| 摘要 |
The subject of the invention is 7-substituted 3-carboxy-oxadiazino-quinoline derivatives of formula(I) in which: either R1 represents: H, OH, NH2 , -(CH2)m - NRaRb in which m = 0, 1 or 2, Ra and Rb are identical or different and represent H, linear, branched or cyclic (C1-C6) alkyl, (C3-C6) cycloalkyl-(C1-C6)-alkyl; or also represent Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd; or Ra and Rb form together with the nitrogen atom, an Rc radical; Rc represents a saturated, unsaturated or aromatic 5- to 6-member ring containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted by 1 to 3 (C1-C6) alkyl radicals, said ring being linked, if appropriate, to the nitrogen atom of NRaRb by a nitrogen atom or a carbon atom; Rd represents a linear or branched (C1-C6) alkyl or (C3-C6) cyclic alkyl radical, optionally substituted by 1 to 4 halogens; or R1 represents Rc or CHReRc or CHReRd; Rc and Rd are as defined above, Re represents H, OH, NH2, NH-(C1-C6)-alk or N-(C1-C6)-alk2, or NH-(C1-C7)-acyl or NHRc, Rc being as defined above; R2 represents: H, (CH2)m-NRaRb, Rc, CHReRc or CHReRd, Ra, Rb, Rc, Rd and Re are as defined above; 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 Rc or NH2, or one H and the other one (CH2)m-NRaRb in which Ra and Rb represent H or (C1-C6) alkyl or C(O)Rd, in which Rd represents an unsubstituted linear or branched (C1-C6) alkyl or (C3-C6) cyclic alkyl radical; - or R1 has the above definition except H and R2 and R'2 together represent gem (C1-C6) dialkyl or (C1-C6) alkyl-oxime, or R2 and R'2 represent respectively Rc or Rd and OH, NH2, NHRc or NHRf, Rc and Rd being as defined above and Rf being a (C1- C7) acyl radical; - or R1 represents H and R2 and R'2 together represent (C1-C6) alkyl-oxime or one represents Rc and the other one represents OH, NH2, NHRc or NHRf, Rc and Rf being defined as above; n is 0 or 1; R3 and R'3, identical or different, represent H or (C3-C6) alkyl optionally substituted by 1 to 3 halogens or R3 represents a (C1-C6) alkoxy carbonyl group and R'3 represents H; R4 represents methyl optionally substituted by one to three halogens; R5 represents H, (C1-C6) alkyl or (C7-C12) arylalkyl; R6 represents H, fluorine, NO2, CF3 or CN. And examples of which are: 8-fluoro-3-methyl-6-oxo-9-[3-(pyrazin-2-ylaminomethyl)-pyrrolidin-1-yl]-2,3-dihydro-6H-1-oxa-3,3a-diaza-phenalene-5-carboxylic acid and 9·{ 3-[di-pyrazin·2-yl·amino)·methyl]pyrrolidin-1·yl} S·fluoro-3-methyl- 6-oxo-2,3-dihydro-6H-l-oxa-3,3a-diaza-phenalene-5-carboxylic acid and 9-{ 3-[di-pyridin-2-yl-amino)-methyl]pyrrolidin-l-yl} S-fluoro-3-methyl-6-oxo-2.3-dihydro-6H-l-oxa-3,3a-diaza-phenalene-5-carboxylic acid
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