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1. 发明授权

US06693090B2 19-norsteroids substituted in position 11&bgr;, preparation process and intermediates, application as medicines and pharmaceutical compositions containing them 有权
标题翻译：在位置11beta上取代的19-去偶星，制备方法和中间体，作为药物和含有它们的药物组合物的应用
公开(公告)号：US06693090B2
公开(公告)日：2004-02-17
申请号：US10119903
申请日：2002-04-10
申请人： Francois Nique
发明人： Francois Nique
IPC分类号： A61K3156
CPC分类号： C07J31/006 , C07J41/0083 , C07J43/003 , Y02P20/55
摘要： A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification which compounds are useful for the treatment of osteoporosis.
摘要翻译：选自由取代基中的烷基化合物组成的组的化合物定义为说明书中所述，该化合物可用于治疗骨质疏松症。

2. 发明授权

US06423700B1 17-halogenated 19-nor steroids, method and intermediates for preparing same, use as medicines and pharmaceutical compositions containing same 有权
标题翻译： 17-卤化的19-或类固醇，其制备方法和中间体，用作药物和含有它们的药物组合物
公开(公告)号：US06423700B1
公开(公告)日：2002-07-23
申请号：US09720565
申请日：2001-01-05
申请人： Yasmina Bouali , Jacques Mauger , Patrick Van De Velde , Francois Nique
发明人： Yasmina Bouali , Jacques Mauger , Patrick Van De Velde , Francois Nique
IPC分类号： A61K3158
CPC分类号： C07J41/0083
摘要： A compound of the formula wherein the substituents are as defined in the application and its non-toxic, pharmaceutically acceptable acid and base salts useful for hormone replacement for treating menopause or perimenopause without activity at the uterine level treating osteoporosis and strengthening cardiovascular protection in warm-blooded animals.
摘要翻译：取代基中的取代基的化合物如本申请中所定义，并且其无毒的药学上可接受的酸和碱盐可用于激素替代以治疗绝经或围绝经期，而在子宫水平治疗骨质疏松症和加强温血血管内的心血管保护动物。

3. 发明授权

US06399766B2 4-halogenated steroids, their preparation process and intermediates, their use as medicaments and the pharmaceutical compositions containing them 有权
标题翻译： 4-卤代类固醇，其制备方法和中间体，它们作为药物的用途和含有它们的药物组合物
公开(公告)号：US06399766B2
公开(公告)日：2002-06-04
申请号：US09757679
申请日：2001-01-10
申请人： Yamina Bouali , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
发明人： Yamina Bouali , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
IPC分类号： C07J100
CPC分类号： C07J41/0083
摘要： A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.
摘要翻译：本发明的主题是式（I）的化合物：其中X是卤素原子，D表示任选取代的五价或六价环的其余部分，并且任选地带有不饱和键，R 1，R 2，R 3，R 4，Y和 n如说明书中所定义，其制备方法和中间体，它们作为药物的用途以及含有它们的组合物。

4. 发明授权

US06281204B1 19-nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, and the intermediates of this process, their use as medicaments and compositions 失效
标题翻译： 19-还没有在位置11beta具有硫代碳链的类固醇，其制备方法和该方法的中间体，以及该方法的中间体，它们作为药物和组合物的用途
公开(公告)号：US06281204B1
公开(公告)日：2001-08-28
申请号：US08244735
申请日：1994-06-09
申请人： Andre Claussner , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
发明人： Andre Claussner , Francois Nique , Jean-Georges Teutsch , Patrick Van De Velde
IPC分类号： A61K3158
CPC分类号： C07J31/006 , C07J41/0005 , C07J41/0016 , C07J41/0083 , C07J43/003
摘要： Compounds of formula (I), wherein R17 and R′17 are such that: either R17 and R′17 together form ketone, hydrazono, oxime or methylene, or R17 is hydroxyl, hydroxymethyl or acyloxy and R′17 is hydrogen, alkyl or optionally substitued alkenyl or alkynyl; R3 is hydrogen or alkyl; R16 is hydrogen, halogen or alkyl; m is 0, 1 or 2; X, Y and Z are such that: X is methylene, arylene or arylenoxy bonded to the steroid by a carbon atom; Y is a saturated or unsaturated straight or branched aliphatic chain which is optionally interrupted by oxygen; and Z is aryl, arylalkyl or straight or branched alkyl; addition salts thereof, a preparation method therefor, medicinal uses thereof, compositions containing said compounds, and resulting novel intermediates.
摘要翻译：式（I）化合物，其中R 17和R 17如此：R 17和R 17一起形成酮，亚肼基，肟或亚甲基，或R 17为羟基，羟甲基或酰氧基，R 17为氢，烷基或任选取代的烯基或炔基; R3是氢或烷基; R16是氢，卤素或烷基; m为0,1或2; X，Y和Z使得：X是亚甲基，亚芳基或亚芳基氧基通过碳原子键合到类固醇; Y是任选被氧中断的饱和或不饱和直链或支链脂族链; Z为芳基，芳烷基或直链或支链烷基; 其加成盐，其制备方法，其医药用途，含有所述化合物的组合物，以及所得的新型中间体。

