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1. 发明申请

WO2007116092A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：WO2007116092A1
公开(公告)日：2007-10-18
申请号：PCT/EP2007/053560
申请日：2007-04-12
申请人： PROBIODRUG AG , THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas
发明人： THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas
IPC分类号： C07D233/64 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
CPC分类号： C07D409/06 , C07D233/64 , C07D401/06 , C07D403/06 , C07D405/06
摘要： The present invention provides compounds of formula (I), wherein: R 1 , R 2 , R 3 , R 4 and R 5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.
摘要翻译：本发明提供式（I）化合物，其中：R 1，R 2，R 3，R 4， SUP＆gt;和＆lt; 5＆gt;在整个说明书和权利要求书中都被定义。式（I）化合物可用于治疗神经疾病和神经变性疾病，例如，焦虑，抑郁，阿尔茨海默病等

2. 发明申请

WO2010026212A1 NOVEL INHIBITORS 审中-公开
标题翻译：新型抑制剂
公开(公告)号：WO2010026212A1
公开(公告)日：2010-03-11
申请号：PCT/EP2009/061453
申请日：2009-09-04
申请人： PROBIODRUG AG , ALMSTETTER, Michael , DEMUTH, Hans-Ulrich , HAMANN, Antje , HEISER, Ulrich , HOFFMANN, Torsten , SOMMER, Robert , THORMANN, Michael , TREML, Andreas , GAERTNER, Ulf-Torsten
发明人： ALMSTETTER, Michael , DEMUTH, Hans-Ulrich , HAMANN, Antje , HEISER, Ulrich , HOFFMANN, Torsten , SOMMER, Robert , THORMANN, Michael , TREML, Andreas , GAERTNER, Ulf-Torsten
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/433 , A61K31/437 , A61P29/00 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/04
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , 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。

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

WO2008055950A1 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：WO2008055950A1
公开(公告)日：2008-05-15
申请号：PCT/EP2007/062037
申请日：2007-11-08
申请人： PROBIODRUG AG , THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko
发明人： THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/41 , A61P25/28
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R 2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, -C(O)O-alkyl and -C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)O-alkyl and -C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R 2 together with R 4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R 3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, amino, halogen, haloalkyl, hydroxyl, -alkoxy, -thioalkyl, -C(O)OH and -C(O)O-alkyl; alkenyl; -alkyl- aryl; -alkyl(aryl) 2 , -alkyl(heteroaryl) 2 , -alkyl(aryl)(heteroaryl), -alkyl-heteroaryl; -alkyl-heterocyclyl which heterocyclyl group may optionally be substituted by one or more groups selected from alkyl, hydroxy and oxo; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-aryl; -aryl-O-aryl, -heteroaryl-heteroaryl; -aryl; heteroaryl; heterocyclyl; -aryl-alkyl-aryl; -aryl-O-alkyl-aryl; -alkyl-C(O)-NH-alkyl-aryl; -alkyl-C(O)-NH-alkyl-heteroaryl; -alkyl-C(O)-NH- alkyl-heterocyclyl; -alkyl-C(O)-(N-piperidinyl) or -alkyl-C(O)-(N-pyrrolidinyl) in which piperidinyl or pyrrolidinyl may optionally be fused to optionally substituted phenyl. R 4 represents H or 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，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，其可以任选地被一个或多个选自氨基，卤素，羟基， - 烷氧基， - 硫代烷基，-C（O）O-烷基和-C（O）哦; 碳环基，其可任选被一个或多个选自烷基，卤代烷基，氨基，卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）O-烷基和-C（O）OH的基团取代; 烯基; 炔基; 烷基 - 芳基; 烷基 - 杂芳基; 烷基 - 杂环基; 烷基 - 碳环基; 芳基 - 杂芳基; - 杂芳基 - 芳基; - 杂芳基 - 杂芳基; - 芳基 - 芳基; 芳基（单环或双环）; 杂芳基（单环或双环）; 杂环; 或R 2与R 4一起可以形成任选被一个或多个烷基取代的碳环基; R 3表示烷基，其可任选被一个或多个选自氨基，卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O- 烷基; 碳环基，其可以任选被一个或多个选自烷基，氨基，卤素，卤代烷基，羟基， - 烷氧基， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; 烯基; - 烷基 - 芳基; - 烷基（芳基）2 - ， - 烷基（杂芳基）2 - ， - 烷基（芳基）（杂芳基）， - 烷基 - 杂芳基; - 烷基 - 杂环基，该杂环基可以任选被一个或多个选自烷基，羟基和氧代的基团取代; 烷基 - 碳环基; 芳基 - 杂芳基; - 杂芳基 - 芳基; - 芳基 - 芳基; 芳基-O-芳基， - 杂芳基 - 杂芳基; 芳基; 杂; 杂环; - 芳基 - 烷基 - 芳基; - 芳基-O-烷基 - 芳基; - 烷基-C（O）-NH-烷基 - 芳基; - 烷基-C（O）-NH - 烷基 - 杂芳基; - 烷基-C（O）-NH-烷基 - 杂环基; - 烷基-C（O） - （N-哌啶基）或 - 烷基-C（O） - （N-吡咯烷基），其中哌啶基或吡咯烷基可任选地与任选取代的苯基稠合。 R 4表示H或烷基。

