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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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3.发明授权Use of pyrazolobenzoxazines in method of treating cerebral senescence and cerebral hypoxin 失效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
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。
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公开(公告)号：US4831043A
公开(公告)日：1989-05-16
申请号：US155303
申请日：1988-02-12
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。
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公开(公告)号：US4503053A
公开(公告)日：1985-03-05
申请号：US532740
申请日：1983-09-15
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。
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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。
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公开(公告)号：US5149696A
公开(公告)日：1992-09-22
申请号：US484424
申请日：1990-02-23
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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公开(公告)号：US5108996A
公开(公告)日：1992-04-28
申请号：US497562
申请日：1990-03-21
CPC分类号： C07J1/0048 , C07J1/0044 , C07J43/003
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.2 and R'.sub.2 are individually hydrogen or methyl, R.sub.11 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom adjacent to the 11-carbon atom being a carbon, the wavy lines at the 13 and 17-positions indicate that when the 13-methyl is .alpha., R'.sub.17 group is .beta. and R.sub.17 is .alpha. and when the 13-methyl is .sub..beta., R.sub.17 is .sub..beta. and R'.sub.17 is .alpha., R.sub.17 is --OH or acyloxy of 1 to 18 carbon atoms and R'.sub.17 is ##STR2## is hydrogen or --OH or acyloxy of 1 to 18 carbon atoms, Z is selected from the group consisting of a single bond, alkylene of 1 to 5 carbon atoms and alkenylene and alkynylene of 2 to 5 carbon atoms and P is selected from the group consisting of pyrimidinyl and pyridyl optionally substituted with 1 or 2 individual members of the group consisting of amino, alkylamino and dialkylamino of 1 to 4 alkyl carbon atoms and (B aminated 5- or 6-membered heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms) and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and anti-oxidant activity.
摘要翻译： 选自下式的化合物的化合物其中R 2和R 12独立地是氢或甲基，R 11是具有1至18个碳原子的有机基团，任选地含有至少一个与原子相邻的原子的杂原子 11碳原子是碳，13位和17位的波浪线表示当13-甲基是α时，R'17基团是β，R17是α，当13-甲基是β时，R17是 β和R'17是α，R17是-OH或1至18个碳原子的酰氧基，R'17是氢或-OH或含1至18个碳原子的酰氧基，Z选自 由单键键合，1至5个碳原子的亚烷基和2至5个碳原子的亚烯基和亚炔基组成的组，P选自嘧啶基和吡啶基，任选被1或2个独立成员取代的氨基 ，烷基氨基和1至4个烷基碳原子的二烷基氨基和（B胺化的5或6元环 任选被1至3个碳原子的烷基取代的杂环）及其无毒的药学上可接受的具有抗炎和抗氧化活性的酸加成盐。
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公开(公告)号：US4737505A
公开(公告)日：1988-04-12
申请号：US757515
申请日：1985-07-19
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/445 , A61P25/04 , C07D401/04
CPC分类号： C07D401/04
摘要： Novel indole of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 12 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, cyanoalkyl of 3 to 8 carbon atoms, hydroxyalkyl of 2 to 8 carbon atoms, --(CH.sub.2).sub.n --O--B, ##STR2## aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, CF.sub.3 --, CF.sub.3 O--, --NH.sub.2 and --NO.sub.2 and cycloalkyl alkyl of 4 to 12 carbon atoms, n is one integer from 2 to 8, B is selected from the group consisting of aryl and heteroaryl, both optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, hydroxyalkyl of 1 to 5 carbon atoms, nitro, amino, CF.sub.3 --, alkenyl and alkenyloxy of 2 to 5 carbon atoms and alkynyl and alkynyloxy of 2 to 5 carbon atoms, a and b are both hydrogen or a is hydrogen and b is --OH or alkoxy of 1 to 8 carbon atoms or a and b together form a carbon-carbon bond and the 2-oxo with dotted lines indicates its possible presence with the double bond in the indole ring missing and its non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity of the morphine type.
摘要翻译： 其中R选自氢，1至8个碳原子的烷基和7至12个碳原子的芳烷基的式VI的新型吲哚，Z选自氢，1至 具有2至8个碳原子的烯基，3至8个碳原子的氰基烷基，2至8个碳原子的羟烷基， - （CH 2）n OB，7-12个碳原子的芳基，其任选被至少一个 由1至5个碳原子的烷基和烷氧基组成的组，卤素，-OH，CF 3 - ，CF 3 O-，-NH 2和-NO 2以及4至12个碳原子的环烷基烷基，n是2至8的一个整数 B选自芳基和杂芳基，两者任选被至少一个由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，-OH，1-5个碳原子的羟基烷基，硝基 ，2至5个碳原子的氨基，CF 3 - ，链烯基和烯氧基以及2至5个碳原子的炔基和炔氧基，a和ba 氢或a是氢并且b是-OH或1-8个碳原子的烷氧基或a和b一起形成碳 - 碳键，并且具有虚线的2-氧代表示其在吲哚中可能存在双键 戒指及其无毒，药学上可接受的具有吗啡类止痛活性的酸加成盐。
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公开(公告)号：US4699907A
公开(公告)日：1987-10-13
申请号：US941037
申请日：1986-12-12
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。
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