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1. 发明授权

US06806282B2 Branched substituted amino derivatives of 3-amino-1-phenyl-1h-[1,2,4]triazol, methods for producing them and pharmaceutical compositions containing them 有权
标题翻译： 3-氨基-1-苯基-1h- [1,2,4]三唑的支链取代氨基衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US06806282B2
公开(公告)日：2004-10-19
申请号：US10149499
申请日：2002-06-12
申请人： Michel Geslin , Danielle Gully , Jean-Pierre Maffrand , Pierre Roger
发明人： Michel Geslin , Danielle Gully , Jean-Pierre Maffrand , Pierre Roger
IPC分类号： A61K314196
CPC分类号： C07D249/14
摘要： The present invention relates to novel branched substituted amino derivatives of 3-amino-1-phenyl-1H-[1,2,4]triazole, processes for their preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及3-氨基-1-苯基-1H- [1,2,4]三唑的新的支链取代氨基衍生物，其制备方法和包含它们的药物组合物。

2. 发明授权

US08420679B2 Aminothiazole derivatives and their use as CRF receptor ligands 有权
标题翻译：氨基噻唑衍生物及其作为CRF受体配体的用途
公开(公告)号：US08420679B2
公开(公告)日：2013-04-16
申请号：US11740001
申请日：2007-04-25
申请人： Evelyne Fontaine , Michel Geslin , Danielle Gully , Antoine Pradines , Pierre Roger
发明人： Evelyne Fontaine , Michel Geslin , Danielle Gully , Antoine Pradines , Pierre Roger
IPC分类号： A61K31/425
CPC分类号： C07D417/12 , C07D277/42
摘要： Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotrophin releasing factor (CRF) antagonists.
摘要翻译：取代的4-苯基-2-氨基噻唑衍生物，其制备方法及其作为促肾上腺皮质激素释放因子（CRF）拮抗剂的用途。

3. 发明授权

US06586456B1 Aminothiazole derivatives and their use as CRF receptor ligands 有权
标题翻译：氨基噻唑衍生物及其作为CRF受体配体的用途
公开(公告)号：US06586456B1
公开(公告)日：2003-07-01
申请号：US10031038
申请日：2002-04-17
申请人： Evelyne Fontaine , Michel Geslin , Danielle Gully , Antoine Pradines , Pierre Roger
发明人： Evelyne Fontaine , Michel Geslin , Danielle Gully , Antoine Pradines , Pierre Roger
IPC分类号： A61K31426
CPC分类号： C07D417/12 , C07D277/42
摘要： Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotropin releasing factor (CRF) antagonists.
摘要翻译：取代的4-苯基-2-氨基噻唑衍生物，其制备方法及其作为促肾上腺皮质激素释放因子（CRF）拮抗剂的用途。

4. 发明授权

US06344470B1 Aminothiazole derivatives, method of preparation and pharmaceutical compositions containing same 失效
标题翻译：氨基噻唑衍生物，制备方法和含有它们的药物组合物
公开(公告)号：US06344470B1
公开(公告)日：2002-02-05
申请号：US09269516
申请日：1999-04-02
申请人： Evelyne Fontaine , Danielle Gully , Pierre Roger , Camille Georges Wermuth
发明人： Evelyne Fontaine , Danielle Gully , Pierre Roger , Camille Georges Wermuth
IPC分类号： A61K31425
CPC分类号： C07D277/42 , C07D277/40
摘要： The subject of the invention is the compounds of formula: in which R1, R2, R3, R4, R5 and R6 are as defined in Claim 1. The compounds have a high affinity for CRF receptors.
摘要翻译：本发明的主题是下式的化合物：其中R 1，R 2，R 3，R 4，R 5和R 6如权利要求1中所定义。该化合物对CRF受体具有高亲和力。

