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    • 8. 发明申请
    • COMPOUNDS
    • 化合物
    • WO2004071389A2
    • 2004-08-26
    • PCT/EP2004/001507
    • 2004-02-13
    • GLAXO GROUP LIMITEDBARKER, Michael, DavidDEMAINE, Derek, AnthonyHOUSE, DavidINGLIS, Graham, George, AdamJOHNSTON, Michael, JohnJONES, Haydn, TerenceMACDONALD, Simon, John, FawcettMCLAY, Iain McFarlaneSHANAHAN, StephenSKONE, Philip, AlanVINADER, Maria, Victoria
    • BARKER, Michael, DavidDEMAINE, Derek, AnthonyHOUSE, DavidINGLIS, Graham, George, AdamJOHNSTON, Michael, JohnJONES, Haydn, TerenceMACDONALD, Simon, John, FawcettMCLAY, Iain McFarlaneSHANAHAN, StephenSKONE, Philip, AlanVINADER, Maria, Victoria
    • A61K
    • C07D265/02C07D413/12
    • A compound of formula (I) wherein: n represents an integer 0, 1 or 2; X represents, O, S, NR 6a , or CHR 6b ; R 1 represents hydrogen, halogen such as F, Cl or Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 or CONR 8 R 9 ; R 2 represents hydrogen, halogen such as F, Cl, Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 or CONR 8 R 9 ; R 3 represents hydrogen, halogen such as F, Cl, Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 , CONR 8 R 9 ; R 4 represents hydrogen, halogen such as F, Cl, Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 or CONR 8 R 9 ; R 5 represents H, C 1-6 alkyl, or C 1-6 alkenyl; R 6a represents hydrogen, C 1-6 alkyl, CO 2 C 1-3 alkyl, COC 1-3 alkyl or SO 2 C 1-3 alkyl; R 6b represents hydrogen, or C 1-6 alkyl; R 7 represents hydrogen, C 1-6 alkyl, C 1-3 alkyleneSiC 1-3 alkyl such as -CH 2 CH 2 Si(CH 3 ) 3 ; R 8 and R 9 independently represent hydrogen or C 1-6 alkyl; including pharmaceutically acceptable esters, amides and carbamates thereof, salts thereof, solvates thereof, and solvates of such pharmaceutically acceptable esters, amides, carbamates and salts.
    • 式(I)的化合物,其中:n表示整数0,1或2; X表示O,S,NR 6a或CHR 6b; R 1表示氢,卤素如F,Cl或Br,NO 2,羟基,氰基,-OC 1-6烷氧基如甲氧基,C 1-6烷基如甲基,NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3,COOR 7或CONR 8 R 9; R 2表示氢,卤素如F,Cl,Br,NO 2,羟基,氰基,-OC 1-6烷氧基如甲氧基,C 1-6烷基如甲基,NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3,COOR 7或CONR 8 R 9; R 3表示氢,卤素如F,Cl,Br,NO 2,羟基,氰基,-OC 1-6烷氧基如甲氧基,C 1-6烷基如甲基,NR 8 R 9如NH 2 ,NR 8 COR 9如-NHCHO或-NHCOCH 3,COOR 7,CONR 8 R 9; R 4表示氢,卤素如F,Cl,Br,NO 2,羟基,氰基,-OC 1-6烷氧基如甲氧基,C 1-6烷基如甲基,NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3,COOR 7或CONR 8 R 9; R 5表示H,C 1-6烷基或C 1-6烯基; R 6a表示氢,C 1-6烷基,CO 2 C 1-3烷基,COC 1-3烷基或SO 2 C 1-3烷基; R 6b表示氢或C 1-6烷基; R 7表示氢,C 1-6烷基,C 1-3亚烷基,C 1-3烷基如-CH 2 CH 2 Si(CH 3)3; R 8和R 9独立地表示氢或C 1-6烷基; 包括其药学上可接受的酯,酰胺和氨基甲酸酯,其盐,溶剂化物,和这些药学上可接受的酯,酰胺,氨基甲酸酯和盐的溶剂合物。