-
31.发明授权
公开(公告)号：US4988708A
公开(公告)日：1991-01-29
申请号：US183911
申请日：1988-04-20
IPC分类号： C07D213/75 , C07D215/56 , C07D265/22 , C07D277/46 , C07D401/12 , C07D417/12 , C07D417/14 , C07D491/04
CPC分类号： C07D213/75 , C07D215/56 , C07D265/22 , C07D277/46 , C07D401/12 , C07D417/12 , C07D417/14 , C07D491/04
摘要： A compound selected from the group consisting of 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 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, A is ##STR2## in which 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 heteroaryl f 3 to 14 carbon atoms optionally substituted with alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids or bases having analgesic and anti-inflammatory activity.
-
公开(公告)号：US4987140A
公开(公告)日：1991-01-22
申请号：US441317
申请日：1989-11-27
IPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/505 , A61P29/00 , C07D213/82 , C07D413/12 , C07D417/12 , C07D417/14
CPC分类号： C07D213/82 , C07D417/12
摘要： Novel pyridines of the formula ##STR1## wherein R is selected from the group consisting of (a) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen --CF.sub.3 and --NO.sub.2 and (b) a 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of (a) alkyl of 1 to 5 carbon atoms, (b) 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms and (c) phenyl and naphthyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --NO.sub.3 and --CF.sub.3, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, --(CF.sub.2).sub.n --CF.sub.3 and ##STR2## n is an integer from 0 to 4 and Alk is alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids and bases having anti-inflammatory and anti-rheumatic properties.
-
公开(公告)号：US4816465A
公开(公告)日：1989-03-28
申请号：US2778
申请日：1987-01-13
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 , C07D401/02
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, 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形式的式Ⅰ'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形成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。
-
公开(公告)号：US4596875A
公开(公告)日：1986-06-24
申请号：US623430
申请日：1984-06-22
IPC分类号： C07D215/56 , A61K31/47 , A61P25/04 , A61P29/00 , C07D209/38 , C07D265/22 , C07D277/46 , C07D401/12 , C07D417/12 , C07D491/04 , C07D491/048 , C07D215/22 , C07D417/06
CPC分类号： C07D265/22 , C07D209/38 , C07D277/46 , C07D401/12 , C07D417/12 , C07D491/04
摘要： Novel 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, --CF.sub.3, --OCF.sub.3 and --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 thiazolyl, 4,5-dihydro-thiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidinyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and 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, --CF.sub.3, --NO.sub.2 and halogen, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.4 is 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 hydrogen, alkyl of 1 to 4 carbon atoms and ##STR2## R.sub.5 ' is selected from the group consisting of alkyl of 1 to 4 carbon atoms and aryl and their non-toxic, pharmaceutically acceptable acid addition salts and salts with non-toxic, pharmaceutically acceptable bases having very good analgesic activity and a non-negligible anti-inflammatory activity and novel intermediates.
摘要翻译： 下式的新型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，-CF 3，-OCF 3和-SCF 3，R 1选自氢和1至4个碳原子的烷基，R 2选自噻唑基， 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，全部任选被1至4个碳原子的烷基取代，并且苯基任选被至少一个由-OH，1-4个碳原子的基团取代 1至4个碳原子的烷氧基，-CF 3，-NO 2和卤素，R 3选自氢，1至4个碳原子的烷基和芳基，R 4选自氢， 1至4个碳原子和芳基，R 5选自氢，1至4个碳原子的烷基 R 5'选自1至4个碳原子的烷基和芳基及其无毒的药学上可接受的酸加成盐和与具有非常好的止痛活性的无毒，药学上可接受的碱的盐，以及 不可忽略的抗炎活性和新型中间体。
-
公开(公告)号：US4486438A
公开(公告)日：1984-12-04
申请号：US498832
申请日：1983-05-27
IPC分类号： C07D215/56 , A61K31/47 , A61P25/04 , A61P29/00 , C07D209/38 , C07D265/22 , C07D277/46 , C07D401/12 , C07D417/12 , C07D491/04 , C07D491/048 , C07D215/36
CPC分类号： C07D265/22 , C07D209/38 , C07D277/46 , C07D401/12 , C07D417/12 , C07D491/04
摘要： Novel 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, --CF.sub.3, --OCF.sub.3 and --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 thiazolyl, 4,5-dihydro-thiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidinyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and 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, --CF.sub.3, --NO.sub.2 and halogen R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.4 is 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 hydrogen, alkyl of 1 to 4 carbon atoms and ##STR2## R.sub.5 ' is selected from the group consisting of alkyl of 1 to 4 carbon atoms and aryl and their non-toxic, pharmaceutically acceptable acid addition salts and salts with non-toxic, pharmaceutically acceptable bases having very good analgesic activity and a non-negligible anti-inflammatory activity and novel intermediates.
