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    Decahydroquinoline compounds
    1.
    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。

    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。

    Novel hydroquinolines useful as intermediates
    5.
    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。

    4H-triazolo[4,3-a][1,4]benzodiazepines
    6.
    发明授权
    4H-triazolo[4,3-a][1,4]benzodiazepines 失效
    4H-三唑并[4,3-a] [1,4]苯并二氮杂卓

    公开(公告)号：US4987131A

    公开(公告)日：1991-01-22

    申请号：US491264

    申请日：1990-03-08

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

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

    IPC分类号： A61K31/55 ,  A61P25/04 ,  A61P29/00 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： Novel 4H-triazolo[4,3-a][1,4]benzodiazepines 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 and R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --NH.sub.2, --NHalk wherein alk is alkyl of 1 to 4 carbon atoms, ##STR2## and alk.sub.1 and alk.sub.2 are individually alkyl of 1 to 4 carbon atoms, halogen, --NO.sub.2 and --CF.sub.3 in any position of the benzene rings with the proviso that R.sub.5 and R.sub.6 are not both hydrogen and their non-toxic, pharmaceutically acceptable acid addition salts having good analgesic activity.

    摘要翻译： 新颖的式（Ia）[1,4]苯并二氮杂其中R 1和R 2分别选自氢和1至5个碳原子的烷基，R 3，R 4， R5和R6分别选自氢，-OH，具有1-4个碳原子的烷基和烷氧基，-NH2，-NHalk，其中alk是1至4个碳原子的烷基，＆lt; IMAGE＆gt;和alk1和alk2是 单独的1-4个碳原子的烷基，卤素，-NO 2和-CF 3在苯环的任何位置，条件是R 5和R 6不是氢，也不是它们无毒的药学上可接受的具有良好镇痛活性的酸加成盐。

    Decahydroquinolines and 5,6,7,8 tetrahydroquinolines
    8.
    发明授权
    Decahydroquinolines and 5,6,7,8 tetrahydroquinolines 失效
    十氢喹啉和5,6,7,8四氢喹啉

    公开(公告)号：US4950760A

    公开(公告)日：1990-08-21

    申请号：US348766

    申请日：1989-05-08

    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： C07D215/40

    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 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。

    Novel 4-hydroxy-3-quinoline-carboxylates having analgesic and anti-inflammatory activity
    9.
    发明授权
    Novel 4-hydroxy-3-quinoline-carboxylates having analgesic and anti-inflammatory activity 失效
    具有止痛和抗炎活性的新型4-羟基-3-喹啉羧酸酯

    公开(公告)号：US4735951A

    公开(公告)日：1988-04-05

    申请号：US790064

    申请日：1985-10-22

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

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

    IPC分类号： A61K31/47 ,  A61P1/04 ,  A61P25/04 ,  A61P29/00 ,  C07D213/75 ,  C07D215/56 ,  C07D265/22 ,  C07D277/46 ,  C07D401/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/048

    CPC分类号： C07D213/75 ,  C07D265/22 ,  C07D277/46 ,  C07D401/12 ,  C07D417/12 ,  C07D491/04

    摘要： Novel optical isomers and racemates of 4-hydroxy-3-quinoline-carboxylates 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, --SCF.sub.3 and --OCF.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-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, R.sub.3 and R.sub.4 are individually 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 aryl of 6 to 14 carbon atoms, heteroaryl of 3 to 14 carbon atoms, alkyl of 1 to 14 carbon atoms, alkyl substituted with --NH.sub.2, --NHAlk or ##STR2## alkenyl of 2 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms substituted with aryl of 6 to 14 carbon atoms, Alk and Alk' are alkyl of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts with the proviso that when X is 8-CF.sub.3, R.sub.1 and R.sub.3 are hydrogen, R.sub.2 is 2-thiazolyl, R.sub.4 is methyl, R.sub.5 is not methyl having analgesic and anti-inflammatory activity.

    摘要翻译： 4-羟基-3-喹啉羧酸盐的新型光学异构体和外消旋物，其中X为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，-SCF 3和-OCF 3，R 1选自氢和1至4个碳原子的烷基，R 2选自 由噻唑基，4,5-二氢噻唑基，吡啶基，恶唑基，异恶唑基，咪唑基，嘧啶基和四唑基组成，全部任选被1至4个碳原子的烷基取代，苯基被至少一个由-OH，烷基和 1至4个碳原子的烷氧基，-CF 3，-NO 2和卤素，R 3和R 4分别选自氢，1至4个碳原子的烷基和芳基，R 5选自6 至14个碳原子，3至14个碳原子的杂芳基，1至14个碳原子的烷基，烷基取代基 具有2至6个碳原子的-NH 2，-NHA 1k或2个碳原子的烯基，2至6个碳原子被6至14个碳原子的芳基取代的烯基，Alk和Alk'是1至6个碳原子的烷基， 无毒，药学上可接受的酸加成盐，条件是当X为8-CF 3时，R 1和R 3为氢，R 2为2-噻唑基，R 4为甲基，R 5为不具有镇痛和抗炎活性的甲基。

    Anti-inflammatory and analgesig thiophene acetic acid derivatives, compositions, and method of use therefor
    10.
    发明授权
    Anti-inflammatory and analgesig thiophene acetic acid derivatives, compositions, and method of use therefor 失效
    抗炎和止痛噻吩乙酸衍生物，组合物及其用途

    公开(公告)号：US4719224A

    公开(公告)日：1988-01-12

    申请号：US836844

    申请日：1986-03-06

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

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

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P9/00 ,  A61P9/10 ,  A61P25/04 ,  A61P29/00 ,  C07D333/50 ,  C07D333/78 ,  C07D409/04 ,  C07D401/12 ,  C07D413/12

    CPC分类号： C07D333/50 ,  C07D333/78 ,  C07D409/04

    摘要： Novel optically active isomers or racemic mixtures of thiophene acetic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Y is selected from the group consisting of --OR.sub.2 and ##STR2## R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and ##STR3## n is an integer from 2 to 5, X' and X" are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom form an optionally unsaturated heterocycle of 5 to 6 ring members, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids and bases having a good analgesic and anti-inflammatory activity and inhibition of 5-lipoxygenase and cyclooxygenase, a process and intermediates for their preparation.

    摘要翻译： 新颖的旋光异构体或式Ia的噻吩乙酸衍生物的外消旋混合物，其中R 1选自氢和1至5个碳原子的烷基，Y选自-OR 2和 图像> R2选自氢，1至5个碳原子的烷基，并且 n是2至5的整数，X'和X“分别选自氢和烷基的 1至5个碳原子或与氮原子一起形成5至6个环成员的任选不饱和杂环，R3和R4分别选自氢和1至5个碳原子的烷基，它们的无毒， 具有良好的止痛和抗炎活性的酸和碱的药学上可接受的盐和5-脂氧合酶和环加氧酶的抑制，其制备方法和中间体。