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.

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。

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。

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。

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。

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。

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。

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。

公开(公告)号：US5278180A

公开(公告)日：1994-01-11

申请号：US863801

申请日：1992-05-04

申请人： Francois Clemence ,  Claudine Maushart ,  Philippe Mackiewicz ,  Francoise Delevallee

发明人： Francois Clemence ,  Claudine Maushart ,  Philippe Mackiewicz ,  Francoise Delevallee

IPC分类号： C07D249/08 ,  A61K31/41

CPC分类号： C07D249/08

摘要： A novel process for the preparation of 4H-1,2,4-triazoles in their racemic or optically active forms of the formula ##STR1## wherein the compounds have analgesic activity.

摘要翻译： 一种用于制备其式（*化学结构*）I的外消旋或光学活性形式的4H-1,2,4-三唑的新方法，其中化合物具有止痛活性。

公开(公告)号：US4904655A

公开(公告)日：1990-02-27

申请号：US302810

申请日：1989-01-26

申请人： Nurgun Aktogu ,  Francoise Delevallee ,  Francois Clemence ,  Claude Oberlander

发明人： Nurgun Aktogu ,  Francoise Delevallee ,  Francois Clemence ,  Claude Oberlander

IPC分类号： C07D209/14 ,  A61K31/535 ,  A61P25/04 ,  A61P25/06 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  C07D209/18 ,  C07D413/06 ,  C07D498/14 ,  C07D498/22

CPC分类号： C07D498/22

摘要： Novel compounds selected from the group consisting of all possible racemic or optically active forms of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 5 carbon atoms, -OH, -CF.sub.3 and -NO.sub.2 and ##STR2## is selected from the group consisting of ##STR3## and their non-toxic, pharmaceutically acceptable acid addition salts having a very good analgesic activity as well as antidepressive, neuronal protective, anti-anoxic, anti-ischemic and no-otropic activities.

摘要翻译： 选自下列化合物的新化合物：所有可能的外消旋或旋光活性形式的下式化合物其中R 1和R 2分别选自氢，烷基和1至5个碳原子的烷基，-OH ，-CF 3和-NO 2和选自及其无毒的药学上可接受的具有非常好的镇痛活性的酸加成盐以及抗抑郁，神经元保护，抗缺氧，抗 - 缺血和非嗜性活动。