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    • 3. 发明申请
    • BENZOTHIAZINONE DERIVATIVES AS ANTI -TUBERCULOSIS AGENTS
    • 苯并噻嗪酮衍生物作为抗肿瘤药物
    • WO2013038259A1
    • 2013-03-21
    • PCT/IB2012/001788
    • 2012-09-14
    • THE UNIVERSITY OF QUEENSLANDCOOPER, MatthewZUEGG, JohannesBECKER, BerndTOMISLAV, Karoli
    • COOPER, MatthewZUEGG, JohannesBECKER, BerndTOMISLAV, Karoli
    • C07D417/04A61K31/5415A61P31/06
    • C07D417/04
    • Novel benzothiazinone derivatives of formula (I) or pharmaceutically acceptable salts or solvates thereof have been found to be effective against Mycobacterium tuberculosis strains and may thus be useful in the treatment of tuberculosis: wherein EWG (electron withdrawing group) = NO 2 , CN, CF 3 , F, Cl, Br, OCF 3 , OH, OR, OCHF 2 , COOR, wherein R is hydrogen or a straight or branched C 1 -C 4 alkyl group, X = a bond or a straight or branched C 1 -C 4 alkylene group which may be substituted with a group selected from F, Cl, Br, I or C 1 -C 4 alkoxy; Y = hydrogen, a straight or branched C 1 -C 4 alkyl group, OH or OR, wherein R is hydrogen or a straight or branched C 1 -C 4 alkyl group; n = 0, 1 or 2; R 1 , R 2 = hydrogen or substituent (s) which may be the same or different from each other and are selected from the group consisting of D, F, Cl, Br, CF 3 , a straight or branched C 1 -C 4 alkyl group, a phenyl group, OR, SR, NR 3 R 4 , wherein R, R 3 , R 4 may be the same or different from each other and are hydrogen or a straight or branched C 1 -C 4 alkyl group or a phenyl group.
    • 已经发现新的式(I)苯并噻嗪酮衍生物或其药学上可接受的盐或溶剂合物对结核分枝杆菌菌株有效,因此可用于治疗结核病:其中EWG(吸电子基团)= NO 2,CN,CF 3, F,Cl,Br,OCF 3,OH,OR,OCHF 2,COOR,其中R为氢或直链或支链C 1 -C 4烷基,X =可被直链或支链C 1 -C 4烷基取代的键或直链或支链C 1 -C 4亚烷基 选自F,Cl,Br,I或C 1 -C 4烷氧基的基团; Y =氢,直链或支链C 1 -C 4烷基,OH或OR,其中R是氢或直链或支链C 1 -C 4烷基; n = 0,1或2; R 1,R 2 =氢或可以彼此相同或不同的取代基,并且选自D,F,Cl,Br,CF 3,直链或支链C 1 -C 4烷基,苯基 基团,OR,SR,NR 3 R 4,其中R 3,R 3,R 4可以彼此相同或不同,并且是氢或直链或支链C 1 -C 4烷基或苯基。