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    Decahydroquinolines and central analgesic method of use thereof
    2.
    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
    4.
    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.

    Novel indanes
    5.
    发明授权
    Novel indanes 失效
    新的indanes

    公开(公告)号：US5234944A

    公开(公告)日：1993-08-10

    申请号：US970776

    申请日：1992-11-03

    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： C07D295/135 ,  C07D311/96

    CPC分类号： C07D295/135 ,  C07D311/96

    摘要： A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula ##STR1## wherein R.sub.6 is selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually hydrogen or alkyl of 1 to 5 carbon atoms or taken together with the carbon atoms to which they are attached form a cycloalkyl of 3 to 6 carbon atoms optionally containing a heteroatom selected from the group consisting of --S--, --O-- and --N--, one of A and B has the formula ##STR2## and the other has the formula ##STR3## R is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Z is selected from the group consisting of --(CH.sub.2).sub.n --, branched alkylene of 2 to 8 carbon atoms and --CH.sub.2 O--, n is an integer of 0 to 5, X, X' and X" are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 4 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.2, mono and dialkylamino of 1 to 4 alkyl carbon atoms and sulfamino, R.sub.3 and R.sub.4 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 attached form a 5 to 6 member heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR4## R.sub.1 ' is hydrogen or alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having a strong affinity for optical receptors, central analgesic, diuretic, anti-arrythmic, hypotensive and cerebral anti-ischemic activity.

    摘要翻译： 选自下组的对映异构体和非对映异构体形式的化合物及其混合物，其中R 6选自氢，卤素和1至5个碳原子的烷基和烷氧基，R 1和R 2分别为 氢或1至5个碳原子的烷基或与它们所连接的碳原子一起形成3至6个碳原子的环烷基，任选地含有选自-S - ， - O-和-N - ，A和B中的一个具有式，另一个具有式（Ia）的化合物，其选自氢和1至5个碳原子的烷基，Z选自 - （ CH 2）n支链亚烷基，-CH 2 O-，n为0〜5的整数，X，X'和X“分别选自氢，烷基和烷氧基的1 至4个碳原子，卤素，-OH，-CF 3，-NO 2，-NH 2，1至4个烷基的单和二烷基氨基 碳原子和磺氨基，R3和R4分别选自氢和1至5个碳原子的烷基，或与它们所连接的氮原子一起形成5至6个成员杂环，任选地含有 由-O-，-S-和R IMA'组成的基团是氢或1至4个碳原子的烷基，它们对光学受体具有强亲和力的无毒的药学上可接受的酸加成盐，中枢性镇痛药，利尿剂， 抗焦虑，降压和脑抗缺血活性。

    Novel 4-hydroxy-3-pyridine-carboxamides useful for treating inflammation and rheumatism
    6.
    发明授权
    Novel 4-hydroxy-3-pyridine-carboxamides useful for treating inflammation and rheumatism 失效
    用于治疗炎症和风湿病的新型4-羟基-3-吡啶 - 甲酰胺

    公开(公告)号：US4925859A

    公开(公告)日：1990-05-15

    申请号：US167375

    申请日：1988-03-31

    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 hetercyclic 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.

    摘要翻译： 式（I）的新吡啶，其中R选自（a）任选被至少一个由1-5个碳原子的羟基，烷基和烷氧基组成的组中的一个取代基取代的苯基，卤素，-CF 3 和（b）任选被1至5个碳原子的烷基取代的5至6元杂环，R 1和R 2分别选自（a）1至5个碳原子的烷基，（b）5 至（C）任选被1至5个碳原子的烷基取代的6元杂环，和（c）任选被至少一个选自1至5个碳原子的烷基和烷氧基的基团取代的苯基和萘基，卤素，-NO 3和 -CF 3，R 3选自氢，1〜5个碳原子的烷基， - （CF 2）n -CF 3，n为0〜4的整数，Alk为1〜5个碳原子的烷基 和它们的无毒，药学上可接受的盐与酸和碱具有抗炎和抗风湿性 matic属性。

    Certain 1,3-dihydro-1-[heterocyclic)imino]-furo-[3,4-b]quinoline 9-ol compounds having analgesic and anti-inflammatory activity
    8.
    发明授权
    Certain 1,3-dihydro-1-[heterocyclic)imino]-furo-[3,4-b]quinoline 9-ol compounds having analgesic and anti-inflammatory activity 失效
    具有止痛和抗炎活性的某些1,3-二氢-1- [杂环的]亚氨基] - 呋喃并[3,4-b]喹啉-9-醇化合物

