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公开(公告)号：US4650811A
公开(公告)日：1987-03-17
申请号：US691163
申请日：1985-01-14
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P3/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P7/00 , A61P9/06 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/02 , A61P43/00 , C07D209/08 , C07D209/30 , C07D209/34 , C07D407/12 , C07D209/12
CPC分类号： C07D407/12 , C07D209/08 , C07D209/30 , C07D209/34
摘要： 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.
摘要翻译： 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。 -
公开(公告)号：US5086070A
公开(公告)日：1992-02-04
申请号：US514692
申请日：1990-04-26
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P7/02 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D209/08 , C07D209/26 , C07D209/28 , C07D209/34 , C07D403/10 , C07D405/10 , C07D405/12
CPC分类号： C07D405/12 , C07D209/08 , C07D209/34
摘要： Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having antiarhythmic activity.
摘要翻译： 具有抗心律失常活性的所有非对映异构体形式的新颖的4-苄基-1H-吲哚与式（Ⅰ）的混合物。
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公开(公告)号：US4791109A
公开(公告)日：1988-12-13
申请号：US883915
申请日：1986-07-10
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/445 , A61K31/495 , A61P9/06 , C07D209/08 , C07D209/34 , A61K31/535 , C07D413/12
CPC分类号： C07D209/34 , C07D209/08
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-arrhythmic properties.
摘要翻译： 式I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组成的组中取代的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位的芳烷基 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 2至5个碳原子的羧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＆lt; IMAGE＆gt; 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 具有显着的抗心律失常性质。
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公开(公告)号：US5380722A
公开(公告)日：1995-01-10
申请号：US66565
申请日：1993-05-25
IPC分类号： C07D209/08 , C07D209/34 , A61K31/535 , A61K31/495 , C07D403/00 , C07D413/00
CPC分类号： C07D209/08 , C07D209/34
摘要： Novel indole-carboxamides of the formula ##STR1## and their non-toxic pharmaceutically acceptable acid addition salts having remarkable anti-arrhytmic properties.
摘要翻译： 新颖的式I的吲哚 - 甲酰胺及其无毒的药学上可接受的酸加成盐具有显着的抗arrhyty性质。
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公开(公告)号：US5182282A
公开(公告)日：1993-01-26
申请号：US781070
申请日：1991-10-11
IPC分类号： C07D209/08 , C07D209/34 , C07D405/12
CPC分类号： C07D405/12 , C07D209/08 , C07D209/34
摘要： Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having anti-arhythmic activity.
摘要翻译： 具有抗心律失常活性的所有非对映异构体形式的新颖的4-苄基-1H-吲哚与式（Ⅰ）的混合物。
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6.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
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/535 , A61P9/00 , A61P9/06 , A61P43/00 , C07D209/08 , C07D209/34 , C07D405/12 , C07D209/04
CPC分类号： C07D405/12 , C07D209/08 , C07D209/34
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。
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公开(公告)号：US5084455A
公开(公告)日：1992-01-28
申请号：US438525
申请日：1989-11-17
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.0 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-arrhythmic properties.
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公开(公告)号：US4853408A
公开(公告)日：1989-08-01
申请号：US853030
申请日：1986-04-17
IPC分类号： C07D209/08 , C07D209/34
CPC分类号： C07D209/34 , C07D209/08
摘要： Novel 4-phenylpropyl-indoles of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, linear alkyl of 1 to 5 carbon atoms, branched alkyl of 3 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms cycloalkylalkyl of 4 to 7 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle containing another heteroatom selected from the group consisting of oxygen, sulfur and nitrogen optionally substituted with a member of the group consisting of alkyl of 1 to 5 carbon atoms, phenyl, naphthyl and aralkyl of 7 to 12 carbon atoms, a together with b forms .dbd.0 or a together with c form a carbon-carbon bond, b is hydrogen or with a forms .dbd.0, c is hydrogen or with a forms a carbon-carbon bond, the dotted line is an optional carbon-carbon bond, A is --(CH.sub.2).sub.n --, is an integer from 2 to 5, R.sub.2 is selected from the group consisting of hydrogen, linear alkyl of 1 to 5 carbon atoms and branched alkyl of 3 to 5 carbon atoms, x is hydrogen or -OH or together with y forms .dbd.0 and y is hydrogen or together with x forms .dbd.0 and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable antiarythmic properties and blocking of slow calcicosodic canals.