摘要翻译： 下式的新型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，-CF 3，-OCF 3和-SCF 3，R 1选自氢和1至4个碳原子的烷基，R 2选自噻唑基， 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，全部任选被1至4个碳原子的烷基取代，并且苯基任选被至少一个由-OH，1-4个碳原子的基团取代 1至4个碳原子的烷氧基，-CF 3，-NO 2和卤素R 3选自氢，1至4个碳原子的烷基和芳基，R 4选自氢，烷基1 至4个碳原子和芳基，R 5选自氢，1至4个碳原子的烷基和 R5'选自1-4个碳原子的烷基和芳基及其无毒的药学上可接受的酸加成盐和盐与具有非常好的止痛活性的无毒的药学上可接受的碱， - 轻微的抗炎活性和新颖的中间体。
-
公开(公告)号：US4450167A
公开(公告)日：1984-05-22
申请号：US398575
申请日：1982-07-15
申请人： Odile Le Martret , Daniel Humbert , Peter F. Hunt
发明人： Odile Le Martret , Daniel Humbert , Peter F. Hunt
IPC分类号： C07D215/48 , A61K31/47 , A61P25/20 , C07D215/54 , C07D215/56 , C07D401/12
CPC分类号： C07D401/12 , C07D215/54 , C07D215/56
摘要： Novel 3-quinoline-carboxamides of the formula ##STR1## wherein R is in 6 or 7-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, --CF.sub.3, --SCF.sub.3 and CH.sub.3 S--, R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, phenyl and benzyl, R.sub.2 is --NHR.sub.4, R.sub.4 is selected from the group consisting of alkyl of 2 to 6 carbon atoms, substituted aryl of 6 to 10 carbon atoms and substituted heterocycle of an aromatic character of 3 to 5 carbon atoms with the proviso that when R.sub.4 is a mono substituted aryl or heterocycle, the substituent is different from R of the quinoline when it is a halogen and R.sub.3 is selected from the group consisting of hydrogen and --OH and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anxiolytic properties capable of lessening emotional reactions and diminishing states of psychic tension and their preparation.
摘要翻译： 式（Ⅰ）的新型3-喹啉 - 甲酰胺其中R为6或7位，选自氢，卤素，1至6个碳原子的烷基，3至6个碳原子的环烷基， 1至6个碳原子的烷氧基，-CF 3，-SCF 3和CH 3 S - ，R 1选自氢，1至6个碳原子的烷基，苯基和苄基，R 2是-NHR 4，R 4选自 由2至6个碳原子的烷基，6至10个碳原子的取代的芳基和3至5个碳原子的芳族特征的取代杂环组成，条件是当R4是单取代的芳基或杂环时，取代基不同 当喹啉为卤素时，R 3选自氢和-OH，并且其无毒的药学上可接受的酸加成盐具有显着的抗焦虑性能，能够减轻情绪反应和心理紧张状态的降低， 准备 离子。
-
37.发明授权2-Trifluoromethyl-3-quinoline carboxamides, analgesic and anti-inflammatory compositions and methods employing them 失效2-三氟甲基-3-喹啉羧酰胺，止痛剂和抗炎组合物和使用它们的方法
公开(公告)号：US4299831A
公开(公告)日：1981-11-10
申请号：US097711
申请日：1979-11-27
IPC分类号： C07D413/12 , A61K31/47 , A61K31/505 , A61P25/04 , A61P29/00 , C07D215/56 , C07D401/12 , C07D417/12
CPC分类号： C07D215/56
摘要： Novel 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, straight or branched alkyl and alkoxy of 1 to 5 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 optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic and anti-inflammatory activity and novel intermediates and process for their preparation.
摘要翻译： 具有式“IMAGE”I'的新型3-喹啉甲酰胺，其中X'为5,6,7或8-位，并且选自氢，卤素，直链或支链烷基和烷氧基，为1至5 碳原子，-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，其全部任选被1至4个碳原子的烷基取代，并且任选被至少一个由1至4个碳原子的烷基和烷氧基取代的基团，-CF 3，-NO 2和 卤素及其无毒，药学上可接受的具有镇痛和抗炎活性的酸加成盐和新型中间体及其制备方法。
-
公开(公告)号：US5234944A
公开(公告)日：1993-08-10
申请号：US970776
申请日：1992-11-03
IPC分类号： C07D295/135 , C07D311/96
CPC分类号： C07D295/135 , C07D311/96
摘要： A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula ##STR1## wherein R.sub.6 is selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually hydrogen or alkyl of 1 to 5 carbon atoms or taken together with the carbon atoms to which they are attached form a cycloalkyl of 3 to 6 carbon atoms optionally containing a heteroatom selected from the group consisting of --S--, --O-- and --N--, one of A and B has the formula ##STR2## and the other has the formula ##STR3## R is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Z is selected from the group consisting of --(CH.sub.2).sub.n --, branched alkylene of 2 to 8 carbon atoms and --CH.sub.2 O--, n is an integer of 0 to 5, X, X' and X" are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 4 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.2, mono and dialkylamino of 1 to 4 alkyl carbon atoms and sulfamino, R.sub.3 and R.sub.4 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 attached form a 5 to 6 member heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR4## R.sub.1 ' is hydrogen or alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having a strong affinity for optical receptors, central analgesic, diuretic, anti-arrythmic, hypotensive and cerebral anti-ischemic activity.
