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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

US3981861A Antibiotic aminoglycosides, processes of preparation and pharmaceutical compositions 失效
标题翻译：抗生素氨基糖苷类，制备方法和药物组合物
公开(公告)号：US3981861A
公开(公告)日：1976-09-21
申请号：US556405
申请日：1975-03-07
申请人： Jean Bernard Chazan , Daniel Coussediere , Jean-Claude Gasc
发明人： Jean Bernard Chazan , Daniel Coussediere , Jean-Claude Gasc
IPC分类号： C07H15/23 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , B01J23/00 , B01J27/00 , C07B61/00 , C07H15/234 , C07H15/22
CPC分类号： C07H15/234
摘要： There are disclosed pharmaceutically-active aminoglycosides comprising 4-0-(2',6'-diamino 2', 3', 4', 6'-tetradesoxy .alpha.,D-erythrohexopyrannosyl) 6-0-(3"-methylamino 3", 4", 6"-tridesoxy .alpha.,D-xylohexopyrannosyl) 2-desoxystreptamine of the formula: ##SPC1##And the addition salts thereof with mineral acids or organic acids. Also disclosed are methods for preparation of the novel products as well as certain novel intermediate products. There are also disclosed pharmaceutical compositions in which the novel products are the active agents as well as methods for use of compositions as antibiotic agents.
摘要翻译：公开了含有4-0-（2'，6'-二氨基2'，3'，4'，6'-四氧硫基α，D-赤式吡喃葡萄糖基）6-0-（3“ - 甲基氨基3 “4”，6“ - 三酰氧基α，D-木糖六吡喃糖基）2-脱氧神经胺如下：

7. 发明授权

US4736042A 2,3-dihydro indoles 失效
标题翻译： 2,3-二氢吲哚
公开(公告)号：US4736042A
公开(公告)日：1988-04-05
申请号：US72359
申请日：1987-07-13
申请人： Jean-Claude Gasc , Lucien Nedelec , Claude Rettien , Dinah W. Nanopoulos
发明人： Jean-Claude Gasc , Lucien Nedelec , Claude Rettien , Dinah W. Nanopoulos
IPC分类号： A61K31/535 , A61P9/12 , A61P25/28 , C07D209/08 , C07D413/04
CPC分类号： C07D413/04 , C07D209/08
摘要： Novel racemic mixtures and optical isomers of 4-morpholinyl-1H-indoles of the formula: ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of hydroxymethyl, alkylthiomethyl of 1 to 3 alkyl carbons, cyanomethyl and carboxy optionally esterified with an aliphatic alcohol of 1 to 5 carbon atoms or optionally amidified with an amine of the formula ##STR2## R.sub.3 is alkyl of 1 to 4 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having the ability to activate neurons and to protect the same against ischemic or anoxic aggressions.
摘要翻译： 4-吗啉基-1H-吲哚的新型外消旋混合物和旋光异构体，其分子式如下：其中R和R 1分别选自氢和1至4个碳原子的烷基，R 2选自由羟甲基，1至3个烷基碳的烷硫基甲基，任选地被1至5个碳原子的脂族醇酯化的氰基甲基和羧基，或任选地与下式的胺酰胺化：具有1至4个碳原子的烷基和R 4 选自氢和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，其具有激活神经元的能力并保护其相对于缺血性或缺氧性侵袭。

8. 发明授权

US4412988A Hexapeptides 失效
标题翻译：六肽
公开(公告)号：US4412988A
公开(公告)日：1983-11-01
申请号：US310392
申请日：1981-10-09
申请人： Jean-Claude Gasc , Serge Geoffre , Michel Hospital , Jacques Laurent
发明人： Jean-Claude Gasc , Serge Geoffre , Michel Hospital , Jacques Laurent
IPC分类号： A61K38/00 , A61P25/00 , C07K1/04 , C07K7/06 , C07C103/52 , A61K37/02
CPC分类号： C07K7/06 , A61K38/00 , Y10S930/26 , Y10S930/27
摘要： Novel hexapeptides of the formulaCys--X--Y--D--Lys--Z Iwherein X is a sequence selected from the group consisting of Ala--Ala and Glu--His, Y is selected from the group consisting of Cys and Phe and Z is Phe when Y is Cys or Z is Cys when Y is Phe, the two Cys groups in the molecule being joined by a disulfide bridge, and their functional derivatives such as their non-toxic, pharmaceutically acceptable acid addition salts, salts with bases, esters and amides and metallic complexes thereof having an influence on the memory process and their preparation.
摘要翻译：式Cys-XYD-Lys-Z I的新型六肽，其中X为选自Ala-Ala和Glu-His的序列，Y选自Cys和Phe，Z为Phe时，Y为当Y为Phe时，Cys或Z为Cys，分子中的两个Cys基团通过二硫键连接，其功能衍生物如其无毒的药学上可接受的酸加成盐，与碱，酯和酰胺的盐和金属其复合物对记忆过程及其制备有影响。

