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1. 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。

2. 发明授权

US5108996A 19-nor-3-keto steroids 失效
标题翻译： 19-NOR-3-KETO STEROIDS
公开(公告)号：US5108996A
公开(公告)日：1992-04-28
申请号：US497562
申请日：1990-03-21
申请人： Andre Claussner , Jacques Leclaire , Lucien Nedelec , Daniel Philibert
发明人： Andre Claussner , Jacques Leclaire , Lucien Nedelec , Daniel Philibert
IPC分类号： A61K31/58 , A61P3/06 , A61P39/02 , C07J1/00 , C07J43/00
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。

3. 发明授权

US4737505A Analgesic 4-substituted indoles 失效
标题翻译：止痛剂4-取代吲哚
公开(公告)号：US4737505A
公开(公告)日：1988-04-12
申请号：US757515
申请日：1985-07-19
申请人： Jacques Guillaume , Francois Clemence , Lucien Nedelec , Francoise DeLevallee
发明人： Jacques Guillaume , Francois Clemence , Lucien Nedelec , Francoise DeLevallee
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。

4. 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。

5. 发明授权

US4435408A Dopaminergic stimulating and antianoxic 4-substituted 2H-indole-2-ones 失效
标题翻译：多巴胺能刺激和抗氧化4-取代的2H-吲哚-2-酮
公开(公告)号：US4435408A
公开(公告)日：1984-03-06
申请号：US398576
申请日：1982-07-15
申请人： Lucien Nedelec , Jacques Guillaume , Claude Dumont
发明人： Lucien Nedelec , Jacques Guillaume , Claude Dumont
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/445 , A61P25/00 , C07D401/04
CPC分类号： C07D401/04 , Y10S514/878
摘要： Novel 2H-indole-2-ones 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, a and b are both hydrogen or together form a carbon-carbon bond, Z is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, hydroxyalkyl of 2 to 8 carbon atoms, aryloxyalkyl of 7 to 12 carbon atoms, cycloalkylalkyl of 4 to 12 carbon atoms, alkenyl and alkynyl of 3 to 8 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, --OH, --CF.sub.3, --OCF.sub.3, --NO.sub.2 and --NH.sub.2 and their nontoxic, pharmaceutically acceptable acid addition salts having remarkable dopaminergic stimulating and antianoxic properties and their preparation.
摘要翻译：式中，R为选自氢，碳原子数为1〜8的烷基，碳原子数为7〜12的芳烷基的新的2-吲哚-2-酮，a和b均为氢或一起形成碳 - 碳键，Z选自氢，1至8个碳原子的烷基，2至8个碳原子的羟烷基，7至12个碳原子的芳氧基烷基，4至12个碳原子的环烷基烷基，烯基 3至8个碳原子的炔基和7至12个碳原子的芳烷基，任选被至少一个由1-4个碳原子的烷氧基，卤素，1-4个碳原子的烷基，-OH， - CF3，-OCF3，-NO2和-NH2及其无毒的药学上可接受的酸加成盐，具有显着的多巴胺能刺激和抗氧化性质及其制备。