5. 发明授权

US5880135A Substituted 4-phenylaminothiazoles, their process of preparation and the pharmaceutical compositions containing them 失效
公开(公告)号：US5880135A
公开(公告)日：1999-03-09
申请号：US945098
申请日：1997-12-22
申请人： Danielle Gully , Pierre Roger , Camille Georges Wermuth
发明人： Danielle Gully , Pierre Roger , Camille Georges Wermuth
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/535 , A61P5/00 , A61P5/04 , C07D277/42 , C07D417/12
CPC分类号： C07D417/12 , C07D277/42
摘要： A compound, as well as its stereoisomers and addition salts, possssing antagonist activity with respect to corticotropin releasing hormone (CRF) has the formula: ##STR1## in which R.sub.1, and R.sub.21 which are identical or different, are independently selected from a halogen atom; a (C.sub.1 -C.sub.5)hydroxyalkyl radical; a (C.sub.1 -C.sub.5)alkyl; a (C.sub.7 -C.sub.10)aralkyl; a (C.sub.1 -C.sub.5)alkoxy; a trifluoromethyl; a nitro; a nitrile; an --SR group in which R is selected from hydrogen, a (C.sub.1 -C.sub.5)alkyl radical and a (C.sub.7 -C.sub.10)aralkyl radical; an --S--CO--R group in which R is selected from a (C.sub.1 -C.sub.5)alkyl radical and an aralkyl radical in which the aryl part is (C.sub.6 -C.sub.8) and the alkyl part is (C.sub.1 -C.sub.4); a --COOR' group in which R' is selected from hydrogen and a (C.sub.1 -C.sub.5)alkyl; a --CONR--R'R" group with R' and R" as defined above for R'; an --NR'R" group with R' and R" as defined above for R'; a --CONRaRb or --NRaRb group in which Ra and Rb constitute, with the nitrogen atom to which they are bonded, a 5- to 7-membered heterocycle; and an --NHCO--NR'R" group with R' and R" as defined above for R'; R.sub.3 represents hydrogen or is as defined above for R.sub.1 and R.sub.2 ; R.sub.4 is selected from a hydrogen atom; a (C.sub.1 -C.sub.5)alkyl; a halogen, a hydroxymethyl group; and a formyl group; R.sub.5 is selected from a (C.sub.1 -C.sub.5)alkyl; a (C.sub.3 -C.sub.7)cycloalkyl group; a cycloalkylalkyl group in which the cycloalkyl part is (C.sub.3 -C.sub.7) and the alkyl part is (C.sub.1 -C.sub.5); and alkenyl containing 5 to 6 carbon atoms; n represents zero or one; R.sub.6 is selected from a (C.sub.1 -C.sub.5)alkyl; an alkoxyalkyl in which the alkyl parts are (C.sub.1 -C.sub.5); a (C.sub.3 -C.sub.7)cycloalkyl; a cycloalkylalkyl group in which the cycloalkyl part is (C.sub.3 -C.sub.7) and the alkyl part is (C.sub.1 -C.sub.5); a cycloalkyloxyalkyl radical in which the cycloalkyl is (C.sub.3 -C.sub.7) and the alkyl part is (C.sub.1 -C.sub.4); a hydroxyalkyloxyalkyl radical in which the alkyls are (C.sub.2 -C.sub.10); and an alkoxyalkyloxyalkyl radical in which the alkyls are (C.sub.3 -C.sub.12); Z represents an optionally substituted bi- or tricyclic aromatic or heteroaromatic group.

