公开(公告)号：US5081113A

公开(公告)日：1992-01-14

申请号：US497564

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 ,  A61P29/00 ,  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.6 is selected from the group consisting of halogen, --CH.sub.3, fluorine and chlorine, R.sub.9 and R.sub.11 together form a second bond at 9(11) or R.sub.9 is hydrogen or fluorine and R.sub.11 is selected from the group consisnting of hydrogen, --OH and .dbd.O, the dotted lines in rings A and B indicate a possible additonal bond at 1(2) and 6(7), R.sub.17 is hydrogen or acyl or an organic carboxylic acid of 1 to 18 carbon atoms, R'.sub.17 is ##STR2## 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, P is pyrimidinyl or pyridyl optionally substituted with one or two individual members of the group consisting of --NH.sub.2, alkylamino, dialkylamino and aminated 5- or 6- membered heterocycles optionally substituted with alkyl of 1 to 3 carbon atoms and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and anti-oxidation activity.

摘要翻译： 选自下列化合物的化合物其中R 6选自卤素，-CH 3，氟和氯，R 9和R 11一起在9（11）或R9上形成第二个键 是氢或氟并且R 11选自氢，-OH和= O的基团，环A和B中的虚线表示在1（2）和6（7）处可能的附加键，R 17是氢或酰基 或具有1至18个碳原子的有机羧酸，R'17是选自单键，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，P 是任选被一个或两个独立的由-NH 2，烷基氨基，二烷基氨基和胺化的5-或6-元杂环取代的嘧啶基或吡啶基，任选被1至3个碳原子的烷基取代，其无毒的药学上可接受的 具有抗炎和抗氧化的酸加成盐 dation活动。

公开(公告)号：US5006518A

公开(公告)日：1991-04-09

申请号：US292475

申请日：1988-12-30

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： A61K31/57 ,  A61K31/575 ,  A61P3/04 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P25/20 ,  A61P43/00 ,  C07J41/00

CPC分类号： C07J41/0033 ,  C07J41/0083

摘要： Novel 19-nor steroids of the formula ##STR1## wherein R' is selected from the group consisting of propyl, propenyl, iodoethenyl, iodoethynyl or --C.tbd.C--CH.sub.2 --Hal.sub.1, Hal.sub.1 is selected from the group consisting of fluorine, chlorine and bromine and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiglucocorticoid and antiprogestomimetic activity.

摘要翻译： 新颖的19-或类固醇，其中R'选自丙基，丙烯基，碘代乙烯基，碘乙炔基或-C 3位C-CH 2 -H Hal 1，Hal1选自氟，氯 和溴及其无毒的药学上可接受的酸加成盐，其具有显着的抗糖皮质激素和止汗模拟活性。

公开(公告)号：US4987128A

公开(公告)日：1991-01-22

申请号：US18199

申请日：1987-02-24

申请人： Lucien Nedelec ,  Francois Nique ,  Anne-Marie Moura

发明人： Lucien Nedelec ,  Francois Nique ,  Anne-Marie Moura

IPC分类号： A61K31/585 ,  A61P9/00 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J33/00 ,  C07J43/00 ,  C07J53/00

CPC分类号： C07J21/006 ,  C07J1/007 ,  C07J21/003 ,  C07J33/005 ,  C07J43/006

摘要： Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.2 is methyl or ethyl, X and Y taken together form a member selected from the group consisting of ##STR2## Alk is alkyl of 1 to 8 carbon atoms or X is hydroxy and Y is ##STR3## or X is optionally acylated or etherified hydroxy and Y is selected from the group consisting of --CH.sub.2 --CH.sub.2 --CH.sub.2 --OH, hydrogen, R.sub.4, and --CH.sub.2 --CH.sub.2 --COOM, M is selected from the group consisting of hydrogen, --NH.sub.4 and alkali metal and R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, the dotted lines indicate the optional presence of a second carbon-carbon bond when R.sub.6 and R.sub.7 and the carbon to which they are attached do not form cyclopropyl and the wavy lines indicate that R.sub.6 and R.sub.7 may be in the .alpha. or .beta. position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen, R.sub.2 is methyl, X is optionally acylated or etherified hydroxy, Y is hydrogen or R.sub.4 and the dotted lines are not a second carbon-carbon bond having aldosterone antagonistic activity and increased hydrosodic diuresis with organic potassium conservation with little secondary hormone effects.