摘要翻译： 式（Ⅰ）的新型4-苯丙基 - 吲哚，其中R和R 1分别选自氢，1〜5个碳原子的直链烷基，3〜5个碳原子的支链烷基，3〜7的环烷基 4至7个碳原子的碳原子环烷基烷基和7至12个碳原子的任选取代的芳烷基，或与R 1和R一起与氮原子一起形成含有选自氧，硫和氮的另外的杂原子的任选不饱和的杂环， 具有1至5个碳原子的烷基的基团，苯基，萘基和7至12个碳原子的芳烷基，以及b形式= 0或a与c一起形成碳 - 碳键，b是氢 或形式= 0，c为氢或形成碳 - 碳键，虚线为任选的碳 - 碳键，A为 - （CH 2）n - ，为2至5的整数，R 2为 选自氢，线性烷基 1个1-5个碳原子的烷基和3至5个碳原子的支链烷基，x是氢或-OH或y一起形成= 0，y是氢或x形式= 0，它们的无毒的药学上可接受的酸 加成盐具有显着的抗血栓性质和阻塞缓慢的钙沉积管。
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公开(公告)号：US4737505A
公开(公告)日：1988-04-12
申请号：US757515
申请日：1985-07-19
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/445 , A61P25/04 , C07D401/04
CPC分类号： C07D401/04
摘要： Novel indole of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 12 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, cyanoalkyl of 3 to 8 carbon atoms, hydroxyalkyl of 2 to 8 carbon atoms, --(CH.sub.2).sub.n --O--B, ##STR2## aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, CF.sub.3 --, CF.sub.3 O--, --NH.sub.2 and --NO.sub.2 and cycloalkyl alkyl of 4 to 12 carbon atoms, n is one integer from 2 to 8, B is selected from the group consisting of aryl and heteroaryl, both optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, hydroxyalkyl of 1 to 5 carbon atoms, nitro, amino, CF.sub.3 --, alkenyl and alkenyloxy of 2 to 5 carbon atoms and alkynyl and alkynyloxy of 2 to 5 carbon atoms, a and b are both hydrogen or a is hydrogen and b is --OH or alkoxy of 1 to 8 carbon atoms or a and b together form a carbon-carbon bond and the 2-oxo with dotted lines indicates its possible presence with the double bond in the indole ring missing and its non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity of the morphine type.
摘要翻译： 其中R选自氢，1至8个碳原子的烷基和7至12个碳原子的芳烷基的式VI的新型吲哚，Z选自氢，1至 具有2至8个碳原子的烯基，3至8个碳原子的氰基烷基，2至8个碳原子的羟烷基， - （CH 2）n OB，7-12个碳原子的芳基，其任选被至少一个 由1至5个碳原子的烷基和烷氧基组成的组，卤素，-OH，CF 3 - ，CF 3 O-，-NH 2和-NO 2以及4至12个碳原子的环烷基烷基，n是2至8的一个整数 B选自芳基和杂芳基，两者任选被至少一个由1至5个碳原子的烷基和烷氧基组成的组中的一个取代，卤素，-OH，1-5个碳原子的羟基烷基，硝基 ，2至5个碳原子的氨基，CF 3 - ，链烯基和烯氧基以及2至5个碳原子的炔基和炔氧基，a和ba 氢或a是氢并且b是-OH或1-8个碳原子的烷氧基或a和b一起形成碳 - 碳键，并且具有虚线的2-氧代表示其在吲哚中可能存在双键 戒指及其无毒，药学上可接受的具有吗啡类止痛活性的酸加成盐。
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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＆lt; IMAGE＆gt; 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。
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