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1. 发明授权

US4588731A Derivatives of isoxazolo[4,5-c]quinoline(2H)-3-one and method of preparation and use as anxiolytic agents 失效
标题翻译：异恶唑并[4,5-c]喹啉（2H）-3-酮的衍生物和制备和用作抗焦虑剂的方法
公开(公告)号：US4588731A
公开(公告)日：1986-05-13
申请号：US747665
申请日：1985-06-21
申请人： Daniel Humbert , Jean-Claude Gasc , Peter F. Hunt
发明人： Daniel Humbert , Jean-Claude Gasc , Peter F. Hunt
IPC分类号： C07D215/56 , C07D498/04 , A61K31/42 , C07D215/00 , C07D498/02
CPC分类号： C07D215/56
摘要： Novel isoxazoloquinolinones of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and CF.sub.3 -- and R.sub.1 is phenyl optionally substituted by at least one member selected from the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms having anxiolytic activity and their preparation and novel intermediates.
摘要翻译：新的式（I）的异恶唑啉喹啉酮，其中R选自氢，氟，氯，溴，1至5个碳原子的烷基和烷氧基，-NO 2和CF 3 - ，R 1是任选被至少取代的苯基选自卤素和具有1-5个碳原子的烷基和烷氧基的一个成员具有抗焦虑活性及其制备和新的中间体。

2. 发明授权

US4591589A 2-aryl pyrazolo[4,3-c]cinnolin-3-ones 失效
标题翻译： 2-芳基吡唑并[4,3-c]噌啉-3-酮
公开(公告)号：US4591589A
公开(公告)日：1986-05-27
申请号：US692030
申请日：1985-01-16
申请人： Jean-Claude Gasc , Daniel Humbert , Peter F. Hunt
发明人： Jean-Claude Gasc , Daniel Humbert , Peter F. Hunt
IPC分类号： C07D487/04 , A61K31/50 , C07D487/02
CPC分类号： C07D487/04
摘要： Novel pyrazolo[4,3-c]cinnolin-3-one derivatives of the formula ##STR1## wherein R may be in the 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and --CF.sub.3 and R' is hydrogen or R and R' taken together form an alkylenedioxy of 1 to 4 carbon atoms at the 7- or 8-positions and R.sub.1 is selected from the group consisting of phenyl, pyridyl, thiazolyl, dihydrothiazolyl and thienyl, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, mono-, di- and tri- halomethyl and aralkoxy of 7 to 12 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic properties and novel intermediates therefore.
摘要翻译：新的吡唑并[4,3-c]噌啉-3-酮衍生物，其中R可以在7-或8-位，并且选自氢，卤素，烷基和烷氧基， 1至5个碳原子，-NO 2和-CF 3和R'是氢或R和R'在一起形成在7或8位上具有1至4个碳原子的亚烷基二氧基，并且R 1选自苯基，吡啶基，噻唑基，二氢噻唑基和噻吩基，其全部任选被至少一个由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，7至12个碳原子的一，二和三卤代甲基和芳烷氧基因此具有抗焦虑性质的原子及其无毒的药学上可接受的酸加成盐。

3. 发明授权

US4988692A 2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepines 失效
标题翻译： 2,4-二氧代-5-苯基-2,3,4,5-四氢-1H-1,5-苯并二氮杂卓
公开(公告)号：US4988692A
公开(公告)日：1991-01-29
申请号：US457237
申请日：1989-12-27
申请人： Jean-Claude Gasc , Daniel Humbert
发明人： Jean-Claude Gasc , Daniel Humbert
IPC分类号： A61K31/55 , A61P3/04 , A61P25/18 , A61P43/00 , C07D243/12 , C07D403/12
CPC分类号： C07D403/12 , C07D243/12
摘要： A compound in all possible isomeric forms and mixtures thereof of the formula ##STR1## wherein X and X' are individually selected from the group consisting of hydrogen, halogen, cyano, --NO.sub.2, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms, R is hydrogen or alkyl of 1 to 8 carbon atoms and Ar is selected from the group consisting of an unsubstituted or substituted aryl of 6 to 14 carbon atoms, an unsubstituted or substituted aromatic heterocyclic or a heterocyclic united with an unsubstituted or substituted aryl having cholecystokinine antagonistic activity.
摘要翻译：具有式I的所有可能的异构体形式的化合物及其混合物，其中X和X'分别选自氢，卤素，氰基，-NO 2，-CF 3和1至8碳的烷基和烷氧基原子，R为氢或1至8个碳原子的烷基，Ar选自未取代或取代的6至14个碳原子的芳基，未取代或取代的芳族杂环或杂环与未取代或取代的芳基具有胆囊收缩素拮抗作用。

