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    • 2. 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。
    • 4. 发明申请
    • HISTAMINE H3 RECEPTOR LIGANDS
    • 组胺H3受体配体
    • WO1997029092A1
    • 1997-08-14
    • PCT/GB1997000358
    • 1997-02-10
    • JAMES BLACK FOUNDATION LIMITEDKALINDJIAN, Sarkis, BarretSHANKLEY, Nigel, PaulTOZER, Matthew, JohnMcDONALD, Iain, MairPETHER, Michael, JohnHARPER, Elaine, AnneWATT, Gillian, FairfullCOOKE, TraceyLOW, Caroline, Minli, Rachel
    • JAMES BLACK FOUNDATION LIMITED
    • C07D233/54
    • C07D233/64C07D401/12
    • Compounds of formula (I) or (II) wherein R is C4 to C20 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen, and up to three carbon atoms may be replaced by oxygen, nitrogen or sulphur atoms, provided that R does not contain an -O-O- group), R is H or C1 to C3 alkyl, m is from 1 to 15, n is from 2 to 6, each X group is independently (a), or one X group is -N(R )-, -O- or -S- and the remaining X groups are independently (a), wherein R is H, C1 to C6 alkyl, -CO2R , -CONR 2, -CR 2OR or -OR (in which R and R are H or C1 to C3 alkyl), and R is H or C1 to C6 alkyl, each Y group is independently -C(R )R -, or up to two Y groups are -N(R )-, -O- or -S- and the remaining Y groups are independently -C(R )R -, wherein R is as defined above, one R group in the structure is imidazoyl or imidazoylalkyl and the remaining R groups are H or C1 to C6 alkyl, and Z is > C(R )NR - or > N-, wherein R is any of the groups recited above for R , and pharmaceutically acceptable salts thereof are ligands at histamine H3 receptors.
    • 其中R 1为C 4 -C 20烃基(其中一个或多个氢原子可被卤素取代,最多三个碳原子)可以被氧,氮或硫原子代替的式(I)或(II)化合物 条件是R 1不含-OO-基),R 2为H或C 1至C 3烷基,m为1至15,n为2至6,每个X基团独立地为(a )或一个X基团是-N(R 4) - , - O-或-S-,其余的X基团独立地为(a),其中R 3为H,C 1至C 6烷基,-CO 2 R -CONR 5,-CR 5 OR 2或-OR 5(其中R 5和R 6为H或C 1至C 3烷基) 4>是H或C 1至C 6烷基,每个Y基团独立地是-C(R 3)R 4 - 或至多两个Y基团是-N(R 4) - , - O-或 -S-,其余的Y基团独立地是-C(R 3)R 4 - ,其中R 3如上定义,结构中的一个R 4基团是咪唑基或咪唑基烷基,剩余的 R 4基团是H或C 1至C 6烷基,Z是> C(R 7)NR 2 - 或> N-,其中R 7是任何基团 R 3所示的化合物及其药学上可接受的盐是组胺H3受体的配体。