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1. 发明授权

US5627201A Phenylimidazolidines having antiandrogenic activity 失效
标题翻译：具有抗雄激素活性的苯基咪唑烷
公开(公告)号：US5627201A
公开(公告)日：1997-05-06
申请号：US372648
申请日：1995-01-13
申请人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
发明人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
IPC分类号： C07D233/72 , C07D233/74 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88 , A61K31/415
CPC分类号： C07D233/74 , C07D233/72 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88
摘要： A compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --NO.sub.2 and halogen, R.sub.2 is --CF.sub.3 or halogen, --A--B-- is selected from the group consisting of ##STR2## X is --O-- or --S--, R.sub.3 is selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted with at least one member of the group consisting of --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted with a member of the group consisting of halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl and alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted with at least one member of the group consisting of oxygen, nitrogen and sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A--B-- is ##STR3## X is oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen and R.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.
摘要翻译：式Ⅰ化合物，其中R 1选自-CN，-NO 2和卤素，R 2为-CF 3或卤素，-AB-选自下组：X为-O - 或-S-，R 3选自氢，烷基，烯基和至多12个碳原子的炔基，最多12个碳原子的芳基和芳烷基，全部任选被至少一个成员组成的基团的至多7个碳原子的-OH，卤素，-SH，-CN，酰基和酰氧基，至多12个碳原子的芳基，-O-芳基，-O-芳烷基-S-芳基，芳基和芳烷基任选地被卤素，-CF 3，烷基，烷氧基，烯基，烯氧基，炔基和炔氧基取代，硫任选被氧化成砜或亚砜，游离，酯化，酰胺化或成盐的羧基，-NH 2，单和 3至6个环成员的二烷基氨基和杂环基并含有至少一个选自氧，硫的杂原子 ur和氮，烷基，烯基和炔基任选地被至少一个由氧，氮和硫组成的组中任意地被氧化成亚砜或砜，具有1-6个碳原子的烷基的三烷基甲硅烷基和酰基和酰氧基 1至7个碳原子的有机羧酸，Y是-O - ， - S-或-NH-，但其中-AB-是X的化合物是氧，R 3是氢，Y是氧或-NH - ，R 2是-CF 3或卤素，R 1是-NO 2或卤素及其无毒的药学上可接受的酸加成盐。

2. 发明授权

US5411981A Phenylimidazolidines having antiandrogenic activity 失效
标题翻译：具有抗雄激素活性的苯基咪唑烷
公开(公告)号：US5411981A
公开(公告)日：1995-05-02
申请号：US64257
申请日：1993-05-18
申请人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
发明人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
IPC分类号： C07D233/72 , C07D233/74 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88 , A61K31/415
CPC分类号： C07D233/74 , C07D233/72 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88
摘要： A compound of the formula ##STR1## wherein R.sub.1 is --CN, --NO.sub.2 or halogen, R.sub.2 is --CF.sub.3 or halogen, --A-B-- is of ##STR2## X is --O-- or --S--, R.sub.3 is hydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted by halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted by at least one oxygen, nitrogen or sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A-B-- is ##STR3## X is oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen and R.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.
摘要翻译：其中R 1是-CN，-NO 2或卤素，R 2是-CF 3或卤素，-AB-的化合物，其中X是-O-或-S-，R 3是氢，烷基至多12个碳原子的烯基或炔基，最多12个碳原子的芳基和芳烷基，全部任选被-OH，卤素，-SH，-CN，最多7个碳原子的酰基和酰氧基取代， - 芳基， - 任选被卤素，-CF 3，烷基，烷氧基，烯基，链烯氧基，炔基或炔氧基取代的芳基和芳烷基，其中硫任选被氧化成砜的O-芳基，至多12个碳原子的-O-芳烷基-S-芳基或亚砜，游离，酯化，酰胺化或盐化的羧基，-NH 2，单和二烷基氨基和3至6个环成员的杂环，并含有至少一个选自氧，硫和氮的杂原子，烷基，烯基和炔基任选地被至少一个氧，氮或硫任选地中断，所述氧，氮或硫任选地被氧化成亚砜或砜，具有烷基的三烷基甲硅烷基 1至6个碳原子，1至7个碳原子的有机羧酸的酰基和酰氧基，Y为-O - ， - S-或-NH-，但其中-AB-为X的化合物为氧， R3是氢，Y是氧或-NH-，R2是-CF3或卤素，R1是-NO2或卤素及其无毒的药学上可接受的酸加成盐。