6. 发明授权

US4332808A Dopaminergically stimulating 4-substituted indoles 失效
标题翻译：多巴胺能刺激4-取代吲哚
公开(公告)号：US4332808A
公开(公告)日：1982-06-01
申请号：US221927
申请日：1980-12-31
申请人： Jacques Guillaume , Lucien Nedelec , Claude Dumont , Robert Fournex
发明人： Jacques Guillaume , Lucien Nedelec , Claude Dumont , Robert Fournex
IPC分类号： C07D401/04 , A61K31/44 , A61K31/445 , C07D401/02
CPC分类号： C07D401/04
摘要： Novel indoles 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, X is selected from the group consisting of hydrogen and alkyl of 1 to 18 carbon atoms, Y is selected from the group consisting of hydrogen and halogen, Z is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, hydroxy alkyl of 1 to 8 carbon atoms, aryloxyalkyl of 7 to 12 carbon atoms, arylalkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, --OH, --CF.sub.3, --OCF.sub.3, --NO.sub.2 and NH.sub.2, cycloalkylalkyl of 4 to 12 carbon atoms, alkenyl of 3 to 8 carbon atoms and alkynyl of 3 to 8 carbon atoms, and a and b may each be hydrogen or form a double bond or a is hydrogen and b is selected from the group consisting of --OH and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic stimulating properties optionally accompanied with adrenergic and serotoninergic activity and their preparation and novel intermediates.
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新颖的吲哚，其中R选自氢和1至18的烷基 Y选自氢和卤素，Z选自氢，1至8个碳原子的烷基，1至8个碳原子的羟基烷基，7至12个碳原子的芳氧基烷基，任选被至少一个卤素，1-4个碳原子的烷氧基，1-4个碳原子的烷基，-OH，-CF 3，-OCF 3，-NO 2和NH 2取代的7-12个碳原子的芳基烷基 4至12个碳原子的环烷基烷基，3至8个碳原子的链烯基和3至8个碳原子的炔基，a和b可各自为氢或形成双键，或a为氢，b选自的-OH和1至8个碳原子的烷氧基，并且它们是无毒的，药学上可接受的具有任选伴随肾上腺素能和5-羟色胺能活性的多巴胺能刺激性质的酸加成盐及其制备和新型中间体。

7. 发明授权

US4318910A Indolobenzoxazines 失效
标题翻译：吲哚溴嗪
公开(公告)号：US4318910A
公开(公告)日：1982-03-09
申请号：US246169
申请日：1981-03-23
申请人： Lucien Nedelec , Andre Pierdet , Claude Dumont
发明人： Lucien Nedelec , Andre Pierdet , Claude Dumont
IPC分类号： A61K31/535 , A61P9/12 , A61P25/00 , A61P43/00 , C07D209/90 , C07D498/06 , A01N43/84
CPC分类号： C07D209/90
摘要： Novel indolobenzoxazines of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and optionally substituted aralkyl of 7 to 12 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, optionally substituted alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, alkenyl and alkynyl of 3 to 7 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms and the dotted line between 5 and 5a indicates the optional presence of a double bond and their non-toxic, pharmaceutically acceptable acid addition salts having hypotensive, antihypertensive and dopaminergic agonist properties and a process for their preparation.
摘要翻译：式“IMAGE”I'的新型吲哚并恶嗪其中R选自氢，1至5个碳原子的烷基和任选取代的7至12个碳原子的芳烷基，R 1选自氢，氯和溴，R 2'选自氢，任选取代的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7个碳原子的链烯基和炔基，以及7-12个碳原子的任选取代的芳烷基原子和5和5a之间的虚线表示任选存在双键及其无毒的药学上可接受的具有降压，抗高血压和多巴胺能激动剂性质的酸加成盐及其制备方法。

8. 发明授权

US4046901A Phenylpiperidines 失效
标题翻译：苯基哌啶
公开(公告)号：US4046901A
公开(公告)日：1977-09-06
申请号：US686076
申请日：1976-05-13
申请人： Lucien Nedelec , Jacques Guillaume , Claude Dumont
发明人： Lucien Nedelec , Jacques Guillaume , Claude Dumont
IPC分类号： C07D211/22 , C07D211/42 , C07D211/72 , C07F3/02 , A61K31/445
CPC分类号： C07F3/02 , C07D211/22 , C07D211/42 , C07D211/72
摘要： Novel compounds selected from the group consisting of phenylpiperidines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen and an acyl of aliphatic carboxylic acid of 2 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts possessing dopaminergic properties and some of which possess hypotensive properties and their preparation.
摘要翻译：选自式I的苯基哌啶的新型化合物，其中X选自氢和2至6个碳原子的脂族羧酸的酰基及其无毒的药学上可接受的酸加成盐具有多巴胺能力，其中一些具有降血压特性及其制备。

