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1. 发明授权

US4503053A C-Homo-9-oxa-ergolines 失效
标题翻译： C-同-9-氧杂 - 麦角碱
公开(公告)号：US4503053A
公开(公告)日：1985-03-05
申请号：US532740
申请日：1983-09-15
申请人： Lucien Nedelec , Jean-Claude Gasc , Patrick Fauveau
发明人： Lucien Nedelec , Jean-Claude Gasc , Patrick Fauveau
IPC分类号： A61K31/535 , A61P25/00 , A61P43/00 , C07D209/00 , C07D265/00 , C07D498/06
CPC分类号： C07D209/94 , C07D498/06
摘要： Novel C-homo-9-oxa-ergolines of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine or taken with b forms .dbd.0, a and b form a carbon-carbon bond or a is hydrogen when R.sub.1 and b form .dbd.0, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aralkyl of 7 to 12 carbon atoms and cycloalkylalkyl of 4 to 7 carbon atoms, R.sub.3 is selected from the group consisting of hydroxymethyl, alkylthiomethyl of 1 to 5 alkyl carbon atoms, cyanomethyl, carboxy optionally esterified with an aliphatic alcohol of 1 to 5 carbon atoms and ##STR2## R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.5 is alkyl of 1 to 4 carbon atoms or R.sub.4 and R.sub.5 taken with the nitrogen atom form a saturated heterocycle optionally containing a second heteroatom having dopaminergic agonist, serotoninergic and antihypertensive activity as well as prolactin secretion inhibition and antianoxic activities and their preparation and intermediates.
摘要翻译：式（Ⅰ）的新型C-高-9-氧杂 - 麦角醇其中R选自氢和1至4个碳原子的烷基，R 1选自氢，氯和溴或以b形式= 0取代，a和b形成碳 - 碳键，或者当R 1和b形成= 0时，a为氢，R 2选自氢，1至4个碳原子的烷基，7至 12个碳原子和4至7个碳原子的环烷基烷基，R 3选自羟甲基，1至5个烷基碳原子的烷基硫甲基，氰基甲基，任选被1至5个碳原子的脂族醇酯化的羧基， R4选自氢和1-4个碳原子的烷基，R5是1-4个碳原子的烷基或R4和R5与氮原子一起形成饱和杂环，任选地含有具有多巴胺能激动剂的第二个杂原子，5-羟色胺能和抗高血压活动以及催乳素分泌抑制和抗氧化活性及其制备和中间体。

2. 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。

3. 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。

4. 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。

5. 发明授权

US4661482A Use of pyrazolobenzoxazines in method of treating cerebral senescence and cerebral hypoxin 失效
标题翻译：在治疗脑衰老和脑缺氧的方法中使用吡唑并苯恶嗪
公开(公告)号：US4661482A
公开(公告)日：1987-04-28
申请号：US833347
申请日：1986-02-25
申请人： Lucien Nedelec , Patrick Fauveau , Gilles Hamon , Claude Oberlander
发明人： Lucien Nedelec , Patrick Fauveau , Gilles Hamon , Claude Oberlander
IPC分类号： A61K31/535 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/00 , A61P7/00 , A61P9/12 , A61P25/00 , A61P25/28 , C07D265/36 , C07D498/04 , C07D265/34
CPC分类号： C07D265/36
摘要： Novel pyrazolobenzoxazines of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl or 4 to 7 carbon atoms, alkenyl and alkynyl of 3 to 5 carbon atoms with the proviso that the multiple bond is not between the carbon .alpha.- and .beta.- to the nitrogen atom, aralkyl of 7 to 12 carbon atoms and aralkyl of 7 to 12 carbon atoms substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, amino, -OH and halogen, X is selected from the group consisting of hydrogen and --CH.sub.2 --S--Alk, Alk is alkyl of 1 to 5 carbon atoms, the wavy line indicates the .alpha.- or .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic agonistic, hypotensive, antihypertensive and antianoxic properties and their preparation.
摘要翻译：新颖的式（Ⅰ）的吡唑并苯并恶嗪其中R选自氢，1至5个碳原子的烷基，环烷基烷基或4至7个碳原子，3至5个碳原子的链烯基和炔基，条件是多个键不在与氮原子的碳原子和β之间，7-12个碳原子的芳烷基和7至12个碳原子的芳烷基被至少一个由1至5个碳原子的烷基和烷氧基组成的组取代的芳烷基碳原子，氨基，-OH和卤素，X选自氢和-CH 2 -S-Alk，Alk是1至5个碳原子的烷基，波浪线表示α或β位，它们的具有多巴胺能激动，降血压，抗高血压和抗痉挛性质的无毒，药学上可接受的酸加成盐及其制备。

