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    • 3. 发明申请
    • DIBENZONAPHTHYRIDINE DERIVATIVES AND METHODS OF USE THEREOF
    • 二苯并噻吩衍生物及其使用方法
    • WO2007070319A3
    • 2007-11-01
    • PCT/US2006046646
    • 2006-12-06
    • WYETH CORPGOPALSAMY ARIAMALASHI MENGXIAOKUTTERER KRISTINAARNDT KIM TIMOTHY
    • GOPALSAMY ARIAMALASHI MENGXIAOKUTTERER KRISTINAARNDT KIM TIMOTHY
    • C07D471/04A61K31/4375A61P35/02
    • C07D471/04
    • The present invention relates to Dibenzonaphthyridine Derivatives , compositions comprising an ef fective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a proliferative disorder, comprising administering to a subj ect in need thereof an ef f ective amount of a Dibenzonaphthyridine Derivative of formula ( I ) : or a pharmaceutically acceptable salt thereof, wherein R 1 is -H, -OH, -O-C 1 ,-C 6 alkyl, -halo, -C 2 -C 6 alkenyl, -C 2 -C 6 alkynyl, -N(R I8 ) 2 , -NH-OR 18 or-C(0)N(R l8 ) 2 ; R 2 is -H, -0-C 1 -C 6 alkyl, -halo, -C 2 -C 6 alkenyl, -C 2 -C 6 alkynyl, -NHR 17 . -N(R I7 ) 2 , -NH-OR 18 or -C(O)N(R I8 ) 2 , such that when R 1 is -OH or -0-C1-C 6 alkyl, R 2 is hydrogen; R 3 , R 4 , R 5 , R 6 , R 7 , R 8 . R 9 and R 10 are each independently -H, -halo, -OH, -SH, -N(R I2 ) 2 , -NHOR 12 , -CN, -NO 2 , -CF 3 , -OCF 3 , -C 1 -C 6 alkyl, -C 2 -C 6 alkenyl, -C2-C6 alkynyl, -C 3 -C 8 cycloalkyl, -C 3 -C 8 cycloalkenyl, -phenyl, -benzyl, -(CH 2 ) n -O-C 1 -C 6 alkyl, -0-C 2 -C 6 alkenyl, -0-C 2 -C 6 alkynyl, -O-phenyl, -S-phenyl, -NH-C 1 -C 6 alkyl, -(CH 2 ) n -C(O)-R 11 , -(CH 2 ) n -O)-R 11 , -(CH 2 ) n -NHC(O)-R 11 , -S-C 1 -C 6 alkyl, -S(O)-C 1 -C 6 alkyl, -SO 2 -C 1 -C 6 alkyl, -SO 2 NH-C 1 -C 6 alkyl, -SO 2 NH-C 2 -C 6 alkenyl, -SO 2 NH-C 2 -C 6 alkynyl, -Y-(CH 2 ) K -M- CH(R 14 )R 15 , -Y-(CH 2 ) g -R 16 , -Y-(CH 2 ) k -M-(CH 2 ) p -R 16 , -Y-(CH 2 ) k -(W) a -(CH 2 ) q -Z, -Y-(CH 2 ) P - (Z)_-(CH2)q-Z, or such that R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are not simultaneously hydrogen.
    • 本发明涉及二苯并萘啶衍生物,包含有效量的二苯并萘啶衍生物的组合物和治疗或预防增殖性疾病的方法,其包括向有需要的受试者施用有效量的式(I)的二苯并吡啶衍生物 ):或其药学上可接受的盐,其中R 1是-H,-OH,-OC 1,C 6 -C 6烷基, - 卤素,-C 2 -C 6亚烷基,-C 2 -C 6 - 炔基,-N(R -NH-OR 18或-C(O)N(R 18))SUB > 2 ; R 2是-H,-O-C 1 -C 6烷基, - 卤素,-C 2 - -C 6亚烯基,-C 2 -C 6炔基,-NHR 17。 -N(R I7)2,-NH-OR 18或-C(O)N(R 100) >),使得当R 1是-OH或-O-C 1 -C 6烷基时,R 2, SUP>是氢; R 3,R 4,R 5,R 6,R 7, [R 8 。 R 9和R 10各自独立地为-H, - 卤素,-OH,-SH,-N(R 12) 2个,-NHOR 12,-CN,-NO 2,-CF 3,-OCF 3, C 1 -C 6烷基,-C 2 -C 6亚烷基,-C 2 -C 6亚烷基,-C 2 -C 6 - C 6炔基,-C 3 -C 8环烷基,-C 3 -C 8环烯基, - 苯基, - 苄基, - (CH 2 CH 2)n -OC 1 -C 6烷基,-O-C 1 -C 6烷基, C 2 -C 6亚烷基,-O-C 2 -C 6炔基,-O-苯基,-S - 苯基,-NH-C 1 -C 6烷基, - (CH 2 CH 2)n -C( O)-R 11, - (CH 2)n -O - )-R 11, - (CH -NO(O)-R 11,-SC 1 -C 6,-C(O)-R 11, 烷基,-S(O)-C 1 -C 6烷基,-SO 2 -C 1 -C 6烷基, -SO 2 -C 6烷基,-SO 2 NH-C 1 -C 6烷基,-SO 2 - , - 2个NH 2 C 2 -C 6亚烷基,-SO 2 NH- C 1 -C 6烷基,-Y-(CH 2 CH 2)n -M-CH(R 14) R 15,-Y-(CH 2)n -R 16,-Y-(CH 2) (CH 2 ķ -M-(CH 2 p -R 16 - (CH 2)n - (CH 2)n - (CH 2)n - (CH 2) -Z,-Y-(CH 2)2 - (Z)_-(CH 2)q Z,或使得R 3 R 4,R 5,R 5,R 6,R 7,R 8, R 9,R 9和R 10不是同时为氢。