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75 条记录 (耗时 0.022 秒)

    Pyridines
    35.
    发明授权
    Pyridines 失效
    吡啶类

    公开(公告)号：US4987140A

    公开(公告)日：1991-01-22

    申请号：US441317

    申请日：1989-11-27

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

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

    IPC分类号： C07D213/75 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/505 ,  A61P29/00 ,  C07D213/82 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

    CPC分类号： C07D213/82 ,  C07D417/12

    摘要： Novel pyridines of the formula ##STR1## wherein R is selected from the group consisting of (a) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen --CF.sub.3 and --NO.sub.2 and (b) a 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of (a) alkyl of 1 to 5 carbon atoms, (b) 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms and (c) phenyl and naphthyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --NO.sub.3 and --CF.sub.3, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, --(CF.sub.2).sub.n --CF.sub.3 and ##STR2## n is an integer from 0 to 4 and Alk is alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids and bases having anti-inflammatory and anti-rheumatic properties.

    Decahydroquinolines and analgesic use thereof
    37.
    发明授权
    Decahydroquinolines and analgesic use thereof 失效
    十氢喹啉及其止痛用途

    公开(公告)号：US4816465A

    公开(公告)日：1989-03-28

    申请号：US2778

    申请日：1987-01-13

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

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

    IPC分类号： A61K31/47 ,  A61K31/4709 ,  A61P9/00 ,  A61P9/06 ,  A61P25/04 ,  C07D215/18 ,  C07D215/40 ,  C07D333/00 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D401/02

    CPC分类号： C07D401/06 ,  C07D215/18 ,  C07D215/40 ,  C07D409/06

    摘要： Novel enantiomeric and diastereoisomeric forms of decahydroquinolines 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 or taken together with the nitrogen atom to which they are connected form a 5 to 6 member heterocycle optionally including another heteroatom and optionally substituted, A is selected from the group consisting of --(CH.sub.2).sub.n -- and alkylene substituted with an alkyl and having 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, naphthyl indenyl, monocyclic heterocycle of 5 to 6 members and a bicyclic heterocycle all being unsubstituted or substituted by one or more substituents and their non-toxic, pharmaceutically acceptable acid addition salts and quaternary ammonium salts having central analgesic properties.

    摘要翻译： 新颖的对映异构体和非对映异构形式的式Ⅰ'的十氢喹啉其中R 1和R 2分别选自氢和1至5个碳原子的烷基或与它们连接的氮原子一起形成5 至6元杂环，任选地包括另外的杂原子和任选取代的A选自 - （CH 2）n - 和被烷基取代并具有2-8个碳原子的亚烷基，n是0-5的整数，Z 选自5至6个成员的任选取代的苯基，萘基茚基，单环杂环和全部未被取代或被一个或多个取代基取代的双环杂环，及其无毒的药学上可接受的酸加成盐和季铵盐 具有中枢镇痛特性。

    Novel indole carboxamides
    38.
    发明授权
    Novel indole carboxamides 失效
    新型吲哚甲酰胺

    公开(公告)号：US4791109A

    公开(公告)日：1988-12-13

    申请号：US883915

    申请日：1986-07-10

    申请人： Francois Clemence ,  Jacques Guillaume ,  Gilles Hamon

    发明人： Francois Clemence ,  Jacques Guillaume ,  Gilles Hamon

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/445 ,  A61K31/495 ,  A61P9/06 ,  C07D209/08 ,  C07D209/34 ,  A61K31/535 ,  C07D413/12

    CPC分类号： C07D209/34 ,  C07D209/08

    摘要： Novel indole-carboxamides 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, --CF.sub.3, CH.sub.3 S--, --NH.sub.2 and --NO.sub.2 or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl, aralkyl of 7 to 12 carbon atoms and substituted phenyl, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, chlorine, bromine, iodine, --NO.sub.2, --NH.sub.2, acylamide of an aliphatic carboxylic acid of 2 to 5 carbon atoms and mono and dialkylamino with alkyl of 1 to 5 carbon atoms, a and b form .dbd.O and c is hydrogen or a and c form a carbon-carbon bond and b is hydrogen, A is selected from the group consisting of --(CH.sub.2).sub.n --and ##STR3## n is an integer from 2 to 5, m is an integer from 1 to 3, B is ##STR4## R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anti-arrhythmic properties.

    摘要翻译： 式I的新型吲哚甲酰胺其中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，-CF 3，CH 3 S - ， - NH 2和-NO 2组成的组中取代的7至12个碳原子，或者R 1和R 3与氮原子一起形成 任选地含有-O - ， - S-和R'的成员的任选的不饱和杂环选自氢，1至5个碳原子的烷基，苯基，萘基，7位的芳烷基 至12个碳原子和取代的苯基，R 3选自氢，1至5个碳原子的烷基，1至3个碳原子的烷氧基，氯，溴，碘，-NO 2，-NH 2，脂族 2至5个碳原子的羧酸和一烷基和二烷基氨基 1至5个碳原子，a和b形式= O，c是氢或a和c形成碳 - 碳键，b是氢，A选自 - （CH 2）n - 和＆lt; IMAGE＆gt; n 是2至5的整数，m是1至3的整数，B是选自氢和1至5个碳原子的烷基及其无毒的药学上可接受的酸加成盐 具有显着的抗心律失常性质。

