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78 条记录 (耗时 0.02 秒)

    Substituted derivatives of 20,21-dinoreburnamenine, their use as medicaments and the pharmaceutical compositions containing them
    3.
    发明授权
    Substituted derivatives of 20,21-dinoreburnamenine, their use as medicaments and the pharmaceutical compositions containing them 失效
    其作为药物和含有它们的药物组合物的二十二碳三烯酸的取代衍生物

    公开(公告)号：US5093337A

    公开(公告)日：1992-03-03

    申请号：US391511

    申请日：1989-07-18

    申请人： Nurgun Aktogu ,  Francois Clemence ,  Claude Oberlander

    发明人： Nurgun Aktogu ,  Francois Clemence ,  Claude Oberlander

    IPC分类号： C07D461/00 ,  A61K20060101 ,  A61K31/435 ,  A61K31/445 ,  A61K31/475 ,  A61K31/495 ,  A61P9/08 ,  A61P9/10 ,  A61P25/00 ,  A61P25/24 ,  A61P25/26 ,  C07D20060101

    CPC分类号： C07D461/00

    摘要： The invention concerns compounds of formula (I); ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, identical or different, stand for hydrogen, halogen, alkyl or alkoxy (C.sub.1-5), hydroxy, trifluoromethyl, nitro, amino, alkylamino, dialkylamino, acylamino, R.sub.1, R.sub.2 and R.sub.3 being unable to stand for hydrogen simultaneously and in which (a) stands for (b), (c), or (d), all possible isomeric forms of said products of formula (I) being racemic or optically active, as well as their additional salts with acids, their preparation and the new intermediate products obtained, their application as drugs in particular nootropes, antidepressants, neuronal protectors, anti-anoxics, anti-ischemics, and the compositions containing them.

    摘要翻译： PCT No.PCT / FR88 / 00562 Sec。 371日期：1989年7月18日 102（e）日期1989年7月18日PCT提交1988年11月16日PCT公布。 出版物WO89 / 04830 日期：1989年6月1日。本发明涉及式（I）化合物。 其中R1，R2和R3相同或不同，代表氢，卤素，烷基或烷氧基（C1-5），羟基，三氟甲基，硝基，氨基，烷基氨基，二烷基氨基，酰基氨基， R1，R2和R3不能同时代表氢，其中（a）代表（b），（c）或（d），所有式（I）产物的所有可能的异构形式是外消旋或光学活性的 以及它们与酸的附加盐，它们的制备和获得的新的中间产物，它们作为药物特别是助推剂，抗抑郁药，神经元保护剂，抗缺氧剂，抗缺血剂以及含有它们的组合物的应用。

    Decahydroquinolines and central analgesic method of use thereof
    4.
    发明授权
    Decahydroquinolines and central analgesic method of use thereof 失效
    十氢喹啉和中枢镇痛药的使用方法

    公开(公告)号：US4877796A

    公开(公告)日：1989-10-31

    申请号：US084456

    申请日：1987-08-12

    申请人： Francois Clemence ,  Odile Le Martret ,  Francoise Delevallee ,  Michel Fortin

    发明人： Francois Clemence ,  Odile Le Martret ,  Francoise Delevallee ,  Michel Fortin

    IPC分类号： A61K31/47 ,  A61P7/06 ,  A61P7/10 ,  A61P9/06 ,  A61P9/12 ,  A61P25/04 ,  C07D215/40 ,  C07D401/12 ,  C07D409/12

    CPC分类号： C07D215/40

    摘要： A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms of a decahydroquinoline of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and akyl of 1 to 5 carbon atoms, A is selected from the group consisting of --(CH.sub.2).sub.n --, --CH.sub.2 O-- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthyl, optionally substituted indenyl, optionally substituted heteromonocycle of 5 to 6 members and optionally substituted heterobicycle with the proviso that when Z is o-alkoxy-phenyl, A is not --(CH.sub.2).sub.n -- in which n is O, and their non-toxic, pharmaceutically acceptable acid addition salts and their quaternary ammonium salts and intermediates having analgesic, diuretic, hypotensive, anti-arrithmic and anti-cerebral-ischaemic properties.

    摘要翻译： 选自下式的化合物：其中R 1为1至5个碳原子的烷基，R 2选自氢和1至5个碳原子的烷基的所有对映异构体和非对映异构体形式的十氢喹啉的化合物 原子，A选自 - （CH 2）n - ， - CH 2 O-和被具有总共2至8个碳原子的烷基取代的亚烷基，n是0至5的整数，Z选自 由任选取代的苯基，任选取代的萘基，任选取代的茚基，任选取代的5至6个成员的异单环和任选取代的杂双环，条件是当Z是邻 - 烷氧基 - 苯基时，A不是 - （CH2）n-，其中 n是O，它们的无毒的药学上可接受的酸加成盐及其季铵盐和具有止痛，利尿，降压，抗对数和抗脑缺血性质的中间体。

