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33 条记录 (耗时 0.024 秒)

    19-nor-steroid esters
    1.
    发明授权
    19-nor-steroid esters 失效
    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。

    Amino acid cyclopentanophenonthrene compounds
    2.
    发明授权
    Amino acid cyclopentanophenonthrene compounds 失效
    氨基酸环十二烷基化合物

    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。

    Novel 17-aryl-steroids
    3.
    发明授权
    Novel 17-aryl-steroids 失效
    新型17-芳基类固醇

    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。

    Novel steroids
    7.
    发明授权
    Novel steroids 失效
    新的STEROIDS

    公开(公告)号：US5084450A

    公开(公告)日：1992-01-28

    申请号：US658003

    申请日：1991-02-20

    申请人： Martine Gaillard-Kelly ,  Lucien Nedelec ,  Francois Nique ,  Daniel Philibert

    发明人： Martine Gaillard-Kelly ,  Lucien Nedelec ,  Francois Nique ,  Daniel Philibert

    IPC分类号： A61K31/56 ,  A61P13/02 ,  A61P15/00 ,  A61P19/10 ,  A61P35/00 ,  A61P43/00 ,  C07J1/00 ,  C07J53/00

    CPC分类号： C07J53/001 ,  C07J1/0081

    摘要： Compounds of the formula ##STR1## wherein .dbd.X is .dbd.O or ##STR2## R is hydrogen or acyl of an organic carboxylic acid of 1 to 12 carbon atoms, the wavy lines indicate the .alpha.- or .beta.-position, the dotted line in the 17-position indicates the bond is in the .alpha.-position and the dotted lines in the 9'(10') and 11'(12') positions indicate an optional double bond in the 9'(10') position or two optional double bonds in the 9'(10') and 11'(12') positions having progestomimetic and antiestrogenic activity.

    摘要翻译： 式（I）其中= X为=或R为氢或具有1至12个碳原子的有机羧酸的酰基的化合物，波浪线表示α或β位，虚线 在17位表示键位于α位，9'（10'）和11'（12'）位置中的虚线表示9'（10'）位置中的任选双键或两个 9'（10'）和11'（12'）位置的任选双键具有假激动和抗雌激素活性。

    Novel 19-nor-steroids
    8.
    发明授权
    Novel 19-nor-steroids 失效
    新型19-类固醇

    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。

    Novel 10.beta.-alkynyl-steroids
    9.
    发明授权
    Novel 10.beta.-alkynyl-steroids 失效
    新型10个β-炔基 - 类固醇

    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。