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1. 发明授权

US06790971B1 19-Nor-steroids 失效
标题翻译： 19-非类固醇
公开(公告)号：US06790971B1
公开(公告)日：2004-09-14
申请号：US08442957
申请日：1995-05-17
申请人： Andrè Claussner , Lucien Nedelec , Daniel Philibert , Patrick Van De Velde , François Nique , Jean-Georges Teutsch
发明人： Andrè Claussner , Lucien Nedelec , Daniel Philibert , Patrick Van De Velde , François Nique , Jean-Georges Teutsch
IPC分类号： C07J100
CPC分类号： C07J43/003 , C07J41/0077 , C07J41/0083 , C07J63/008
摘要： A 19-nor-steroid having a formula selected from the group consisting of wherein the A and B rings have a structure selected from the group consisting of having hormonal properties and their preparation and novel intermediates.
摘要翻译：具有选自A和B环中的式的19-去甲基甾体具有选自具有激素性质及其制备和新型中间体的结构。

2. 发明授权

US5707982A 19-nor-steroids 失效
标题翻译： 19-类固醇
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：

3. 发明授权

US5149696A 19.fwdarw.nor.fwdarw.steroids 失效
标题翻译： 19-> NOR-> STEROIDS
公开(公告)号：US5149696A
公开(公告)日：1992-09-22
申请号：US484424
申请日：1990-02-23
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
CPC分类号： C07J41/0083 , C07J41/0077 , C07J43/003
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and intermediates.
摘要翻译：具有下式的新型19-去甲类固醇：其中A和B环具有选自具有激素性质的组合和其制备和中间体的结构的结构。

4. 发明授权

US5290771A 19-nor-steroids 失效
标题翻译： 19-类固醇
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。

5. 发明授权

US5108996A 19-nor-3-keto steroids 失效
标题翻译： 19-NOR-3-KETO STEROIDS
公开(公告)号：US5108996A
公开(公告)日：1992-04-28
申请号：US497562
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 , 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.2 and R'.sub.2 are individually hydrogen or methyl, R.sub.11 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom adjacent to the 11-carbon atom being a carbon, the wavy lines at the 13 and 17-positions indicate that when the 13-methyl is .alpha., R'.sub.17 group is .beta. and R.sub.17 is .alpha. and when the 13-methyl is .sub..beta., R.sub.17 is .sub..beta. and R'.sub.17 is .alpha., R.sub.17 is --OH or acyloxy of 1 to 18 carbon atoms and R'.sub.17 is ##STR2## is hydrogen or --OH or acyloxy of 1 to 18 carbon atoms, 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 and P is selected from the group consisting of pyrimidinyl and pyridyl optionally substituted with 1 or 2 individual members of the group consisting of amino, alkylamino and dialkylamino of 1 to 4 alkyl carbon atoms and (B aminated 5- or 6-membered heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms) and its non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and anti-oxidant activity.
摘要翻译：选自下式的化合物的化合物其中R 2和R 12独立地是氢或甲基，R 11是具有1至18个碳原子的有机基团，任选地含有至少一个与原子相邻的原子的杂原子 11碳原子是碳，13位和17位的波浪线表示当13-甲基是α时，R'17基团是β，R17是α，当13-甲基是β时，R17是 β和R'17是α，R17是-OH或1至18个碳原子的酰氧基，R'17是氢或-OH或含1至18个碳原子的酰氧基，Z选自由单键键合，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组成的组，P选自嘧啶基和吡啶基，任选被1或2个独立成员取代的氨基，烷基氨基和1至4个烷基碳原子的二烷基氨基和（B胺化的5或6元环任选被1至3个碳原子的烷基取代的杂环）及其无毒的药学上可接受的具有抗炎和抗氧化活性的酸加成盐。

6. 发明授权

US5166146A Amino acid cyclopentanophenonthrene compounds 失效
标题翻译：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。

7. 发明授权

US4943566A Novel 17-aryl-steroids 失效
标题翻译：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。

8. 发明授权

US4921846A Novel 17-hetero substituted steroids 失效
标题翻译：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。

9. 发明授权

US4900725A Steroids including a spiro ring in position 17, the process for their preparation and their use 失效
标题翻译：类固醇包括位置17的螺环，其制备方法及其应用
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。

10. 发明授权

US5276023A 19-nor-steroid esters 失效
标题翻译： 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。

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