    Ethenylphenol-indoles having antiarythmic utility
    5.
    发明授权
    Ethenylphenol-indoles having antiarythmic utility 失效
    具有抗血浆效用的乙烯基苯酚吲哚

    公开(公告)号：US4650811A

    公开(公告)日：1987-03-17

    申请号：US691163

    申请日：1985-01-14

    申请人： Jacques Guillaume ,  Francois Clemence ,  Neil L. Brown

    发明人： Jacques Guillaume ,  Francois Clemence ,  Neil L. Brown

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P3/00 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  A61P7/00 ,  A61P9/06 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/02 ,  A61P43/00 ,  C07D209/08 ,  C07D209/30 ,  C07D209/34 ,  C07D407/12 ,  C07D209/12

    CPC分类号： C07D407/12 ,  C07D209/08 ,  C07D209/30 ,  C07D209/34

    摘要： Novel ethenylphenol indoles of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with 1 to 3 members of the group consisting of halogen, methyl, ethyl, methoxy, ethoxy, methylthio, --CF.sub.3, --NH.sub.2 and --NO.sub.2 or R and R.sub.1 together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a second heteroatom selected from the group consisting of --O--, --S-- and ##STR2## R' is hydrogen or alkyl of 1 to 5 carbon atoms, a together with X is .dbd.0 and b is hydrogen or a together with b is a carbon-carbon bond and X is hydrogen, the dotted line indicates the possibility of a double bond with the compounds having the trans configuration if a double bond, A is selected from the group consisting of ##STR3## and --(CH.sub.2).sub.n --, n is 2,3,4 or 5, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms with the proviso that R and R.sub.1 are not both hydrogen when A is ##STR4## and their non-toxic, pharmaceutically acceptable acid addition salts having anti-arrhythmic and anti hypertensive properties and the property of blocking slow calcium-sodium channels and novel intermediates.

    摘要翻译： 式Ⅰ的新型乙烯基苯酚吲哚，其中R和R 1分别选自氢，1至5个碳原子的烷基，3至7个碳原子的环烷基，4至7个碳原子的环烷基烷基和芳烷基 任选被1至3个由卤素，甲基，乙基，甲氧基，乙氧基，甲硫基，-CF 3，-NH 2和-NO 2组成的组中任意取代的7至12个碳原子，或者R和R 1与氮原子一起形成任选不饱和的 任选地含有选自-O - ， - S-和R'的第二杂原子的杂环是氢或1至5个碳原子的烷基，以及X是= 0，b是氢或一起 其中b是碳 - 碳键，X是氢，虚线表示与具有反式构型的化合物具有双键的可能性，如果双键，A选自和 - （CH2 ）n-，n为2,3,4或5，R2选自c 存在氢和1至5个碳原子的烷基，条件是当A为A时，R和R1不同时为氢，并且它们具有抗心律失常和抗高血压性质的无毒的药学上可接受的酸加成盐和其特性 阻断缓慢的钙钠通道和新型中间体。

    [4H]-1,3-Benzodioxin-2-carboxylic acids
    6.
    发明授权
    [4H]-1,3-Benzodioxin-2-carboxylic acids 失效
    [4H] -1,3-苯并二恶英-2-羧酸

    公开(公告)号：US4281012A

    公开(公告)日：1981-07-28

    申请号：US034432

    申请日：1979-04-30

    申请人： Daniel Humbert ,  Francois Clemence ,  Michele Dagnaux

    发明人： Daniel Humbert ,  Francois Clemence ,  Michele Dagnaux

    IPC分类号： A61K31/335 ,  A61K31/357 ,  A61P3/04 ,  A61P9/00 ,  C07C39/17 ,  C07C39/28 ,  C07C39/367 ,  C07C39/373 ,  C07C39/42 ,  C07C41/30 ,  C07C43/23 ,  C07C45/46 ,  C07C49/83 ,  C07C49/84 ,  C07D319/08

    CPC分类号： C07D319/08 ,  C07C39/17 ,  C07C39/28 ,  C07C39/367 ,  C07C39/373 ,  C07C39/42 ,  C07C41/30 ,  C07C45/46 ,  C07C49/83 ,  C07C49/84 ,  C07C2101/14

    摘要： Novel racemates and optically active isomers and mixtures of isomers of [4H]-1,3-benzodioxin-2-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, dialkylamino alkyl with alkyls of 1 to 5 carbon atoms, alkali metal, alkaline earth metal, aluminum, --NH.sub.4, non-toxic pharmaceutically acceptable amines, 2,3-dihydroxypropanyl and (2,2-dimethyl-1,3-dioxolan-4-yl)-methyl, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.3 and R.sub.6 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, ethenyl and cyclohexyl and taken together with the carbon atom to which they are attached form cyclohexyl, R.sub.5 is selected from the group consisting of hydrogen and halogen or R.sub.1 and R.sub.2 have the above definitions, R.sub.6 is ##STR2## R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, --CF.sub.3, cyclohexyl, alkoxy of 1 to 3 carbon atoms, alkyl of 1 to 3 carbon atoms and p-chlorophenoxy and R.sub.3 is selected from the group consisting of 2-propenyl, ethenyl, cyclohexyl, benzyl, hydrogen and alkyl of 1 to 5 carbon atoms with the proviso that when R.sub.3 is alkyl, at least one of R.sub.4 and R.sub.5 is no hydrogen or halogen and when R.sub.3 is hydrogen, at least one of R.sub.4 and R.sub.5 is not hydrogen, halogen or --CF.sub.3 and the non-toxic, pharmaceutically acceptable acid addition salts thereof when R.sub.1 is dialkylaminoalkyl which have a marked hypolipemiant activity and reduces the plasmatic level of lipids, triglycerides and cholestrol and their preparation.