3. 发明授权

US5084450A Novel steroids 失效
标题翻译：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。

4. 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：

5. 发明授权

US4912097A Novel 11 .beta.-alkynylphenyl-10-nor-steroids 失效
标题翻译：新型11β-炔基苯基-10-nor-类固醇
公开(公告)号：US4912097A
公开(公告)日：1990-03-27
申请号：US044958
申请日：1987-04-30
申请人： Jean-Georges Teutsch , Michel Klich , Daniel Philibert
发明人： Jean-Georges Teutsch , Michel Klich , Daniel Philibert
IPC分类号： A61K31/56 , A61P5/00 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J15/00 , C07J17/00 , C07J19/00 , C07J21/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J63/00 , C07J71/00 , C07J73/00
CPC分类号： C07J7/0045 , C07J1/0081 , C07J15/00 , C07J21/003 , C07J21/006 , C07J43/003 , C07J51/00 , C07J63/008 , C07J71/0015
摘要： Novel 11.beta.-alkynylphenyl-19-nor-steroids of the formula ##STR1## wherein R.sub.1 is alkynyl of 2 to 8 carbon atoms optionally substituted with at least one member of the group consisting of --OH halogen, trialkylsilyl of 1 to 6 alkyl carbon atoms, alkoxy and alkylthio of 1 to 6 carbon atoms and dialkylamino of 1 to 6 alkyl carbon atoms having remarkably antiprogestomimetic and antiglucocorticoidal activity.
摘要翻译：新颖的式11的β-炔基苯基-19-去甲甾族化合物，其中R 1为2至8个碳原子的炔基，任选被至少一个选自-OH卤素，1至6个烷基的三烷基甲硅烷基具有1-6个碳原子的烷氧基和烷硫基以及1至6个烷基碳原子的二烷基氨基具有显着的抗动脉硬化和抗皮质醇活性。

6. 发明授权

US4634696A Novel 11 beta-substituted-19-nor-steroids 失效
标题翻译：新型11型β-取代-19-去甲甾类
公开(公告)号：US4634696A
公开(公告)日：1987-01-06
申请号：US760703
申请日：1985-07-30
申请人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert
发明人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert
IPC分类号： A61K31/565 , A61P5/38 , C07J1/00 , C07J21/00 , C07J41/00 , C07J43/00 , C07J71/00 , A61K31/56
CPC分类号： C07J1/0088 , C07J1/0059 , C07J1/007 , C07J21/006 , C07J41/0077 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J71/0063
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antigluococorticoid activity, their preparation and novel intermediates.
摘要翻译：式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃至少8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：（a）（c）＆lt; IMAGE＆gt;（d）和＆lt; IMAGE＆gt;（e）R'和R“分别选自氢，-CN和1至4个碳原子的烷基，其中至少一个是其它 R x选自氢和ORe，Re选自氢，任选取代的1至6个碳原子的烷基和酰基，R a可以在E或Z位置，如波浪线，并且选自和酰氧基，Ra'和Ra“是烷基 1至4个碳原子或与氮原子一起形成任选含有另一个杂原子的5至6个链成员的杂环，条件是当A和B为至少一个氮，磷或硅原子时， A和B是，R1不是直链烷基及其无毒的药学上可接受的酸加成盐，具有显着的抗皮质激素活性，其制备和新型中间体。

