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1. 发明申请

US20080064720A1 2,6-Quinolinyl And 2,6-Naphthyl Derivatives, Processes For Preparing Them And Their Uses As Vla-4 Inhibitors 失效
标题翻译： 2,6-喹啉基和2,6-萘衍生物，制备它们的方法及其用途作为Vla-4抑制剂
公开(公告)号：US20080064720A1
公开(公告)日：2008-03-13
申请号：US10513347
申请日：2003-04-15
申请人： Marie-Agnes Lassoie , Laurent Knerr , Theirry Demaude , Francoise De Laveleye-Defais , Thierry Kogej , Luc Quere , Sylvain Routier , Gerald Guillaumet
发明人： Marie-Agnes Lassoie , Laurent Knerr , Theirry Demaude , Francoise De Laveleye-Defais , Thierry Kogej , Luc Quere , Sylvain Routier , Gerald Guillaumet
IPC分类号： C07D215/14 , A61K31/192 , A61K31/47 , A61K31/4709 , A61P1/00 , A61P17/00 , A61P37/00 , C07C55/30
CPC分类号： C07C309/65 , C07D215/227
摘要： The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals for the treatment of VLA-4 dependent inflammatory diseases such as for example asthma, allergic rhinitis, sinusitis, conjunctivitis, food allergy, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and atherosclerosis. Formula (I): wherein X is N or CH.
摘要翻译：本发明涉及式（I）的2,6-喹啉基和2,6-萘基衍生物，其制备方法，含有它们的药物组合物及其作为用于治疗VLA-4依赖性炎性疾病的药物的用途，例如哮喘，过敏性鼻炎，鼻窦炎，结膜炎，食物过敏，牛皮癣，荨麻疹，瘙痒，湿疹，类风湿性关节炎，炎性肠病，多发性硬化和动脉粥样硬化。式（I）：其中X是N或CH。

2. 发明申请

US20100105681A1 2,6-QUINOLINYL AND 2,6-NAPHTHYL DERIVATIVES, PROCESSES FOR PREPARING THEM AND THEIR USES AS VLA-4 INHIBITORS 审中-公开
标题翻译： 2,6-喹啉和2,6-萘衍生物，其制备方法及其用作VLA-4抑制剂
公开(公告)号：US20100105681A1
公开(公告)日：2010-04-29
申请号：US12604959
申请日：2009-10-23
申请人： Marie-Agnes Lassoie , Laurent Knerr , Thierry Demaude , Françoise De Laveleye-Defais , Thierry Kogej , Luc Quere , Sylvain Routier , Gerald Guillaumet
发明人： Marie-Agnes Lassoie , Laurent Knerr , Thierry Demaude , Françoise De Laveleye-Defais , Thierry Kogej , Luc Quere , Sylvain Routier , Gerald Guillaumet
IPC分类号： A61K31/5377 , C07D215/14 , A61K31/47 , A61P29/00 , C07D215/20 , A61K31/4704 , A61K31/4709 , C07D413/12 , A61P19/02 , A61P37/08
CPC分类号： C07C309/65 , C07D215/227
摘要： The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及2,6-喹啉基和2,6-萘基衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

3. 发明授权

US07638630B2 2,6-quinolinyl and 2,6-naphthyl derivatives, processes for preparing them and their uses as VLA-4 inhibitors 失效
标题翻译： 2,6-喹啉基和2,6-萘基衍生物，其制备方法及其作为VLA-4抑制剂的用途
公开(公告)号：US07638630B2
公开(公告)日：2009-12-29
申请号：US10513347
申请日：2003-04-15
申请人： Marie-Agnès Lassoie , Laurent Knerr , Thierry Demaude , Françoise De Laveleye-Defais , Thierry Kogej , Luc Quere , Sylvain Routier , Gerald Guillaumet
发明人： Marie-Agnès Lassoie , Laurent Knerr , Thierry Demaude , Françoise De Laveleye-Defais , Thierry Kogej , Luc Quere , Sylvain Routier , Gerald Guillaumet
IPC分类号： C07D215/38
CPC分类号： C07C309/65 , C07D215/227
摘要： The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals for the treatment of VLA-4 dependent inflammatory diseases such as for example asthma, allergic rhinitis, sinusitis, conjunctivitis, food allergy, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and atherosclerosis. Formula (I): wherein X is N or CH.
摘要翻译：本发明涉及式（I）的2,6-喹啉基和2,6-萘基衍生物，其制备方法，含有它们的药物组合物及其作为用于治疗VLA-4依赖性炎性疾病的药物的用途，例如哮喘，过敏性鼻炎，鼻窦炎，结膜炎，食物过敏，牛皮癣，荨麻疹，瘙痒，湿疹，类风湿性关节炎，炎性肠病，多发性硬化和动脉粥样硬化。式（I）：其中X是N或CH。