6. 发明授权

US4493836A 9-Oxalysergic acid derivatives and uses thereof 失效
标题翻译： 9-氧肉桂酸衍生物及其用途
公开(公告)号：US4493836A
公开(公告)日：1985-01-15
申请号：US493355
申请日：1983-05-10
申请人： Lucien Nedelec , Andre Pierdet , Patrick Fauveau
发明人： Lucien Nedelec , Andre Pierdet , Patrick Fauveau
IPC分类号： A61K31/535 , A61P9/12 , A61P43/00 , C07D209/00 , C07D209/90 , C07D265/00 , C07D498/06 , C07D498/04
CPC分类号： C07D209/90
摘要： Novel derivatives of 9-oxalysergic acid of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aralkyl of 7 to 12 carbon atoms and cycloalkylalkyl of 4 to 7 carbon atoms, R.sub.3 is selected from the group consisting of --CH.sub.2 OH, alkylthiomethyl with 1 to 4 alkyl carbon atoms, --CH.sub.2 CN, --COOH, --COOAlk and ##STR2## Alk is alkyl of 1 to 5 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.5 is alkyl of 1 to 5 carbon atoms or R.sub.4 and R.sub.5 together with the nitrogen form a saturated heterocycle optionally containing another heteroatom and their non-toxic, pharmaceutically acceptable acid addition salts having essentially dopaminergic agonist activity, inhibiting activity of prolactin secretion, serotoninergic activity and antihypertensive activity and their preparation.
摘要翻译：其中R选自氢和1至4个碳原子的烷基，其中R选自氢，氯和溴，R2选自下列化学式的9-氧代戊酸的新型衍生物：其中R选自氢，由氢，1-4个碳原子的烷基，7-12个碳原子的芳烷基和4-7个碳原子的环烷基烷基组成的组中，R3选自-CH2OH，具有1-4个烷基碳原子的烷硫基甲基，-CH 2 CN，-COOH，-COOAlk和Alk是1至5个碳原子的烷基，R 4选自氢和1至5个碳原子的烷基，R 5是1至5个碳原子的烷基或R 4和R 5与氮一起形成任选地含有另外的杂原子的饱和杂环及其无毒的药学上可接受的酸加成盐，其具有基本上多巴胺能激动剂活性，抑制催乳素分泌的活性，血清素能活性和抗高血压随行活动及其准备。

7. 发明授权

US4831043A Dopaminergic benzimidazol-2-ones 失效
标题翻译：多巴胺能苯并咪唑-2-酮
公开(公告)号：US4831043A
公开(公告)日：1989-05-16
申请号：US155303
申请日：1988-02-12
申请人： Patrick Fauveau , Lucien Nedelec , Constantin Agouridas , Gilles Hamon
发明人： Patrick Fauveau , Lucien Nedelec , Constantin Agouridas , Gilles Hamon
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/451 , A61P1/04 , A61P1/08 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D211/26 , C07D401/04
CPC分类号： C07D401/04 , C07D211/26
摘要： Novel benzimidazol-2-ones of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, alkenyl and alkynyl of 3 to 5 carbon atoms with the multiple bond not between the carbons .alpha.- and .beta.- to the nitrogen and aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, --OH, alkoxy of 1 to 5 carbon atoms, phenoxy and phenylalkoxy of 7 to 9 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic, antiulcerous, and antihypertensive and vasodilatatory activity.
摘要翻译：式Ⅰ的新型苯并咪唑-2-酮其中R选自氢，1至5个碳原子的烷基，4至7个碳原子的环烷基烷基，3至5个碳原子的链烯基和炔基，选择不是碳原子的碳原子和碳原子之间的碳原子数为7〜12个碳原子的碳原子和碳原子数为1〜5的烷基和烷氧基中的至少一个成员所取代的碳原子和R1之间的多重键，由氢，-OH，1至5个碳原子的烷氧基，7至9个碳原子的苯氧基和苯基烷氧基组成的组，以及它们具有多巴胺能，抗溃疡和抗高血压和血管扩张活性的无毒的药学上可接受的酸加成盐。