9. 发明授权

US5707982A 19-nor-steroids 失效
标题翻译： 19-类固醇
公开(公告)号：US5707982A
公开(公告)日：1998-01-13
申请号：US68735
申请日：1993-05-28
申请人： Andre Claussner , Daniel Philibert , Lucien Nedelec , Patrick Van De Velde , Francois Nique , Jean-Georges Teutsch
发明人： Andre Claussner , Daniel Philibert , Lucien Nedelec , Patrick Van De Velde , Francois Nique , Jean-Georges Teutsch
IPC分类号： C07J41/00 , C07J43/00 , C07J63/00 , C07J1/00 , A61K31/565 , A61K31/58
CPC分类号： C07J41/0077 , C07J41/0083 , C07J43/003 , C07J63/008
摘要： A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##
摘要翻译：具有选自由下列组成的组的19-去甲甾醇类型：其中A和B环具有选自下组的结构：

10. 发明授权

US5276023A 19-nor-steroid esters 失效
标题翻译： 19-类固醇酯
公开(公告)号：US5276023A
公开(公告)日：1994-01-04
申请号：US876181
申请日：1992-04-30
申请人： Martine Moguilewsky , Lucien Nedelec , Francois Nique , Daniel Philibert
发明人： Martine Moguilewsky , Lucien Nedelec , Francois Nique , Daniel Philibert
IPC分类号： C07J1/00 , C07J31/00 , C07J41/00 , A61K31/56 , A61K31/58 , C07J17/00
CPC分类号： C07J41/0083 , C07J1/0096 , C07J31/006
摘要： A compound of the formula ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon of 1 to 8 carbon atoms, R.sub.2 and R.sub.3 are individually hydrogen or alkyl of 1 to 4 carbon atoms, G is a hydrocarbon of 1 to 18 carbon atoms optionally containing at least one heteroatom and linked to the steroid nucleus by a carbon atom, X is X.sub.A or X.sub.B, X.sub.A is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, aralkyl of 7 to 15 carbon atoms, acyl of an organic carboxylic acid of 1 to 8 carbon atoms and Y is -B-O--CO--A-Z, B is a saturated or unsaturated, linear or branched alkylene of 1 to 8 carbon atoms, A is a saturated or unsaturated, linear or branched alkylene of 1 to 6 carbon atoms and optionally interrupted or ended by a bivalent aromatic or is a bivalent aromatic and Z is --COOH or --SO.sub.3 H which may be salified with an alkali metal, alkaline earth metal, an organic amine or --NH.sub.4 or X.sub.B is --COAZ, A and Z are defined as above and Y is selected from the group consisting of --C.tbd.C--R.sub.4, --CH.dbd.CH--R.sub.4 and --CH.sub.2 --CH.sub.2 --R.sub.4, R.sub.4 is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 6 carbon atoms, trialkylsilyl having 3 to 12 carbon atoms and phenyl, the alkyl and phenyl being optionally substituted and the 13-wavy line indicates that R.sub.1 can be in the .alpha.- or .beta.-position having antiprogestomimetic and antiglucocorticoid properties among others.
摘要翻译：式Ⅰ化合物，其中R 1是1至8个碳原子的脂族烃，R 2和R 3分别是氢或1至4个碳原子的烷基，G是1至18个碳原子的烃，任选地含有至少一个杂原子并通过碳原子与类固醇核连接，X是XA或XB，XA选自氢，1至8个碳原子的烷基，7至15个碳原子的芳烷基，有机酸的酰基 1至8个碳原子的羧酸，Y是-BO-CO-AZ，B是1至8个碳原子的饱和或不饱和的直链或支链亚烷基，A是1至8个碳原子的饱和或不饱和的直链或支链亚烷基 6个碳原子，并且任选地被二价芳族中间或结束，或者是二价芳族，Z是-COOH或-SO 3 H，其可以用碱金属，碱土金属，有机胺或-NH 4或XB盐化为-COAZ， A和Z定义如上，Y选自-C 3OND C-R 4，-CH = CH-R 4和-CH 2 -CH 2 -R 4，R 4选自氢，卤素，1至6个碳原子的烷基，具有3至12个碳原子的三烷基甲硅烷基和苯基，所述烷基和苯基任选被取代， 13波浪线表示R1可以是具有止汗模拟和抗糖皮质激素特性的α-或β-位。

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