. , RAMSBECK, Daniel
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28 , A61P25/14
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoisomers and polymorphs thereof wherein: R 1 represents C 2-8 alkyl; C 2-8 alkenyl; -(C 1-6 alkyl)-aryl; -(C 1-6 alkyl)-heteroaryl; -(C 1-6 alkyl)- carbocyclyl; -(C 1-6 alky)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C 1-4 alkyl, C 1-4 fluoroalkyl, C 1-4 alkoxy, C 1-4 fluoroalkoxy, hydroxy, -SO 2 (C 1-4 alkyl), -SO 2 N(C 1-4 alkyl)(C 1-4 alkyl), -SOC 1-4 alkyl, -SOC 3-6 cycloalkyl -C(O)O(C 1-4 alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from -C 1-4 alkyl, -C 1-4 alkoxy, hydroxyl, halogen and oxo; R 2 represents H; C 1-4 alkyl or halogen; R 3 represents H; C 1-4 alkyl or halogen; and R 4 represents H; C 1-4 alkyl or halogen.
摘要翻译：本发明涉及式（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或溶剂化物，包括所有互变异构体，立体异构体和多晶型物，其中：R 1表示C _{2-8 烷基; ç_{2-8 烯基; - （C _{1-6 烷基） - 芳基; - （C _{1-6 烷基） - 杂芳基; - （C 1-6烷基） - 碳环基; - （C _{1-6 烷基） - 杂环基; 芳基; - 杂芳基; 碳环基或杂环基; 其中所述芳基或杂芳基可以任选地被一个或多个选自C 1-4 - 烷基，C 1-4 - 烷基，C 1-4 - 4烷氧基，C 1-4卤代烷氧基，羟基，-SO 2（C 1-4烷基），-SO 3 - （C 1-4烷基）（C 1-4烷基），-SOC 1-4烷基（C 1-4烷基），-SOC 3-6环烷基-C（O）O（C 1-4烷基），苄氧基和苯基; 并且其中所述碳环基和杂环基可任选地被一个或多个选自-C 1-4烷基，-C 1-4烷氧基，羟基，卤素和氧; R 2表示H; C 1-4烷基或卤素; R 3表示H; C 1-4烷基或卤素; R 4表示H; C 1-4烷基或卤素。}}}}}

3. 发明申请

WO2012123563A1 BENZ IMIDAZOLE 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苯并咪唑衍生物
公开(公告)号：WO2012123563A1
公开(公告)日：2012-09-20
申请号：PCT/EP2012/054631
申请日：2012-03-16
申请人： PROBIODRUG AG , HEISER, Ulrich , RAMSBECK, Daniel
发明人： HEISER, Ulrich , RAMSBECK, Daniel
IPC分类号： C07D401/14 , C07D403/04 , C07D413/14 , C07D417/14 , A61K31/4184 , A61P25/28
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/4409 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K38/2026 , A61K38/21 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： The invention relates to novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R a , n, R 1 and R 2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
摘要翻译：本发明涉及式（I）的新型杂环衍生物：或其药学上可接受的盐，溶剂化物或多晶型物，包括其所有互变异构体和立体异构体，其中R a，n，R 1和R 2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）。

4. 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。

5. 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.

6. 发明申请

WO2012163773A1 RADIOLABELLED GLUTAMINYL CYCLASE INHIBITORS 审中-公开
标题翻译：无定形谷氨酰胺环化酶抑制剂
公开(公告)号：WO2012163773A1
公开(公告)日：2012-12-06
申请号：PCT/EP2012/059649
申请日：2012-05-24
申请人： PROBIODRUG AG , HEISER, Ulrich , RAMSBECK, Daniel , DEMUTH, Hans-Ulrich
发明人： HEISER, Ulrich , RAMSBECK, Daniel , DEMUTH, Hans-Ulrich
IPC分类号： A61K51/04 , A61K101/00
CPC分类号： A61K51/0453 , C07B59/002
摘要： The invention relates to the use of radiolabelled glutaminyl cyclase (QC) inhibitors as imaging agents, in particular but not exclusively as medical imaging agents for the detection of neurological disorders. The invention also relates to pharmaceutical compositions comprising said radiolabelled inhibitors and to methods and kits for detecting neurological disorders.
摘要翻译：本发明涉及放射性标记的谷氨酰胺环化酶（QC）抑制剂作为显像剂的用途，特别但不排他地用作用于检测神经障碍的医学成像剂。本发明还涉及包含所述放射性标记的抑制剂的药物组合物和用于检测神经障碍的方法和试剂盒。

7. 发明申请

WO2011131748A2 NOVEL INHIBITORS 审中-公开
标题翻译：新型抑制剂
公开(公告)号：WO2011131748A2
公开(公告)日：2011-10-27
申请号：PCT/EP2011/056396
申请日：2011-04-21
申请人： PROBIODRUG AG , HEISER, Ulrich , RAMSBECK, Daniel , HOFFMANN, Torsten , BOEHME, Livia
发明人： HEISER, Ulrich , RAMSBECK, Daniel , HOFFMANN, Torsten , BOEHME, Livia
IPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14 , A61K31/4184 , A61P25/00
CPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
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.
摘要翻译：本发明涉及作为谷氨酰胺酰环化酶抑制剂的新型杂环衍生物（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。

8. 发明授权

EP2560953B1 INHIBITORS OF GLUTAMINYL CYCLASE 有权转让
标题翻译：谷氨酰胺的抑制剂
公开(公告)号：EP2560953B1
公开(公告)日：2016-01-06
申请号：EP11715924.4
申请日：2011-04-21
申请人： Probiodrug AG
发明人： HEISER, Ulrich , RAMSBECK, Daniel , HOFFMANN, Torsten , BOEHME, Livia
IPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14 , A61K31/4184 , A61P25/00
CPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14

9. 发明公开

EP2560953A2 NOVEL INHIBITORS 有权转让
标题翻译：谷氨酰胺的抑制剂
公开(公告)号：EP2560953A2
公开(公告)日：2013-02-27
申请号：EP11715924.4
申请日：2011-04-21
申请人： Probiodrug AG
发明人： HEISER, Ulrich , RAMSBECK, Daniel , HOFFMANN, Torsten , BOEHME, Livia
IPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14 , A61K31/4184 , A61P25/00
CPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
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.

10. 发明公开

EP2686313A1 BENZ IMIDAZOLE DERIVATIVES AS INHIBITORS OF GLUTAMINYL CYCLASE 有权转让
标题翻译：苯并咪唑衍生物ALS抑制剂谷氨酰胺酰基
公开(公告)号：EP2686313A1
公开(公告)日：2014-01-22
申请号：EP12709323.5
申请日：2012-03-16
申请人： Probiodrug AG
发明人： HEISER, Ulrich , RAMSBECK, Daniel
IPC分类号： C07D401/14 , C07D403/04 , C07D413/14 , C07D417/14 , A61K31/4184 , A61P25/28
CPC分类号： C07D403/04 , A61K31/4184 , A61K31/4409 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K38/2026 , A61K38/21 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).

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