Amino-(hydroxy)alkoxy-4-phenylpropyl indoles having antiarrythmic
activity
    51.
    发明授权
    Amino-(hydroxy)alkoxy-4-phenylpropyl indoles having antiarrythmic activity 失效
    氨基(羟基)烷氧基-4-苯基丙基吲哚具有抗焦虑活性

    公开(公告)号:US4808609A

    公开(公告)日:1989-02-28

    申请号:US878195

    申请日:1986-06-25

    摘要: A compound selected from the group consisting of hydroxyalkoxy-4-phenylpropyl-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, --CF.sub.3, --NO.sub.2, CH.sub.3 S-- and --NH.sub.2 or R.sub.1 and R together with the nitrogen atom to which they are attached form an optionally unsaturated heterocycle optionally containing --S--, --O-- or ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl and phenylalkyl of 7 to 12 carbon atoms, a and b form =O and c is hydrogen or a and c form a carbon-carbon bond and b is hydrogen, the dotted line is an optional double bond, A is ##STR3## m is 1,2 or 3, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, x is selected from the group consisting of hydrogen and --OH and y is hydrogen or x together with y is =O and their non-toxic, pharmaceutically acceptable acid addition salts having antiarrhythmic activity and blocking of slow calcico-sodic canals and a process and novel intermediates for their preparation.

    摘要翻译: 选自下式的羟基烷氧基-4-苯基丙基 - 吲哚的化合物,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7至12个碳原子的芳烷基,任选被1至3个卤素,甲基,乙基,甲氧基,乙氧基,-CF 3,-NO 2,CH 3 S - 和-NH 2 或R 1和R 2与它们所连接的氮原子一起形成任选含有-S-,-O-或R'的任选不饱和杂环,其选自氢,1至5个碳原子的烷基 7至12个碳原子的苯基,萘基和苯基烷基,a和b形式= O,c是氢或a和c形成碳 - 碳键,b是氢,虚线是任选的双键, 图像> m是1,2或3,R2选自氢和1t的烷基 o 5个碳原子,x选自氢和-OH,y是氢或x和y一起是它们的无毒的药学上可接受的酸加成盐,具有抗心律不齐活性和缓慢钙沉积的阻断 运河和一个过程和新的中间体为他们的准备。

    Certain 1,3-dihydro-1-[heterocyclic)imino]-furo-[3,4-b]quinoline 9-ol
compounds having analgesic and anti-inflammatory activity
    52.
    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

    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。

    Alkyl .beta.-oxo-benzenepropanoates
    53.
    发明授权
    Alkyl .beta.-oxo-benzenepropanoates 失效
    烷基β-氧代 - 苯丙酸酯

    公开(公告)号:US4687857A

    公开(公告)日:1987-08-18

    申请号:US660414

    申请日:1984-10-12

    CPC分类号: C07D277/46

    摘要: Novel alkyl .beta.-oxo-benzenepropanoates 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 hydrogen, thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, thienyl, benzothiazolyl and phenyl optionally substituted with at least one member of the group consisting of halogen, alkoxy of 1 to 4 carbon atoms, hydroxy, phenyl, CF.sub.3 --, NO.sub.2 -- alkyl of 1 to 4 carbon atoms and alkyl of 1 to 4 carbon atoms substituted with amino, alkylamino or dialkylamino with alkyls of 1 to 3 carbon atoms or R.sub.1 ' and R.sub.2 ' taken together with the nitrogen atom to which they are attached form a member of the group consisting of thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, thienyl and benzothiazolyl with the double bond being attached to the nitrogen atom, R is alkyl of 1 to 8 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 4 carbon atoms, R.sub.4 is hydrogen or halogen and R.sub.5 is halogen and a process for their preparation and a process for the preparation of compounds of the formula ##STR2## wherein X, R.sub.1 ', R.sub.2 ', R.sub.3, R.sub.4 and R.sub.5 have the above definition.

    摘要翻译: 新颖的式(I)的烷基β-氧代 - 苯丙酸酯,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 - ,CF 3 S-和CF 3 O-,R 1'选自氢和1至4个碳原子的烷基,R 2'选自氢,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,噻吩基,苯并噻唑基和任选被至少一个选自卤素,1-4个碳原子的烷氧基,羟基,苯基,CF 3 - ,具有1至4个碳原子的NO 2 - 烷基和1至4个碳原子的烷基被氨基,烷基氨基或二烷基氨基与1至3个碳原子的烷基取代,或者R 1'和R 2'与它们所在的氮原子一起 连接形成由噻唑基,4,5-二氢噻唑基,吡啶基,恶唑基组成的组的成员 ,异恶唑基,咪唑基,嘧啶基,四唑基,噻吩基和苯并噻唑基,其双键连接到氮原子上,R是1至8个碳原子的烷基,R3选自氢,卤素和1至4的烷基 碳原子,R 4为氢或卤素,R 5为卤素及其制备方法及其制备方法,其中X,R 1',R 2',R 3,R 4和R 5具有上述 定义。

    Novel 4H-1,2,4-triazole derivatives
    54.
    发明授权
    Novel 4H-1,2,4-triazole derivatives 失效
    新型4H-1,2,4-三唑衍生物

    公开(公告)号:US4659729A

    公开(公告)日:1987-04-21

    申请号:US582051

    申请日:1984-02-21

    摘要: 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.

