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    • 11. 发明授权
    • Hydroquinone derivative and pharmaceutical use thereof
    • 对苯二酚衍生物及其药物用途
    • US5821247A
    • 1998-10-13
    • US933208
    • 1997-09-16
    • Yoshiaki IsobeYuso GotoMasanori TobeOsamu Takahashi
    • Yoshiaki IsobeYuso GotoMasanori TobeOsamu Takahashi
    • C07D239/54C07D239/545C07D405/12A61K31/51
    • 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; and dotted 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,所述对苯二酚衍生物由式(I)表示:未取代的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。
    • 12. 发明申请
    • Novel uracil derivatives and medicinal use thereof
    • 新型尿嘧啶衍生物及其药用
    • US20060094737A1
    • 2006-05-04
    • US10528373
    • 2003-09-17
    • Yoshiaki IsobeMasanori TobeYoshifumi InoueMasakazu Isobe
    • Yoshiaki IsobeMasanori TobeYoshifumi InoueMasakazu Isobe
    • A61K31/513C07D405/02C07D239/54
    • C07D239/545A61K31/513C07D405/06C07D405/12C07D405/14
    • It is intended to provide an uracil derivative represented by the following general formula (I): (I) wherein X represents a group selected from among NHCO, NHCH2, CO, CONH and CH2NH; R1 represents hydrogen or optionally substituted C1-6 alkyl; R2 represents a group of the following general formula (II) or (III): (II) (III) (wherein m is 0 or 1; n is an integer of from 1 to 3; Y represents OH or NH2; and a dotted line shows a binding position), provided that when R2 is a group of the general formula (III), X represents NHCO or NHCH2; R3 and R4 independently represent each hydrogen or C1-6 alkyl; and Ar represents phenyl substituted by C1-6 alkyl at the o- and m-positions, optionally substituted heteroaryl or a bicyclic aromatic group; its pharmaceutically acceptable salt, and a remedy containing the above uracil derivative or its pharmaceutically acceptable salt as the active ingredient for, in particular, allergic diseases relating to a type IV allergic reaction, i.e., a novel compound useful in treating diseases in which a type IV allergic reaction participates and a remedy for allergic diseases containing the same as the active ingredient.
    • 旨在提供由以下通式(I)表示的尿嘧啶衍生物:(I)其中X表示选自NHCO,NHCH 2,CO,CONH和CH 2的基团 NH; R 1表示氢或任选取代的C 1-6烷基; R 2表示下述通式(II)或(III)的基团:(II)(III)(其中m为0或1; n为1至3的整数; Y 表示OH或NH 2,虚线表示结合位置),条件是当R 2为通式(III)的基团时,X表示NHCO或 NHCH 2