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10 条记录 (耗时 0.012 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。

    Application of 1-(3'-trifluoromethyl-4'-nitrophenyl)-4,4'-dimethylimidazoline 2,5-dione in the treatment of hormone-dependent cancers other than that of the prostate
    2.
    发明授权
    Application of 1-(3'-trifluoromethyl-4'-nitrophenyl)-4,4'-dimethylimidazoline 2,5-dione in the treatment of hormone-dependent cancers other than that of the prostate 失效
    1-（3'-三氟甲基-4'-硝基苯基）-4,4'-二甲基咪唑啉2,5-二酮在治疗激素依赖性癌症以外的应用

    公开(公告)号：US5084472A

    公开(公告)日：1992-01-28

    申请号：US529948

    申请日：1990-05-29

    申请人： Martine Moguilewsky ,  Marie M. Bouton

    发明人： Martine Moguilewsky ,  Marie M. Bouton

    IPC分类号： A61K31/415

    CPC分类号： A61K31/415

    摘要： A method of treating hormone-dependent cancer of an organ selected from the group consisting of bladder, brain, breast, lymphatic systems, kidney, liver, skin and ovaries in warm-blooded animals having such a cancer comprising administering to said warm-blooded animals an amount of 1-(3-'trifluoromethyl-4'-nitro-phenyl)-4,4-dimethyl-imidazoline-2,5-dione sufficient to combat said hormone-dependent cancer.

    摘要翻译： 一种在具有这种癌症的温血动物中治疗选自膀胱，脑，乳腺，淋巴系统，肾脏，肝脏，皮肤和卵巢的器官的激素依赖性癌症的方法，包括向所述温血动物施用 一定量的足以抵抗所述激素依赖性癌症的1-（3-三氟甲基-4'-硝基 - 苯基）-4,4-二甲基 - 咪唑啉-2,5-二酮。

    Amino acid cyclopentanophenonthrene compounds
    5.
    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
    6.
    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 17-hetero substituted steroids
    7.
    发明授权
    Novel 17-hetero substituted steroids 失效
    新型17-取代类固醇

    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。