4. 发明申请

US20120095022A1 DERIVATIVES OF 10-AMINO-1,2,3,4-TETRAHYDROPYRIDO[2,1-A]ISOINDOL-6(10BH)-ONES, METHOD FOR PREPARATION THEREOF AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译： 10-氨基-1,2,3,4-四氢吡啶并[2,1-A]异吲哚-6（10BH） - 酮的衍生物及其制备方法及其治疗用途
公开(公告)号：US20120095022A1
公开(公告)日：2012-04-19
申请号：US13256017
申请日：2010-03-11
申请人： Sylvain Cesar Leonce Routier , Gerald Guillaumet , Rajaa Boulahjar , Laurent Meijer , Matteo Chiurato
发明人： Sylvain Cesar Leonce Routier , Gerald Guillaumet , Rajaa Boulahjar , Laurent Meijer , Matteo Chiurato
IPC分类号： A61K31/497 , A61K31/439 , A61K31/437 , C07D471/20 , C07D471/04 , A61P11/06 , A61P35/00 , A61P25/28 , A61P25/16 , A61P25/00 , A61P31/12 , A61P37/02 , A61P17/00 , A61P17/06 , A61K31/506
CPC分类号： C07D471/20 , C07D471/04 , C07D491/20 , C07D495/20
摘要： The present invention relates to compounds having the following general formula (I): wherein: A represents a SO2 or CX group, X representing O or S; R1, R2, R″, R4 represent in particular H, R represents in particular an alkyl group or an aryl group, as well as to the pharmaceutically acceptable salts thereof, the compound of formula (I) taking the form of a pure stereoisomer or an enantiomer and/or diastereoisomer mixture, including racemic mixtures.
摘要翻译：本发明涉及具有以下通式（I）的化合物：其中：A表示SO2或CX基，X表示O或S; R 1，R 2，R“，R 4特别表示H，R表示特别是烷基或芳基，以及其药学上可接受的盐，式（I）化合物以纯立体异构体或对映异构体和/或非对映异构体混合物，包括外消旋混合物。

5. 发明授权

US07115752B2 Substituted cyclic compounds 失效
标题翻译：取代的环状化合物
公开(公告)号：US07115752B2
公开(公告)日：2006-10-03
申请号：US10948410
申请日：2004-09-23
申请人： Daniel Lesieur , Frederique Klupsch , Gerald Guillaumet , Marie-Claude Viaud , Michel Langlois , Caroline Bennejean , Pierre Renaud , Philippe Delagrange
发明人： Daniel Lesieur , Frederique Klupsch , Gerald Guillaumet , Marie-Claude Viaud , Michel Langlois , Caroline Bennejean , Pierre Renaud , Philippe Delagrange
IPC分类号： C07D209/04 , A61K31/40 , C07D333/53 , A61K31/385
CPC分类号： C07D207/27 , C04B35/632 , C07C233/43 , C07C233/62 , C07C233/65 , C07C237/48 , C07C271/20 , C07C275/24 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/14 , C07D209/20 , C07D209/60 , C07D213/70 , C07D221/10 , C07D231/12 , C07D233/42 , C07D233/56 , C07D233/84 , C07D235/06 , C07D249/08 , C07D261/20 , C07D307/81 , C07D307/92 , C07D311/58 , C07D311/60 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/58 , C07D333/74 , C07D335/06 , C07D335/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D407/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D495/14
摘要： The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t-R5 group wherein t and R5 are as defined in the description.
摘要翻译：本发明涉及式（I）化合物：R-A-R'其中：A如说明书中所定义; R表示基团（V），（VI），（VII）或（VIII），其中E，Q，R 1，R 2，R 3 ＆lt; / SUP＆gt;，v和R 4如在说明书中所定义的; R'表示 - （CH 2）2-t-R 5 - 基，其中t和R 5如说明书中所定义。