摘要翻译： 选自下组的对映异构体和非对映异构体形式的化合物及其混合物，其中R 6选自氢，卤素和1至5个碳原子的烷基和烷氧基，R 1和R 2分别为 氢或1至5个碳原子的烷基或与它们所连接的碳原子一起形成3至6个碳原子的环烷基，任选地含有选自-S - ， - O-和-N - ，A和B中的一个具有式
，另一个具有式（Ia）的化合物，其选自氢和1至5个碳原子的烷基，Z选自 - （ CH 2）n支链亚烷基，-CH 2 O-，n为0〜5的整数，X，X'和X“分别选自氢，烷基和烷氧基的1 至4个碳原子，卤素，-OH，-CF 3，-NO 2，-NH 2，1至4个烷基的单和二烷基氨基 碳原子和磺氨基，R3和R4分别选自氢和1至5个碳原子的烷基，或与它们所连接的氮原子一起形成5至6个成员杂环，任选地含有 由-O-，-S-和R IMA'组成的基团是氢或1至4个碳原子的烷基，它们对光学受体具有强亲和力的无毒的药学上可接受的酸加成盐，中枢性镇痛药，利尿剂， 抗焦虑，降压和脑抗缺血活性。 -
39.发明授权N-substituted derivatives of .alpha.-mercapto alkylamines, their preparation process and the intermediates obtained, their use as medicaments and the compositions containing them 失效（ALPHA）-MERCAPTO ALKYLAMINES的N-取代衍生物，其制备方法和所获得的中间体，它们作为药物和包含它们的组合物使用
公开(公告)号：US5190974A
公开(公告)日：1993-03-02
申请号：US725985
申请日：1991-07-05
IPC分类号： A61K31/17 , C07C319/20 , C07C323/41 , C07C323/44 , C07C327/30 , C07C327/42 , C07C331/24 , C07C335/04 , C07D211/58 , C07D213/75 , C07D243/08 , C07D243/24 , C07D295/10 , C07D295/15 , C07D295/215 , C07D295/32
CPC分类号： C07D213/75 , C07C323/44 , C07C327/30 , C07D211/58 , C07D243/08 , C07D243/24 , C07D295/15 , C07D295/215
摘要： Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein n, R.sub.1, R.sub.2, X, A, R.sub.3A and R.sub.4A are set forth in the claims and their non-toxic, pharmaceutically acceptable acid addition salts having excellent analgesic, psychotropic and enkephalinase inhibiting properties.
摘要翻译： 新颖的α-巯基 - 烷基胺在所有可能的外消旋，对映异构体和非对映异构体形式的式IA中，其中n，R1，R2，X，A，R3A和R4A在权利要求书中阐述，并且其无毒的药学上可接受的 酸加成盐具有优异的镇痛，精神病和脑啡肽酶抑制特性。
-
40.发明授权Novel 4-hydroxy-3-pyridine-carboxamides useful for treating inflammation and rheumatism 失效用于治疗炎症和风湿病的新型4-羟基-3-吡啶 - 甲酰胺
公开(公告)号：US4925859A
公开(公告)日：1990-05-15
申请号：US167375
申请日：1988-03-31
IPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/505 , A61P29/00 , C07D213/82 , C07D413/12 , C07D417/12 , C07D417/14
CPC分类号： C07D213/82 , C07D417/12
摘要： Novel pyridines of the formula ##STR1## wherein R is selected from the group consisting of (a) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --CF.sub.3 and --NO.sub.2 and (b) a 5 to 6 member hetercyclic optionally substituted with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of (a) alkyl of 1 to 5 carbon atoms, (b) 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms and (c) phenyl and naphthyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --NO.sub.3 and --CF.sub.3, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, --(CF.sub.2).sub.n --CF.sub.3 and ##STR2## n is an integer from 0 to 4 and Alk is alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids and bases having anti-inflammatory and anti-rheumatic properties.
摘要翻译： 式（I）的新吡啶，其中R选自（a）任选被至少一个由1-5个碳原子的羟基，烷基和烷氧基组成的组中的一个取代基取代的苯基，卤素，-CF 3 和（b）任选被1至5个碳原子的烷基取代的5至6元杂环，R 1和R 2分别选自（a）1至5个碳原子的烷基，（b）5 至（C）任选被1至5个碳原子的烷基取代的6元杂环，和（c）任选被至少一个选自1至5个碳原子的烷基和烷氧基的基团取代的苯基和萘基，卤素，-NO 3和 -CF 3，R 3选自氢，1〜5个碳原子的烷基， - （CF 2）n -CF 3，n为0〜4的整数，Alk为1〜5个碳原子的烷基 和它们的无毒，药学上可接受的盐与酸和碱具有抗炎和抗风湿性 matic属性。
-
-
-
-
-
-
-
-
-
搜索结果
50 条记录 (耗时 0.034 秒)