6. 发明授权

US5464847A Branched alkylamino derivatives of thiazole, processes for preparing them and pharmaceutical compositions containing them 失效
标题翻译：噻唑的支链烷基氨基衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5464847A
公开(公告)日：1995-11-07
申请号：US80172
申请日：1993-06-23
申请人： Gilles Courtemanche , Claudie Gautier , Danielle Gully , Pierre Roger , Gerard Valette , Camille G. Wermuth
发明人： Gilles Courtemanche , Claudie Gautier , Danielle Gully , Pierre Roger , Gerard Valette , Camille G. Wermuth
IPC分类号： A61K31/425 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4439 , A61P5/38 , A61P25/18 , A61P25/20 , C07D213/38 , C07D213/61 , C07D277/20 , C07D277/42 , C07D277/44 , C07D417/06 , C07D417/12
CPC分类号： C07D417/12 , C07D277/42
摘要： The invention relates to the derivatives of formula I: ##STR1## in which R.sub.1 represents a phenyl or naphthyl radical (optionally substituted), R.sub.2 represents a hydrogen or halogen atom or an alkyl, hydroxymethyl or formyl radical, R.sub.3 represents an alkyl, cycloalkyl, alkenyl, cycloalkylalkyl or phenyl radical, R.sub.4 represents a hydrogen atom or an alkyl, cycloalkyl or cycloalkylalkyl radical, R.sub.5 represents an alkyl, cycloalkyl, cycloalkylalkyl or alkenyl radical or a radical of formula B: ##STR2## (p=0, 1, 2 or 3), R.sub.6 represents a phenyl, pyridyl, imidazolyl, pyrrolyl, thienyl or furyl radical, optionally substituted, or a cycloalkyl radical,m and n, which may be identical or different, each represent 0 or 1,their possible stereoisomers and their addition salts.
摘要翻译：本发明涉及式I的衍生物：其中R 1表示苯基或萘基（任选取代的），R 2表示氢或卤素原子或烷基，羟甲基或甲酰基，R 3表示烷基，，环烷基，烯基，环烷基烷基或苯基，R 4表示氢原子或烷基，环烷基或环烷基烷基，R 5表示烷基，环烷基，环烷基烷基或烯基或式B的基团： = 0,1,2或3），R 6表示苯基，吡啶基，咪唑基，吡咯基，噻吩基或呋喃基，任选取代的或环烷基，m和n可以相同或不同，各自表示0或1 ，它们可能的立体异构体及其加成盐。

7. 发明授权

US07951821B2 N-[phenyl(piperidin-2-yl)methyl]benzamide derivatives, preparation thereof, and use thereof in therapy 失效
标题翻译： N- [苯基（哌啶-2-基）甲基]苯甲酰胺衍生物，其制备及其在治疗中的用途
公开(公告)号：US07951821B2
公开(公告)日：2011-05-31
申请号：US11680782
申请日：2007-03-01
申请人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Benoit Marabout , Pierre Roger , Mireille Sevrin
发明人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Benoit Marabout , Pierre Roger , Mireille Sevrin
IPC分类号： A61K31/445
CPC分类号： C07D211/26
摘要： This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.
摘要翻译：本发明公开了一种通式（I）的化合物，其中R 1表示氢原子或任选取代的烷基，或环烷基烷基，或任选取代的苯基烷基或烯基，X表示氢原子或一个或多个选自卤素原子和三氟甲基，烷基和烷氧基的取代基，R 2表示一个或多个选自卤素原子，任选取代的烷氧基和任选取代的氨基的取代基。本发明的化合物表现出治疗效用。

8. 发明授权

US07205319B2 N-[phenyl (piperidin-2-yl) methyl]benzamide derivatives, preparation thereof, and use thereof in therapy 失效
标题翻译： N- [苯基（哌啶-2-基）甲基]苯甲酰胺衍生物，其制备及其在治疗中的用途
公开(公告)号：US07205319B2
公开(公告)日：2007-04-17
申请号：US11045247
申请日：2005-01-28
申请人： Gihad Dargazanli , Geneviève Estenne-Bouhtou , Benoît Marabout , Pierre Roger , Mireille Sevrin
发明人： Gihad Dargazanli , Geneviève Estenne-Bouhtou , Benoît Marabout , Pierre Roger , Mireille Sevrin
IPC分类号： A61K31/445 , C07D413/02
CPC分类号： C07D211/26
摘要： This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.
摘要翻译：本发明公开并要求通式（I）的化合物，