    摘要翻译: 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。

    Anti-inflammatory 2-substituted-4-hydroxy-3-quinoline carboxamides
    55.
    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

    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。

    (4-Phenyl-piperazino alkyl)-3-benzoyl-benzene alkanoates
    56.
    发明授权
    (4-Phenyl-piperazino alkyl)-3-benzoyl-benzene alkanoates 失效
    (4-苯基 - 哌嗪基烷基)-3-苯甲酰基 - 苯基链烷酸酯

    公开(公告)号:US4147790A

    公开(公告)日:1979-04-03

    申请号:US869361

    申请日:1978-01-13

    CPC分类号: C07D295/088

    摘要: Benzophenones of the formula ##STR1## wherein X.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, X.sub.2 is selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 5 carbon atoms, m is a whole number from 1 to 10, n is a whole number from 2 to 5 and Y is in the 2,3 or 4-position and is selected from the group consisting of hydrogen, halogen, CF.sub.3 --, CF.sub.3 O--, CF.sub.3 S--, alkyl of 1 to 8 carbon atoms and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and their preparation.

    摘要翻译: 其中X 1选自氢和1至5个碳原子的烷基,X 2选自氢,卤素和1至5个碳原子的烷氧基, m为1〜10的整数,n为2〜5的整数,Y为2,3或4位,选自氢,卤素,CF 3 - ,CF 3 O-,CF 3 S - ,1〜8个碳原子的烷基和1〜8个碳原子的烷氧基,以及它们具有止痛活性的无毒,药学上可接受的酸加成盐及其制备方法。

    Quinoline-3-carboxamides
    57.
    发明授权
    Quinoline-3-carboxamides 失效
    喹啉-3-甲酰胺

    公开(公告)号:US4107310A

    公开(公告)日:1978-08-15

    申请号:US766487

    申请日:1977-02-07

    CPC分类号: C07D215/56 C07F3/02

    摘要: Novel quinoline-3-carboxamides of the formula ##STR1## wherein R.sub.1 is in the 5,6,7 or 8-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3, --OCF.sub.3, --SCF.sub.3, straight chain alkyl of 1 to 4 carbon atoms, branched alkyl of 3 to 5 carbon atoms and alkoxy of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and methyl, R.sub.3 is selected from the group consisting of thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl and imidazolyl and R.sub.4 is selected from the group consisting of hydrogen, hydroxyl, alkyl of 1 to 4 carbon atoms, phenyl and benzyl with the proviso that when R.sub.1 is in the 7 or 8-position and is halogen, --CH.sub.3, --OCF.sub.3 or --SCF.sub.3 and R.sub.4 is hydrogen, R.sub.3 is not thiazolyl, pyridinyl or oxazolyl and the non-toxic, pharmaceutically acceptable acid addition salts when R.sub.3 is imidazolyl or 4,5-dihydrothiazolyl having analgesic activity and their preparation and novel intermediates therefore.

    摘要翻译: 式(Ⅰ)的新型喹啉-3-甲酰胺其中R 1为5,6,7或8位且选自氢,卤素,-CF 3,-OCF 3,-SCF 3,直链 1至4个碳原子的烷基,3至5个碳原子的支链烷基和1至4个碳原子的烷氧基,R2选自氢和甲基,R3选自噻唑基,4,5 - 二氢噻唑基,吡啶基,恶唑基和咪唑基,R4选自氢,羟基,1至4个碳原子的烷基,苯基和苄基,条件是当R1为7或8位且为卤素时, -CH 3,-OCF 3或-SCF 3和R 4为氢,R 3不是噻唑基,吡啶基或恶唑基,当R 3为具有镇痛作用的咪唑基或4,5-二氢噻唑并且其制备和新颖的无毒的药学上可接受的酸加成盐 因此中间体。

    Novel 1,4-benzodioxanes
    58.
    发明授权
    Novel 1,4-benzodioxanes 失效
    新的1,4-苯并二氧杂环己烷

    公开(公告)号:US4100291A

    公开(公告)日:1978-07-11

    申请号:US791927

    申请日:1977-04-28

    CPC分类号: C07D319/20

    摘要: Novel 1,4-benzodioxanes of the formula ##STR1## wherein R' is selected from the group consisting of hydrogen, alkoxy of 1 to 5 carbon atoms, chlorine, bromine and fluorine, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and Y and Z are hydrogen or together form a double bond in the form of their racemic mixtures or optically active isomers and their non-toxic, pharmaceutically acceptable acid addition salts having antihypertensive activity and a novel process and novel intermediates for their preparation.

    摘要翻译: 式I'的新型1,4-苯并二氧恶烷其中R'选自氢,1至5个碳原子的烷氧基,氯,溴和氟,R 1和R 2分别选自 的氢和1至5个碳原子的烷基,Y和Z是氢或一起形成其外消旋混合物或光学活性异构体形式的双键及其具有抗高血压活性的无毒的药学上可接受的酸加成盐和新颖的 工艺和新型中间体的制备。

    Novel p-(4-tetrahydropyranyl)-phenoxy-compounds
    59.
    发明授权
    Novel p-(4-tetrahydropyranyl)-phenoxy-compounds 失效
    新型对 - (4-四氢吡喃基) - 苯氧基化合物

    公开(公告)号:US4078076A

    公开(公告)日:1978-03-07

    申请号:US690010

    申请日:1976-05-26

    CPC分类号: C07D309/04 C07D309/06

    摘要: Novel pyranic derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and cations of alkali metals, alkaline earth metals, aluminum, amines and ammonium R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and X is selected from the group consisting of hydrogen, chlorine and bromine having hypolipemic activity and reducing the level of total lipids in plasma.

    摘要翻译: 其中R选自氢,1至6个碳原子的烷基和碱金属,碱土金属,铝,胺和铵的阳离子的新颖的吡喃衍生物,其中R 1和R 2分别选自 由氢和1-4个碳原子的烷基组成的组,X选自具有降血脂活性的氢,氯和溴,并降低血浆中总脂质的含量。