6. 发明授权

US5322944A Process for the synthesis of enantiomers of 3-aminochroman compounds 失效
标题翻译：合成3-氨基苯并二氢吡喃化合物对映异构体的方法
公开(公告)号：US5322944A
公开(公告)日：1994-06-21
申请号：US906572
申请日：1992-06-30
申请人： Gerald Guillaumet , Claude Fugier , Jean-Claude J. Souvie , Gerard Adam , Pierre Renard , Daniel-Henri Caignard
发明人： Gerald Guillaumet , Claude Fugier , Jean-Claude J. Souvie , Gerard Adam , Pierre Renard , Daniel-Henri Caignard
IPC分类号： A61K31/40 , A61K31/42 , A61K31/435 , A61P25/00 , C07D311/58 , C07D335/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/056 , C07D498/04 , C07D471/10
CPC分类号： C07D335/06 , C07D311/58 , C07D405/12 , C07D409/12
摘要： Process for preparing enantiomers of general formula (I): ##STR1## where Z, R.sub.1, R.sub.2, R.sub.3 and n are defined in the description. The compounds obtained according to the invention are useful as medicinal products.
摘要翻译：制备通式（I）的对映异构体的方法：其中Z，R1，R2，R3和n在说明书中定义。根据本发明获得的化合物可用作药用产品。

7. 发明授权

US5273994A 3-aminochroman compounds 失效
标题翻译： 3-氨基苯并二氢吡喃化合物
公开(公告)号：US5273994A
公开(公告)日：1993-12-28
申请号：US958965
申请日：1992-10-09
申请人： Gerald Guillaumet , Beatrice Guardiola
发明人： Gerald Guillaumet , Beatrice Guardiola
IPC分类号： C07D311/58 , C07D405/12 , C07D498/04 , A61K31/47 , C07D405/04
CPC分类号： C07D405/12 , C07D311/58
摘要： The invention relates to the derivatives of general formula (I): ##STR1## in which: Z represents an oxygen atom or a sulfur atom,R.sub.1 represents a hydrogen atom or an alkyl group,R.sub.2 represents a hydrogen atom or an alkyl group,1.ltoreq.n.ltoreq.6,R.sub.3 represents a nitrile group, an optionally substituted amino group or any one of the groups described in the description, andmedicinal products containing the same.
摘要翻译：本发明涉及通式（I）的衍生物：其中：Z表示氧原子或硫原子，R1表示氢原子或烷基，R2表示氢原子或烷基基团，n代表腈基，任选取代的氨基或说明书中所述的任何一个基团，以及含有该基团的药物。

8. 发明授权

US5061713A Analgesic oxazolopyridine compounds 失效
标题翻译：镇痛恶唑吡啶化合物
公开(公告)号：US5061713A
公开(公告)日：1991-10-29
申请号：US564033
申请日：1990-08-07
申请人： Gerald Guillaumet , Christine Flouzat , Jacqueline Bonnet
发明人： Gerald Guillaumet , Christine Flouzat , Jacqueline Bonnet
IPC分类号： A61K31/44 , A61K31/50 , A61K31/505 , A61K31/53 , A61P25/04 , C07D498/04
CPC分类号： C07D498/04
摘要： Compound of general formula (I): ##STR1## in which: X, Y, Z and T each represent, independently of one another, a nitrogen atom, a --CH.dbd. group or a group CW, in which W represents a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group, on condition that only one of them represents a nitrogen atom,Ra, Rb, Rc, Rd and Re represent, independently of one another, a hydrogen atom, a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group,B represents a hydrogen atom and D a hydroxyl group, or B and D simultaneously represent an oxygen atom,n represents 1 or 2, andR.sub.1 represents a hydrogen atom, a linear or branched lower alkyl, linear or branched lower alkenyl, aryl or lower arylalkyl group or a cycloalkyl group having 3 to 7 carbon atoms, it being possible for each of the lower alkyl, lower alkenyl, aryl, lower arylalkyl and cycloalkyl groups to be substituted with one or more halogen atoms or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group,their isomers, epimers and diastereoisomers, and addition salts with a pharmaceutically acceptable acidare useful in the treatment of pain.
摘要翻译：通式（I）的化合物：其中：X，Y，Z和T各自独立地表示氮原子，-CH =基团或基团CW，其中W表示卤素原子或任选被一个或多个卤素原子取代的低级烷基或烷氧基，例如三氟甲基，条件是只有一个表示氮原子，Ra，Rb，Rc，Rd和Re独立地表示另一方面，氢原子，卤原子或任选被一个或多个卤素原子取代的低级烷基或烷氧基，例如三氟甲基，B表示氢原子，D表示羟基，或者B和D同时表示氧原子，n表示1或2，R1表示氢原子，直链或支链的低级烷基，直链或支链的低级烯基，芳基或低级芳基烷基或具有3至7个碳原子的环烷基，每种的低级烷基，低级烯基，芳基，低级芳基烷基和环亚烷基被一个或多个卤素原子取代的烷基或任选被一个或多个卤素原子取代的低级烷基或烷氧基，例如三氟甲基，它们的异构体，差向异构体和非对映异构体，以及与药学上可接受的酸的加成盐是有用的在治疗疼痛。

