Novel therapeutic compositions and method involving thiazol-carboxamides
    61.
    发明授权
    Novel therapeutic compositions and method involving thiazol-carboxamides 失效
    涉及噻唑 - 甲酰胺的新型治疗组合物和方法

    公开(公告)号:US3966950A

    公开(公告)日:1976-06-29

    申请号:US539327

    申请日:1975-01-08

    CPC分类号: C07D295/13 C07D277/56

    摘要: Novel thiazolcarboxamides of the formula ##EQU1## wherein R is selected from the group consisting of alkyl of 1 to 6 carbon atoms and phenyl, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, n is a whole number from 2 to 5 and X and X.sub.1 are individually selected from the group consisting of hydrogen, halogen, trifluoromethyl and alkyl, alkoxy and alkylthio of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having .alpha.-adrenolytic activity and their preparation.

    摘要翻译: 式O分子式CN-(CH2)n-NNI | R1的新型噻唑羧酰胺其中R选自1至6个碳原子的烷基和苯基,R 1选自氢和1的烷基 至4个碳原子,n为2至5的整数,X和X 1分别选自氢,卤素,三氟甲基和具有1至4个碳原子的烷基,烷氧基和烷硫基,并且其无毒的,药学上 具有α-脱水活性的可接受的酸加成盐及其制备。

    8-amino decahydroquinolines and medicinal use thereof
    66.
    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

    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.

    N-(1H-indole-4-yl)-benzamides
    67.
    发明授权
    N-(1H-indole-4-yl)-benzamides 失效
    N-(1H-吲哚基-4-基) - 苯甲酰胺

    公开(公告)号:US4908367A

    公开(公告)日:1990-03-13

    申请号:US136118

    申请日:1987-12-21

    IPC分类号: C07D209/08 C07D209/34

    CPC分类号: C07D209/08 C07D209/34

    摘要: Novel indole carboxamides 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, --CF.sub.3, CH.sub.3 S--, --NH.sub.2 and --NO.sub.2 or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl, aralkyl of 7 to 12 carbon atoms and substituted phenyl, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, chlorine, bromine, iodine, --NO.sub.2, --NH.sub.2, acylamide of an aliphatic carboxylic acid of 2 to 5 carbon atoms and mono and dialkylamino with alkyl of 1 to 5 carbon atoms, a and b form .dbd.O and c is hydrogen or a and c form a carbon-carbon bond and b is hydrogen, A is selected from the group consisting of --(CH.sub.2).sub.n -- and ##STR3## n is an integer from 2 to 5, m is an integer from 1 to 3, B is ##STR4## R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anti-arrhytmic properties.

    摘要翻译: 式IMA的新型吲哚甲酰胺其中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基烷基, 任选被1至3个由卤素,甲基,乙基,甲氧基,乙氧基,-CF 3,CH 3 S - , - NH 2和-NO 2组成的基团取代的7至12个碳原子,或者R 1和R 3与氮原子一起形成 任选地含有-O - , - S-和R'的成员的任选的不饱和杂环选自氢,1至5个碳原子的烷基,苯基,萘基,7至 12个碳原子和取代的苯基,R 3选自氢,1至5个碳原子的烷基,1至3个碳原子的烷氧基,氯,溴,碘,-NO 2,-NH 2,脂族羧酸的酰基酰胺 2至5个碳原子的酸和一烷基和二烷基氨基 1至5个碳原子,a和b形式= O,c是氢或a和c形成碳 - 碳键,b是氢,A选自 - (CH 2)n - 和< IMAGE> n 是2至5的整数,m是1至3的整数,B是选自氢和1至5个碳原子的烷基及其无毒的药学上可接受的酸加成盐 具有显着的抗arrhytmic性质。

    4-(1H-indol-3-yl)-.alpha.-methyl-piperidine-1-ethanol derivatives
    68.
    发明授权
    4-(1H-indol-3-yl)-.alpha.-methyl-piperidine-1-ethanol derivatives 失效
    4-(1H-吲哚-3-基)-α-甲基 - 哌啶-1-乙醇衍生物