9. 发明授权

US4699907A 4-morpholinyl-1H-indoles, pharmaceutical compositions and use 失效
标题翻译： 4-吗啉基-1H-吲哚，药物组合物和用途
公开(公告)号：US4699907A
公开(公告)日：1987-10-13
申请号：US941037
申请日：1986-12-12
申请人： Jean-Claude Gasc , Lucien Nedelec , Claude Rettien , Dinah W. Nanopoulos
发明人： Jean-Claude Gasc , Lucien Nedelec , Claude Rettien , Dinah W. Nanopoulos
IPC分类号： A61K31/535 , A61P9/12 , A61P25/28 , C07D209/08 , C07D413/04 , C07D413/02
CPC分类号： C07D413/04 , C07D209/08
摘要： Novel racemic mixtures and optical isomers of 4-morpholinyl-1H-indoles of the formula: ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of hydroxymethyl, alkylthiomethyl of 1 to 3 alkyl carbons, cyanomethyl and carboxy optionally esterified with an aliphatic alcohol of 1 to 5 carbon atoms or optionally amidified with an amine of the formula ##STR2## R.sub.3 is alkyl of 1 to 4 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having the ability to activate neurons and to protect the same against ischemic or anoxic aggressions.
摘要翻译： 4-吗啉基-1H-吲哚的新型外消旋混合物和光学异构体，其具有下式：其中R和R 1分别选自氢和1至4个碳原子的烷基，R 2选自由羟甲基，1至3个烷基碳的烷硫基甲基，任选地被1至5个碳原子的脂族醇酯化的氰基甲基和羧基，或任选地与下式的胺酰胺化：具有1至4个碳原子的烷基和R 4 选自氢和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，其具有激活神经元的能力并保护其相对于缺血性或缺氧性侵袭。

10. 发明授权

US3959255A Antibiotic aminoglycosides, and process of preparation 失效
标题翻译：抗生素氨基糖苷类及其制备方法
公开(公告)号：US3959255A
公开(公告)日：1976-05-25
申请号：US464934
申请日：1974-04-29
申请人： Jean-Bernard Chazan , Daniel Coussediere , Jean-Claude Gasc
发明人： Jean-Bernard Chazan , Daniel Coussediere , Jean-Claude Gasc
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , B01J23/00 , B01J31/00 , C07B61/00 , C07H15/18 , C07H15/234 , C07H15/22
CPC分类号： C07H15/18 , C07H15/234
摘要： There are disclosed pharmaceutically-active aminoglycosides comprising 4-O-[2',6'-diamino-2',6'-didesoxy-.alpha.-D-glucopyranosyl] 6-O-[3"-methylamino-3",4",6"-tridesoxy-.alpha.-D-xylohexopyranosyl] 2-desoxy streptamine of the formula: ##SPC1##And the addition salts thereof with mineral acids or organic acids. Also disclosed are methods for preparation of the novel products as well as certain novel intermediate products. There are also disclosed pharmaceutical compositions in which the novel products are the active agents as well as methods for use of compositions as antibiotic agents.
摘要翻译：公开了含有4-O- [2'，6'-二氨基-2'，6'-二氧杂-α-D-吡喃葡萄糖基] 6-O- [3“ - 甲基氨基-3”的药物活性氨基糖苷类， 4“，6” - 三氧基-α-D-木糖六吡喃糖基] 2-脱氧链霉胺，其结构如下：

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