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。

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。

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。

公开(公告)号：US07202255B2

公开(公告)日：2007-04-10

申请号：US10531393

申请日：2003-10-17

申请人： Gerard Coudert ,  Nathalie Ayerbe ,  Franck Lepifre ,  Sylvain Routier ,  Daniel-Henri Caignard ,  Pierre Renard ,  John Hickman ,  Alain Pierre ,  Stephane Leonce

发明人： Gerard Coudert ,  Nathalie Ayerbe ,  Franck Lepifre ,  Sylvain Routier ,  Daniel-Henri Caignard ,  Pierre Renard ,  John Hickman ,  Alain Pierre ,  Stephane Leonce

IPC分类号： A61K31/437 ,  C07D491/22

CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D491/14

摘要： Compounds of formula (I): wherein: A is as defined in the description, Y represents a group selected from an oxygen atom and a methylene group, R2 represents a hydrogen atom and in that case: R3 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl, aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) and SO2CF3, or R2 and R3 form a bond, R1 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl and aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) or a linear or branched (C1–C6)alkylene chain, Z1 and Z2 each represent a hydrogen atom or Z1 and Z2, together with the carbon atoms carrying them, form a phenyl group. Medicaments.

摘要翻译： 式（I）的化合物：

公开(公告)号：US10059704B2

公开(公告)日：2018-08-28

申请号：US14112864

申请日：2012-04-20

申请人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

发明人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

IPC分类号： C07D451/04 ,  A61K51/04 ,  C07D453/02 ,  C07D455/02

CPC分类号： C07D451/04 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07D453/02 ,  C07D455/02 ,  G01N2333/70571 ,  G01N2800/28 ,  G01N2800/2821

摘要： A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN′ groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.

公开(公告)号：US07001906B2

公开(公告)日：2006-02-21

申请号：US10481991

申请日：2002-06-28

申请人： Michelle Prudhomme ,  Christelle Marminon ,  Sylvain Routier ,  Gérard Coudert ,  Jean-Yves Merour ,  John Hickman ,  Alain Pierre ,  Pierre Renard ,  Bruno Pfeiffer

发明人： Michelle Prudhomme ,  Christelle Marminon ,  Sylvain Routier ,  Gérard Coudert ,  Jean-Yves Merour ,  John Hickman ,  Alain Pierre ,  Pierre Renard ,  Bruno Pfeiffer

IPC分类号： A61K31/4985 ,  A61K31/437 ,  C07D491/22 ,  C07D405/14

CPC分类号： C07H15/252

摘要： Compounds of formula (I): wherein: W1 and W2, together with the carbon atoms to which they are bonded, represent a phenyl group or a pyridyl group, and at least one of the groups W1 or W2 represents a pyridyl group, R1 and R2 each represent a group of formula U-V as defined in the description, X and X1 each represent a hydrogen atom or a hydroxy, alkoxy, mercapto or alkylthio group, Y and Y1 each represent a hydrogen atom, or X and Y, X1 and Y1, together with the carbon atom carrying them, represent a carbonyl or thiocarbonyl group, R4 and R5 are as defined in the description, Q1, Q2 represent a hydrogen atom, or Q1 and Q2, together with the carbon atoms carrying them, form an aromatic bond. Medicaments.

摘要翻译： 式（I）化合物：化学式id =“CHEM-US-00001”num =“000

公开(公告)号：US20130109693A1

公开(公告)日：2013-05-02

申请号：US13695001

申请日：2011-04-28

申请人： Sylvain Routier ,  Gérald Guillaumet ,  Abdellatif Tikad ,  Oussama Dehbi

发明人： Sylvain Routier ,  Gérald Guillaumet ,  Abdellatif Tikad ,  Oussama Dehbi

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to a compound of the following general formula (I): wherein: R1 is notably H, a halogen or an aryl group, R2 is notably a halogen or an aryl group, R3 is notably a halogen, or an aryl or heteroaryl group, as well as to its pharmaceutically acceptable salts, its hydrates or its polymorphic crystalline structures, its racemates, diastereoisomers or enantiomers, except the compound 1-(2,4-diaminopyrido[3,2-d]pyrimidin-7-yl)-3,6,6-trimethyl-6,7-dihydro-1H-indol-4(5H)-one.