4. 发明授权

US5064853A 4(2-indolyl)2-amino-pentanedioic acids and cholecyostokinin use thereof 失效
标题翻译： 4（2-吲哚基）2-氨基 - 戊二酸和其选择性丝氨酸蛋白酶
公开(公告)号：US5064853A
公开(公告)日：1991-11-12
申请号：US478479
申请日：1990-02-12
申请人： Jean-Claude Gasc , Daniel Humbert , Mario Vekens
发明人： Jean-Claude Gasc , Daniel Humbert , Mario Vekens
IPC分类号： A61K31/00 , A61K31/195 , A61K31/198 , A61K31/225 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/44 , A61K31/4406 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/495 , A61P1/00 , A61P25/00 , C07C233/45 , C07C235/12 , C07C237/22 , C07C253/16 , C07C255/27 , C07D209/42 , C07D211/60 , C07D213/82 , C07D215/54 , C07D401/12 , C07D417/12
CPC分类号： C07D213/82 , C07C237/22 , C07D209/42 , C07D211/60 , C07D215/54 , C07D401/12 , C07C2103/32
摘要： All possible isomeric forms and mixtures thereof of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of indolyl, pyridyl, piperidinyl, quinolyl, thiazolyl and aryl of 6 to 14 carbon atoms and aralkyl of 7 to 18 carbon atoms with the latter two being unsubstituted or substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2, R.sub.2 is selected from the group consisting of ##STR2## Ar' are selected from the group consisting of pyridyl, indolyl, thiazolyl and aryl of 6 to 14 carbon atoms with the latter and the phenyl ring of b) being substituted or substrituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2 and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together with the nitrogen to which they are attached form a 5 to 7 member hydrocarbyl ring optionally containing an oxygen or a second nitrogen unsubstituted or substituted with at least one member of the group consisting of alkyl of 1 to 8 carbon atoms, aryl of 6 to 14 carbon atoms and ##STR3## Ar and Ar' having the above definitions and R.sub.4 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, ##STR4## and aralkyl of 7 18 carbon atoms unsubstituted or substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 8 carbon atoms, dialkylamino with alkyls of 1 to 8 carbon atoms, --CF.sub.3, --CN and --NO.sub.2, Alk.sub.1 is an alkylene of 2 to 8 carbon atoms and alk.sub.2 and Alk.sub.3 are individually alkyl of 1 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms having cholecystokinin agonistic or antagonistic activity.
摘要翻译：其中R 1选自吲哚基，吡啶基，哌啶基，喹啉基，噻唑基和6至14个碳原子的芳基和7至18个碳原子的芳烷基的所有可能的异构体形式及其混合物后两者是未取代的或被至少一个由1至8个碳原子的烷基和烷氧基组成的组中的至少一个取代，二烷基氨基与1至8个碳原子的烷基，-CF 3，-CN和-NO 2，R 2 （a）（b）Ar'选自吡啶基，吲哚基，噻唑基和6至14个碳原子的芳基，后者为苯基，b为苯环）被至少一个由1至8个碳原子的烷基和烷氧基组成的组中的至少一个取代或取代，二烷基氨基与1至8个碳原子的烷基，-CF 3，-CN和-NO 2，R 3是氢或 R2和R3与它们所连接的氮一起形成5 至7元烃基环，任选地含有氧或未被取代或被至少一个由1至8个碳原子的烷基取代的第二个氮，或6-14个碳原子的芳基和具有上述定义和R 4选自氢，1至8个碳原子的烷基，3至8个碳原子的环烷基，未取代的或未被至少一个成员取代的7-18个碳原子的芳烷基由1至8个碳原子的卤素，烷基和烷氧基组成的基团，具有1至8个碳原子的烷基的二烷基氨基，-CF 3，-CN和-NO 2，Alk 1是2至8个碳原子的亚烷基，alk 2和Alk 3分别具有1至8个碳原子的烷基或具有缩胆囊素激动或拮抗活性的3至8个碳原子的环烷基。

