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    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them
    2.
    发明授权
    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them 失效
    具有抗精神病活性的新型1,3-二取代吡咯并[1,2-a]吖庚因衍生物和含有它们的药物组合物

    公开(公告)号：US4769366A

    公开(公告)日：1988-09-06

    申请号：US839101

    申请日：1986-03-13

    申请人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    发明人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    IPC分类号： A61K31/55 ,  A61P25/18 ,  C07D487/04 ,  A61K31/395 ,  C07D223/00

    CPC分类号： C07D487/04

    摘要： Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C,or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain,and the pharmaceutically acceptable salts thereof,are useful as antipsychotics.

    摘要翻译： 吡咯并[1,2-a]吖庚因酮衍生物，其中R 3为H或卤素，（A）R为苄基或苯硫基，其中苯基任选被一个或多个卤素或羟基取代 ，烷基，烷氧基或烷硫基，R 1和R 2可以相同或不同，表示任选被二烷基氨基取代的烷基，其中烷基任选地连接以形成被烷基取代的1-吡咯烷基，哌啶子基，吗啉代或1-哌嗪基环 或者R1和R2形成选自吡咯烷，哌啶，吗啉和哌嗪的杂环，被烷基，烯基（2至4 C），任选被卤素，烷基，烷氧基，烷硫基，CF 3，COOH取代的苄基或苯乙基取代， 羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或烷基羰氧基烷基，其中烷基羰基具有2至18个C，或（B）R是任选被一个或多个卤素或羟基，烷基，烷氧基或烷硫基取代的苯基， 和R2一起形成被羟烷基（2〜4 C），烯基（2〜4 C），炔基（2〜4 C），任选被卤素，烷基，烷氧基，烷硫基，CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环 ，CF 3，COOH，羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或其中烷基羰基具有2至18个C的烷基羰氧基烷基，所述烷基除了另外说明的含有1至4个C的直链或支链以外， 其盐可用作抗精神病药。

    Process for preparing pyrrolo(1,2-A)azepinone derivatives
    3.
    发明授权
    Process for preparing pyrrolo(1,2-A)azepinone derivatives 失效
    制备吡咯（1,2-A）氮杂酮衍生物的方法

    公开(公告)号：US4826974A

    公开(公告)日：1989-05-02

    申请号：US116725

    申请日：1987-11-04

    申请人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    发明人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    IPC分类号： A61K31/55 ,  A61P25/18 ,  C07D487/04 ,  C07D487/06 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D487/04

    摘要： Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain, and the pharmaceutically acceptable salts thereof, are useful as antipsychotics.

    摘要翻译： 吡咯并[1,2-a]吖庚因酮衍生物，其中R 3为H或卤素，（A）R为苄基或苯硫基，其中苯基任选被一个或多个卤素或羟基取代 ，烷基，烷氧基或烷硫基，R 1和R 2可以相同或不同，表示任选被二烷基氨基取代的烷基，其中烷基任选地连接以形成被烷基取代的1-吡咯烷基，哌啶子基，吗啉代或1-哌嗪基环 或者R1和R2形成选自吡咯烷，哌啶，吗啉和哌嗪的杂环，被烷基，烯基（2至4 C），任选被卤素，烷基，烷氧基，烷硫基，CF 3，COOH取代的苄基或苯乙基取代， 羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或烷基羰氧基烷基，其中烷基羰基具有2至18个C，或（B）R是任选被一个或多个卤素或羟基，烷基，烷氧基或烷硫基取代的苯基， 和R2一起形成被羟烷基（2〜4 C），烯基（2〜4 C），炔基（2〜4 C），任选被卤素，烷基，烷氧基，烷硫基，CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环 ，CF 3，COOH，羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或其中烷基羰基具有2〜18个碳原子的烷基羰氧基烷基，所述烷基除了另外说明的含有1〜4个C的直链或支链， 其盐可用作抗精神病药。

    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    9.
    发明授权
    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
    醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法

    公开(公告)号：US06841562B2

    公开(公告)日：2005-01-11

    申请号：US10659095

    申请日：2003-09-10

    申请人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： A61P31/04 ,  C07D211/60 ,  C07D401/06 ,  C07D409/14 ,  A61K31/44 ,  C07D215/12 ,  C07D215/18

    CPC分类号： C07D401/06 ,  C07D211/60 ,  C07D409/14 ,  Y02P20/55

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents.

    摘要翻译： 通式（I）的喹啉基丙基哌啶衍生物，其中R 1a是氢，卤素，羟基，氨基，烷基氨基，二烷基氨基，羟基氨基，烷氧基氨基或烷基烷氧基氨基，R 1b是氢，或者R 1a和R 1b形成氧代，R 2是羧基，羧甲基或羟甲基， 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基，或与任选被卤素或三氟甲基取代的环烷硫基（3至7个成员）或与杂芳硫基（ 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基或R3是被苯基或杂芳基取代的炔丙基，被苯基或杂芳基取代 R4是烷基，烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基，其各种异构体形式，分别或混合物，和 它们的盐，它们的制备方法和中间体以及含有它们的组合物。 这些新型衍生物是有效的抗菌剂。