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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。

    2-iminobenzothiazoline derivatives, their preparation and pharmaceutical compositions containing them
    4.
    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
    7.
    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
    8.
    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。

    Phenothiazine derivative
    10.
    发明授权
    Phenothiazine derivative 失效
    苯并噻嗪衍生物

    公开(公告)号：US3987042A

    公开(公告)日：1976-10-19

    申请号：US621617

    申请日：1975-10-10

    申请人： Claude Gueremy ,  Robert Labey ,  Didier Wirth ,  Maurice Auclair

    发明人： Claude Gueremy ,  Robert Labey ,  Didier Wirth ,  Maurice Auclair

    IPC分类号： C07D453/02

    CPC分类号： C07D453/02

    摘要： Phenothiazine derivatives are described of the formula ##SPC1##In which X.sub.1 and X.sub.2, which may be the same or different, are H, R, F, Cl, Br, OR, CN, --COR, CH.sub.3, --S--R, --SOR, --SO.sub.2 R or --SO.sub.2 N(CH.sub.3).sub.2, where R is an alkyl group having from 1 to 4 carbon atoms, and the quinuclidine ring is substituted by the group --(CH.sub.2).sub.x -- in the 2- or 3- position, x being 1 or 2 when said group is substituted in the 2-position and being 0 or 1 when said group is substituted in the 3-position (because of electronic hindrance), and their acid addition and quaternary ammonium salts, have valuable pharmacological properties. In particular, these compounds have anti-histaminic, anti-cholinergic, adrenolytic, neuro-sedative, tranquillizing and/or spasmolytic properties.These compounds are prepared by condensing an appropriate phenothiazine with a quinuclidine derivative of the formula ##SPC2##In which x has the above-stated meaning and Z is a halogen atom or a reactive ester group.