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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：US5068244A
公开(公告)日：1991-11-26
申请号：US312885
申请日：1989-02-17
IPC分类号： A61K31/165 , A61K31/33 , A61K31/38 , A61K31/381 , A61K31/40 , A61P7/10 , A61P9/06 , A61P9/12 , A61P25/04 , A61P25/28 , C07C67/00 , C07C209/00 , C07C209/16 , C07C209/60 , C07C211/42 , C07C215/44 , C07C215/70 , C07C217/74 , C07C233/79 , C07C235/14 , C07C271/52 , C07D295/12 , C07D295/135 , C07D333/54 , C07D333/60 , C07D521/00
CPC分类号： C07D295/135 , C07D333/60
摘要： Novel all possible enantiomeric and diastereoisomeric forms of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2, --NH.sub.2 and mono and dialkylamino of 1 to 5 alkyl carbon atoms, n is 1 or 2, A and B have the trans configuration, one of A and B being ##STR2## R.sub.2 is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2)--.sub.n2, n.sub.2 being an integer from 0 to 5 or branched alkylene of 2 to 8 carbon atoms or --CH.sub.2 --O--, Y is selected from the group consisting of phenyl, naphthyl, indenyl, heteromonocycle of 5 to 6 ring atoms and heterobicycle, all optionally having at least one substituent and the other of A and B is ##STR3## R.sub.4 and R.sub.5 individually being selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen to which they are attached form a 5 to 6 ring heterocycle optionally containing a heteroatom selected from the group consisting of --O--, --S-- and --NH-- with the proviso 1) A is ##STR4## wherein R.sub.4 l and R.sub.5 have the above definitions and B is ##STR5## wherein R.sub.2, Z and Y have the above definition or 2) Z is --(CH.sub.2).sub.n2 -- and n.sub.2 is 0,2,3,4 or 5 or branched alkylene of 2 to 8 carbon atoms or --CH.sub.2 O-- yr 3) Y is phenyl substituted with at least one member of the group consisting of alkyl of 1 to 5 carbon atoms, alkoxy of 2 to 5 carbon atoms, --NH.sub.2 and mono and dialkylamino or 4) Y is naphthyl, indenyl, heteromonocycle of 5 to 6 ring atoms or heterobicycle, all optionally substituted with at least one substituent, except unsubstituted benzothiophene or 5) R.sub.1 is --NO.sub.2 or 6) R.sub.2 is alkyl of 4 to 5 carbon atoms or 7) R.sub.1 is hydrogen, n.sub.1 is 1, A is ##STR6## Y is selected from the group consisting of 3,4-dimethoxy-phenyl, 4-nitro-phenyl and benzothienyl and B is pyrrolidinyl or 8) R.sub.1 is hydrogen, n.sub.1 is 2, A is ##STR7## Y is selected from the group consisting of 3,4-dimethoxy-phenyl, 3,4-dichloro-phenyl, 4-trifluoromethyl-phenyl, 4-nitro-phenyl and benzothienyl and B is pyrrolidinyl and their non-toxic, pharmaceutically acceptable acid addition salts having central analgesic properties and a strong affinity for opiate receptors.
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公开(公告)号：US4988810A
公开(公告)日：1991-01-29
申请号：US389805
申请日：1989-08-04
IPC分类号： C07D215/18 , C07D215/40
CPC分类号： C07D215/18 , C07D215/40
摘要： Novel enantiomeric and diastereoisomeric forms of decahydroquinolines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom to which they are connected from a 5 to 6 member heterocycle optionally including another heteroatom and optionally substituted, A is selected from the group consisting of --(CH.sub.2).sub.n -- and alkylene substituted with an alkyl and having 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, naphthyl indenyl, monocyclic heterocycle of 5 to 6 members and a bicyclic heterocycle all being unsubstituted or substituted by one or more substituents and their non-toxic, pharmaceutically acceptable acid addition salts and quaternary ammonium salts having central analgesic properties.
摘要翻译： 新颖的对映异构体和非对映异构体形式的式Ia的十氢喹啉其中R 1和R 2分别选自氢和1至5个碳原子的烷基或与它们连接的氮原子一起5 至6元杂环，任选地包括另外的杂原子和任选取代的A选自 - （CH 2）n - 和被烷基取代并具有2-8个碳原子的亚烷基，n是0-5的整数，Z 选自5至6个成员的任选取代的苯基，萘基茚基，单环杂环和全部未被取代或被一个或多个取代基取代的双环杂环，及其无毒的药学上可接受的酸加成盐和季铵盐 具有中枢镇痛特性。
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公开(公告)号：US4987131A
公开(公告)日：1991-01-22
申请号：US491264
申请日：1990-03-08
IPC分类号： A61K31/55 , A61P25/04 , A61P29/00 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel 4H-triazolo[4,3-a][1,4]benzodiazepines of the formula ##STR1## wherein 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 R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --NH.sub.2, --NHalk wherein alk is alkyl of 1 to 4 carbon atoms, ##STR2## and alk.sub.1 and alk.sub.2 are individually alkyl of 1 to 4 carbon atoms, halogen, --NO.sub.2 and --CF.sub.3 in any position of the benzene rings with the proviso that R.sub.5 and R.sub.6 are not both hydrogen and their non-toxic, pharmaceutically acceptable acid addition salts having good analgesic activity.
