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1. 发明授权

US08420684B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08420684B2
公开(公告)日：2013-04-16
申请号：US11937146
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： A61K31/4166 , A61K31/4178 , C07D233/70 , C07D233/88
CPC分类号： C07D405/14 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/14
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.
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 1表示杂芳基; 羧基 - 杂芳基; - 烯基杂芳基或 - 烷基杂芳基; R 2表示可任意被羟基取代的烷基; 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; 杂芳基; 或杂环基，其可任选被一个或多个选自烷基氧基和羟基的基团取代; R3表示可以任选被选自烷氧基，胺，羟基和-C（O）O烷基的更多个基团之一取代的烷基; 碳环基，其可任选被一个或多个选自烷基卤代烷基，烷氧基，胺，羟基和-C（O）O烷基的基团取代; - 烷基 - 芳基; - 烷基（芳基）2; - 烷基 - 杂芳基 - 烷基（杂芳基）2; - 烷基（杂芳基）（芳基）; 芳基-O-芳基; 芳基; 杂环基， - 烷基-C（O） - 杂环基， - 烷基 - 杂环基， - 烷基-C（O）-NR5 - 杂环基或 - 烷基（杂环基）2，其中任意一个组杂环基可以任选被一个或多个基团取代选自烷基羟基和氧代; 杂芳基或 - 羟基烷基芳基; R 4表示H或C 1-3烷基; R5表示H或C1-3烷基; X表示O或S.

2. 发明授权

US08278345B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08278345B2
公开(公告)日：2012-10-02
申请号：US11937149
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： A61K31/4025 , A61K31/4178 , C07D207/00 , C07D403/06 , C07D233/56
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.
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; R2表示氢; 卤素; 烯基; 炔基; - 烯基芳基; 烯基杂芳基烷基，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; - 烷基羧基 - 烷基杂环基芳基; 杂芳基; 杂环基 - 烷基芳基; - 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; R3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; 杂芳基; -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 1是咪唑基， - 环保基 - 咪唑基， - 烯基 - 咪唑基或 - 咪唑基，那么R 3可以不是-C（O）R 5。

3. 发明申请

US20080221086A1 Novel Inhibitors of Glutaminyl Cyclase 有权
标题翻译：新型抑制谷氨酰胺环化酶
公开(公告)号：US20080221086A1
公开(公告)日：2008-09-11
申请号：US11937146
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： C07D403/02 , C07D401/14 , C07D403/14 , C07D411/14 , A61K31/4178 , A61K31/4725 , A61K31/5377 , A61K31/551 , A61P31/00 , A61P37/00 , A61P35/00 , A61P25/00 , A61K31/541 , A61K31/495 , A61K31/445 , C07D413/14 , C07D405/00 , C07D401/02
CPC分类号： C07D405/14 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/14
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.
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，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中R 1表示杂芳基; 羧基 - 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; 杂芳基; 或杂环基，其可任选被一个或多个选自烷基氧基和羟基的基团取代; R 3表示可任意被选自烷氧基，胺，羟基和-C（O）O烷基中的一个以上基团取代的烷基; 碳环基，其可任选被一个或多个选自烷基卤代烷基，烷氧基，胺，羟基和-C（O）O烷基的基团取代; - 烷基 - 芳基; - 烷基（芳基）2。 - 烷基 - 杂芳基; - 烷基（杂芳基）2 - - 烷基（杂芳基）（芳基）; 芳基-O-芳基; 芳基; 杂环基， - 烷基-C（O） - 杂环基， - 烷基 - 杂环基， - 烷基-C（O）-NR 5 - 杂环基或 - 烷基（杂环基）在其中任何一个基团中，杂环基可以任选被一个或多个选自烷基羟基和氧代基团取代; 杂芳基或 - 羟基烷基芳基; R 4表示H或C 1-3烷基; R 5表示H或C 1-3烷基; X表示O或S.

4. 发明申请

US20090269301A1 Novel Inhibitors of Glutaminyl Cyclase 有权
标题翻译：新型抑制谷氨酰胺环化酶
公开(公告)号：US20090269301A1
公开(公告)日：2009-10-29
申请号：US11937149
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： A61K38/20 , C07D403/06 , A61K31/4178 , A61K31/4439 , C07D401/14 , A61P25/28 , A61K31/4709
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.
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; R2表示氢; 卤素; 烯基; 炔基; - 烯基芳基; 烯基杂芳基烷基，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; - 烷基羧基 - 烷基杂环基芳基; 杂芳基; 杂环基; - 烷基芳基; - 烷基（芳基）2， - 烷基杂芳基; 芳基 - 杂芳基; - 杂环基 - 芳基; 芳芳基 - 杂芳基 - 芳基; - 杂芳基 - 杂芳基和-C（O）R 4; R3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; 杂芳基; -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 1是咪唑基， - 环保基 - 咪唑基， - 烯基 - 咪唑基或 - 咪唑基，那么R 3可以不是-C（O）R 5。

5. 发明授权

US07741354B2 Inhibitors of glutaminyl cyclase 有权
公开(公告)号：US07741354B2
公开(公告)日：2010-06-22
申请号：US11937159
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/41 , C07D257/00
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.

