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17 条记录 (耗时 0.024 秒)

    Method of relieving pain with mercaptoalkanamides
    11.
    发明授权
    Method of relieving pain with mercaptoalkanamides 失效
    消除痛觉消炎痛的方法

    公开(公告)号：US5098934A

    公开(公告)日：1992-03-24

    申请号：US542731

    申请日：1990-06-22

    申请人： Jean-Paul Vevert ,  Francoise Delevallee ,  Rogert Deraedt

    发明人： Jean-Paul Vevert ,  Francoise Delevallee ,  Rogert Deraedt

    IPC分类号： C07D257/06 ,  A61K31/16 ,  A61K31/265 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/423 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4409 ,  A61P25/04 ,  A61P43/00 ,  C07C67/00 ,  C07C323/60 ,  C07C325/00 ,  C07C327/32 ,  C07D213/75 ,  C07D235/12 ,  C07D235/14 ,  C07D235/30 ,  C07D257/04 ,  C07D261/14 ,  C07D263/48 ,  C07D263/58 ,  C07D277/00 ,  C07D277/18 ,  C07D277/20 ,  C07D277/46 ,  C07D277/82

    CPC分类号： C07D213/75 ,  C07D235/30 ,  C07D277/18 ,  C07D277/46 ,  C07D277/82

    摘要： Novel .omega.-mercaptopropanamides and their homologs of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and ##STR2## R.sub.1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and halogen, n is an integer from 1 to 5, R.sub.2 is selected from the group consisting of hydrogen alkyl of 1 to 5 carbon atoms and aryl and aralkyl of 6 to 15 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, halogen and --CF.sub.3, R.sub.3 is selected from the group consisting of a) hydrogen, b) phenyl optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --NO.sub.2, halogen, --CF.sub.3, carboxymethyl, alkoxycarbonylmethyl with 1 to 5 alkoxy carbon atoms, aralkoxy of 7 to 15 carbon atoms and ##STR3## and c) a heterocycle selected from the group consisting of thiazolyl, 4,5-dihydro-thiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, benzimidazolyl, benzothiazolyl and benzoxazolyl, all optionally substituted with alkyl of 1 to 5 carbon atoms, X and X' are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their salts with non-taxic, pharmaceutically acceptable acids and bases with the proviso that when R.sub.2 is hydrogen and n is 1, R.sub.3 is not phenyl optionally substituted with at least one member of the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms and when R.sub.2 is methyl and n is 1, R.sub.3 is not phenyl substituted with carboxymethyl having very good analgesic activity and enkephalinase inhibiting activity.

    摘要翻译： 新型ω-巯基丙酰胺及其同系物式（Ⅰ）其中R 1选自氢和R 1'选自1至5个碳原子的烷基和任选被 由1至5个碳原子的-OH，烷基和烷氧基组成的组中的至少一个，-NO 2和卤素，n是1至5的整数，R 2选自1至5个碳的烷基 6至15个碳原子的芳基和芳烷基，任选被至少一个由1至5个碳原子的烷基和烷氧基取代的基团，-OH，卤素和-CF 3，R 3选自 ）氢，b）任选被至少一个由1-5个碳原子的烷基和烷氧基取代的苯基，-OH，-NO 2，卤素，-CF 3，羧甲基，具有1至5个烷氧基碳原子的烷氧羰基甲基， 7至15个碳原子的芳烷氧基和c）a 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，四唑基，苯并咪唑基，苯并噻唑基和苯并恶唑基的杂环，全部任选被1至5个碳原子的烷基取代，X和X “独立地选自氢和1至5个碳原子的烷基，并且它们与非税，药学上可接受的酸和碱的盐，条件是当R 2是氢且n是1时，R 3不是任选被取代的苯基 与卤素和1至5个碳原子的烷基和烷氧基中的至少一个成员，当R 2是甲基且n是1时，R 3不是具有非常好的镇痛活性和脑啡肽酶抑制活性的羧甲基取代的苯基。

    Compositions for reducing abnormal stimulation of endothelin receptors and novel compounds
    12.
    发明授权
    Compositions for reducing abnormal stimulation of endothelin receptors and novel compounds 失效
    用于减少内皮素受体和新化合物的异常刺激的组合物

    公开(公告)号：US5811444A

    公开(公告)日：1998-09-22

    申请号：US776953

    申请日：1997-01-31

    申请人： Bertrand Heckmann ,  Jean-Paul Vevert ,  Jidong Zhang

    发明人： Bertrand Heckmann ,  Jean-Paul Vevert ,  Jidong Zhang

    IPC分类号： A61K31/415 ,  A61K31/4178 ,  A61K31/422 ,  A61P3/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D233/84 ,  C07D405/06

