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    • 3. 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。