发明名称 NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS
摘要 A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, -(CH2)m-NRaRb(m=0.1 or 2), Ra and Rb represent H, linear, branched or cyclic (C1 -C6) alkyl, (C3-C6) cycloalkyl-(C3-C6)- alkyl, Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd; or Ra and Rb with N form an Rc radical; Rc represents a saturated, unsaturated or 5- or 6-members aromatic ring, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted; Rd represents a linear, branched or cyclic (C1-C6) alkyl, optionally substituted by 1 to 4 halogens; or R1 represents Rc or CHReRc or CHReRd; Re represents H, OH, NH2, NH-(C1-C6)-alk or N-(C1-C6)-alk2, or NH-(C1-C7)-acyl or NHRc; R2 represents H, (CH2)m-NRaRb, Rc, CHReRc or CHReRd, and R'2 represents H; it being understood that R1 and R2 cannot at the same time be H or that R1 and R2 or R2 and R1 cannot be one (CH2)m-NRaRb or Rc or H and the other one OH, or one H and the other one NH2, or one H and the other one (CH2)m-NRaRb in which Ra and Rb represent H or alkyl or C(O)Rd, in which Rd represents an unsubstituted alkyl or cycloalkyl; or R1 has the above definition except H and R2 and R'2 together represent gem dialkyl or alkyl-oxime, or R2 and R'2 represent respectively Rc or Rd and OH, NH2, NHRc or NHRf, Rf being a (C1-C7) acyl radical; or R1 represents H and R2 and R'2 together represent alkyl-oxime or one represents Rc and the other one represents OH, NH2, NHRc or NHRf; n is 0 or 1; R3 and R'3 represent H or (C1-C6) alkyl optionally substituted by 1 to 3 halogens or R3 represents (C1-C6) alkoxy carbonyl and R'3 represents H; R4 represents methyl optionally substituted by halogen; R5 represents H, (C1-C6) alkyl or (C7-C12) arylalkyl; R6 represents H, fluorine, NO2, CF3 or CN; in the form of enantiomers or mixtures, as well as their salts with acids and bases; their preparation and their application as anti-bacterials, in both human and veterinary medicine.
申请公布号 US2009221565(A1) 申请公布日期 2009.09.03
申请号 US20090394918 申请日期 2009.02.27
申请人 VETOQUINOL SA 发明人 ROPP SANDRINE;MORICE CHRISTOPHE;GIETHLEN BRUNO;CIAPETTI PAOLA;CHERY-MOZZICONACCI FLORENCE;WERMUTH CAMILLE G.;LEBLANC FRANCOISE;SCHNEIDER MARC
分类号 C07D498/04;A61K31/5383;A61P31/04 主分类号 C07D498/04
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