摘要翻译： 新颖的式10的β-炔基 - 类固醇，其中R选自氢，任选取代的烷基和1至8个碳原子的烷氧基，任选取代的碳原子数2〜8的烯基和炔基，任选地 取代的芳基和芳烷基，任意酯化的羧基，二烷基氨基与1至6个碳原子的烷基，卤素和1至7个烷基碳原子的三烷基甲硅烷基，R 6和R 7与它们所连接的碳原子一起形成环丙基或R6是氢 并且R 7是R 1，R 1选自氢，任选取代的1至6个碳原子的烷基，任选取代的烯基和2至6个碳原子的炔基和乙酰硫基，R 2是甲基或乙基，X和Y一起 形成选自由以下组成的组中的一个成员：Alk为1至8个碳原子的烷基或X为羟基，Y为X或X任选被酰化或醚化羟基，Y选自gro 其由-CH 2 -CH 2 -CH 2 -OH，氢，R 4和-CH 2 -CH 2 -COOM组成，M选自氢，-NH 4和碱金属，R 4选自由以下组成的组： 1至6个碳原子和2至6个碳原子的烯基和炔基，虚线表示当R6和R7以及它们所连接的碳不形成环丙基时，任选存在第二碳 - 碳键，波浪线 表示R6和R7可以在α或β位置，条件是当R6和R7是氢时，R不是氢，R2是甲基，X是任选被酰化或醚化羟基，Y是氢或R4，虚线是 不是具有醛固酮拮抗活性的第二个碳 - 碳键和具有少量次生激素效应的有机钾保护的增加的水溶性利尿。

公开(公告)号：US4874754A

公开(公告)日：1989-10-17

申请号：US157417

申请日：1988-02-17

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

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

IPC分类号： A61K31/58 ,  C07J1/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00

CPC分类号： C07J21/00 ,  C07J1/007 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0044 ,  C07J41/0072 ,  C07J51/00

摘要： Novel 19-nor-steroids of the formula ##STR1## wherein the A ring is either ##STR2## Re is selected from the group consisting of hydrogen, acyl and optionally substituted alkyl of 1 to 6 carbon atoms, R is methyl or ethyl, R.sub.1 is selected from the group consisting of hydroxyl, protected hydroxyl, acyloxy and alkoxy, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, acyl, aralkyl of 7 to 15 carbon atoms, the substituents other than hydrogen being optionally substituted or R.sub.1 and R.sub.2 together form a group selected from the group consisting of ##STR3## A.sub.r is an optionally substituted 5- or 6-membered aryl and their salts with non-toxic, pharmaceutically acceptable bases and acids having antiproliferative, anti-estrogenic and/or estrogenic properties.

摘要翻译： 式（I）的新型19-去甲甾类化合物其中A环为或者选自氢，酰基和任选取代的1至6个碳原子的烷基，R是甲基或 乙基，R 1选自羟基，保护的羟基，酰氧基和烷氧基，R2选自氢，1至8个碳原子的烷基，2至8个碳原子的烯基和炔基，酰基，芳烷基 7至15个碳原子，除氢之外的取代基任选被取代，或者R 1和R 2一起形成选自下列的基团：Ar是任选取代的5或6元芳基， 有毒的，药学上可接受的碱和具有抗增殖，抗雌激素和/或雌激素性质的酸。

公开(公告)号：US4831043A

公开(公告)日：1989-05-16

申请号：US155303

申请日：1988-02-12

申请人： Patrick Fauveau ,  Lucien Nedelec ,  Constantin Agouridas ,  Gilles Hamon

发明人： Patrick Fauveau ,  Lucien Nedelec ,  Constantin Agouridas ,  Gilles Hamon

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。

公开(公告)号：US4736034A

公开(公告)日：1988-04-05

申请号：US29086

申请日：1987-03-23

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： 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。

