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    NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS
    2.
    发明申请
    NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS 失效

    公开(公告)号：US20090221565A1

    公开(公告)日：2009-09-03

    申请号：US12394918

    申请日：2009-02-27

    申请人： Sandrine Ropp ,  Christophe Morice ,  Bruno Giethlen ,  Paola Ciapetti ,  Florence Chery-Mozziconacci ,  Camille G. Wermuth ,  Francoise Leblanc ,  Marc Schneider

    发明人： Sandrine Ropp ,  Christophe Morice ,  Bruno Giethlen ,  Paola Ciapetti ,  Florence Chery-Mozziconacci ,  Camille G. Wermuth ,  Francoise Leblanc ,  Marc Schneider

    IPC分类号： C07D498/04 ,  A61K31/5383 ,  A61P31/04

    CPC分类号： C07D498/06

    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.

    7-substituted 3-carboxy-oxadiazino-quinolone derivatives, their preparation and their application as anti-bacterials
    3.
    发明授权
    7-substituted 3-carboxy-oxadiazino-quinolone derivatives, their preparation and their application as anti-bacterials 失效
    7-取代的3-羧基 - 恶二唑 - 喹诺酮衍生物，其制备及其作为抗菌剂的应用

    公开(公告)号：US07713965B2

    公开(公告)日：2010-05-11

    申请号：US12394918

    申请日：2009-02-27

    申请人： Paola Ciapetti ,  Florence Chery-Mozziconacci ,  Camille G. Wermuth ,  Françoise Leblanc ,  Marc Schneider ,  Sandrine Ropp ,  Christophe Morice ,  Bruno Giethlen

    发明人： Paola Ciapetti ,  Florence Chery-Mozziconacci ,  Camille G. Wermuth ,  Françoise Leblanc ,  Marc Schneider ,  Sandrine Ropp ,  Christophe Morice ,  Bruno Giethlen

    IPC分类号： C07D498/06 ,  A61K31/5365

    CPC分类号： C07D498/06

    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.

    摘要翻译： 本发明的主题是式（I）的化合物：其中R 1表示H，OH，NH 2， - （CH 2）m -NR a R b（m = 0.1或2），R a和R b表示H，直链，支链或 环（C 1 -C 6）烷基，（C 3 -C 6）环烷基 - （C 3 -C 6） - 烷基，R c，S（O）2 C，C（O）R c，S（O）2 R d或C（O） 或R a和R b与N形成R c基团; Rc表示饱和，不饱和或5-或6-元芳环，其含有1至4个选自N，O和S的杂原子，任选地被取代; Rd表示任选被1至4个卤素取代的直链，支链或环状（C 1 -C 6）烷基; 或R1表示Rc或CHRRR或CHRRR; Re表示H，OH，NH2，NH-（C1-C6）-alk或N-（C1-C6）-alk2或NH-（C1-C7） - 酰基或NHRc; R2表示H，（CH2）m-NRaRb，Rc，CHReRc或CHReRd，R'2表示H.