6. 发明申请

US20080207715A1 Novel Inhibitors of Glutaminyl Cyclase 有权
公开(公告)号：US20080207715A1
公开(公告)日：2008-08-28
申请号：US11937159
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/41 , C07D403/02 , A61K35/04 , A61P25/00 , A61P19/00
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.

7. 发明申请

US20080286231A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
公开(公告)号：US20080286231A1
公开(公告)日：2008-11-20
申请号：US12105703
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Andre J. Niestroj , Robert Sommer
发明人： Mirko Buchholz , Ulrich Heiser , Andre J. Niestroj , Robert Sommer
IPC分类号： A61K38/20 , A61K31/4174 , C07D233/61 , A61K31/4184 , A61K38/21 , A61P9/10 , A61P25/28 , C07D405/12 , C07D413/12 , A61K31/5377
CPC分类号： C07D401/12 , C07D233/64 , C07D235/06 , C07D405/12 , C07D409/12 , C07D413/12 , 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.

8. 发明授权

US08809010B2 Method for prophylactic treatment of alzheimer's disease using inhibitors of glutaminyl cyclase and glutamate cyclases 有权
标题翻译：使用谷氨酰胺环化酶和谷氨酸环化酶抑制剂预防性治疗阿尔茨海默病的方法
公开(公告)号：US08809010B2
公开(公告)日：2014-08-19
申请号：US12506823
申请日：2009-07-21
申请人： Torsten Hoffmann , Stephan Schilling , Andre J. Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffmann , 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： Provided herein are methods for treating and preventing neurodegenerative disease in a mammal by administering an inhibitor of glutaminyl cyclase (QC). Neurodegenerative diseases treatable or preventable according to methods described herein include mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia.
摘要翻译：本文提供了通过施用谷氨酰胺环化酶（QC）抑制剂来治疗和预防哺乳动物中的神经变性疾病的方法。根据本文描述的方法可治疗或可预防的神经变性疾病包括轻度认知障碍（MCI），阿尔茨海默病，唐氏综合征中的神经变性，家族性的痴呆和家族性丹麦痴呆。

9. 发明授权

US07803810B2 Inhibitors 有权
标题翻译：抑制剂
公开(公告)号：US07803810B2
公开(公告)日：2010-09-28
申请号：US12045163
申请日：2008-03-10
申请人： Daniel Ramsbeck , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Daniel Ramsbeck , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00
CPC分类号： C07D471/04
摘要： 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: R1 represents C2-8alkyl; C2-8alkenyl; —(C1-6alkyl)-aryl; —(C1-6alkyl)-heteroaryl; —(C1-6alkyl)-carbocyclyl; —(C1-6alkyl)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C1-4alkyl, C1-4-fluoroalkyl, C1-4alkoxy, C1-4-fluoroalkoxy, hydroxy, —SO2(C1-4alkyl), —SO2N(C1-4alkyl)(C1-4alkyl), —SOC1-4alkyl, —SOC3-6cycloalkyl —C(O)O(C1-4alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from —C1-4 alkyl, —C1-4 alkoxy, hydroxyl, halogen and oxo; R2 represents H; C1-4alkyl or halogen; R3 represents H; C1-4alkyl or halogen; and R4 represents H; C1-4alkyl or halogen.
摘要翻译：式（I）的化合物，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合物，包括所有互变异构体，立体异构体和多晶型物，其中：R1代表C2-8烷基; C2-8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 - 氟烷基，C 1-4烷氧基，C 1-4 - 氟烷氧基，羟基，-SO 2（C 1-4烷基），-SO 2 N （C 1-4烷基）（C 1-4烷基），-SOC 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，卤素和氧代的取代基取代; R2表示H; C 1-4烷基或卤素; R3表示H; C 1-4烷基或卤素; 且R 4表示H; C 1-4烷基或卤素。

10. 发明授权

US07371871B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US07371871B2
公开(公告)日：2008-05-13
申请号：US10838993
申请日：2004-05-05
申请人： Stephan Schilling , Andre J. Niestroj , Ulrich Heiser , Mirko Buchholz , Hans-Ulrich Demuth
发明人： Stephan Schilling , Andre J. Niestroj , Ulrich Heiser , Mirko Buchholz , Hans-Ulrich Demuth
IPC分类号： A61K31/4174 , C07D233/61
CPC分类号： C07D207/08 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , 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 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
摘要翻译：本发明涉及作为QC抑制剂的化合物，包括由通式1至9表示的化合物及其组合用于治疗神经元疾病，特别是阿尔茨海默氏病，唐氏综合征，帕金森病，柯达亨廷顿病，致病性精神病症状，精神分裂症，食物摄取受损，睡眠觉醒，能量代谢的稳态调节受损，自主神经功能受损，激素平衡受损，调节受损，体液，高血压，发热，睡眠失调，厌食，焦虑相关障碍，包括癫痫发作，药物戒断和酒精中毒，神经变性疾病，包括认知功能障碍和痴呆。

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