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    Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them
    3.
    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.

    Isoindolinone derivatives, processes for preparing them and medicines containing them
    4.
    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。

    2-iminobenzothiazoline derivatives, their preparation and pharmaceutical compositions containing them
    6.
    发明授权
    2-iminobenzothiazoline derivatives, their preparation and pharmaceutical compositions containing them 失效
    2-亚氨基苯并噻唑啉衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US5008280A

    公开(公告)日：1991-04-16

    申请号：US450231

    申请日：1989-12-13

    申请人： Claude Gueremy ,  Patrick Jimonet ,  Serge Mignani

    发明人： Claude Gueremy ,  Patrick Jimonet ,  Serge Mignani

    IPC分类号： A61K31/425 ,  A61K31/428 ,  A61K31/445 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/28 ,  C07D277/68 ,  C07D277/82 ,  C07D417/06

    CPC分类号： C07D277/82

    摘要： Compounds of the formula: ##STR1## in which - R.sub.1 denotes a polyfluoroalkoxy or polyfluoroalkyl radical, and - R.sub.2 denoteseither a chain --CH.sub.2 --(CH(R.sub.4)).sub.n --R.sub.3, in which R.sub.3 denotes a dialkylamino, piperidino, 1-pyrrolidinyl, mercapto, acylthio, alkylthio, alkylsulphinyl or alkylsulphonyl radical, R.sub.4 denotes a hydrogen atom or an alkyl radical and n is equal to 0 or 1,or a residue of formula: ##STR2## the said alkyl and alkoxy radicals and portions containing 1 to 4 carbon atoms each in a straight or branched chain and said the acyl portions containing 2 to 4 carbon atoms each, and the salts of these compounds, are useful in the treatment of diseases in which glutamate is implicated.

    摘要翻译： 下式的化合物：其中-R 1表示多氟烷氧基或多氟烷基，-R 2表示链-CH 2 - （CH（R 4））n -R 3，其中R 3表示二烷基氨基，哌啶子基 ，1-吡咯烷基，巯基，酰硫基，烷硫基，烷基亚磺酰基或烷基磺酰基，R4表示氢原子或烷基，n等于0或1，或下式的残基：所述烷基和烷氧基， 各直链或支链含有1至4个碳原子的部分和所述酰基部分各自含有2至4个碳原子，并且这些化合物的盐可用于治疗涉及谷氨酸的疾病。

    Derivatives of pyrazole-5-acetic acid
    8.
    发明授权
    Derivatives of pyrazole-5-acetic acid 失效
    吡唑-5-乙酸的衍生物

    公开(公告)号：US3984431A

    公开(公告)日：1976-10-05

    申请号：US589513

    申请日：1975-06-23

    申请人： Claude Gueremy ,  Christian Renault

    发明人： Claude Gueremy ,  Christian Renault

    IPC分类号： C07D231/12 ,  C07D231/14

    CPC分类号： C07D231/12 ,  Y10S514/916

    摘要： Compounds having anti-inflammatory and antipyretic action have the general formula ##SPC1##In which each of R.sub.1 and R.sub.2 is a phenyl group which may be substituted by a halogen atom, an alkyl or alkoxy group having 1 to 4 carbon atoms or a trifluoromethyl group, R.sub.3 is a straight or branched chain saturated or unsaturated aliphatic hydrocarbon group or a cycloaliphatic hydrocarbon group having 3 to 7 carbon atoms, or a benzyl or phenyl group which benzyl or phenyl groups may be substituted in the benzene ring by a halogen atom, an alkyl or alkoxy group having 1 to 4 carbon atoms or a trifluoromethyl group or by any two of these substituents, R.sub.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms and A is a group having one of the formulae --COOH, --COOR.sub.5 and --CONR.sub.6 R.sub.7 in which R.sub.5 is an alkyl group having 1 to 4 carbon atoms or a benzyl group and each of R.sub.6 and R.sub.7 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are attached represents a pyrrolidino, a piperidino or a morpholino group.

    摘要翻译： 具有抗炎和解热作用的化合物具有通式为，其中R 1和R 2为可被卤素原子，具有1至4个碳原子的烷基或烷氧基或三氟甲基取代的苯基，R 3为 苄基或苯基可以在苯环中被卤素原子取代的苄基或苯基，烷基或烷氧基，烷基或烷氧基 具有1至4个碳原子的基团或三氟甲基或通过这些取代基中的任何两个取代基，R 4是氢原子或具有1至4个碳原子的烷基，A是具有下列基团的基团-COOH，-COOR 5和 -CONR 6 R 7，其中R 5为具有1至4个碳原子的烷基或苄基，并且R 6和R 7各自为氢原子或具有1至4个碳原子的烷基或R 6和R 7与氮原子一起与 哪个 y表示吡咯烷子基，哌啶子基或吗啉基。

    Benzothiazole derivatives and medicinal products containing them
    9.
    发明授权
    Benzothiazole derivatives and medicinal products containing them 失效
    苯并噻唑衍生物和含有它们的药用产品

    公开(公告)号：US5340824A

    公开(公告)日：1994-08-23

    申请号：US938153

    申请日：1992-12-02

    申请人： Claude Gueremy ,  Patrick Jimonet ,  Serge Mignani

    发明人： Claude Gueremy ,  Patrick Jimonet ,  Serge Mignani

    IPC分类号： A61K31/445 ,  A61P25/28 ,  C07D277/82 ,  C07D417/12 ,  A61K31/44

    CPC分类号： C07D277/82

    摘要： ##STR1## Compounds of formula (I), in which R
    1 is a polyfluoralkoxy, R
    2 is a sulphur or nitrogen atom substituted by an alkyl radical or a sulfonyl or sulfinyl radical, R
    3 is a phenyl, benzoyl, --NR
    4 R
    5 or piperidinyl-4radical substituted in position 1 by a phenylalkyl radical, R
    4 is an alkyl radical, R
    5 is a phenylalkyl radical, n is equal to 1, 2 or 3, m is equal to 0, 1, 2 or 3. The present invention also relates to the salts of said compounds, processes for the preparation of the latter and drugs containing them.

    摘要翻译： PCT No.PCT / FR91 / 00437 Sec。 371日期1992年12月2日 102（e）日期1992年12月2日PCT提交1991年5月31日PCT公布。 WO91 / 18892 PCT出版物 （I）式（I）化合物，其中R 1是多氟烷氧基，R 2是被烷基或磺酰基或亚磺酰基取代的硫或氮原子，R 3是苯基 ，苯甲酰基，-NR4R5或哌啶基-4-取代的苯基烷基，R4为烷基，R5为苯基烷基，n等于1,2或3，m等于0,1,2或 本发明还涉及所述化合物的盐，其制备方法和含有它们的药物。