    Preparation of amides of 4-hydroxy-3-quinoline-carboxylic acid
    39.
    发明授权
    Preparation of amides of 4-hydroxy-3-quinoline-carboxylic acid 失效
    4-羟基-3-喹啉羧酸的酰胺的制备

    公开(公告)号：US4596875A

    公开(公告)日：1986-06-24

    申请号：US623430

    申请日：1984-06-22

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

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

    IPC分类号： C07D215/56 ,  A61K31/47 ,  A61P25/04 ,  A61P29/00 ,  C07D209/38 ,  C07D265/22 ,  C07D277/46 ,  C07D401/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/048 ,  C07D215/22 ,  C07D417/06

    CPC分类号： C07D265/22 ,  C07D209/38 ,  C07D277/46 ,  C07D401/12 ,  C07D417/12 ,  C07D491/04

    摘要： Novel 4-hydroxy-3-quinoline-carboxamides of the formula ##STR1## wherein X is in the 5,6,7 or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --OCF.sub.3 and --SCF.sub.3, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of thiazolyl, 4,5-dihydro-thiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidinyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.4 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and ##STR2## R.sub.5 ' is selected from the group consisting of alkyl of 1 to 4 carbon atoms and aryl and their non-toxic, pharmaceutically acceptable acid addition salts and salts with non-toxic, pharmaceutically acceptable bases having very good analgesic activity and a non-negligible anti-inflammatory activity and novel intermediates.

    摘要翻译： 下式的新型4-羟基-3-喹啉 - 甲酰胺其中X在5,6,7或8-位，并且选自氢，卤素，1至5个碳原子的烷基 1至4个碳原子的烷氧基，-CF 3，-OCF 3和-SCF 3，R 1选自氢和1至4个碳原子的烷基，R 2选自噻唑基， 二氢 - 噻唑基，吡啶基，恶唑基，异恶唑基，咪唑基，嘧啶基和四唑基，全部任选被1至4个碳原子的烷基取代，并且苯基任选被至少一个由-OH，1-4个碳原子的基团取代 1至4个碳原子的烷氧基，-CF 3，-NO 2和卤素，R 3选自氢，1至4个碳原子的烷基和芳基，R 4选自氢， 1至4个碳原子和芳基，R 5选自氢，1至4个碳原子的烷基 R 5'选自1至4个碳原子的烷基和芳基及其无毒的药学上可接受的酸加成盐和与具有非常好的止痛活性的无毒，药学上可接受的碱的盐，以及 不可忽略的抗炎活性和新型中间体。

    4,5-Bis(aryl)-4H-1,2,4-triazole derivatives and analgesic use
    40.
    发明授权
    4,5-Bis(aryl)-4H-1,2,4-triazole derivatives and analgesic use 失效
    4,5-双（芳基）-4H-1,2,4-三唑衍生物和止痛用途

    公开(公告)号：US4512997A

    公开(公告)日：1985-04-23

    申请号：US552747

    申请日：1983-11-17

    申请人： Jean Meier ,  Francois Clemence

    发明人： Jean Meier ,  Francois Clemence

    IPC分类号： A61K31/41 ,  A61P25/04 ,  C07C243/38 ,  C07D249/08 ,  C07D317/46 ,  C07D405/04 ,  A61K31/395

    CPC分类号： C07D249/08 ,  C07C243/38 ,  C07D317/46 ,  Y10S514/886

    摘要： Novel 4H-1,2,4-triazoles of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be in different positions of the benzene rings and are individually selected from the group consisting of hydrogen, --OH, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, --CF.sub.3, --NO.sub.2, --NH.sub.2 and --NH--AlK and ##STR2## and AlK, AlK.sub.1 and AlK.sub.2 are alkyl of 1 to 4 carbon atoms or R.sub.1 and R.sub.2 together and/or R.sub.3 and R.sub.4 together are methylenedioxy, R is selected from the group consisting hydrogen, alkyl of 1 to 4 carbon atoms, --CH.sub.2 --COOH and --CH.sub.2 --COOAlK.sub.3 and AlK.sub.3 is alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable analgesic activity and a novel method for their preparation.

    摘要翻译： 式（Ⅰ）的新型4H-1,2,4-三唑其中R 1，R 2，R 3和R 4可以在苯环的不同位置，并且分别选自氢，-OH， 1至4个碳原子的烷氧基，1至4个碳原子的烷氧基，卤素，-CF 3，-NO 2，-NH 2和-NH-AlK，和AlK，AlK1和AlK2是1至4个碳原子的烷基， R 2一起和/或R 3和R 4一起是亚甲二氧基，R选自氢，1至4个碳原子的烷基，-CH 2 -COOH和-CH 2 -COOAlK 3，AlK 3是1至4个碳原子的烷基， 无毒，药学上可接受的具有显着镇痛活性的酸加成盐及其制备方法。