5. 发明申请

WO2008055947A1 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：WO2008055947A1
公开(公告)日：2008-05-15
申请号：PCT/EP2007/062034
申请日：2007-11-08
申请人： PROBIODRUG AG , THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko
发明人： THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/4025 , A61P25/28 , A61P25/14
CPC分类号： C07D405/14 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/04
摘要： The present invention relates to 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 R 1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R 2 represents alkyl, which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl, oxo and hydroxy; R 3 represents alkyl, which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and -C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, alkoxy, amine, hydroxy and -C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl) 2 ; -alkyl-heteroaryl; -alkyl(heteroaryl) 2 ; -alkyl(heteroaryl)(aryl); -aryl-O-aryl; aryl; heterocyclyl, -alkyl-C(O)-heterocyclyl, -alkyl-heterocyclyl, -alkyl-C(O)-NR 5 -heterocyclyl or -alkyl(heterocyclyl) 2 in any of which groups heterocyclyl may be optionally substituted by one or more groups selected from alkyl, hydroxy and oxo; -heteroaryl; or -hydroxyalkylaryl; R 4 represents H or C 1-3 alkyl; R 5 represents H or C 1-3 alkyl; and X represents O or S.
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，溶剂合物或多晶型物，包括其中R 1表示杂芳基的所有互变异构体和立体异构体。碳环基 - 杂芳基; - 烯基杂芳基或 - 烷基杂芳基; R 2表示可任选被羟基取代的烷基; 碳环基，其可任选被一个或多个选自烷基和羟基的基团取代; 芳基; 芳基 - 杂芳基; - 杂芳基 - 芳基; - 芳基 - 杂环基; H; 杂; 或杂环基，其可任选被一个或多个选自烷基，氧代和羟基的基团取代; 代表“SUP”表示

