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35 条记录 (耗时 0.053 秒)

    Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them
    22.
    发明授权
    Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them 失效
    醌基丙基哌啶衍生物，制备方法和中间体，以及包括它们的组合物

    公开(公告)号：US06806277B2

    公开(公告)日：2004-10-19

    申请号：US10622655

    申请日：2003-07-18

    申请人： Eric Bacqué ,  Jean-Luc Malleron ,  Serge Mignani ,  Michel Tabart

    发明人： Eric Bacqué ,  Jean-Luc Malleron ,  Serge Mignani ,  Michel Tabart

    IPC分类号： A61K3147

    CPC分类号： C07D401/06 ,  C07D409/12

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which: R1 is NH2, alkylamino, dialkylamino, hydroxyamino, alkyl(alkyloxy)amino or alkyloxyamino, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is alkyl (1 to 6C) substituted by phenylthio which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2, by cycloalkylthio (3 to 7 members) or by heteroarylthio (5 to 6 members) comprising 1 to 4 heteroatoms selected from N, S and O and optionally itself substituted [by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2] or R3 is propargyl substituted by phenyl which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2 or substituted by cycloalkyl comprising 3 to 7 members or substituted by 5- to 6-membered heteroaryl comprising 1 to 4 heteroatoms chosen from N, O or S and optionally itself substituted by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2, and R4 is alkyl (1 to 6C), alkenyl-CH2—, alkynyl-CH2— (3 to 7C), cycloalkyl or (cycloalkyl)alkyl, in their diastereoisomeric forms or their mixtures, and their pharmaceutically acceptable salts. These novel derivatives are particularly advantageous antimicrobial agents.

    摘要翻译： 通式（I）的喹啉基丙基哌啶衍生物，其中：R1是NH2，烷基氨基，二烷基氨基，羟基氨基，烷基（烷氧基）氨基或烷氧基氨基，R2是羧基，羧甲基或羟甲基，R3是被苯硫基取代的（1-6） 其可以自身携带1至3个选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的取代基，被环烷硫基（3至7个成员）或通过杂芳硫基（5至6个成员）包含1至 4个选自N，S和O的杂原子，并且任选地本身被[由卤素，OH，烷基，烷氧基，CF 3，OCF 3，= O，COOH，烷氧基羰基，CN或NH 2]取代的R 3或被苯基取代的苯基， 被选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的3个取代基，或被包含3至7个成员的环烷基或被包含1至4个选自 N，O或S，以及任选的其自身取代基 CN，NH 2，R 4是烷基（1-6），链烯基-CH 2 - ，炔基-CH 2 - （3至7C），环烷基（C 1 -C 6）烷基，烷氧基羰基， 或（环烷基）烷基，其非对映异构体形式或其混合物及其药学上可接受的盐。这些新型衍生物是特别有利的抗微生物剂。

    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them
    26.
    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。