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    • 1. 发明授权
    • Novel 4H-1,2,4-triazole derivatives
    • 新型4H-1,2,4-三唑衍生物
    • US4727084A
    • 1988-02-23
    • US896858
    • 1986-08-14
    • Jean MeierFrancois Clemence
    • Jean MeierFrancois Clemence
    • A61K31/41A61P25/04C07C243/38C07D249/08C07D317/46C07D405/04
    • C07D249/08C07C243/38C07D317/46Y10S514/886
    • Compounds selected from the group consisting of 4H-1,2,4-triazoles of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be in different positions of the benzene ring, R.sub.1, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, --OH, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, --CH.sub.3, --NO.sub.2, --NH.sub.2 and NH--AlK and ##STR2## R.sub.2 is selected from the group consisting of hydrogen, --OH, alkyl of 1 to 4 carbon atoms, halogen, --CF.sub.3, --NO.sub.2, --NH.sub.2, --NH--AlK and ##STR3## and AlK, AlK.sub.1 and AlK.sub.2 are alkyl of 1 to 4 carbon atoms or R.sub.1 and R.sub.2 together and/or R.sub.3 and R.sub.4 together are methylenedioxy, R is selected from the group consisting of ethyl, --CH.sub.2 --COOH and CH.sub.2 --COOAlK.sub.3 and AlK.sub.3 is alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts, with the proviso that R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are not all hydrogen having a remarkable analgesic activity and a novel method for their preparation.
    • 选自下列化合物的化合物的化合物其中R 1,R 2,R 3和R 4可以位于苯环,R 1,R 3和R 4的不同位置的式Ia, 由氢,-OH,1至4个碳原子的烷基,1至4个碳原子的烷氧基,卤素,-CH 3,-NO 2,-NH 2和NH-AlK和R 2选自下组: 的氢,-OH,1至4个碳原子的烷基,卤素,-CF 3,-NO 2,-NH 2,-NH-AlK和AlGaN,AlK,AlK1和AlK2是1至4个碳原子的烷基或R1和 R 2一起和/或R 3和R 4一起是亚甲二氧基,R选自乙基,-CH 2 -COOH和CH 2 -COOAlK 3,AlK 3是1至4个碳原子的烷基及其无毒的药学上可接受的酸加成 盐,条件是R1,R2,R3和R4不都是具有显着镇痛活性的氢和它们制备的新方法。
    • 3. 发明授权
    • Novel 4H-1,2,4-triazole derivatives
    • 新型4H-1,2,4-三唑衍生物
    • US4659729A
    • 1987-04-21
    • US582051
    • 1984-02-21
    • Jean MeierFrancois Clemence
    • Jean MeierFrancois Clemence
    • A61K31/41A61P25/04C07C243/38C07D249/08C07D317/46C07D405/04A61K31/395
    • C07D249/08C07C243/38C07D317/46Y10S514/886
    • Compounds selected from the group consisting of 4H-1,2,4-triazoles of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be in different positions of the benzene ring, R.sub.1, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, --OH, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, --CF.sub.3, --NO.sub.2, --NH.sub.2 and NH--AlK and ##STR2## R.sub.2 is selected from the group consisting of hydrogen, --OH, alkyl of 1 to 4 carbon atoms, halogen, --CF.sub.3, --NO.sub.2, --NH.sub.2, --NH--AlK and ##STR3## and AlK, AlK.sub.1 and AlK.sub.2 are alkyl of 1 to 4 carbon atoms or R.sub.1 and R.sub.2 together and/or R.sub.3 and R.sub.4 together are methylenedioxy, R is selected from the group consisting of ethyl, --CH.sub.2 --COOH and CH.sub.2 --COOAlK.sub.3 and AlK.sub.3 is alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts, with the proviso that R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are not all hydrogen having a remarkable analgesic activity and a novel method for their preparation.
