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    Inhibitors of glutaminyl cyclase
    11.
    发明授权
    Inhibitors of glutaminyl cyclase 有权
    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。

    Novel Inhibitors of Glutaminyl Cyclase
    12.
    发明申请
    Novel Inhibitors of Glutaminyl Cyclase 有权
    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.

    Novel kinase inhibitors
    16.
    发明申请
    Novel kinase inhibitors 有权
    新型激酶抑制剂

    公开(公告)号：US20120329780A1

    公开(公告)日：2012-12-27

    申请号：US13506510

    申请日：2012-04-23

    申请人： Michael Thormann ,  Andreas Treml ,  Michael Almstetter ,  Nadine Traube

    发明人： Michael Thormann ,  Andreas Treml ,  Michael Almstetter ,  Nadine Traube

    IPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/541 ,  A61P11/06 ,  A61P37/00 ,  A61P37/08 ,  A61P27/02 ,  A61P17/04 ,  C07D487/04 ,  A61P29/00

    CPC分类号： C07D487/04 ,  C07D519/00

    摘要： The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

    摘要翻译： 本发明涉及能够抑制一种或多种激酶，特别是SYK（脾脏酪氨酸激酶），LRRK2（富含亮氨酸重复激酶2）和/或MYLK（肌球蛋白轻链激酶）的新型的式（I）化合物或 其突变体。 该化合物可用于治疗各种疾病。 这些疾病包括自身免疫性疾病，炎性疾病，骨病，代谢疾病，神经和神经退行性疾病，癌症，心血管疾病，过敏症，哮喘，阿尔茨海默病，帕金森病，皮肤病，眼病，感染性疾病和激素相关疾病。

    Novel Inhibitors of Glutaminyl Cyclase
    20.
    发明申请
    Novel Inhibitors of Glutaminyl Cyclase 有权
    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。