    公开(公告)号:US4530932A

    公开(公告)日:1985-07-23

    申请号:US536889

    申请日:1983-09-28

    CPC分类号: C07D401/04

    摘要: Novel 4-(1H-indol-3-yl)-.alpha.-methyl-piperidine-1-ethanol derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2, --NH.sub.2, CF.sub.3 -- and CH.sub.3 S--, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and --OH, Ar is selected from the group consisting of optionally substituted aryl and heteroaryl, the dotted line indicates the optional presence of a double bond and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable antagonistic properties toward calcium ion and antihypertensive activity and certain compounds possess .alpha. and/or .beta.-blocking properties.

    摘要翻译: 新颖的4-(1H-吲哚-3-基)-α-甲基 - 哌啶-1-乙醇衍生物,其中R选自氢,卤素,烷基和烷氧基,其为1至5个 碳原子,-NO 2,-NH 2,CF 3 - 和CH 3 S - ,R 1选自氢和1至5个碳原子的烷基,R 2选自氢,1至5个碳原子的烷基 和-OH,Ar选自任选取代的芳基和杂芳基,虚线表示任选存在双键及其对钙离子和抗高血压活性具有显着拮抗性的无毒的药学上可接受的酸加成盐 并且某些化合物具有α和/或β-阻断性质。

    Analgesic 4-hydroxy-3-quinolinecarboxamides
    70.
    发明授权
    Analgesic 4-hydroxy-3-quinolinecarboxamides 失效
    止痛4-羟基-3-喹啉甲酰胺

    公开(公告)号:US4397856A

    公开(公告)日:1983-08-09

    申请号:US262952

    申请日:1981-05-12

    摘要: Novel compounds 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 O--, CF.sub.3 S-- and CF.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 hydrogen or an optionally unsaturated ring able to contain one or more heteroatoms of the group consisting of --S--, --O-- and --N-- optionally substituted with one or more members of the group consisting of (a) halogens, (b) alkyl of 1 to 4 carbon atoms optionally substituted with NH.sub.2, --NHAlK or --N---(AlK).sub.2 and AlK is alkyl of 1 to 3 carbon atoms, (c) phenyl, (d) alkoxy of 1 to 4 carbon atoms, (e) --OH, (f) --CF.sub.3 and (g) --NO.sub.2 or R.sub.1 ' together with the nitrogen atom to which they are attached form an optionally unsaturated ring, the said ring then being connected to the nitrogen atom by a double bond, R.sub.3 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and halogen, R.sub.5 is a halogen with the proviso that R.sub.3, R.sub.4 and R.sub.5 can not all be fluorine and R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and an acyl of an organic carboxylic acid of 2 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts and their salts with non-toxic, pharmaceutically acceptable bases having a remarkable analgesic activity, a very weak anti-inflammatory activity and a good tolerance by the gastrointestinal system and their preparation and their intermediates.

    摘要翻译: 新颖的式(Ⅰ)化合物,其中X为5,6,7或8位,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 O-,CF 3 S-和CF 3 - ,R''选自氢和1至4个碳原子的烷基,R 2'选自氢或任选不饱和的环,其能够含有一个或多个 任选被一个或多个由(a)卤素,(b)任选被NH 2取代的1至4个碳原子的烷基取代的-S-,-O-和 - NHAlK或-N - (AlK)2,AlK是1至3个碳原子的烷基,(c)苯基,(d)1-4个碳原子的烷氧基,(e)-OH,(f)-CF3和( g)-NO 2或R 1'与它们所连接的氮原子一起形成任选的不饱和环,然后所述环通过双键与氮原子连接,R 3选自组 氢,卤素和1至4个碳原子的烷基,R4选自氢和卤素,R5是卤素,条件是R3,R4和R5不能全部是氟,R6选自 由氢,1-8个碳原子的烷基和2至8个碳原子的有机羧酸的酰基及其无毒的药学上可接受的酸加成盐和它们的盐与无毒的药学上可接受的碱组成的组,其具有 显着的止痛活性,非常弱的抗炎活性和良好的耐胃肠系统及其制备及其中间体。