    摘要翻译： 新颖的外消旋物和光学活性异构体以及式[IMAGE] I的[4H] -1,3-苯并二恶英-2-羧酸化合物的异构体的混合物，其中R 1选自氢，1至5个碳的烷基 原子，具有1至5个碳原子的烷基的二烷基氨基烷基，碱金属，碱土金属，铝，-NH 4，无毒的药学上可接受的胺，2,3-二羟基丙酰基和（2,2-二甲基-1,3-二氧戊环） -4-基） - 甲基，R 2选自氢和1至5个碳原子的烷基，R 3和R 6分别选自氢，1至6个碳原子的烷基，乙烯基和环己基 并且与它们所连接的碳原子一起形成环己基，R 5选自氢和卤素，或者R 1和R 2具有上述定义，R 6和R 5各自独立地选自 的氢，卤素，-CF 3，环己基，1〜3个碳原子的烷氧基 在原子上具有1至3个碳原子的烷基和对氯苯氧基，R3选自2-丙烯基，乙烯基，环己基，苄基，氢和1至5个碳原子的烷基，条件是当R3为烷基 ，R 4和R 5中的至少一个不是氢或卤素，并且当R 3是氢时，当R 1是二烷基氨基烷基时，R 4和R 5中的至少一个不是氢，卤素或-CF 3及其无毒的药学上可接受的酸加成盐 其具有显着的降胆固醇活性并降低脂质，甘油三酯和胆甾醇的血浆水平及其制备。

    Decahydroquinoline compounds
    9.
    发明授权
    Decahydroquinoline compounds 失效
    十氢喹啉化合物

    公开(公告)号：US5254566A

    公开(公告)日：1993-10-19

    申请号：US950087

    申请日：1992-09-22

    申请人： Francois Clemence ,  Gilles Hamon ,  Odile Le Martret

    发明人： Francois Clemence ,  Gilles Hamon ,  Odile Le Martret

    IPC分类号： A61K31/47 ,  A61P9/10 ,  A61P25/04 ,  A61P25/28 ,  C07D215/40 ,  C07D215/42 ,  C07D215/46 ,  A61K31/44 ,  C07D401/04

    CPC分类号： C07D215/42 ,  C07D215/40 ,  C07D215/46

    摘要： A compound selected from the group consisting of racemates, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms optionally substituted with at least one halogen, hydroxy, alkyl or alkoxy of 1 to 4 carbon atoms or taken together with the nitrogen to which they are attached form a heterocycle optionally containing a heteroatom selected from the group consisting of --O--, --S-- and nitrogen optionally substituted with alkyl or alkoxy of 1 to 5 carbon atoms, optionally substituted benzyl and phenyl, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, halogen, hydroxy and alkyl and alkoxy of 1 to 5 carbon atoms optionally substituted with at least one substituent selected from the group consisting of halogen, hydroxy, phenyl and alkyl and alkoxy of 1 to 4 carbon atoms, R.sub.5 is hydrogen or alkyl of 1 to 5 carbon atoms optionally substituted with at least one member of the group consisting of halogen, hydroxy, phenyl and alkyl and alkoxy of 1 to 4 carbon atoms and its non-toxic, pharmaceutically acceptable acid addition salts and quaternary ammonium salts having analgesic activity and their preparation.

    摘要翻译： 选自下列化合物的外消旋物，对映异构体和非对映异构体形式的化合物其中R 1和R 2分别选自氢和1至5个碳原子的烷基，任选被至少取代 1至4个碳原子的一个卤素，羟基，烷基或烷氧基或与它们所连接的氮一起形成任选含有选自-O - ， - S-和选自-O - ， - S- 1至5个碳原子的烷基或烷氧基，任选取代的苄基和苯基，R 3和R 4分别选自氢，卤素，羟基和1至5个碳原子的烷基和烷氧基，任选被至少一个选自 由卤素，羟基，苯基和1-4个碳原子的烷基和烷氧基组成的组，R5是氢或1〜5个碳原子的烷基， 与至少一个由卤素，羟基，苯基和具有1至4个碳原子的烷基和烷氧基组成的组及其无毒的药学上可接受的酸加成盐和具有止痛活性的季铵盐及其制备。