8. 发明授权

US4736034A Novel intermediates for the preparation of 7-hydroxy-indoles 失效
标题翻译：用于制备7-羟基 - 吲哚的新型中间体
公开(公告)号：US4736034A
公开(公告)日：1988-04-05
申请号：US29086
申请日：1987-03-23
申请人： Lucien Nedelec , Patrick Fauveau , Gilles Hamon , Claude Oberlander
发明人： Lucien Nedelec , Patrick Fauveau , Gilles Hamon , Claude Oberlander
IPC分类号： C07D211/22 , A61K31/4427 , A61K31/445 , A61K31/451 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/12 , A61P25/00 , A61P25/02 , C07D211/26 , C07D211/42 , C07D211/70 , C07D401/04
CPC分类号： C07D401/04 , C07D211/26
摘要： A compound selected from the group consisting of a compound of the formulae ##STR1## wherein R.sub.1 ' is selected from the group consisting of alkoxy of 1 to 5 carbon atoms, phenoxy and phenylalkoxy of 7 to 9 carbon atoms, R' is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and phenyl alkyl of 7 to 12 carbon atoms optionally substituted with one or more members of the group consisting of alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, halogen and alkenyl of 3 to 5 carbon atoms and alkynyl of 3 to 5 carbon atoms with the proviso that the multiple bond is not between the carbons .alpha.- and .beta. to the nitrogen atom and B is a reversible secondary amine blocking group and their haloamines.
摘要翻译：选自下列化合物的化合物：其中R 1'选自1至5个碳原子的烷氧基，苯氧基和7至9个碳原子的苯基烷氧基，R'选自式由1至5个碳原子的烷基，4至7个碳原子的环烷基烷基和7至12个碳原子的苯基烷基任选被1至5个碳原子的烷基中的一个或多个成员所取代，至5个碳原子，3至5个碳原子的卤素和烯基和3至5个碳原子的炔基，条件是多重键不在氮原子的α和β之间，而B是可逆的仲胺封闭组及其卤胺。

9. 发明授权

US4694011A Novel 7-hydroxy-indoles 失效
标题翻译：新型7-羟基 - 吲哚
公开(公告)号：US4694011A
公开(公告)日：1987-09-15
申请号：US838242
申请日：1986-03-10
申请人： Lucien Nedelec , Gilles Hamon , Patrick Fauveau , Claude Oberlander
发明人： Lucien Nedelec , Gilles Hamon , Patrick Fauveau , Claude Oberlander
IPC分类号： C07D211/22 , A61K31/4427 , A61K31/445 , A61K31/451 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/12 , A61P25/00 , A61P25/02 , C07D211/26 , C07D211/42 , C07D211/70 , C07D401/04 , C07D209/34 , A61K31/40
CPC分类号： C07D401/04 , C07D211/26
摘要： Novel 7-hydroxy-indoles of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted by one or more members of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen and alkenyl and alkynyl of 3 to 5 carbon atoms with the multiple bond being other than between the carbons .alpha.- and .beta.- to the nitrogen atom, R.sub.1 is selected from the group consisting of --OH, alkoxy of 1 to 5 carbon atoms, phenoxy and phenylalkoxy of 7 to 9 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable dopaminergic properties with few central effects and a novel process and novel intermediates for their preparation.
摘要翻译：式VII的新型7-羟基 - 吲哚，其中R选自氢，1至5个碳原子的烷基，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，任选被由1至5个碳原子的烷基和烷氧基组成的组中的一个或多个成员，具有3至5个碳原子的卤素和链烯基和炔基，多重键不同于与氮原子之间的α-和β-的碳原子， R1选自-OH，1至5个碳原子的烷氧基，7至9个碳原子的苯氧基和苯基烷氧基及其无毒的药学上可接受的酸加成盐，具有极少的中枢效应的显着的多巴胺能性质，工艺和新型中间体的制备。

10. 发明授权

US5149696A 19.fwdarw.nor.fwdarw.steroids 失效
标题翻译： 19-> NOR-> STEROIDS
公开(公告)号：US5149696A
公开(公告)日：1992-09-22
申请号：US484424
申请日：1990-02-23
申请人： Andre Claussner , Lucien Nedelec , Daniel Philibert , Patrick Van De Velde
发明人： Andre Claussner , Lucien Nedelec , Daniel Philibert , Patrick Van De Velde
IPC分类号： A61K31/56 , A61K31/565 , A61P5/00 , C07J1/00 , C07J41/00 , C07J43/00
CPC分类号： C07J41/0083 , C07J41/0077 , C07J43/003
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and intermediates.
摘要翻译：具有下式的新型19-去甲类固醇：其中A和B环具有选自具有激素性质的组合和其制备和中间体的结构的结构。

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