7. 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。

8. 发明授权

US6011026A Method of treating menopause or perimenopause 有权
标题翻译：治疗绝经或绝经期的方法
公开(公告)号：US6011026A
公开(公告)日：2000-01-04
申请号：US249416
申请日：1999-02-12
申请人： Yamina Bouali , Daniel Philibert , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
发明人： Yamina Bouali , Daniel Philibert , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
IPC分类号： A61K31/56 , A61K31/565 , A61K31/567 , A61K31/58 , A61K31/585 , A61P19/10 , A61P43/00 , C07J41/00
CPC分类号： A61K31/566 , A61K31/565 , A61K31/567 , A61K31/58 , A61K31/585
摘要： A method of treating menopause or perimenopause without estrogenic activity at the uterine level in women comprising administering to women an amount of a steroid of the formula ##STR1## wherein the substituents are defined as in the specification sufficient to treat menopause or perimenopause symptoms without estrogenic activity at the uterine level.
摘要翻译：一种在妇女中治疗绝经期或围绝经期而不具有子宫水平的雌激素活性的方法，包括向妇女施用一定量的下式的类固醇，其中取代基如本说明书中所定义足以治疗子宫内无雌激素活性的绝经期或围绝经期症状水平。

9. 发明授权

US5981516A Method of treating menopause or perimenopause 失效
标题翻译：治疗绝经或绝经期的方法
公开(公告)号：US5981516A
公开(公告)日：1999-11-09
申请号：US993848
申请日：1997-12-18
申请人： Yamina Bouali , Daniel Philibert , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
发明人： Yamina Bouali , Daniel Philibert , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
IPC分类号： A61K31/56 , A61K31/565 , A61K31/567 , A61K31/58 , A61K31/585 , A61P19/10 , A61P43/00 , C07J41/00
CPC分类号： A61K31/566 , A61K31/565 , A61K31/567 , A61K31/58 , A61K31/585
摘要： A method of treating cholesterol without estrogenic activity at the uterine level in women comprising administering to women an amount of a steroid of the formula ##STR1## wherein the substituents are defined as in the specification without estrogenic activity at the uterine level.
摘要翻译：一种治疗妇女在子宫水平没有雌激素活性的胆固醇的方法，包括向妇女施用一定量的下式的类固醇，其中取代基如本说明书所述，而在子宫水平下没有雌激素活性。

10. 发明授权

US5043332A Novel 11.beta.-substituted -19-nor-steriods 失效
标题翻译：新型11β-取代-19-去甲基异亮氨酸
公开(公告)号：US5043332A
公开(公告)日：1991-08-27
申请号：US421526
申请日：1989-10-13
申请人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert , Germain Costerousse
发明人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert , Germain Costerousse
IPC分类号： C07J1/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J63/00 , C07J71/00
CPC分类号： C07J41/0094 , C07J1/0059 , C07J1/007 , C07J1/0088 , C07J21/006 , C07J41/0016 , C07J41/0077 , C07J41/0083 , C07J43/003 , C07J51/00 , C07J63/008 , C07J7/0005 , C07J71/001 , C07J71/0063
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R'.sub.a and R".sub.a are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom--with the proviso that when A and B are ##STR4## wherein R' and R" are both hydrogen, R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiglucocorticoid activity, their preparation and novel intermediates.
摘要翻译：式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃至少8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：（a）（c）图像（d）图像（e）R'和R“分别选自氢，-CN和1至4个碳原子的烷基，R x选自由氢和ORe组成，Re选自氢，任选取代的1至6个碳原子的烷基和酰基，Ra可以在如波形线所示的E或Z位置，并且选自的＆lt; IMAGE＆gt;和酰氧基，R'a和R'a是1〜4个碳原子的烷基或与n 氢原子形成任选含有另一个杂原子的5至6个链成员的杂环，条件是当A和B为其中R'和R“均为氢时，R 1包含至少一个氮，磷或硅原子当A和B是时，R1不是具有显着的抗糖皮质激素活性的直链烷基及其无毒的药学上可接受的酸加成盐，其制备和新的中间体。

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