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    Isoindolinone derivatives, processes for preparing them and medicines containing them
    1.
    发明授权
    Isoindolinone derivatives, processes for preparing them and medicines containing them 失效
    异吲哚啉酮衍生物，其制备方法和含有它们的药物

    公开(公告)号：US4999355A

    公开(公告)日：1991-03-12

    申请号：US319302

    申请日：1989-03-06

    申请人： Marie-Therese Comte ,  Claude Gueremy ,  Gerard Ponsinet

    发明人： Marie-Therese Comte ,  Claude Gueremy ,  Gerard Ponsinet

    IPC分类号： C07D209/46 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/495 ,  A61P43/00 ,  C07D209/48 ,  C07D209/50 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14

    CPC分类号： C07D209/48 ,  C07D401/06 ,  C07D401/14

    摘要： Compounds of formula: ##STR1## in which: either R.sub.1 represents 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl or 4-(4-fluorophenyl)-1,2,3,6-tetrahydro-1-pyridyl, R.sub.2 represents hydrogen, alkoxy of 1 or 2 carbon atoms, hydroxyl, alkyl, alkylthio, alkylcarbonyloxy, phenylalkylcarbonyloxy, phenylalkyl or --NR.sub.4 R.sub.5 in which R.sub.4 represents hydrogen or alkyl and R.sub.5 represents alkyl, phenyl, monohalogenated phenyl or pyridyl, and R.sub.3 represents a hydrogen atom, or else R.sub.2 represent phenyl and R.sub.3 represents hydrogen or hydroxyl;or R.sub.1 represnets 4-phenyl-1-piperazinyl whose phenyl nucleus has a substituent halogen atom or hydroxyl radical in the 4-position, R.sub.2 represents alkoxy and R.sub.3 represents hydrogen;it being understood that when R.sub.1 represents the 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl radical, R.sub.2 is not hydroxyl and that, unless otherwise stated, the alkyl and alkoxy radicals and the alkyl and alkoxy portions contain 1 to 4 carbon atoms each in a straight or branched chain, and addition salts thereof with an inorganic or organic acid, are useful in therapy for their serotonin antagonist properties.

    摘要翻译： 式（I）的化合物，其中：R 1表示4-苯基-1,2,3,6-四氢-1-吡啶基或4-（4-氟苯基） 四氢-1-吡啶基，R 2表示氢，1或2个碳原子的烷氧基，羟基，烷基，烷硫基，烷基羰基氧基，苯基烷基羰氧基，苯基烷基或-NR4R5，其中R4表示氢或烷基，R5表示烷基，苯基，单卤代苯基或吡啶基 ，R 3表示氢原子，或者R 2表示苯基，R 3表示氢或羟基; 或R 1表示4-苯基-1-哌嗪基，其苯基在4-位上具有取代基的卤原子或羟基，R2表示烷氧基，R3表示氢; 应当理解，当R 1表示4-苯基-1,2,3,6-四氢-1-吡啶基时，R 2不是羟基，除非另有说明，烷基和烷氧基以及烷基和烷氧基部分含有 每个直链或支链的碳原子数为1至4个碳原子，和其与无机或有机酸的加成盐可用于治疗其5-羟色胺拮抗剂性质。

    Process for preparing pyrrolo(1,2-A)azepinone derivatives
    4.
    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。

    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them
    5.
    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。