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    TRICYCLIC ANTIBIOTICS
    1.
    发明申请
    TRICYCLIC ANTIBIOTICS 有权
    TRICYCLIC抗生素

    公开(公告)号：US20120245345A1

    公开(公告)日：2012-09-27

    申请号：US13511292

    申请日：2010-12-17

    申请人： Bérangère Gaucher ,  Franck Hubert Danel ,  XiaoHu Tang ,  Tong Xie ,  Lin Xu

    发明人： Bérangère Gaucher ,  Franck Hubert Danel ,  XiaoHu Tang ,  Tong Xie ,  Lin Xu

    IPC分类号： C07D491/052 ,  C07D498/14 ,  C07D495/04 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D491/04 ,  C07D491/052 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14

    摘要： Compound of formula (I): wherein A1 represents —O—, —S— or —N—R3; A2 represents —CH2—, —O—, —N—R4, —C(═O)— or —CH(O—R4)—; A3 represents C3-C8cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, C2-C4alkenylene, >C═O or a group selected from —C2H4NH—, —C2H4O—, and —C2H4S— being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is un-substituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted; R3, R4 and R5 independently of one another, represent hydrogen or C1-C6alkyl; X1 and X2 independently of one another, represent a nitrogen atom or CR2, with the proviso that at least one of X1 and X2 represents a nitrogen atom; m is 1; and the (CH2)m moiety is optionally substituted by C1-C4alkyl; halogen, carboxy, hydroxy, C1-C4alkoxy, C1-C4-alkylcarbonyloxy, amino, mono- or di-(C1-C4alkyl)amino or acylamino n is 0, 1 or 2 or pharmaceutically acceptable salt thereof are valuable for use as a medicament for the treatment of bacterial infections.

    摘要翻译： 式（I）化合物：其中A1表示-O - ， - S-或-N-R 3; A 2表示-CH 2 - ， - O - ， - N-R 4，-C（= O） - 或-CH（O-R 4） - ; A3表示C3-C8亚环烷基; 饱和和不饱和的4至8元杂环基与1,2或3个选自氮，氧和硫的杂原子，该基团A3为未取代或取代的; A4表示C1-C4亚烷基，C2-C4亚烯基，> C = O或选自-C2H4NH-，-C2H4O-和-C2H4S-的基团，其通过碳原子连接到相邻的NR5-基团; 并且G表示未取代或取代的芳基或杂芳基，R 1和R 2彼此独立地表示氢或选自羟基，卤素，巯基，氰基，硝基，C 1 -C 6烷基，C 1 -C 6烷氧基， C 1 -C 6烷硫基，C 1 -C 6烷基羰基氧基，C 1 -C 6烷基磺酰氧基，C 1 -C 6杂烷基羰氧基，C 5 -C 6杂环羰基氧基，C 1 -C 6杂烷氧基，其中杂烷基，杂烷氧基或杂环基包含1,2或3个选自氮，氧和硫的杂原子，其中烷基部分 是未取代的或进一步取代的; R 3，R 4和R 5彼此独立地表示氢或C 1 -C 6烷基; X 1和X 2彼此独立地表示氮原子或CR 2，条件是X 1和X 2中的至少一个表示氮原子; m为1; （CH 2）m部分任选被C 1 -C 4烷基取代; 卤素，羧基，羟基，C 1 -C 4烷氧基，C 1 -C 4烷基羰基氧基，氨基，单 - 或二 - （C 1 -C 4烷基）氨基或酰氨基n是0,1或2或其药学上可接受的盐对于用作药物是有价值的 用于治疗细菌感染。