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1.发明授权Substituted derivatives of 20,21-dinoreburnamenine, their use as medicaments and the pharmaceutical compositions containing them 失效其作为药物和含有它们的药物组合物的二十二碳三烯酸的取代衍生物
公开(公告)号：US5093337A
公开(公告)日：1992-03-03
申请号：US391511
申请日：1989-07-18
IPC分类号： C07D461/00 , A61K20060101 , A61K31/435 , A61K31/445 , A61K31/475 , A61K31/495 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/24 , A61P25/26 , C07D20060101
CPC分类号： C07D461/00
摘要： The invention concerns compounds of formula (I); ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, identical or different, stand for hydrogen, halogen, alkyl or alkoxy (C.sub.1-5), hydroxy, trifluoromethyl, nitro, amino, alkylamino, dialkylamino, acylamino, R.sub.1, R.sub.2 and R.sub.3 being unable to stand for hydrogen simultaneously and in which (a) stands for (b), (c), or (d), all possible isomeric forms of said products of formula (I) being racemic or optically active, as well as their additional salts with acids, their preparation and the new intermediate products obtained, their application as drugs in particular nootropes, antidepressants, neuronal protectors, anti-anoxics, anti-ischemics, and the compositions containing them.
摘要翻译： PCT No.PCT / FR88 / 00562 Sec。 371日期：1989年7月18日 102（e）日期1989年7月18日PCT提交1988年11月16日PCT公布。 出版物WO89 / 04830 日期：1989年6月1日。本发明涉及式（I）化合物。 其中R1，R2和R3相同或不同，代表氢，卤素，烷基或烷氧基（C1-5），羟基，三氟甲基，硝基，氨基，烷基氨基，二烷基氨基，酰基氨基， R1，R2和R3不能同时代表氢，其中（a）代表（b），（c）或（d），所有式（I）产物的所有可能的异构形式是外消旋或光学活性的 以及它们与酸的附加盐，它们的制备和获得的新的中间产物，它们作为药物特别是助推剂，抗抑郁药，神经元保护剂，抗缺氧剂，抗缺血剂以及含有它们的组合物的应用。
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2.发明授权
公开(公告)号：US4904655A
公开(公告)日：1990-02-27
申请号：US302810
申请日：1989-01-26
IPC分类号： C07D209/14 , A61K31/535 , A61P25/04 , A61P25/06 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , C07D209/18 , C07D413/06 , C07D498/14 , C07D498/22
CPC分类号： C07D498/22
摘要： Novel compounds selected from the group consisting of all possible racemic or optically active forms of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 5 carbon atoms, -OH, -CF.sub.3 and -NO.sub.2 and ##STR2## is selected from the group consisting of ##STR3## and their non-toxic, pharmaceutically acceptable acid addition salts having a very good analgesic activity as well as antidepressive, neuronal protective, anti-anoxic, anti-ischemic and no-otropic activities.
摘要翻译： 选自下列化合物的新化合物：所有可能的外消旋或旋光活性形式的下式化合物其中R 1和R 2分别选自氢，烷基和1至5个碳原子的烷基，-OH ，-CF 3和-NO 2和
选自 及其无毒的药学上可接受的具有非常好的镇痛活性的酸加成盐以及抗抑郁，神经元保护，抗缺氧，抗 - 缺血和非嗜性活动。 -
3.发明授权Substituted derivatives of 20,21-dinoreburnamenine, their preparation process and the new intermediates thus obtained, their use as medicaments and the pharmaceutical compositions containing them 失效取代的衍生物20,21-二内啡宁，其制备方法和由此获得的新中间体，它们作为药物的用途和含有它们的药物组合物
公开(公告)号：US5332748A
公开(公告)日：1994-07-26
申请号：US5662
申请日：1993-01-19
IPC分类号： C07D461/00 , A61K20060101 , A61K31/435 , A61K31/445 , A61K31/475 , A61K31/495 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/24 , A61P25/26 , C07D20060101 , A61K31/44
CPC分类号： C07D461/00
摘要： A compound and all possible racemic or optically active isomer forms, selected from the group consisting of compound of the formula ##STR1## wherein the substituents are defined as set forth in the application as filed. Useful for treating cerebral insufficiencies of anoxic or ischemic origin.
