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    • 10. 发明申请
    • NOVEL INHIBITORS OF GLUTAMINYL CYCLASE
    • GLUTAMINYL CYCLASE的新型抑制剂
    • WO2008055950A1
    • 2008-05-15
    • PCT/EP2007/062037
    • 2007-11-08
    • PROBIODRUG AGTHORMANN, MichaelALMSTETTER, MichaelTREML, AndreasHEISER, UlrichBUCHHOLZ, Mirko
    • THORMANN, MichaelALMSTETTER, MichaelTREML, AndreasHEISER, UlrichBUCHHOLZ, Mirko
    • C07D401/12C07D401/14C07D403/12C07D403/14C07D405/12C07D405/14C07D409/14C07D417/14A61K31/41A61P25/28
    • C07D403/12C07D401/12C07D401/14C07D403/14C07D405/12C07D405/14C07D409/14C07D417/14
    • 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.
    • 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。