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    • 5. 发明授权
    • Adenine compound and use thereof
    • 腺嘌呤化合物及其用途
    • US07754728B2
    • 2010-07-13
    • US10528343
    • 2003-09-26
    • Yoshiaki IsobeHaruo TakakuHaruhisa OgitaMasanori TobeAyumu KurimotoTetsuhiro OginoHitoshi Fujita
    • Yoshiaki IsobeHaruo TakakuHaruhisa OgitaMasanori TobeAyumu KurimotoTetsuhiro OginoHitoshi Fujita
    • C07D473/18C07D473/16A61K31/522A61P11/06A61P37/08
    • A61K31/5377A61K31/522A61K31/55
    • A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.
    • 用作局部给药的药物,其作为抗过敏剂有效。 用于局部给药的药物含有作为活性成分的由通式(1)表示的腺嘌呤化合物:[其中环A表示6至10元,单或双环,芳族烃或5至10元,单或双环, 含有1至3个选自0至2个氮原子,0或1个氧原子和0或1个硫原子的杂原子的芳族杂环; n为0〜2的整数, m为0〜2的整数; R代表卤代,(取代)烷基等; X1代表氧,硫,NR1(R1代表氢或烷基)或单键; Y1表示单键,亚烷基等; Y2表示单键,亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10(其中R 10表示(un)取代的烷基等)等)或该化合物的药学上可接受的盐。
    • 9. 发明授权
    • Type 2 helper T cell-selective immune response suppressors
    • 2型辅助性T细胞选择性免疫应答抑制剂
    • US06376501B1
    • 2002-04-23
    • US09582176
    • 2000-06-21
    • Yoshiaki IsobeHaruhisa OgitaMasanori TobeHaruo TakakuHiroyuki MatsuiHideyuki Tomizawa
    • Yoshiaki IsobeHaruhisa OgitaMasanori TobeHaruo TakakuHiroyuki MatsuiHideyuki Tomizawa
    • A61K3152
    • A61K31/522A61K31/52C07D473/00C07D473/34
    • The present invention relates to a type 2 helper T cell-selective immune response inhibitor, an immune response regulator and an anti-allergic agent, individually comprising, as an active ingredient, a purine derivative represented by General Formula (I): wherein R2 is hydrogen or a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; R6 is hydroxyl, amino or amino which is mono- or di-substituted by a hydrocarbon group(s); R8 is hydroxyl, mercapto, acyloxy or hydrocarbon group-substituting oxycarbonyloxy; and R9 is a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; or its tautomer or a salt of the purine derivative or the tautomer.
    • 本发明涉及一种2型辅助性T细胞选择性免疫应答抑制剂,免疫应答调节剂和抗过敏剂,其各自包含作为活性成分的由通式(I)表示的嘌呤衍生物:其中R 2为氢 或其中不直接结合嘌呤骨架的-CH 2可以被CO,SO 2,O或S取代的烃基,并且不直接键合到嘌呤骨架上的CH可以被N,C-卤素或C-CN R6是羟基,被一个或多个烃基单取代或二取代的氨基或氨基; R8是羟基,巯基,酰氧基或烃基取代的氧羰基氧基; 并且R 9是其中不直接结合嘌呤骨架的-CH 2可以被CO,SO 2,O或S取代的烃基,并且不直接键合到嘌呤骨架上的CH可以被N,C-卤素或C- CN;或其互变异构体或嘌呤衍生物或互变异构体的盐。
    • 10. 发明授权
    • Hydroquinone derivative and pharmaceutical use thereof
    • 对苯二酚衍生物及其药物用途
    • US5877318A
    • 1999-03-02
    • US113826
    • 1998-07-10
    • Yoshiaki IsobeYuso GotoMasanori TobeOsamu Takahashi
    • Yoshiaki IsobeYuso GotoMasanori TobeOsamu Takahashi
    • C07D239/54C07D239/545C07D405/12
    • C07D239/545C07D405/12
    • Disclosed is a hydroquinone derivative or a pharmaceutically acceptable salt thereof, the hydroquinone derivative being represented by formula (I): ##STR1## wherein R.sup.1 is a phenyl group which is unsubstituted or substituted with a substituent or substituents each independently selected from the group consisting of a halogen atom, a C1-4 alkyl group and a C1-4 alkoxy group;R.sup.2 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.3 and R.sup.4 is independently a hydrogen atom or a C1-4 alkyl group;R.sup.5 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.6, R.sup.7 and R.sup.8 is independently a hydrogen atom or a C1-4 alkyl group;P is a hydroxyl group;Q is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group;P may form together with Q an ether bond;R is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group, provided that when one of said Q and said R is an oxo group, the other is also an oxo group;X is a single bond, an --NR.sup.10 -- group or a --CH.sub.2 --NR.sup.10 -- group in which R.sup.10 is a hydrogen atom or a C1-4 alkyl group;Y is a methylene group or a carbonyl group; anddotted bonds in a six membered ring represent that said six membered ring has the maximum number of double bonds.
    • 公开了氢醌衍生物或其药学上可接受的盐,氢醌衍生物由式(I)表示:未取代或被各自独立地选自卤素原子,C 1-4烷基的取代基或取代基取代 和C 1-4烷氧基; R2是氢原子或C1-4烷基; R 3和R 4各自独立地为氢原子或C 1-4烷基; R5是氢原子或C1-4烷基; R6,R7和R8各自独立地为氢原子或C1-4烷基; P是羟基; Q是羟基,C 1-4烷氧基,C 1-18酰氧基或氧代基; P可与Q形成醚键; R是羟基,C 1-4烷氧基,C 1-18酰氧基或氧代基,条件是当所述Q和所述R中的一个是氧代基时,另一个也是氧代基; X是单键,-NR 10 - 基或-CH 2 -NR 10 - 基,其中R 10是氢原子或C 1-4烷基; Y是亚甲基或羰基; 六元环中的点状键表示所述六元环具有最大数量的双键。