摘要翻译： 本发明涉及以下通式（I）的化合物：其中：R 1特别是H，卤素或芳基，R 2特别是卤素或芳基，R 3特别是卤素，或芳基或 以及其药学上可接受的盐，其水合物或其多晶型结构，其外消旋物，非对映异构体或对映异构体，除了化合物1-（2,4-二氨基吡啶并[3,2-d]嘧啶-7-基 ）-3,6,6-三甲基-6,7-二氢-1H-吲哚-4（5H） - 酮。

公开(公告)号：US20140030191A1

公开(公告)日：2014-01-30

申请号：US14112864

申请日：2012-04-20

申请人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

发明人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

IPC分类号： C07D451/04 ,  C07D453/02 ,  A61K51/04

CPC分类号： C07D451/04 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07D453/02 ,  C07D455/02 ,  G01N2333/70571 ,  G01N2800/28 ,  G01N2800/2821

摘要： A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN′ groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.

摘要翻译： 具有以下通式（I）的化合物：其中：X是氮原子，Y是碳原子; 或X为碳原子，Y为氮原子; Ar基团是芳基或杂芳基; 并且RN和RN'基团与它们所结合的碳原子一起形成单环或双环氮杂环烷基。 还描述了其药学上可接受的盐，其水合物或多晶型结构以及其外消旋物，非对映异构体或其对映异构体。

公开(公告)号：US20060040930A1

公开(公告)日：2006-02-23

申请号：US10531393

申请日：2003-10-17

申请人： Gerard Coudert ,  Nathalie Ayerbe ,  Franck Lepiere ,  Sylvain Routier ,  Daniel-Henri Caignard ,  Pierre Renard ,  John Hickman ,  Alain Pierre ,  Stephane Leonce

发明人： Gerard Coudert ,  Nathalie Ayerbe ,  Franck Lepiere ,  Sylvain Routier ,  Daniel-Henri Caignard ,  Pierre Renard ,  John Hickman ,  Alain Pierre ,  Stephane Leonce

IPC分类号： A61K31/5383 ,  A61K31/4745 ,  C07D491/14 ,  C07D471/14

CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D491/14

摘要： Compounds of formula (I): wherein: A is as defined in the description, Y represents a group selected from an oxygen atom and a methylene group, R2 represents a hydrogen atom and in that case: R3 represents a group selected from a hydrogen atom and the groups linear or branched (C1-C6)alkyl, aryl, aryl-(C1-C6)alkyl (in which the alkyl moiety is linear or branched) and SO2CF3, or R2 and R3 form a bond, R1 represents a group selected from a hydrogen atom and the groups linear or branched (C1-C6)alkyl, aryl and aryl-(C1-C6)alkyl (in which the alkyl moiety is linear or branched) or a linear or branched (C1-C6)alkylene chain, Z1 and Z2 each represent a hydrogen atom or Z1 and Z2, together with the carbon atoms carrying them, form a phenyl group. Medicaments.

摘要翻译： 式（I）的化合物：其中：A如说明书中所定义，Y表示选自氧原子和亚甲基的基团，R 2表示氢原子，在这种情况下：R 3 表示选自氢原子和直链或支链（C 1 -C 6 -C 6）烷基，芳基，芳基 - （ C 1 -C 6 -C 6烷基（其中烷基部分是直链或支链的）和SO 2 -C 3 C 3 >或R 2和R 3'形成键，R 1表示选自氢原子和直链或支链基团的基团（ C 1 -C 6 -C 6烷基，芳基和芳基 - （C 1 -C 6 -C 6）烷基（在 其中烷基部分是直链或支链的）或直链或支链（C 1 -C 6 -C 6）亚烷基链，Z 1和Z 2， 各自表示氢原子或Z 1和Z 2，以及带有它们的碳原子形成苯基。 药剂