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    • 10. 发明申请
    • PHOSPHATE TRANSPORT INHIBITORS
    • 磷酸盐运输抑制剂
    • WO03080630A2
    • 2003-10-02
    • PCT/US0308449
    • 2003-03-19
    • GENZYME CORPJOZEFIAK THOMASBASTOS CECILIA MHUVAL CHAD C
    • JOZEFIAK THOMASBASTOS CECILIA MHUVAL CHAD C
    • A61K45/00A61K31/663A61K31/785A61P5/18A61P7/00A61P13/12A61P19/00A61P19/10A61P43/00C07F9/30C07F9/32C07F9/38C07F9/40C07F9/553C07F9/655C08F8/40C08F30/02C07F9/02
    • C07F9/65502C07F9/3821C07F9/4012C07F9/5537C08F8/40C08F30/02Y02P20/55
    • Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I). R1 and R2 are independently -H, an electron withdrawing group or a C1-C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or -CR1R2P(O)(OH)-. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from -C1, -Br, -F, -CN, -NO2, -OR , -N(R )2, -COOR , -CON(R )2, -COR , -S(O)R , -S(O)2R , -S(O)2N(R )2, -NR S(O)2R , -NR COR , a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each R is independently -H, lower alkyl, substituted lower alkyl, aryl or substituted aryl. Each Rb is independently -H, a lower alkyl group, or a phosphate protecting group.
    • 公开了由结构式(I)表示的磷酸盐转运抑制化合物。 R1和R2独立地为-H,吸电子基团或C1-C10烷基。 Y是共价键,取代的亚甲基,未取代的亚甲基或-CR 1 R 2 P(O)(OH) - 。 R 3是任选地包含一个或多个胺,铵,醚,硫醚或亚苯基连接基团的烃基,任选地包含一个或多个胺,铵,醚,硫醚或亚苯基连接基团的取代烃基,杂芳基,取代的杂芳基 基团或被一个或多个选自-C 1,-Br,-F,-CN,-NO 2,-OR a,-N(R a)2,-COOR a, -CON(R a)2,-COR a,-S(O)R a,-S(O)2 R a,-S(O)2 N(R a)2, -NR a S(O)2 R a,-NR a COR a,卤代低级烷基,芳基,取代芳基或卤代烷氧基。 每个R a独立地为-H,低级烷基,取代的低级烷基,芳基或取代的芳基。 每个R b独立地为-H,低级烷基或磷酸酯保护基团。