发明名称 ANTIBACTERIAL COMPOUNDS
摘要 The present invention relates to cephalosporin antibacterial compounds of Formula (I):;;or corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.
申请公布号 US2014249126(A1) 申请公布日期 2014.09.04
申请号 US201214349754 申请日期 2012.10.04
申请人 GLAXO GROUP LIMITED ;Shionogi & Co., Ltd. 发明人 Liao Xiangmin;Pearson Neil David;Pendrak Israil;Sano Masayuki
分类号 C07D501/60 主分类号 C07D501/60
代理机构 代理人
主权项 1. A compound of Formula (II): wherein: X is N, or C—Ra; R1 and R2 each are hydrogen, (C1-6)alkyl, or (CH2)p-C(O)ORb; R3 and R4 each are hydrogen, OH or ORc; wherein: Ra is hydrogen or halogen;Rb or Rc each is H, (C1-6)-alkyl, an alkali metal or negative charge; A is R5 or —NRdC(O)R5 wherein Rd is H or (C1-6)-alkyl R5 is an optionally saturated or unsaturated monocyclic heterocyclic ring or an optionally saturated or unsaturated bi-cyclic or fused heterocyclic ring; wherein: each monocyclic heterocyclic ring has from 3 to 7 ring atoms and contains up to four heteroatoms;each fused heterocyclic ring optionally includes carbocyclic rings or heterocyclic rings of up to four heteroatoms;R5 optionally is substituted by one or more of the following substituents selected from —H, —OH, Oxo (═O), —CN, —NO2, -halogen, -straight or branched C1-6 alkyl, -straight or branched C1-6 haloalkyl, C3-6-cycloalkyl, -straight or branched C1-6 straight or branched alkoxy, —OC(O)OH, —OC(O)Re, —C(O)ORf, —O(CH2)yORg, —NRhRi, —SO2Rj, —S(CH2)qRk, —NRlC(O)Rm, aryl or heteroaryl;wherein: hetero atoms are selected from oxygen, nitrogen or sulphur,carbocyclic rings or heterocyclic rings for each fused heterocyclic ring systems include non-aromatic rings or aromatic rings;monocyclic heterocyclic rings or fused heterocyclic rings include substituted aromatic and non-aromatics;each Re, Rf, Rg, Rh, Ri, Rj, Rk, Rl, or Rm each is selected from H, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy;each aryl or heteroaryl as defined above is optionally substituted with one or more of the following substituents selected from H, —OH, —CN, —NO2, -halogen, C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, —OC(O)OH, —OC(O)Rn, —C(O)ORo, —O(CH2)y—ORp, —NRqRr, —SO2Rs, —S(CH2)y—Rt, —NRuC(O)Rv;wherein: Rn, Ro, Rp, Rq, Rr, Rs, Rt, Ru, or Rv each are selected from C1-6 alkyl, C1-6-haloalkyl, or C1-6-alkoxy; n, m, o, p, q or y each are 0 or an integer from 1 to 5; or a pharmaceutically acceptable salt thereof.
地址 Greenford, Middlesex GB