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

    公开(公告)号:US5021420A

    公开(公告)日:1991-06-04

    申请号:US375934

    申请日:1989-07-06

    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.

    2-iminobenzothiazoline derivatives, their preparation and pharmaceutical
compositions containing them
    5.
    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

    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。

    Benzothiazole derivatives and medicinal products containing them
    7.
    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

    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。

    Isoindolinone derivatives, processes for preparing them and medicines
containing them
    9.
    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

    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。

    Derivatives of pyrazole-5-acetic acid
    10.
    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

    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。