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    Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them
    67.
    发明授权
    Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them 失效

    公开(公告)号：US5021420A

    公开(公告)日：1991-06-04

    申请号：US375934

    申请日：1989-07-06

    申请人： Marie-Iherese Comte ,  Claude Gueremy ,  Jean-Luc Malleron ,  Serge Mignani ,  Jean-Francois Peyronel ,  Alain Truchon

    发明人： Marie-Iherese Comte ,  Claude Gueremy ,  Jean-Luc Malleron ,  Serge Mignani ,  Jean-Francois Peyronel ,  Alain Truchon

    IPC分类号： A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P43/00 ,  C07D275/06 ,  C07D417/00 ,  C07D417/06 ,  C07D417/14 ,  C07D513/06

    CPC分类号： C07D275/06 ,  C07D417/06 ,  C07D417/14 ,  C07D513/06

    摘要： This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.a piperidino radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or a hydroxy, alkyl or alkoxy radical, (c) two phenyl radicals, (d) a bis(4-fluorophenyl)methylene radical, (e) a 4-fluorobenzoyl radical, (f) a 2-oxo-1-benzimidazolinyl radical, (g) a 2-oxo-1-benzimidazolinyl radical substituted in the 3-position by an alkylcarbonyl or benzoyl radical, (b) a hydroxy radical and a phenyl radical optionally substituted with an alkyl, alkoxy or hydroxy radical or a halogen atom, (i) a 3-indolyl radical, (j) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (k) a 3-(5-hydroxyindolyl) radical.either:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical,with the reservation that when R.sub.6 represents a propylene radical substituted in the 2-position by a dialkylamino, piperidino, morpholino or thiomorpholino radical, R.sub.1 cannot be a radical containing a hydroxy radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

    Process for preparing 3-fluoroquinolines
    69.
    发明授权
    Process for preparing 3-fluoroquinolines 失效
    制备3-氟喹啉的方法

    公开(公告)号：US07396934B2

    公开(公告)日：2008-07-08

    申请号：US10985533

    申请日：2004-11-10

    申请人： Youssef El-Ahmad ,  Jean-Pierre Leconte ,  Joël Malpart ,  Serge Mignani ,  Stéphane Mutti ,  Michel Tabart

    发明人： Youssef El-Ahmad ,  Jean-Pierre Leconte ,  Joël Malpart ,  Serge Mignani ,  Stéphane Mutti ,  Michel Tabart

    IPC分类号： C07D215/38 ,  C07D215/18

    CPC分类号： C07D215/38 ,  C07D215/18 ,  Y02P20/55

    摘要： The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.

    摘要翻译： 本发明涉及式（I）的3-氟喹啉的新型制备方法，其中R 1，R 2，R 3和R 3， 代表：a）氟; b）任选被一至三个氟取代的烷基，其中R 5是烷基，氢或羟基保护基或NR' 其中R'和R“表示烷基，氢或氨基保护基的”R“ c）OR 6其中R 6表示氢，苯酚保护基或任选被氟取代的烷基，OR 5或N >或如上定义的NR'R“ d）NR'1 R“1其中R'1和R”1 <1的数值为 或者代表被氟取代的烷基，其具有如上定义的OR 5或NR'R“; e）其中R aa代表氢，烷基或羧基保护基，以及新的中间体化合物的CO 2 CO 2。 式（I）的喹啉是可用于制备具有抗菌活性的化合物的中间体，特别在申请WO 02/40474或WO 02/72572中有所描述。