    • 选自下列化合物的化合物的化合物其中R 1,R 2,R 3和R 4可以位于苯环,R 1,R 3和R 4的不同位置的式Ia, 由氢,-OH,1至4个碳原子的烷基,1至4个碳原子的烷氧基,卤素,-CF 3,-NO 2,-NH 2和NH-AlK和R 2选自下组: 的氢,-OH,1至4个碳原子的烷基,卤素,-CF 3,-NO 2,-NH 2,-NH-AlK和AlGaN,AlK,AlK1和AlK2是1至4个碳原子的烷基或R1和 R 2一起和/或R 3和R 4一起是亚甲二氧基,R选自乙基,-CH 2 -COOH和CH 2 -COOAlK 3,AlK 3是1至4个碳原子的烷基及其无毒的药学上可接受的酸加成 盐,条件是R1,R2,R3和R4不都是具有显着镇痛活性的氢和它们制备的新方法。
    • 8. 发明授权
    • Decahydroquinolines and central analgesic method of use thereof
    • 十氢喹啉和中枢镇痛药的使用方法
    • US4877796A
    • 1989-10-31
    • US084456
    • 1987-08-12
    • Francois ClemenceOdile Le MartretFrancoise DelevalleeMichel Fortin
    • Francois ClemenceOdile Le MartretFrancoise DelevalleeMichel Fortin
    • A61K31/47A61P7/06A61P7/10A61P9/06A61P9/12A61P25/04C07D215/40C07D401/12C07D409/12
    • C07D215/40
    • 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.
    • 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。
    • 9. 发明授权
    • Ethenylphenol-indoles having antiarythmic utility
    • 具有抗血浆效用的乙烯基苯酚吲哚
    • US4650811A
    • 1987-03-17
    • US691163
    • 1985-01-14
    • Jacques GuillaumeFrancois ClemenceNeil L. Brown
    • Jacques GuillaumeFrancois ClemenceNeil L. Brown
    • A61K31/40A61K31/403A61K31/404A61P3/00A61P3/04A61P3/08A61P3/10A61P7/00A61P9/06A61P9/12A61P13/02A61P15/00A61P25/02A61P43/00C07D209/08C07D209/30C07D209/34C07D407/12C07D209/12
    • C07D407/12C07D209/08C07D209/30C07D209/34
    • Novel ethenylphenol indoles of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with 1 to 3 members of the group consisting of halogen, methyl, ethyl, methoxy, ethoxy, methylthio, --CF.sub.3, --NH.sub.2 and --NO.sub.2 or R and R.sub.1 together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a second heteroatom selected from the group consisting of --O--, --S-- and ##STR2## R' is hydrogen or alkyl of 1 to 5 carbon atoms, a together with X is .dbd.0 and b is hydrogen or a together with b is a carbon-carbon bond and X is hydrogen, the dotted line indicates the possibility of a double bond with the compounds having the trans configuration if a double bond, A is selected from the group consisting of ##STR3## and --(CH.sub.2).sub.n --, n is 2,3,4 or 5, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms with the proviso that R and R.sub.1 are not both hydrogen when A is ##STR4## and their non-toxic, pharmaceutically acceptable acid addition salts having anti-arrhythmic and anti hypertensive properties and the property of blocking slow calcium-sodium channels and novel intermediates.
