公开(公告)号：US4218375A

公开(公告)日：1980-08-19

申请号：US701152

申请日：1976-06-30

申请人： Lucien Nedelec ,  Jacques Guillaume ,  Claude Dumont

发明人： Lucien Nedelec ,  Jacques Guillaume ,  Claude Dumont

IPC分类号： A61K31/55 ,  A61P25/20 ,  A61P43/00 ,  C07D495/04 ,  C07D513/02

CPC分类号： C07D495/04

摘要： Novel 4H-thieno-[3,2-b][1]-benzazepines of the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and halogen, X and Y are hydrogen or together form a carbon-carbon double bond, p is 2 or 3 and A is selected from the group consisting of alkyl of 1 to 5 carbon atoms and hydroxyalkyl of 2 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having neuro sedative and antihistaminic properties and their preparation and intermediates therefor.

摘要翻译： 式其中R，R 1和R 2分别选自氢和卤素的新的4H-噻吩并[3,2-b] [1] - 苯并氮杂，其中X和Y是氢或一起形成 碳 - 碳双键，p为2或3，A选自1至5个碳原子的烷基和2至5个碳原子的羟烷基及其无毒的药学上可接受的具有神经镇静剂的酸加成盐 和抗组胺性质及其制备及其中间体。

公开(公告)号：US4154852A

公开(公告)日：1979-05-15

申请号：US835171

申请日：1977-09-20

申请人： Lucien Nedelec ,  Daniel Frechet ,  Claude Dumont

发明人： Lucien Nedelec ,  Daniel Frechet ,  Claude Dumont

IPC分类号： A61K31/13 ,  A61K31/04 ,  A61K31/135 ,  A61P25/24 ,  A61P25/26 ,  C07C57/145 ,  C07C57/15 ,  C07C67/00 ,  C07C209/00 ,  C07C209/36 ,  C07C209/60 ,  C07C211/42 ,  C07C211/57 ,  C07C213/00 ,  C07C217/74 ,  C07C225/00 ,  A01N9/20 ,  C07C87/64 ,  C07C91/28 ,  C07C93/14

CPC分类号： C07C57/15 ,  C07C57/145

摘要： Novel 7-aminobenzocycloheptenes of the formula ##STR1## wherein X is selected from the group consisting of --NO.sub.2, --NH.sub.2, CH.sub.3 O-- and --OH, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.2 is alkyl of 1 to 5 carbon atoms and R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a saturated heterocycle of 4 to 6 ring carbon atoms optionally containing a second heteroatom in the ring and optionally substituted with an alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts in optically active or racemic mixture form having antidepressant activity and a process for their preparation.

摘要翻译： 新颖的式I的7-氨基苯并环庚烯，其中X选自-NO 2，-NH 2，CH 3 O-和-OH，R 1选自氢和1至5个碳原子的烷基， R 2是1至5个碳原子的烷基，R 1和R 2与它们所连接的氮原子一起形成4至6个环碳原子的饱和杂环，任选地在该环中含有第二个杂原子且任选地被1个 至5个碳原子及其无毒的药学上可接受的酸加成盐，其具有抗抑郁活性的旋光或外消旋混合物形式及其制备方法。

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：

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。

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。

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。

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。

公开(公告)号：US4313944A

公开(公告)日：1982-02-02

申请号：US237062

申请日：1981-02-23

申请人： Lucien Nedelec ,  Daniel Frechet ,  Claude Dumont

发明人： Lucien Nedelec ,  Daniel Frechet ,  Claude Dumont

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/535 ,  A61P1/04 ,  A61P9/12 ,  A61P25/00 ,  C07D209/94 ,  C07D498/06 ,  C07D498/04

CPC分类号： C07D209/94

摘要： Novel compounds selected from the group consisting of optically active isomers and racemic mixtures of cycloheptindoles 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 and R.sub.2 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 7 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic agonist and antianoxic properties and a process for their preparation and novel intermediates.

摘要翻译： 新型化合物，其选自光学活性异构体和式Ⅺ的环庚啶的外消旋混合物，其中R选自氢，1至5个碳原子的烷基和7至12个碳的任选取代的芳烷基 原子，R 1选自氢，氯和溴，R 2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7个碳的链烯基和炔基 原子和任选取代的7-12个碳原子的芳烷基及其无毒的药学上可接受的具有多巴胺能激动剂和抗氧化性质的酸加成盐及其制备方法和新型中间体。

公开(公告)号：US4296126A

公开(公告)日：1981-10-20

申请号：US13831

申请日：1979-02-22

申请人： Lucien Nedelec ,  Daniel Frechet ,  Claude Dumont

发明人： Lucien Nedelec ,  Daniel Frechet ,  Claude Dumont

IPC分类号： A61K31/135 ,  A61K31/16 ,  A61K31/165 ,  A61P3/04 ,  C07C67/00 ,  C07C213/00 ,  C07C217/48 ,  C07C233/16 ,  C07C233/25 ,  A01N37/30 ,  C07C93/02

CPC分类号： A61K31/135 ,  C07C233/16

摘要： Novel benzene-propanamines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, chlorine, fluorine and bromine, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.2 is alkyl of 1 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, chlorine, bromine, --CF.sub.3, methyl and methoxy when R.sub.4 is nitro and R.sub.3 is selected from the group consisting of amino and acetamido when R.sub.4 is hydrogen and their non-toxic, pharmaceutically acceptable acid addition salts having anorexigenic activity and inhibit serotonine uptake in vivo and in vitro and their preparation.

摘要翻译： 具有式“IMAGE”I'的新型苯丙胺，其中X选自氢，氯，氟和溴，R 1选自氢和1至5个碳原子的烷基，R 2是烷基 当R 4为硝基时，R 3选自氢，氯，溴，-CF 3，甲基和甲氧基，当R 4为氢时，R 3选自氨基和乙酰氨基， 具有厌食活性的药学上可接受的酸加成盐，并且在体内和体外抑制血清素摄取及其制备。

公开(公告)号：US4232031A

公开(公告)日：1980-11-04

申请号：US100909

申请日：1979-12-06

申请人： Claude Dumont ,  Jacques Guillaume ,  Lucien Nedelec

发明人： Claude Dumont ,  Jacques Guillaume ,  Lucien Nedelec

IPC分类号： C07D401/04 ,  A61K20060101 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/475 ,  A61P1/08 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  B01J23/04 ,  C07D20060101 ,  C07D209/04 ,  C07D211/68 ,  C07D211/70 ,  C07D401/02

CPC分类号： C07D401/04

摘要： A novel process for the preparation of piperidylindoles of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms and X is selected from the group consisting of hydrogen, nitro, fluorine, bromine, chlorine and alkoxy of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts thereof by reacting an indole of the formula ##STR2## with 4-piperidone hydrochloride in an alkaline medium to obtain the compound of formula I which is optionally salified and the novel product, 5-nitro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole and its non-toxic, pharmaceutically acceptable acid addition salts.

摘要翻译： 一种制备式Ia的哌啶子基吲哚的新方法，其中R选自氢和1至3个碳原子的烷基，X选自氢，硝基，氟，溴， 氯和具有1至3个碳原子的烷氧基以及它们的无毒的药学上可接受的酸加成盐，其通过使式II的吲哚与4-哌啶酮盐酸盐在碱性介质中反应，得到式I化合物，其为 任选地盐化，并且新产物5-硝基-3-（1,2,3,6-四氢吡啶-4-基）-1H-吲哚及其无毒的药学上可接受的酸加成盐。