公开(公告)号：US4694011A

公开(公告)日：1987-09-15

申请号：US838242

申请日：1986-03-10

申请人： Lucien Nedelec ,  Gilles Hamon ,  Patrick Fauveau ,  Claude Oberlander

发明人： Lucien Nedelec ,  Gilles Hamon ,  Patrick Fauveau ,  Claude Oberlander

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。

公开(公告)号：US4335135A

公开(公告)日：1982-06-15

申请号：US236610

申请日：1981-02-23

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

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

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/535 ,  A61P1/04 ,  A61P9/12 ,  A61P25/00 ,  C07D209/94 ,  C07D498/06 ,  C07D209/80

CPC分类号： C07D209/94

摘要： Novel trans cyclohept[c,d]indolols 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 and R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having hypotensive and antihypertensive activity and a process for their preparation.

摘要翻译： 新型的反式环庚烯[c，d]吲哚洛尔式其中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 由氢，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个碳原子的任选取代的芳烷基组成的组，以及它们具有低血压和抗高血压活性的无毒的药学上可接受的酸加成盐 他们的准备。

公开(公告)号：US4333939A

公开(公告)日：1982-06-08

申请号：US163967

申请日：1980-06-30

申请人： Jacques Guillaume ,  Lucien Nedelec ,  Claude Dumont

发明人： Jacques Guillaume ,  Lucien Nedelec ,  Claude Dumont

IPC分类号： C07D209/08 ,  A61K31/44 ,  C07D401/04

CPC分类号： C07D209/08 ,  Y10S514/872

摘要： Novel tetrahydro-pyridinyl-indoles of the formula ##STR1## wherein R is selected from the group consisting of amino, trifluoromethyl and methylthio, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressive, antiparkinson and antiemetic activity and their preparation.

摘要翻译： 式VI的新的四氢 - 吡啶基 - 吲哚，其中R选自氨基，三氟甲基和甲硫基，R 1和R 2分别选自氢和1至3个碳原子的烷基，它们的 无毒，药学上可接受的具有抗抑郁，抗帕金森和止吐活性的酸加成盐及其制备。

公开(公告)号：US4324790A

公开(公告)日：1982-04-13

申请号：US163966

申请日：1980-06-30

申请人： Jacques Guillaume ,  Lucien Nedelec ,  Claude Dumont

发明人： Jacques Guillaume ,  Lucien Nedelec ,  Claude Dumont

IPC分类号： C07D401/04 ,  A61K31/404 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/445 ,  A61P1/08 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D209/08 ,  A61K31/44

CPC分类号： C07D209/08

摘要： Novel tetranydro-pyridinyl-indoles of the formula ##STR1## wherein X is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 5 carbon atoms, alkynyl of 3 to 5 carbon atoms, cycloalkyl of 5 to 6 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, aralkyl of 7 to 12 carbon atoms, hydroxyalkyl of 2 to 5 carbon atoms and phenoxyalkyl of 1 to 5 alkyl carbon atoms, R is selected from the group consisting of hydrogen, halogen, alkoxy of 1 to 3 carbon atoms, nitro, amino, trifluoromethyl and methylthio, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms with the proviso that if R is hydrogen, halogen or alkoxy of 1 to 3 carbon atoms, X must be hydroxyalkyl or phenoxyalkyl and their non-toxic, pharmaceutically acceptable acid addition salts having neuroleptic, antipsychotic and antiemetic activity and their preparation.

摘要翻译： 新颖的式IV的四氢吡啶基 - 吲哚，其中X选自1至6个碳原子的烷基，2至5个碳原子的链烯基，3至5个碳原子的炔基，5至5的环烷基 6个碳原子，4至7个碳原子的环烷基烷基，7至12个碳原子的芳烷基，2至5个碳原子的羟基烷基和1至5个烷基碳原子的苯氧基烷基，R选自氢，卤素，烷氧基 1至3个碳原子的硝基，氨基，三氟甲基和甲硫基，R 1和R 2分别选自氢和1至3个碳原子的烷基，条件是如果R是氢，卤素或1至 3个碳原子，X必须是羟基烷基或苯氧基烷基及其无毒，药学上可接受的具有神经安定药，抗精神病药和止吐药活性的酸加成盐及其制备。