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。

公开(公告)号：US5290771A

公开(公告)日：1994-03-01

申请号：US875460

申请日：1992-04-29

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 ,  A61K31/58

CPC分类号： C07J41/0083 ,  C07J41/0077 ,  C07J43/003

摘要： The novel compounds of the invention are 19 nor-steroids of the formula: ##STR1## Where A, B, C, D, X, Y, Z, R.sub.17, and R.sup.1 are as defined in the specification, having hormonal properties and their preparation and intermediates.

摘要翻译： 本发明的新化合物是下式的19种类固醇：其中A，B，C，D，X，Y，Z，R 17和R 1如说明书中所定义，具有激素性质及其 制剂和中间体。

公开(公告)号：US5166146A

公开(公告)日：1992-11-24

申请号：US568597

申请日：1990-08-16

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 ,  A61K31/56 ,  C07J41/00 ,  C07J63/00

CPC分类号： C07J41/0083 ,  C07J63/008

摘要： A compound of the formula ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon of 1 to 8 carbon atoms, R.sub.a and R.sub.b are individually hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is hydrogen or optionally substituted alkyl of 1 to 12 carbon atoms, n is an integer from 1 to 6, Z is free carboxy or salified with an alkali metal, alkaline earth metal or NH.sub.4 and X is the remainder of an optionally substituted and optionally unsaturated 5 or 6-member ring and the wavy line indicates the .alpha.- or .beta.-position for R.sub.1 having anti-glucocorticoid activity.

摘要翻译： 式（I）的化合物其中R 1是1至8个碳原子的脂族烃，R a和R b分别是氢或1至4个碳原子的烷基，R 2是氢或任选取代的1至12的烷基 碳原子，n为1至6的整数，Z为游离羧基或用碱金属，碱土金属或NH 4盐化，X为任选取代的和任选不饱和的5或6元环的其余部分，波浪线 表示具有抗糖皮质激素活性的R1的α或β位。

公开(公告)号：US4943566A

公开(公告)日：1990-07-24

申请号：US225305

申请日：1988-07-28

申请人： Lucien Nedelec ,  Francois Nique ,  Daniel Philibert ,  Martine Moguilewsky ,  Marie-Madeleine Bouton

发明人： Lucien Nedelec ,  Francois Nique ,  Daniel Philibert ,  Martine Moguilewsky ,  Marie-Madeleine Bouton

IPC分类号： A61K31/56 ,  A61K31/565 ,  A61K31/58 ,  A61P35/00 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

CPC分类号： C07J21/006 ,  C07J1/0081 ,  C07J31/006 ,  C07J41/0083

摘要： A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom connected to the C ring by a carbon atom, R.sub.2 is methyl or ethyl, the A and B rings being selected from the group consisting of ##STR2## Re is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl and the D ring is selected from the group consisting of ##STR3## one of R.sub.3 and R.sub.4 is selected from the group consisting of hydroxy, protected hydroxy, acyl and alkoxy and the other is an optionally substituted aryl, R.sub.5 is an optionally substituted aryl and their non-toxic, pharmaceutically acceptable salts with acids and bases with the proviso that when the A and B rings are ##STR4## R.sub.1 is ##STR5## R.sub.2 is methyl, R.sub.3 is --OH, R.sub.4 is phenyl having anti proliferative properties.

摘要翻译： 选自下列化合物的化合物：其中R 1是具有1至18个碳原子的有机物，其任选地含有至少一个与碳原子连接在C环上的杂原子，R2是甲基或乙基， A和B环选自 + TR Re选自氢，任选取代的1至6个碳原子的烷基和酰基，D环选自 的R 3和R 4中的一个选自羟基，保护的羟基，酰基和烷氧基，另一个是任选取代的芳基，R 5是任选取代的芳基及其与酸的无毒的药学上可接受的盐 碱基，条件是当A和B环为R 1时，R 2为甲基，R 3为-OH，R 4为具有抗增殖性质的苯基。

公开(公告)号：US4921846A

公开(公告)日：1990-05-01

申请号：US245750

申请日：1988-09-16

申请人： Lucien Nedelec ,  Andre Claussner ,  Daniel Philibert ,  Martine Moguilewsky

发明人： Lucien Nedelec ,  Andre Claussner ,  Daniel Philibert ,  Martine Moguilewsky

IPC分类号： A61K31/58 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00

CPC分类号： C07J41/0083 ,  C07J21/00 ,  C07J21/006 ,  C07J31/006 ,  C07J71/001

摘要： Steroids with a 17-spiro substituent of 3,4 or 6 ring members of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of carbocyclic aryl, heterocyclic aryl and aralkyl, R.sub.2 is a hydrocarbon of 1 to 18 carbon atoms in the .alpha.-or .beta.-position, the wavy line of the spiro ether indicates the oxygen is .alpha.-or .beta.-, X is selected from the group consisting of --CH.dbd.CH--CH.sub.2 --CH.sub.2 -- and --(CH.sub.2).sub.n --, n is 1, 2 or 4, the A and B rings have a structure selected from the group consisting of ##STR2## R' and R" are individually hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.e is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, substituted alkyl of 1 to 6 carbon atoms and acyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiprogestomimetic activity.

