中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

22 records (took 0.027 seconds)

    Inhibitors of glutaminyl cyclase
    2.
    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：US08420684B2

    公开(公告)日：2013-04-16

    申请号：US11937146

    申请日：2007-11-08

    Applicant: Michael Thormann ,  Michael Altmstetter ,  Andreas Treml ,  Ulrich Heiser ,  Mirko Buchholz ,  Andre J. Niestroj

    Inventor： Michael Thormann ,  Michael Altmstetter ,  Andreas Treml ,  Ulrich Heiser ,  Mirko Buchholz ,  Andre J. Niestroj

    IPC: A61K31/4166 ,  A61K31/4178 ,  C07D233/70 ,  C07D233/88

    CPC classification number: C07D405/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14

    Abstract: 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.

    Abstract translation: 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.

Patent Agency Ranking