5. 发明授权

US4855302A Certain azaspirodecane compounds and a method of inducing an anxiolytic activity 失效
标题翻译：某些azaspirodecane化合物和诱导抗焦虑活性的方法
公开(公告)号：US4855302A
公开(公告)日：1989-08-08
申请号：US131186
申请日：1987-12-10
申请人： Jean-Claude Gasc , Lucien Nedelec , Daniel Humbert , Ana Maria Boaventura
发明人： Jean-Claude Gasc , Lucien Nedelec , Daniel Humbert , Ana Maria Boaventura
IPC分类号： A61K31/4427 , A61K31/445 , A61P25/20 , C07D401/14
CPC分类号： C07D401/14
摘要： A compound selected from the group consisting of azaspirodecane derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, alkoxy of 1 to 3 carbon atoms, --NO.sub.2, --NH.sub.2 and CH.sub.3 S-- in the 4,5 or 6 position of the ring, R' is oxo or hydrogen or --OH or alkyl of 1 to 3 carbon atoms and the dotted line indicates a carbon-carbon bond in the 2,3-position, n is 2,3,4 or 5 and the dotted line in the piperidyl ring is an optional carbon-carbon bond and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anxiolytic activity.
摘要翻译：选自下式的化合物的化合物其中R选自氢，氟，氯，溴，1至3个碳原子的烷氧基，-NO 2，-NH 2和CH 3 S - 的烷基硫代十一烷衍生物，在环的4,5或6位，R'是氧代或氢或-OH或1至3个碳原子的烷基，虚线表示2,3位上的碳 - 碳键，n是2 ，3,4或5，哌啶环中的虚线是任选的碳 - 碳键及其无毒的药学上可接受的酸加成盐，具有显着的抗焦虑活性。

6. 发明授权

US4450166A N-(4,5-Dihydro-thiazol-2-yl)-3-quinoline-carboxamides having anxiolytic activity 失效
标题翻译：具有抗焦虑活性的N-（4,5-二氢 - 噻唑-2-基）-3-喹啉 - 甲酰胺
公开(公告)号：US4450166A
公开(公告)日：1984-05-22
申请号：US386597
申请日：1982-06-09
申请人： Francois Clemence , Peter F. Hunt , Odile Le Martret , Daniel Humbert
发明人： Francois Clemence , Peter F. Hunt , Odile Le Martret , Daniel Humbert
IPC分类号： C07D215/56 , C07D417/12 , A61K31/47
CPC分类号： C07D417/12 , C07D215/56
摘要： Novel N-(4,5-dihydro-thiazol-2-yl)-4-hydroxy-3-quinoline-carboxamides of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, halogen, linear alkyl of 1 to 4 carbon atoms, branched alkyl of 3 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF.sub.3 --, CF.sub.3 O--, CF.sub.3 S-- and CH.sub.3 S-- in the 6- or 7-position and their non-toxic, pharmaceutically acceptable acid addition salts having a strong anxiolytic activity and a remarkable affinity for benzodiapines receptors and their preparation.
摘要翻译：新的式（I）的N-（4,5-二氢 - 噻唑-2-基）-4-羟基-3-喹啉 - 甲酰胺其中R选自氢和1至4个碳的烷基原子和R 1选自氢，卤素，1至4个碳原子的直链烷基，3至5个碳原子的支链烷基，1至4个碳原子的烷氧基，CF 3 - ，CF 3 O-，CF 3 S-和CH 3 S - 6-或7-位及其无毒的药学上可接受的酸加成盐，其具有强的抗焦虑活性和对苯并二氮杂受体的显着亲和力及其制备。