    • 式Ⅰ的新型乙烯基苯酚吲哚,其中R和R 1分别选自氢,1至5个碳原子的烷基,3至7个碳原子的环烷基,4至7个碳原子的环烷基烷基和芳烷基 任选被1至3个由卤素,甲基,乙基,甲氧基,乙氧基,甲硫基,-CF 3,-NH 2和-NO 2组成的组中任意取代的7至12个碳原子,或者R和R 1与氮原子一起形成任选不饱和的 任选地含有选自-O - , - S-和R'的第二杂原子的杂环是氢或1至5个碳原子的烷基,以及X是= 0,b是氢或一起 其中b是碳 - 碳键,X是氢,虚线表示与具有反式构型的化合物具有双键的可能性,如果双键,A选自和 - (CH2 )n-,n为2,3,4或5,R2选自c 存在氢和1至5个碳原子的烷基,条件是当A为A时,R和R1不同时为氢,并且它们具有抗心律失常和抗高血压性质的无毒的药学上可接受的酸加成盐和其特性 阻断缓慢的钙钠通道和新型中间体。
    • 10. 发明授权
    • [4H]-1,3-Benzodioxin-2-carboxylic acids
    • [4H] -1,3-苯并二恶英-2-羧酸
    • US4281012A
    • 1981-07-28
    • US034432
    • 1979-04-30
    • Daniel HumbertFrancois ClemenceMichele Dagnaux
    • Daniel HumbertFrancois ClemenceMichele Dagnaux
    • A61K31/335A61K31/357A61P3/04A61P9/00C07C39/17C07C39/28C07C39/367C07C39/373C07C39/42C07C41/30C07C43/23C07C45/46C07C49/83C07C49/84C07D319/08
    • C07D319/08C07C39/17C07C39/28C07C39/367C07C39/373C07C39/42C07C41/30C07C45/46C07C49/83C07C49/84C07C2101/14
    • Novel racemates and optically active isomers and mixtures of isomers of [4H]-1,3-benzodioxin-2-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, dialkylamino alkyl with alkyls of 1 to 5 carbon atoms, alkali metal, alkaline earth metal, aluminum, --NH.sub.4, non-toxic pharmaceutically acceptable amines, 2,3-dihydroxypropanyl and (2,2-dimethyl-1,3-dioxolan-4-yl)-methyl, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.3 and R.sub.6 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, ethenyl and cyclohexyl and taken together with the carbon atom to which they are attached form cyclohexyl, R.sub.5 is selected from the group consisting of hydrogen and halogen or R.sub.1 and R.sub.2 have the above definitions, R.sub.6 is ##STR2## R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, --CF.sub.3, cyclohexyl, alkoxy of 1 to 3 carbon atoms, alkyl of 1 to 3 carbon atoms and p-chlorophenoxy and R.sub.3 is selected from the group consisting of 2-propenyl, ethenyl, cyclohexyl, benzyl, hydrogen and alkyl of 1 to 5 carbon atoms with the proviso that when R.sub.3 is alkyl, at least one of R.sub.4 and R.sub.5 is no hydrogen or halogen and when R.sub.3 is hydrogen, at least one of R.sub.4 and R.sub.5 is not hydrogen, halogen or --CF.sub.3 and the non-toxic, pharmaceutically acceptable acid addition salts thereof when R.sub.1 is dialkylaminoalkyl which have a marked hypolipemiant activity and reduces the plasmatic level of lipids, triglycerides and cholestrol and their preparation.
    • 新颖的外消旋物和光学活性异构体以及式[IMAGE] I的[4H] -1,3-苯并二恶英-2-羧酸化合物的异构体的混合物,其中R 1选自氢,1至5个碳的烷基 原子,具有1至5个碳原子的烷基的二烷基氨基烷基,碱金属,碱土金属,铝,-NH 4,无毒的药学上可接受的胺,2,3-二羟基丙酰基和(2,2-二甲基-1,3-二氧戊环) -4-基) - 甲基,R 2选自氢和1至5个碳原子的烷基,R 3和R 6分别选自氢,1至6个碳原子的烷基,乙烯基和环己基 并且与它们所连接的碳原子一起形成环己基,R 5选自氢和卤素,或者R 1和R 2具有上述定义,R 6和R 5各自独立地选自 的氢,卤素,-CF 3,环己基,1〜3个碳原子的烷氧基 在原子上具有1至3个碳原子的烷基和对氯苯氧基,R3选自2-丙烯基,乙烯基,环己基,苄基,氢和1至5个碳原子的烷基,条件是当R3为烷基 ,R 4和R 5中的至少一个不是氢或卤素,并且当R 3是氢时,当R 1是二烷基氨基烷基时,R 4和R 5中的至少一个不是氢,卤素或-CF 3及其无毒的药学上可接受的酸加成盐 其具有显着的降胆固醇活性并降低脂质,甘油三酯和胆甾醇的血浆水平及其制备。