发明名称 NOVEL 7-SUBSTITUTED DERIVATIVES OF 3-CARBOXY-OXADIAZINO-QUINOLONES, PREPARATION THEREOF AND USE THEREOF AS ANTI-BACTERIAL AGENTS
摘要 The invention relates to compounds of the formula (I)in which either Ris H, OH, NH, -(CH)-NraRb, wherein m=0, 1 or 2; Ra and Rb, identical or different, are H, linear, branched or cyclic (1-6c)alkyl; or Rc, C(O)Rc, S(O)Rd, or C(O)Rd; or Ra and Rb form with N an Rc radical; Rc is an optionally saturated, unsaturated or aromatic cycle with 5 or 6 carbon atoms, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted by 1-3 alkyl (1-6c) radicals, wherein said cycle being optionally connected to the nitrogen atom of NRaRb by a carbon atom; Rd is linear, branched or cyclic (1-6c)alkyl optionally substituted by 1 to 4 halogens; or Ris CHReRc or CHReRd; Rc and Rd are as defined above, Re is H, OH, NH, NH-alk(1-6c) or N-alk(1-6c) or NH-acyl(1-7c) or NHRc, where Rc being as defined above; Ris H, (CH)-NRaRb, Rc, CHReRc or CHReRd, where Ra, Rb, Rc, Rd and Re are as defined above; and R'is H; provided that Rand Rcannot at the same time be H or that Rand Ror Rand Rcannot be one (CH)-NRaRb or Rc or H and the other one OH, or one H and the other one Rc or NH, or one H and the other one (CH)-NRaRb in which Ra and Rb is H or alkyl (1-6c) or C(O)Rd, in which Rd is alkyl(1-6c) or unsabstituted cycloalkyl(3-6c); or Rand R'together are gem-dialkyl(1-6c); or Rand R'are alkyl(1-6c)oxime or one is Rc and the other is OH; n is 0 or 1; Rand R', identical or different, are H or (1-6c)alkyl optionally substituted by 1 to 3 halogens or Ris (1-6c)alkoxy carbonyl and R'is H; Ris methyl optionally substituted by 1 to 3 halogen atoms; Ris H, (1-6c)alkyl or (7-12c)arylalkyl; Ris H, fluorine; as enantiomers or mixtures, as well as to their salts with acids and bases; to their preparation and their application as anti-bacterials, in both human andveterinary medicine.
申请公布号 EA018348(B1) 申请公布日期 2013.07.30
申请号 EA20100071014 申请日期 2009.02.26
申请人 VETOQUINOL SA 发明人 CIAPETTI PAOLA;CHERY-MOZZICONACCI FLORENCE;WERMUTH CAMILLE, G.;LEBLANC FRANCOISE;SCHNEIDER MARC;ROPP SANDRINE;MORICE CHRISTOPHE;GIETHLEN BRUNO
分类号 C07D498/06;A61K31/5395;A61P31/04 主分类号 C07D498/06
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