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    • 1. 发明申请
    • 1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS HISTAMINE H3 RECEPTOR LIGANDS
    • 1H-4(5) - 取代的咪唑衍生物,它们的制备及其作为组胺H3受体配体的用途
    • WO9905114A3
    • 1999-04-22
    • PCT/GB9802067
    • 1998-07-14
    • BLACK JAMES FOUNDATIONTOZER MATTHEW JOHNKALINDJIAN SARKIS BARRETLINNEY IAN DUNCANSTEEL KATHERINE ISABEL MARYPETHER MICHAEL JOHNCOOKE TRACEY
    • TOZER MATTHEW JOHNKALINDJIAN SARKIS BARRETLINNEY IAN DUNCANSTEEL KATHERINE ISABEL MARYPETHER MICHAEL JOHNCOOKE TRACEY
    • C07D233/54C07D417/04A61K31/415A61K31/425
    • C07D233/64C07D417/04
    • Compounds of formula (I) wherein R is selected from C1 to C6 alkyl, C1 to C6 alkoxy, C1 to C6 alkylthio, carboxy, carboxy (C1 to C6)alkyl, formyl, C1 to C6 alkylcarbonyl, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, aryl, C1 to C6 alkylaryl, halo, sulfamoyl and cyano; R is C1 to C20 hydrocarbylene, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 6 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group, and provided also that the atom in R which is linked to the -SO2- moiety is a carbon atom; R is hydrogen or C1 to C15 hydrocarbyl, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 3 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group; X is a bond or -NR -, wherein R is hydrogen or non-aromatic C1 to C5 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen atoms and up to 2 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group), aryl(C1 to C3)alkyl or R represents a bond to R ; and a is from 0 to 2, and their pharmaceutically acceptable salts are useful as histamine H3 receptor ligands.
    • 其中R 1选自C 1 -C 6烷基,C 1 -C 6烷氧基,C 1 -C 6烷硫基,羧基,羧基(C 1 -C 6)烷基,甲酰基,C 1 -C 6烷基羰基,C 1 -C 6烷基羰基烷氧基 硝基,三卤代甲基,羟基,氨基,C1-C6烷基氨基,二(C1-C6烷基)氨基,芳基,C1-C6烷基芳基,卤素,氨磺酰基和氰基; R 2为C 1至C 20亚烃基,其中一个或多个氢原子可以被卤素原子置换,且至多6个碳原子可以被氧,氮或硫原子置换,条件是R 2不含 并且还提供了与-SO 2 - 部分连接的R 2中的原子是碳原子; R 3是氢或C 1至C 15烃基,其中一个或多个氢原子可以被卤素原子代替并且至多3个碳原子可以被氧,氮或硫原子代替,条件是R 3不是 包含一个-OO-组; X是键或-NR 4 - ,其中R 4是氢或非芳族C 1 -C 5烃基(其中一个或多个氢原子可以被卤素原子取代并且至多2个碳原子可以被取代 (其中R 4不含-OO-基团),芳基(C 1 -C 3)烷基或R 4表示与R 2的键; a为0-2,并且它们的药学上可接受的盐可用作组胺H3受体配体。