5. 发明授权

US08168667B2 Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such 有权
标题翻译：咪唑烷衍生物，其用途，其制备方法和包含其的组合物
公开(公告)号：US08168667B2
公开(公告)日：2012-05-01
申请号：US12751158
申请日：2010-03-31
申请人： Francois Nique , Catherine Jagerschmidt , Philippe Clement-Lacroix
发明人： Francois Nique , Catherine Jagerschmidt , Philippe Clement-Lacroix
IPC分类号： A61K31/4166 , C07D233/02
CPC分类号： C07D233/78 , A61K31/4166 , C07D233/86 , C07D235/02 , C07D309/10 , C07D409/06
摘要： Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.
摘要翻译：式（I）化合物：其中X为O或S，R1为酰基，醛，环烷基，任选取代的烷基，烯基或炔基，R2为H，烷基，羟基烷基，卤代烷基，烯基或炔基; 取代的烷基; 烷基羰基; R3和R4是H，卤素，烷基，烯基，炔基，烷氧基，烷硫基，羟基烷基，卤代烷基，卤代烯基或卤代炔基; 或R 3和R 4形成任选的芳族或杂环的任选取代的环，R 5是H，卤素，三氟甲基，-CN或-NO 2; 不是所有的R 3，R 4和R 5是H，R 6和R 9是H，卤素，OH; 烷基，羟基烷基，烷氧基，硫代烷基，卤代烷基，烯基或炔基; R7和R8是H，卤素，OH，SH; 任选被OH和/或卤素取代的烷氧基或烷硫基; R7和R8之一不是H或卤素; 或者R 7和R 8中的一个是药学上可接受的酯或硫代酯基团，或者R 6是C 1-3烷基，或者与R 1或R 2一起代表C1-3亚烷基或亚烯基连接基团，任选地被甲基，三氟甲基，OH ，或卤素及其药学上可接受的盐和酯可用作选择性雄激素调节剂。

6. 发明授权

US07449572B2 Process and intermediates for preparing 17-halogenated 19-norsteroid compounds 有权
标题翻译：制备17-卤代19-降胆固醇化合物的方法和中间体
公开(公告)号：US07449572B2
公开(公告)日：2008-11-11
申请号：US10834638
申请日：2004-04-29
申请人： Francois Nique , Christian Moratille , Patrick Roussel , Joëlle Bousquet
发明人： Francois Nique , Christian Moratille , Patrick Roussel , Joëlle Bousquet
IPC分类号： C07J43/00 , C07J1/00
CPC分类号： A61K31/58 , A61K31/56 , C07J1/00 , C07J43/00 , C07J75/00
摘要： The invention relates to a process for preparing compounds of formula (I): in which R1, R2, R3, n and X are as defined in the description, and to the intermediate compounds for implementing this process.
摘要翻译：本发明涉及制备式（I）化合物的方法：其中R 1，R 2，R 3，n和X 如在说明书中所定义，以及用于实施该方法的中间体化合物。

7. 发明授权

US07381718B2 Method for preparing oestrogen derivatives 有权
标题翻译：雌激素衍生物的制备方法
公开(公告)号：US07381718B2
公开(公告)日：2008-06-03
申请号：US10480618
申请日：2002-06-12
申请人： Francoise Benedetti , Alain Mazurie , Francois Nique , Denis Prat , Christian Wehrey
发明人： Francoise Benedetti , Alain Mazurie , Francois Nique , Denis Prat , Christian Wehrey
IPC分类号： A61K31/58 , C07J1/00 , C07J43/00
CPC分类号： C07J73/003 , C07J41/0083 , C07J75/00 , Y02P20/55
摘要： A process for the preparation of compounds of formula (I) in which R1, R2, R3 and n are defined as indicated in the description, use of said compounds as intermediates for the preparation of estrogen derivatives as well as the intermediates of this process.
摘要翻译：制备其中R 1，R 2，R 3和n的式（I）化合物的方法如描述，所述化合物作为制备雌激素衍生物的中间体的用途以及该方法的中间体。

8. 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：

9. 发明授权

US5705494A Anti-estrogenic activity of II.beta.-substituted-19-NOR Steroids 失效
标题翻译： IIβ取代-19-NOR类固醇的抗雌激素活性
公开(公告)号：US5705494A
公开(公告)日：1998-01-06
申请号：US512284
申请日：1995-08-08
申请人： Francois Nique , Jean-Georges Teutsch , Patrick Van de Velde
发明人： Francois Nique , Jean-Georges Teutsch , Patrick Van de Velde
IPC分类号： A61K31/56 , A61K31/565 , A61K31/57 , A61K31/575 , A61K31/58 , A61P1/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/00 , A61P5/26 , A61P5/28 , A61P5/30 , A61P5/32 , A61P5/38 , A61P5/42 , A61P5/44 , A61P5/46 , A61P9/10 , A61P9/12 , A61P15/00 , A61P15/04 , A61P15/08 , A61P17/00 , A61P19/10 , A61P25/20 , A61P35/00 , A61P37/04 , A61P43/00 , C07J1/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J75/00
CPC分类号： C07J41/0083 , C07J1/0059 , C07J41/0072 , C07J43/003
摘要： Disclosed is a method of inducing anti-estrogenic activity in warm-blooded animals by the administration of a compound of the formula ##STR1## wherein the substituents are as defined in the specification.
摘要翻译：公开了通过施用式I化合物在温血动物中诱导抗雌激素活性的方法，其中取代基如说明书中所定义。

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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