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    Decahydroquinolines and central analgesic method of use thereof
    1.
    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。

    8-amino decahydroquinolines and medicinal use thereof
    2.
    发明授权
    8-amino decahydroquinolines and medicinal use thereof 失效
    8-氨基十氢喹啉及其医药用途

    公开(公告)号：US4963567A

    公开(公告)日：1990-10-16

    申请号：US371995

    申请日：1989-06-27

    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 alkyl 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 hetero-bicycle 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.

    Pyridines
    5.
    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
    6.
    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。

    Preparation of amides of 4-hydroxy-3-quinoline-carboxylic acid
    7.
    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-Hydroxy-3-quinoline-carboxylic acid derivatives
    8.
    发明授权
    4-Hydroxy-3-quinoline-carboxylic acid derivatives 失效
    4-羟基-3-喹啉羧酸衍生物

    公开(公告)号：US4486438A

    公开(公告)日：1984-12-04

    申请号：US498832

    申请日：1983-05-27

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

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

    IPC分类号： C07D215/56 ,  A61K31/47 ,  A61P25/04 ,  A61P29/00 ,  C07D209/38 ,  C07D265/22 ,  C07D277/46 ,  C07D401/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/048 ,  C07D215/36

    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，烷基1 至4个碳原子和芳基，R 5选自氢，1至4个碳原子的烷基和 R5'选自1-4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盐与具有非常好的止痛活性的无毒的药学上可接受的碱， - 轻微的抗炎活性和新颖的中间体。

    Novel hydroquinolines useful as intermediates
    9.
    发明授权
    Novel hydroquinolines useful as intermediates 失效
    新型氢醌可用作中间体

    公开(公告)号：US4988810A

    公开(公告)日：1991-01-29

    申请号：US389805

    申请日：1989-08-04

    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： C07D215/18 ,  C07D215/40

    CPC分类号： C07D215/18 ,  C07D215/40

    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 from 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体形式的式Ia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。