发明名称 Tricyclic antibiotics
摘要 The present invention relates to antibacterial compounds of formula I:; wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
申请公布号 US9120822(B2) 申请公布日期 2015.09.01
申请号 US201414546589 申请日期 2014.11.18
申请人 BASILEA PHARMACEUTICA AG 发明人 Gaucher, Jr. Berangere;Danel Franck Hubert;Tang XiaoHu;Xie Tong;Xu Lin
分类号 C07D513/04;C07D491/04;C07D495/04;C07D491/052;C07D491/147;C07D498/04;C07D498/14 主分类号 C07D513/04
代理机构 代理人
主权项 1. A compound of formula (I): wherein A1 represents —O—, —S— or —N(R3)-; A2 represents —CH2—, —O—, —C(═O)— or —CH(O—R4)-; A3 represents C3-C8cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur, wherein A3 is unsubstituted or substituted by a substituent selected from the group consisting of hydroxyl, C1-C4alkyl, C1-C4alkoxy, cyano, aminocarbonyl, (C1-C4alkyl)aminocarbonyl, C1-C4alkoxycarbonyl and a carboxylic acid group; 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 a unsubstituted or substituted benzo[1,4]thiazine or a pyrido[1,4]thiazine group, wherein the benzo or pyrido moiety of the benzo[1,4]thiazine or pyrido[1,4]thiazine group may be substituted by one or more substituents selected from the group consisting of a fluorine, a chlorine, a bromine and a iodine atom; a carboxy group, a C1-C4alkyl group, which is unsubstituted or further substituted by fluoro; an alkoxy group, a mono- or di(C1-C4alkyl)amino group, an OH group, SH group, NH2 group, cyano group and NO2 group and the thiazin moiety fused to said benzene or pyrido group may be substituted by one of more substituents selected from the group consisting of a fluorine, chlorine, bromine and iodine atom and a carboxy, alkyl, alkoxy, mono- or di(C1-C4alkyl)amino, OH, SH, NH2, cyano, NO2, ═O, ═S and ═NH group; R1 and R2 independently of one another, represent hydrogen or a substituent selected from the group consisting of hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy and C1-C6heteroalkoxy, wherein the heteroalkyl, heteroalkoxy or heterocyclyl substituent comprise 1, 2 or 3 heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur, and in which the alkyl moieties in the alkyl containing substituents are unsubstituted; 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 linked to A1 in formula (I) is optionally substituted by C1-C4alkyl; halogen, carboxy, hydroxy, C1-C4alkoxy, alkylcarbonyloxy, amino, mono- or di-(C1-C4alkyl)amino or acylamino; and n is 0, 1 or 2, or a pharmaceutically acceptable salt, hydrate or solvate thereof.
地址 Basel CH
您可能感兴趣的专利