    公开(公告)号：US4736033A

    公开(公告)日：1988-04-05

    申请号：US945777

    申请日：1986-12-23

    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

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

    摘要： A 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, --CH.sub.3, --OCF.sub.3 or --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 a heterocycle connected to the nitrogen by a carbon atom selected from thiazolyl, 4,5-dihydro-thiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidinyl or tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms or 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, --CH.sub.3, --NO.sub.2 or halogen, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms or aryl, R.sub.4 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms or aryl, and their non-toxic, pharmaceutically acceptable acid addition salts and salts with non-toxic, pharmaceutically acceptable bases having very good analgesis activity and a non-negligible anti-inflammatory activity and novel intermediates.

    摘要翻译： 下式的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，-CH 3，-OCF 3或-SCF 3，R 1选自氢和1至4个碳原子的烷基，R 2选自与氮连接的杂环 通过选自噻唑基，4,5-二氢 - 噻唑基，吡啶基，恶唑基，异恶唑基，咪唑基，嘧啶基或四唑基的碳原子，全部任选被1至4个碳原子的烷基取代，或任选被至少一个 由-OH，1〜4个碳原子的烷基，1〜4个碳原子的烷氧基，-CH 3，-NO 2或卤素组成的基团，R 3选自氢，1〜4个碳原子的烷基或芳基， R4选自氢，1至4个碳原子的烷基或芳基，它们的无毒，pha 药物上可接受的酸加成盐和与无毒的药学上可接受的碱的盐具有非常好的镇痛活性和不可忽略的抗炎活性和新的中间体。

    Anti-inflammatory 2-substituted-4-hydroxy-3-quinoline carboxamides
    9.
    发明授权
    Anti-inflammatory 2-substituted-4-hydroxy-3-quinoline carboxamides 失效
    抗炎2-取代-4-羟基-3-喹啉羧酰胺

    公开(公告)号：US4636512A

    公开(公告)日：1987-01-13

    申请号：US748743

    申请日：1985-06-25

    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 ,  A61P37/00 ,  C07D265/22 ,  C07D277/46 ,  C07D401/04 ,  C07D401/12 ,  C07D413/06 ,  C07D417/12 ,  C07D417/14 ,  C07D215/22

    CPC分类号： C07D265/22 ,  C07D277/46 ,  C07D413/06 ,  C07D417/12 ,  C07D417/14 ,  Y02P20/55

    摘要： Novel racemates or optically active forms of 2-amino-4-hydroxy-3-quinoline carboxylic acid derivatives 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 --, CF.sub.3 S-- and CF.sub.3 O--, 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 (a) thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl, each optionally substituted with alkyl of 1 to 4 carbon atoms and (b) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and 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 2-pyrrolidinyl of the formula ##STR2## R.sub.4 is selected from the group consisting of hydrogen, an amino protective group and ##STR3## R'4 is selected from the group consisting of alkyl 1 to 5 carbon atoms optionally substituted with amino or protected amino, aryl and aralkyl, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, aryl, aralkyl, p-hydroxy-benzyl, lH-indol-3-yl methyl of the formula and --CH.sub.2 SH, the last three being optionally protected by a blocking group and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic and anti-inflammatory activity and novel intermediates.

    摘要翻译： 新颖的外消旋体或光学活性形式的式I的2-氨基-4-羟基-3-喹啉羧酸衍生物，其中X在5-，6-，7-或8-位，并且选自 由氢，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 - ，CF 3 S-和CF 3 O-取代的基团，R 1选自氢和1至4个碳原子的烷基， R 2选自（a）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，各自任选被1至4个碳原子的烷基取代，和（b）任选被 由至少一个由1-4个碳原子的羟基，烷基和烷氧基组成的组，CF 3 - ， - NO 2和卤素，R 3选自下式的2-吡咯烷基：R 4选自 由氢，氨基保护基和 R'4组成的组选自组 g任选被氨基或保护的氨基，芳基和芳烷基取代的1至5个碳原子的烷基，R 5选自氢，1至5个碳原子的烷基，芳基，芳烷基，对羟基 - 苄基， 吲哚-3-基甲基和-CH 2 SH，最后三个任选被封闭基团及其无毒的药学上可接受的具有止痛和抗炎活性的酸加成盐和新的中间体保护。