摘要翻译： 选自下列化合物的化合物和所有可能的外消旋或旋光异构体形式，其中取代基定义如申请所述。 用于治疗缺氧或缺血起源的脑功能不全。
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4.发明授权Method of treating depression with optically active isomers of 20,21-dinoreburnamenines 失效用20,21-二辛胺盐酸光学活性异构体治疗抑郁症的方法
公开(公告)号：US5034396A
公开(公告)日：1991-07-23
申请号：US271733
申请日：1988-11-15
IPC分类号： A61K31/435 , A61P9/00 , A61P9/10 , A61P25/24 , A61P25/26 , A61P25/28 , C07D461/00
CPC分类号： C07D461/00
摘要： A compound selected from the group consisting of optically active isomers of a racemic compound of the formula ##STR1## wherein the 3-hydrogen and 16-hydrogen are trans and ##STR2## is selected from the group consisting of ##STR3## with the --OH being .alpha. or .beta. and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressant activity and an affinity for alpha.sub.2 adrenergic receptors,
摘要翻译： 选自下列化学式的旋光化合物的旋光异构体的化合物其中3-氢和16-氢是反式的，且＆lt; IMAGE＆gt;选自＆lt; IMAGE＆gt;与 - OH是α或β及其无毒的药学上可接受的酸加成盐，其具有抗抑郁活性和对α2肾上腺素能受体的亲和力，
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公开(公告)号：US5424314A
公开(公告)日：1995-06-13
申请号：US207361
申请日：1994-03-07
IPC分类号： A61K31/435 , A61K31/4375 , A61P9/00 , A61P9/10 , A61P25/24 , A61P25/26 , A61P25/28 , C07D461/00 , A61K31/445
CPC分类号： C07D461/00
摘要： A compound in all racemic or optionally active forms selected from the group consisting of a compound of the formula ##STR1## where the substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-anoxic activity and a novel process and intermediates for their preparation.
摘要翻译： 所有外消旋或任选活性形式的化合物，其选自下列化合物：其中取代基如说明书中所定义，及其无毒的药学上可接受的具有抗缺氧性的酸加成盐 活动和一个新的工艺和中间体的准备。
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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。 -
公开(公告)号：US06534515B2
公开(公告)日：2003-03-18
申请号：US08228300
申请日：1994-04-15
IPC分类号： C07D46100
CPC分类号： C07D461/00
摘要： A compound selected from the group consisting of all possible isomers or racemates of a compound of the formula wherein the various substituents are as defined in the specification and its non-toxic, pharmaceutically acceptable salts with acids or bases having anti-anoxic, anti-ischemic and neuronal protective anti-depressant activities.
摘要翻译： 在各种取代基中，选自所有可能的异构体或所述异构体的化合物的外消旋化合物的化合物如说明书及其无毒的药学上可接受的盐，与具有抗缺氧，抗缺血和 神经元保护性抗抑郁活性。
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公开(公告)号：US4112093A
公开(公告)日：1978-09-05
申请号：US807068
申请日：1977-06-16
申请人： Claude Dumont , Claude Oberlander
发明人： Claude Dumont , Claude Oberlander
IPC分类号： C07D405/12 , A61K31/495 , A61P25/00 , A61P25/26 , C07D20060101 , C07D213/74 , C07D295/12 , C07D317/58 , C07D401/04 , C07D405/14
CPC分类号： C07D405/12
摘要： Novel dopaminerginic compositions comprised of an dopaminergically effective amount of at least one member of the group consisting of N-(3,4-methylenedioxy-benzyl)-N'-(2-pyridyl)-piperazine and its non-toxic, pharmaceutically acceptable acid addition salts and an inert pharmaceutical carrier and to a novel method of treating the symptoms of Parkinson disease.
摘要翻译： 由多巴胺能有效量的由N-（3,4-亚甲二氧基 - 苄基）-N' - （2-吡啶基） - 哌嗪及其无毒的药学上可接受的酸组成的组中的至少一个成员组成的新型多巴胺能组合物 加成盐和惰性药物载体，以及治疗帕金森病症状的新方法。
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公开(公告)号：US4736034A
公开(公告)日：1988-04-05
申请号：US29086
申请日：1987-03-23
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。
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公开(公告)号：US4694011A
公开(公告)日：1987-09-15
申请号：US838242
申请日：1986-03-10
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。
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