6. 发明申请

WO2008055945A1 3-HYDR0XY-1,5-DIHYDR0-PYRR0L-2-ONE DERIVATIVES AS INHIBITORS OF GLUTAMINYL CYCLASE FOR THE TREATMENT OF ULCER, CANCER AND OTHER DISEASES 审中-公开
标题翻译：作为治疗胃癌，癌症及其他疾病的谷氨酰胺循环抑制剂的3-羟基-1,5-二氢吲哚-2-基吡啶-2-酮衍生物
公开(公告)号：WO2008055945A1
公开(公告)日：2008-05-15
申请号：PCT/EP2007/062030
申请日：2007-11-08
申请人： PROBIODRUG AG , THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko , NIESTROJ, André Johannes
发明人： THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko , NIESTROJ, André Johannes
IPC分类号： C07D403/04 , C07D403/06 , C07D403/14 , C07D407/14 , C07D417/14 , A61K31/4025 , A61K31/4178 , A61P1/04 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00
CPC分类号： C07D403/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R 1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R 2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O- alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and -C(O)R 4 ; R 3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, -C(O)OH and -C(O)O-alkyl; aryl; heteroaryl; -C(O)R 5 ; R 4 and R 5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl, with the proviso that, when R 1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R 3 may not be -C(O)R 5 .
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，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表示氢; 卤素; 烯基; 炔基; -alkenylaryl; -alkenylheteroaryl; 烷基，其可任选被一个或多个选自卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; 碳环基，其可任选被一个或多个选自烷基，卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; -alkylcarbocyclyl; -alkylheterocyclyl; 芳基; 杂; 杂环; - 烷基; - 烷基（芳基）2， - 烷基杂芳基; 芳基 - 杂芳基; - 杂环基 - 芳基; - 芳基 - 芳基; - 杂芳基 - 芳基; - 杂芳基 - 杂芳基和-C（O）R 4; R 3表示卤素; 任选被一个或多个选自卤素，羟基，烷氧基，硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代的烷基; 芳基; 杂; -C（O）R ^{5 ; R 4和R 5独立地表示烷基，芳基，杂芳基， - 烷基芳基， - 烷基杂芳基，碳环基，杂环基， - 烷基碳环基和 - 烷基杂环基，条件是当R 咪唑基，碳环基 - 咪唑基， - 烯基 - 咪唑基或 - 烷基 - 咪唑基，那么R 3可以不是-C（O）R 5， / SUP>。}

7. 发明公开

EP2091945A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译：新的抑制剂谷氨酰胺
公开(公告)号：EP2091945A1
公开(公告)日：2009-08-26
申请号：EP07822338.5
申请日：2007-11-08
申请人： Probiodrug AG
发明人： THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/4025 , A61P25/28 , A61P25/14
CPC分类号： C07D405/14 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/04
摘要： The present invention relates to 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 R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl, oxo and hydroxy; R3 represents alkyl, which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and -C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, alkoxy, amine, hydroxy and -C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(heteroaryl)2; -alkyl(heteroaryl)(aryl); -aryl-O-aryl; aryl; heterocyclyl, -alkyl-C(O)-heterocyclyl, -alkyl-heterocyclyl, -alkyl-C(O)-NR5-heterocyclyl or -alkyl(heterocyclyl)2 in any of which groups heterocyclyl may be optionally substituted by one or more groups selected from alkyl, hydroxy and oxo; -heteroaryl; or -hydroxyalkylaryl; R4 represents H or C1-3 alkyl; R5 represents H or C1-3 alkyl; and X represents O or S.

8. 发明公开

EP2089383A1 3-HYDR0XY-1,5-DIHYDR0-PYRR0L-2-ONE DERIVATIVES AS INHIBITORS OF GLUTAMINYL CYCLASE FOR THE TREATMENT OF ULCER, CANCER AND OTHER DISEASES 有权
标题翻译： 3-羟基-1,5-二氢 - 吡咯-2-酮衍生物AS溃疡谷氨酰胺酰基，癌症和其他疾病的治疗抑制剂
公开(公告)号：EP2089383A1
公开(公告)日：2009-08-19
申请号：EP07822336.9
申请日：2007-11-08
申请人： Probiodrug AG
发明人： THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko , NIESTROJ, André Johannes
IPC分类号： C07D403/04 , C07D403/06 , C07D403/14 , C07D407/14 , C07D417/14 , A61K31/4025 , A61K31/4178 , A61P1/04 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00
CPC分类号： C07D403/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O- alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and -C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, -C(O)OH and -C(O)O-alkyl; aryl; heteroaryl; -C(O)R5; R4 and R5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl, with the proviso that, when R1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R3 may not be -C(O)R5.