9. 发明授权

US6127369A 5,10-dihydrodipyrido[2,3-b:2,3-e]pyrazin and 5,10-dihydrodipyrido[2,3-b:3,2-e]pyrazin compounds 失效
标题翻译： 5,10-二氢二吡啶并[2,3-b：2,3-e]吡嗪和5,10-二氢二吡啶并[2,3-b：3,2-e]吡嗪化合物
公开(公告)号：US6127369A
公开(公告)日：2000-10-03
申请号：US330496
申请日：1999-06-11
申请人： Paul Caubere , Gerald Guillaumet , Ivan Rodriguez , Karine Vinter-Pasquier , Catherine Kuehm-Caubere , Stephanie Blanchard , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
发明人： Paul Caubere , Gerald Guillaumet , Ivan Rodriguez , Karine Vinter-Pasquier , Catherine Kuehm-Caubere , Stephanie Blanchard , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
IPC分类号： A61K31/00 , A61K31/495 , A61K31/4985 , A61P35/00 , A61P35/02 , C07D471/14
CPC分类号： C07D471/14
摘要： A compound selected from those of formula (I): ##STR1## wherein: X represents N, C or CH,Y represents N when X represents C or CH, or Y represents C or CH when X represents N,R.sub.1 represents an optionally substituted alkyl,R.sub.2 and R.sub.3, which may be identical or different, represent Z or W, as defined in the description,their isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
摘要翻译：选自式（I）的化合物：其中：X表示N，C或CH，Y表示N，当X表示C或CH时，或Y表示C或CH，当X表示N时，R 1表示任选取代的烷基，R 2 和可以相同或不同的R 3表示如说明书中所定义的Z或W，其与药学上可接受的酸或碱的异构体及其加成盐，以及含有该Z可以用于治疗癌症的药物。

10. 发明授权

US5714495A Pyridine compounds as melatonergic agents 失效
标题翻译：吡啶化合物作为褪黑激素药
公开(公告)号：US5714495A
公开(公告)日：1998-02-03
申请号：US631234
申请日：1996-04-12
申请人： Marie-Claude Viaud , Gerald Guillaumet , Daniel Mazeas , Herve Vandepoel , Pierre Renard , Bruno Pfeiffer , Philippe Delagrange
发明人： Marie-Claude Viaud , Gerald Guillaumet , Daniel Mazeas , Herve Vandepoel , Pierre Renard , Bruno Pfeiffer , Philippe Delagrange
IPC分类号： A61K31/435 , A61P25/20 , A61P43/00 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07F7/02 , A61K31/44 , C07D513/04 , C07D491/084
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： The invention relates to a compound selected from those of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and X are as defined in the description and medicinal product containing the same useful for treating a disorder of the melatoninergic system.
摘要翻译：本发明涉及选自式（I）的化合物：其中：R 1，R 2，R 3，R 4，R 5和X如说明书中所定义，含有可用于治疗的药物褪黑激素系统紊乱。

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