公开(公告)号：US11708364B2

公开(公告)日：2023-07-25

申请号：US17216114

申请日：2021-03-29

申请人： AGV Discovery ,  Institut National de la Sante et de la Recherche Medicale (INSERM) ,  Centre National de la Recherche Scientifique (CNRS) ,  Universite De Montpellier

发明人： Jean-François Guichou ,  Cédric Bories ,  Clément Geoffroy ,  Charline Duquenne ,  Muriel Gelin ,  Gilles Labesse ,  Yannick Bessin ,  Loic Mathieu

IPC分类号： A61K31/4353 ,  C07D471/04 ,  A61P35/00 ,  C07D519/00 ,  C07F9/6561 ,  C07D491/048 ,  C07D491/113 ,  C07D491/107

CPC分类号： C07D471/04 ,  A61K31/4353 ,  A61P35/00 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113 ,  C07D519/00 ,  C07F9/6561

摘要： The present invention concerns a compound of formula (I), or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds.

公开(公告)号：US10995089B2

公开(公告)日：2021-05-04

申请号：US15777386

申请日：2016-11-17

申请人： AGV Discovery ENSCM ,  Institut National de la Sante et de la Recherche Medicale (INSERM) ,  Centre National de la Recherche Scientifique (CNRS) ,  Universite de Montpellier

发明人： Jean-François Guichou ,  Cédric Bories ,  Clément Geoffroy ,  Charline Duquenne ,  Muriel Gelin ,  Gilles Labesse ,  Yannick Bessin ,  Loic Mathieu

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D519/00 ,  C07F9/6561 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113

摘要： The present invention concerns a compound of formula (I): H or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds.

公开(公告)号：US20150267181A1

公开(公告)日：2015-09-24

申请号：US14441560

申请日：2013-11-08

申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)

发明人： Pierre-Alexandre Kaminski ,  Gilles Labesse

IPC分类号： C12N9/10 ,  C12N9/24

CPC分类号： C12N9/1077 ,  C12N9/2497 ,  C12Y204/02006

摘要： The present invention relates to enzyme mutants obtained from the nucleoside deoxyribosyltransferase (NDT) of Lactobacilli bacteria. These mutants are surprisingly able to exchange deoxyribose mono-, bi- and triphosphate between various nucleobases. In vitro syntheses have been successfully performed with several nucleobase analogs. These enzyme mutants provide new tools to synthesize, in vitro and/or in vivo, dNTPs or analogs thereof.

摘要翻译： 本发明涉及从乳杆菌属细菌的核苷脱氧核糖基转移酶（NDT）获得的酶突变体。 这些突变体令人惊奇地能够在各种核碱基之间交换脱氧核糖单，双和三磷酸。 已经使用几种核碱基类似物成功地进行了体外合成。 这些酶突变体提供了在体外和/或体内合成dNTP或其类似物的新工具。

公开(公告)号：US10106493B2

公开(公告)日：2018-10-23

申请号：US14906206

申请日：2014-07-17

申请人： INSTITUT DE RECHERCHE POUR LE DEVELOPPEMENT (I.R.D.) ,  UNIVERSITE DE MONTPELLIER ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

发明人： Denis Sereno ,  Gilles Labesse ,  Jean-Francois Alexandre Guichou ,  Corinne Loeuillet ,  Deborah Isabelle Garcia ,  Stephane Delbecq

IPC分类号： C07C259/06 ,  C07C259/10 ,  C07C311/19 ,  C07C311/21 ,  C07D277/30

摘要： Compounds of formula wherein n is 0, 1 or 2; X is and Ar is a benzyl substituted at the meta position by a C1 to C8 alkoxy group, or a pharmaceutically acceptable salt thereof, for treating, preventing or inhibiting a parasitic disease, such as toxoplasmosis, in a subject are provided. Methods for preparing the compounds are also presented.