摘要翻译： 新颖的式（Ia）[1,4]苯并二氮杂其中R 1和R 2分别选自氢和1至5个碳原子的烷基，R 3，R 4， R5和R6分别选自氢，-OH，具有1-4个碳原子的烷基和烷氧基，-NH2，-NHalk，其中alk是1至4个碳原子的烷基，＆lt; IMAGE＆gt;和alk1和alk2是 单独的1-4个碳原子的烷基，卤素，-NO 2和-CF 3在苯环的任何位置，条件是R 5和R 6不是氢，也不是它们无毒的药学上可接受的具有良好镇痛活性的酸加成盐。
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公开(公告)号：US4975427A
公开(公告)日：1990-12-04
申请号：US415196
申请日：1989-09-29
IPC分类号： A61K31/54 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/24 , A61P25/26 , C07D209/14 , C07D417/06 , C07D513/14 , C07D513/22
CPC分类号： C07D417/06 , C07D209/14 , C07D513/14
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, hydroxy, trifluoromethyl and nitro, n is 0,1 or 2 and the group: ##STR2## in all possible racemic or optically active isomer forms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic, anti-anoxic and anti-ischemic neuronal protective properties.
摘要翻译： 选自下列化合物的化合物：其中R 1和R 2分别选自氢，卤素，具有1至5个碳原子的烷基和烷氧基，羟基，三氟甲基和硝基 ，所有可能的外消旋或旋光异构体形式的n为0,1或2，并且组：
+ TR 及其具有止痛，抗缺氧和抗缺血的无毒的药学上可接受的酸加成盐 神经元保护性质。 -
16.发明授权8-amino decahydroquinolines having central nervous system analgesic activity 失效具有中枢神经系统止痛活性的8-氨基十氢喹啉
公开(公告)号：US4968700A
公开(公告)日：1990-11-06
申请号：US217834
申请日：1988-07-11
IPC分类号： A61K31/47 , A61K31/4709 , A61P9/00 , A61P9/06 , A61P25/04 , C07D215/18 , C07D215/40 , C07D333/00 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D401/06 , C07D215/18 , C07D215/40 , C07D409/06
摘要： Novel enantiomeric and diastereoisomeric forms of decahydroquinolines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom to which they are connected form a 5 to 6 member heterocycle optionally including another heteroatom and optionally substituted, A is selected from the group consisting of --(CH.sub.2).sub.n -- and alkylene substituted with an alkyl and having 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, naphthyl indenyl, monocyclic heterocycle of 5 to 6 members and a bicyclic heterocycle all being unsubstituted or substituted by one or more substituents and their non-toxic, pharmaceuically acceptable acid addition salts and quaternary ammonium salts having central analgesic properties.
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公开(公告)号：US4950760A
公开(公告)日：1990-08-21
申请号：US348766
申请日：1989-05-08
IPC分类号： C07D215/40
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 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.
摘要翻译： 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。
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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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20.发明授权Novel 4-hydroxy-3-quinoline-carboxylates having analgesic and anti-inflammatory activity 失效具有止痛和抗炎活性的新型4-羟基-3-喹啉羧酸酯
公开(公告)号：US4735951A
公开(公告)日：1988-04-05
申请号：US790064
申请日：1985-10-22
IPC分类号： A61K31/47 , A61P1/04 , A61P25/04 , A61P29/00 , C07D213/75 , C07D215/56 , C07D265/22 , C07D277/46 , C07D401/12 , C07D417/12 , C07D491/04 , C07D491/048
CPC分类号： C07D213/75 , C07D265/22 , C07D277/46 , C07D401/12 , C07D417/12 , C07D491/04
摘要： Novel optical isomers and racemates of 4-hydroxy-3-quinoline-carboxylates 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, --SCF.sub.3 and --OCF.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 thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.5 is selected from the group consisting of aryl of 6 to 14 carbon atoms, heteroaryl of 3 to 14 carbon atoms, alkyl of 1 to 14 carbon atoms, alkyl substituted with --NH.sub.2, --NHAlk or ##STR2## alkenyl of 2 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms substituted with aryl of 6 to 14 carbon atoms, Alk and Alk' are alkyl of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts with the proviso that when X is 8-CF.sub.3, R.sub.1 and R.sub.3 are hydrogen, R.sub.2 is 2-thiazolyl, R.sub.4 is methyl, R.sub.5 is not methyl having analgesic and anti-inflammatory activity.
摘要翻译： 4-羟基-3-喹啉羧酸盐的新型光学异构体和外消旋物，其中X为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，-SCF 3和-OCF 3，R 1选自氢和1至4个碳原子的烷基，R 2选自 由噻唑基，4,5-二氢噻唑基，吡啶基，恶唑基，异恶唑基，咪唑基，嘧啶基和四唑基组成，全部任选被1至4个碳原子的烷基取代，苯基被至少一个由-OH，烷基和 1至4个碳原子的烷氧基，-CF 3，-NO 2和卤素，R 3和R 4分别选自氢，1至4个碳原子的烷基和芳基，R 5选自6 至14个碳原子，3至14个碳原子的杂芳基，1至14个碳原子的烷基，烷基取代基 具有2至6个碳原子的-NH 2，-NHA 1k或2个碳原子的烯基，2至6个碳原子被6至14个碳原子的芳基取代的烯基，Alk和Alk'是1至6个碳原子的烷基， 无毒，药学上可接受的酸加成盐，条件是当X为8-CF 3时，R 1和R 3为氢，R 2为2-噻唑基，R 4为甲基，R 5为不具有镇痛和抗炎活性的甲基。
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