7. 发明授权

US4450167A 3-Quinoline carboxamides having anxiolytic activity 失效
标题翻译：具有抗焦虑活性的3-喹啉羧酰胺
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。

8. 发明授权

US5621095A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US5621095A
公开(公告)日：1997-04-15
申请号：US594764
申请日：1996-01-31
申请人： Jean-Fran.cedilla.ois Chantot , Solange Gouin d'Ambrieres , Daniel Humbert , Jean-Georges Teutsch
发明人： Jean-Fran.cedilla.ois Chantot , Solange Gouin d'Ambrieres , Daniel Humbert , Jean-Georges Teutsch
IPC分类号： A61K31/54 , A61P31/04 , C07D501/24 , C07D507/00 , C07D513/04 , C07D519/00
CPC分类号： C07D513/04
摘要： The syn isomer of a compound of the formula ##STR1## in the R or S form or a mixture of R and S forms wherein their non-toxic, pharmaceutically acceptable acid addition salts and having antibacterial activity and their preparation wherein the substituents are defined as in the specification.
摘要翻译：具有R或S形式的式I化合物的顺式异构体或R和S形式的混合物，其中其无毒的，药学上可接受的酸加成盐并具有抗菌活性及其制备，其中定义了取代基如说明书中所述。

9. 发明授权

US4294845A 1,3-Benzodioxin derivatives 失效
标题翻译： 1,3-苯并二恶英衍生物
公开(公告)号：US4294845A
公开(公告)日：1981-10-13
申请号：US34431
申请日：1979-04-30
申请人： Daniel Humbert , Francois Clemence , Michele Dagnaux
发明人： Daniel Humbert , Francois Clemence , Michele Dagnaux
IPC分类号： A61K31/335 , A61K31/357 , A61P3/04 , A61P9/00 , C07C39/367 , C07D319/08
CPC分类号： C07D319/08 , C07C39/367
摘要： Novel racemic mixtures or optically active isomers of 1,3-benzodioxins of the formula ##STR1## wherein R.sub.1 ' is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, --NH.sub.4, aluminum, non-toxic, pharmaceutically acceptable amines, alkyl of 1 to 5 carbon atoms, 2,3-dihydroxypropanyl, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl and dialkylaminoalkyl with alkyls of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl and R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen and halogen, and the non-toxic, pharmaceutically acceptable acid addition salts where R.sub.1 ' is dialkylaminoalkyl, with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously having hypolipemic activity and their preparation.
摘要翻译：下式的1,3-苯并二恶英的新型外消旋混合物或光学活性异构体其中R1'选自氢，碱金属，碱土金属，-NH4，铝，无毒，药学上可接受的胺，1至5个碳原子的烷基，2,3-二羟基丙酰基，（2,2-二甲基-1,3-二氧戊环-4-基）甲基和具有1至4个碳原子的烷基的二烷基氨基烷基，R2选自由氢和1至5个碳原子的烷基组成的组，R3选自氢，1至5个碳原子的烷基和苯基，R4和R5分别选自氢和卤素，和无毒，药学上可接受的酸加成盐，其中R1'是二烷基氨基烷基，条件是R2和R3不同时具有降血脂活性及其制备。

10. 发明授权

US4051249A Salts of 2-alkylthiazole-5-methanol derivatives 失效
标题翻译： 2-甲基噻唑-5-甲醇衍生物的盐
公开(公告)号：US4051249A
公开(公告)日：1977-09-27
申请号：US650291
申请日：1976-01-19
申请人： Michel Hardy , Daniel Humbert
发明人： Michel Hardy , Daniel Humbert
IPC分类号： A61K31/426 , C07D277/24 , C07D277/56
CPC分类号： C07D277/56 , C07D277/24
摘要： Non-toxic, pharmaceutically acceptable acid addition salts of a compound of the formula ##STR1## wherein R is an alkyl of 2 to 12 carbon atoms and R' is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and acyl of an organic carboxylic acid of 1 to 12 carbon atoms having antilipolytic activity and a very prolonged vasodilatatory activity.

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