9. 发明申请

US20050159450A1 Derivative of n-[phenyl(piperidin-2-yl)methyl]benzamide, the preparation method thereof and application of same in therapeutics 失效
标题翻译： n- [苯基（哌啶-2-基）甲基]苯甲酰胺的衍生物及其制备方法及其在治疗中的应用
公开(公告)号：US20050159450A1
公开(公告)日：2005-07-21
申请号：US10511886
申请日：2003-04-17
申请人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Florence Medaisko , Pierre Roger , Mireille Sevrin , Corinne Veronique
发明人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Florence Medaisko , Pierre Roger , Mireille Sevrin , Corinne Veronique
IPC分类号： A61K20060101 , A61K31/445 , A61K31/4458 , A61K31/452 , A61P20060101 , A61P1/00 , A61P11/16 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/26 , C07D211/32 , C07D211/94
CPC分类号： C07D211/26
摘要： Compound of general formula (I) in which A represents either a group of formula N—R1 in which R1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a phenylalkyl group, an alkenyl group or an alkynyl group, or a group of formula N+(O−)R1 in which R1 is as defined above, or alternatively a group of formula N+(R′)R1 in which R′ represents an alkyl group and R1 is as defined above, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents a hydrogen atom, one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, amino groups of formula NR3R4 in which R3 and R4 each represent a hydrogen atom or an alkyl group, or form with the nitrogen atom carrying them a pyrrolidine, piperidine or morpholine ring, or an optionally substituted phenyl group. Application in therapy.
摘要翻译：通式（I）的化合物，其中A表示式NR 1的基团，其中R 1表示氢原子，烷基，环烷基，苯基烷基，烯基或炔基，或其中R 1为低级烷基的基团，其中R 1为N（O） > 1 如上所定义，或者可选地，其中R'表示烷基的式N +，（R'）R 1' 如上定义，X表示氢原子或一个或多个选自卤素原子和三氟甲基，烷基和烷氧基的取代基，R 2表示氢原子，一个或多个选自卤素原子和三氟甲基，烷基和烷氧基的更多取代基，式NR 3 R 4的氨基，其中R 3和R“ 或者分别代表氢原子或烷基，或与氮原子一起带有吡咯烷，哌啶或吗啉环的形式，或 n任选取代的苯基。应用于治疗。

10. 发明授权

US4760062A Pharmaceutical compositions of N-heterocyclic benzenesulfonamides and their use 失效
标题翻译： N-杂环苯磺酰胺的药物组合物及其用途
公开(公告)号：US4760062A
公开(公告)日：1988-07-26
申请号：US662178
申请日：1984-10-18
申请人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
发明人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
IPC分类号： A61K31/395 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P25/20 , C07D243/00 , C07D243/08 , C07D295/22 , C07D295/26 , C07D307/68 , C07D405/06
CPC分类号： C07D295/26 , C07C309/00 , C07D243/08 , C07D405/06
摘要： The invention relates to new N-cyclic benzenesulfonamides, their process of preparation and their use as active substance of pharmaceutical compositions. The new benzenesulfonamides according to the invention correspond to the following general formula (I): ##STR1## in which: V represents, for example, hydrogen,W represents, for example CF.sub.3,X represents, for example, hydrogen,Y represents, for example, hydrogen,n is 2 or 3,Z represents, for example, the group NR.sub.4, in which R.sub.4 represents, for example, hydrogen.These compounds are useful in pharmaceutical compositions for the treatment of nervous disorders with anxiety.
摘要翻译：本发明涉及新的N-环苯磺酰胺，其制备方法及其作为药物组合物的活性物质的用途。根据本发明的新型苯磺酰胺对应于以下通式（I）：其中：V表示例如氢，W表示例如CF 3，X表示例如氢，Y 表示例如氢，n为2或3，Z表示例如NR4基团，其中R4表示例如氢。这些化合物可用于用焦虑治疗神经障碍的药物组合物中。

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