    CPC分类号： C07D405/06 ,  A61K31/4178

    摘要： The invention relates to the new use and the new products of formula (I): ##STR1## in which: R.sub.1 =represents hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, formyl, cycloalkyl, optionally interrupted by heteroatoms, R.sub.2, R.sub.3 represent in particular halogen, mercapto, acyl, carboxy, nitro, cyano, amino, carbamoyl, R.sub.4, --OR.sub.4 with R.sub.4 representing in particular hydrogen, alkyl, alkenyl, alkynyl, acyl, amino, --(CH.sub.2).sub.m1 --S(O).sub.m2 --X--R.sub.10 with m1=0 to 4, m2=0 to 2, X represents a single bond or --NH--, --NH--CO--, --NH--CO--NH--, and R.sub.10 represents alkyl, alkenyl or aryl, and Y represents optionally substituted aryl, these products being in all the isomer forms and the salts, as medicaments.

    摘要翻译： PCT No.PCT / FR95 / 01034 Sec。 371日期1997年1月31日 102（e）日期1997年1月31日PCT提交1995年8月1日PCT公布。 公开号WO96 / 04276 日期：1996年2月15日本发明涉及式（I）的新用途和新产物：其中：R1 =羟基，烷基，烯基，炔基，烷氧基，烷硫基，甲酰基，环烷基， 任选地被杂原子中断，R2，R3特别表示卤素，巯基，酰基，羧基，硝基，氰基，氨基，氨基甲酰基，R4，-OR4，其中R4代表特别是氢，烷基，烯基，炔基，酰基，氨基， - （ CH2）m1-S（O）m2-X-R10，其中m1 = 0〜4，m2 = 0〜2，X表示单键或-NH-，-NH-CO-，-NH-CO-NH-， R 10代表烷基，链烯基或芳基，Y代表任意取代的芳基，这些产物是所有的异构体形式和盐，作为药物。

    Alpha-mercaptomethyl-benzene propanamides, pharmaceutical compositions and use
    15.
    发明授权
    Alpha-mercaptomethyl-benzene propanamides, pharmaceutical compositions and use 失效
    α-巯基甲基苯丙酰胺，药物组合物和用途

    公开(公告)号：US4839358A

    公开(公告)日：1989-06-13

    申请号：US159265

    申请日：1988-02-23

    申请人： Jean-Paul Vevert ,  Francoise Delevallee ,  Jean-Claude Gasc ,  Francis Petit

    发明人： Jean-Paul Vevert ,  Francoise Delevallee ,  Jean-Claude Gasc ,  Francis Petit

    IPC分类号： C07D295/22 ,  A61K31/40 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/54 ,  A61K31/55 ,  A61P3/00 ,  A61P25/04 ,  A61P25/24 ,  A61P25/26 ,  C07D211/56 ,  C07D265/30 ,  C07D277/04 ,  C07D295/32

    CPC分类号： C07D295/32

    摘要： Novel .alpha.-mercaptomethyl-benzene propanamides of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and ##STR2## R.sub.1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of --OH, --NO.sub.2, halogen and alkyl and alkoxy of 1 to 5 carbon atoms, X and X' are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 5 carbon atoms, --OH, halogen and --CF.sub.3, R.sub.2 is selected from the group consisting of pyrrolidinyl, morpholinyl, piperidinyl, piperazinyl, tetrahydrothiazinyl and hexahydroazepinyl, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --NO.sub.2, --CF.sub.3, halogen and acyl of an organic carboxylic acid of 1 to 7 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity, antidepression and anxiolytic properties.

    摘要翻译： 式Ⅰ的新型α-巯基甲基 - 苯丙酰胺，其中R 1选自氢和R 1'选自1至5个碳原子的烷基和任选被 由-OH，-NO 2，卤素和1至5个碳原子的烷基和烷氧基组成的组中的至少一个成员，X和X'分别选自氢，烷基和1至5个碳原子的烷氧基， -OH，卤素和-CF 3，R 2选自吡咯烷基，吗啉基，哌啶基，哌嗪基，四氢噻嗪基和六氢氮杂卟啉，全部任选被至少一个由1至5个碳原子的烷基和烷氧基组成的组取代 具有1至7个碳原子的有机羧酸的-OH，-NO 2，-CF 3，卤素和酰基及其具有止痛活性，抗抑郁和抗焦虑性质的无毒的药学上可接受的酸加成盐。