摘要翻译： 具有3,4或6个具有式I的环成员的17-螺环取代基的类固醇，其中R 1选自碳环芳基，杂环芳基和芳烷基，R 2是1至18个碳原子的烃， α - 或β-位，螺醚的波浪线表示氧是α-或β-，X选自-CH = CH-CH 2 -CH 2 - 和 - （CH 2）n - （a）和（b）中，A和B环具有选自下列的结构：（a）（b）（c）和 R' R“分别为氢或1至4个碳原子的烷基，Re选自氢，1至6个碳原子的烷基，1至6个碳原子的取代烷基和酰基及其无毒的药学上 可接受的酸加成盐具有显着的抗切割模拟活性。

公开(公告)号：US4900725A

公开(公告)日：1990-02-13

申请号：US138847

申请日：1987-11-25

申请人： Francois Nioue ,  Lucien Nedelec ,  Daniel Philibert ,  Martine Moguilewsky

发明人： Francois Nioue ,  Lucien Nedelec ,  Daniel Philibert ,  Martine Moguilewsky

IPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/575 ,  A61K31/58 ,  A61K31/585 ,  A61P5/38 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07J1/00 ,  C07J9/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00

CPC分类号： C07J43/003 ,  C07J31/006 ,  C07J33/002 ,  C07J41/0077 ,  C07J41/0083 ,  Y10S514/843

摘要： ##STR1## Products having the formula (I) wherein R
1 is an aryl or aralkyl, R
2 is a hydrocarbonated radical (1-18 carbon atoms), the dotted lines indicate an optional bond, the cycles A, B and C represent (II), (III), (IV), (V), (VI); R' and R" are H, alkyl (1-4 carbon atoms). Re is H, alkyl (1-6 carbon atoms), acyl, and their salts, their preparation, their application as medicaments, the pharmaceutical compositions containing them and intermediaries.

摘要翻译： PCT No.PCT / FR87 / 00096 Sec。 371日期1987年11月25日 102（e）日期1987年11月25日PCT 1987年3月26日PCT公布。 公开号WO87 / 05908 （VI）具有式（I）的产物（VI）具有式（I）的产物：（I） 其中R1是芳基或芳烷基，R2是烃基（1-18个碳原子），虚线表示任选的键，循环A，B和C代表（II），（III），（IV），（ V），（VI）; R'和R“是H，（1-4个碳原子）烷基。 Re是H，烷基（1-6个碳原子），酰基及其盐，它们的制备，它们作为药物的应用，含有它们的药物组合物和中间体。

公开(公告)号：US4774242A

公开(公告)日：1988-09-27

申请号：US16074

申请日：1987-02-18

申请人： Lucien Nedelec ,  Claude Rettien ,  Claude Gueniau

发明人： Lucien Nedelec ,  Claude Rettien ,  Claude Gueniau

IPC分类号： A61K31/535 ,  A61P9/00 ,  A61P9/12 ,  A61P25/00 ,  A61P25/28 ,  C07D209/90 ,  C07D498/06

CPC分类号： C07D209/90

摘要： Novel tetrahydrobenz[c,d]indoles of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and cycloalkyl of 3 to 6 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine and their non-toxic, pharmaceutically acceptable acid addition salts having antianoxic, hypotensive, antihypertensive and dopaminergic agonist activity.

摘要翻译： 式中其中R选自氢，1至6个碳原子的烷基和3至6个碳原子的环烷基的新的四氢苯并[c，d]吲哚，其中R 1选自 氢，氯和溴及其无毒，药学上可接受的酸加成盐，其具有抗疟，降血压，抗高血压和多巴胺能激动剂活性。

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。

公开(公告)号：US4585770A

公开(公告)日：1986-04-29

申请号：US541085

申请日：1983-10-12

申请人： Daniel Frechet ,  Lucien Nedelec ,  Guy Plassard ,  Neil L. Brown

发明人： Daniel Frechet ,  Lucien Nedelec ,  Guy Plassard ,  Neil L. Brown

IPC分类号： C07D487/04 ,  A61K31/55 ,  A61P9/08 ,  A61P9/12 ,  C07D487/06 ,  A61K31/645

CPC分类号： C07D487/06

摘要： Novel 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,l-j-k][1]-benzazepin-2-(1H)-one derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally substituted with a hydroxyl, aryl and aryloxy of 6 to 10 carbon atoms, cycloalkyl of 3 to 7 carbon atoms optionally interrupted with a heteroatom optionally substituted with alkyl of 1 to 4 carbon atoms and the wavy lines indicates that the 7-OH and 6-amino have the trans configuration and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anti-hypertensive and hypotensive activity and vasodilatatory activity and their preparation.

摘要翻译： 新颖的6-氨基-7-羟基-4,5,6,7-四氢 - 咪唑并[4,5-ij] [1] - 苯并氮杂-2-（1H） - 酮衍生物，其中R为 选自氢，任选被6至10个碳原子的羟基，芳基和芳氧基取代的1至8个碳原子的烷基，3至7个碳原子的环烷基任选地被任选被1至 4个碳原子和波浪线表示7-OH和6-氨基具有反式构型及其无毒的药学上可接受的酸加成盐具有显着的抗高血压和降血压活性和血管舒张活性及其制备。

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。