9. 发明公开

EP2086960A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译：谷氨酰胺环化酶的新型抑制剂
公开(公告)号：EP2086960A1
公开(公告)日：2009-08-12
申请号：EP07822341.9
申请日：2007-11-08
申请人： Probiodrug AG
发明人： THORMANN, Michael , ALMSTETTER, Michael , TREML, Andreas , HEISER, Ulrich , BUCHHOLZ, Mirko
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/41 , A61P25/28
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, -C(O)O-alkyl and -C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)O-alkyl and -C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R2 together with R4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, alkoxy-, -thioalkyl, -C(O)OH and -C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, amino, halogen, haloalkyl, hydroxyl, -alkoxy, -thioalkyl, -C(O)OH and -C(O)O-alkyl; alkenyl; -alkyl- aryl; -alkyl(aryl)2, -alkyl(heteroaryl)2, -alkyl(aryl)(heteroaryl), -alkyl-heteroaryl; -alkyl-heterocyclyl which heterocyclyl group may optionally be substituted by one or more groups selected from alkyl, hydroxy and oxo; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-aryl; -aryl-O-aryl, -heteroaryl-heteroaryl; -aryl; heteroaryl; heterocyclyl; -aryl-alkyl-aryl; -aryl-O-alkyl-aryl; -alkyl-C(O)-NH-alkyl-aryl; -alkyl-C(O)-NH-alkyl-heteroaryl; -alkyl-C(O)-NH- alkyl-heterocyclyl; -alkyl-C(O)-(N-piperidinyl) or -alkyl-C(O)-(N-pyrrolidinyl) in which piperidinyl or pyrrolidinyl may optionally be fused to optionally substituted phenyl. R4 represents H or 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，其中：R 1表示杂芳基， - 碳环基 - 杂芳基， - 链烯基杂芳基或 - 烷基杂芳基; R2代表烷基，其可以任选被一个或多个选自氨基，卤素，羟基， - 烷氧基， - 硫代烷基，-C（O）O-烷基和-C（O）OH的基团取代; 碳环基，其可任选地被一个或多个选自烷基，卤代烷基，氨基，卤素，羟基，烷氧基，硫代烷基，-C（O）O-烷基和-C（O）OH的基团取代; 烯基; 炔基; 烷基 - 芳基; 烷基 - 杂芳基; 烷基 - 杂环基; 烷基 - 碳环基; 芳基 - 杂芳基; - 杂芳基 - 芳基; - 杂芳基 - 杂芳基; - 芳基 - 芳基; - 芳基（单环或双环）; 杂芳基（单环或双环）; 杂环; 或者R 2与R 4一起可以形成任选被一个或多个烷基取代的碳环基; R 3代表可以任选被一个或多个选自氨基，卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代的烷基; 碳环基，其可任选地被一个或多个选自烷基，氨基，卤素，卤代烷基，羟基， - 烷氧基， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; 烯基; - 烷基 - 芳基; （芳基）2， - 烷基（杂芳基）2， - 烷基（芳基）（杂芳基）， - 烷基 - 杂芳基; - 杂环基可以任选被一个或多个选自烷基，羟基和氧代的基团取代; 烷基 - 碳环基; 芳基 - 杂芳基; - 杂芳基 - 芳基; - 芳基 - 芳基; - 芳基-O-芳基， - 杂芳基 - 杂芳基; 芳基; 杂; 杂环; - 芳基 - 烷基 - 芳基; - 芳基-O-烷基 - 芳基; - 烷基-C（O）-NH-烷基 - 芳基; - 烷基-C（O）-NH - 烷基 - 杂芳基; - 烷基-C（O）-NH-烷基 - 杂环基; （O） - （N-哌啶基）或 - 烷基-C（O） - （N-吡咯烷基），其中哌啶基或吡咯烷基可任选与任选取代的苯基稠合。 R4代表H或烷基。

10. 发明授权

EP2344157B1 NOVEL INHIBITORS 有权转让
标题翻译：新的抑制剂
公开(公告)号：EP2344157B1
公开(公告)日：2016-05-25
申请号：EP09782605.1
申请日：2009-09-04
申请人： Probiodrug AG
发明人： ALMSTETTER, Michael , DEMUTH, Hans-Ulrich , HAMANN, Antje , HEISER, Ulrich , HOFFMANN, Torsten , SOMMER, Robert , THORMANN, Michael , TREML, Andreas , GAERTNER, Ulf-Torsten
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/433 , A61K31/437 , A61P29/00 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/04 , C07D471/04 , C07D417/14
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04

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