公开(公告)号：EP3924334A1

公开(公告)日：2021-12-22

申请号：EP20705063.4

申请日：2020-02-14

申请人： Centre national de la recherche scientifique ,  Université de Strasbourg ,  ETAT FRANCAIS (Ministère des armées), representé par la Direction Centrale du Service de Santé des Armées

发明人： BAATI, Rachid ,  BROWN, Richard ,  DIAS, José ,  MARYAN-INSTONE, Alex ,  YERRI, Jagadeesh

IPC分类号： C07D213/78 ,  C07D401/06 ,  C07D473/02 ,  C07D473/34 ,  A61K31/44 ,  A61K31/444 ,  A61K31/52 ,  A61K31/522 ,  A61P25/00

公开(公告)号：EP3331859B1

公开(公告)日：2019-10-02

申请号：EP16747883.3

申请日：2016-07-29

申请人： Centre National de la Recherche Scientifique ,  Université de Strasbourg

发明人： BAATI, Rachid ,  BROWN, Richard, C., D. ,  DIAS, José ,  NACHON, Florian ,  DE SOUSA, Julien

IPC分类号： C07D213/74 ,  C07D401/12 ,  A61K31/4709 ,  A61P25/00

公开(公告)号：EP4211127A1

公开(公告)日：2023-07-19

申请号：EP21777280.5

申请日：2021-09-10

申请人： Centre national de la recherche scientifique ,  Université de Strasbourg ,  Etat Français, Service de Santé des Armées représenté par le délégué général de l'armement DGA/S2IE/SDSIE/BPI

发明人： BAATI, Rachid ,  NIMMAKAYALA, Mallikarjuna Reddy ,  DIAS, José ,  NACHON, Florian ,  VOROS, Camille ,  RAZAFINDRAINIBE, Raymond Franck

IPC分类号： C07D401/06 ,  C07D403/06 ,  A61K31/501 ,  A61P39/02

公开(公告)号：EP3915983A1

公开(公告)日：2021-12-01

申请号：EP20305545.4

申请日：2020-05-26

申请人： Centre National de la Recherche Scientifique ,  Université de Strasbourg ,  Etat Français représenté par la Direction Centrale Du Service de Santé des Armées

发明人： BAATI, Rachid ,  DIAS, José ,  NACHON, Florian ,  NIMMAKAYALA, Mallikarjuna Reddy

IPC分类号： C07D417/08 ,  C07D413/08 ,  C07D417/12 ,  A61K31/427 ,  A61K31/422 ,  A61K31/4439 ,  A61P39/00 ,  A61P39/02 ,  A61P25/28 ,  A61P35/00

摘要： The present invention relates to a compound of formula (I):

wherein X is O or S; Y is -CH 2 -CH 2 -, -C=C- or -CH=CH-; Z is -CH 2 -; n is an integer from 0 to 4; and R is an alkyl group, an aryl, a heteroaryl, a cycloalkyl, a heterocyclyl, a biomolecule, a fluorescent probe, or a group -N(R1 )(R2); wherein R1 and R2 are each independently H, an alkyl group, an aryl, a heteroaryl or a cycloalkyl.
It also relates to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable support.
Finally, it relates to the use of such a compound as a medicine, preferably in the treatment of a nervous and/or respiratory failure due to intoxication with at least one organo-phosphorous nerve agent (OPNA); in the treatment of neurological diseases such as Alzheimer's disease; and/or in the treatment of cancer.
The compounds act as reactivators of OPNA-inhibited hAChE (human acetylcholinesterase).
The present description discloses the syntheses of exemplary compounds as well as experimental data on the in vitro reactivation of human acetylcholinesterase (hAChE) by the compounds of the invention (e.g. pages 28 to 56; examples 1 and 2; compounds; tables 1 to 3).
Exemplary compounds are e.g.:

or

公开(公告)号：EP3473618A1

公开(公告)日：2019-04-24

申请号：EP17306407.2

申请日：2017-10-17

申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

发明人： BAATI, Rachid ,  YERRI, Jagadeesh

IPC分类号： C07D401/06 ,  C07D405/06 ,  C07D519/00 ,  C07D213/53 ,  A61K31/44 ,  A61K31/4427 ,  A61P25/00 ,  A61P35/00 ,  A61P31/12

摘要： The present invention relates to a compound of formula (I), as well as to a process for preparing the compounds of formula (I) by a chemoselective Sonogashira reaction.
It also relates to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable support.
Finally, it relates to the use of such a compound as a medicine, preferably in the treatment of a nervous and/or respiratory failure due to intoxication with at least one organophosphorous nerve agent; in the treatment of neurological diseases such as Alzheimer's disease; and/or in the treatment of cancer; and/or for use as antiviral drug.

公开(公告)号：EP4211113A1

公开(公告)日：2023-07-19

申请号：EP21773405.2

申请日：2021-09-09

申请人： Centre National de la Recherche Scientifique ,  Etat Français, Service de Santé des Armées représenté par le délégué général de l'armement DGA/S2IE/SDSIE/BPI ,  Université de Strasbourg

发明人： BAATI, Rachid ,  BROWN, Richard ,  DIAS, José ,  MARYAN-INSTONE, Alex ,  NACHON, Florian ,  YERRI, Jagadeesh ,  VOROS, Camille

IPC分类号： C07D213/65 ,  C07D401/06 ,  A61K31/496 ,  A61K31/44 ,  A61P25/00 ,  A61P25/28 ,  A61P35/00

公开(公告)号：EP4157838A1

公开(公告)日：2023-04-05

申请号：EP21728220.1

申请日：2021-05-25

申请人： Centre national de la recherche scientifique ,  Université de Strasbourg ,  Etat Français représenté par la Direction Centrale Du Service de Santé des Armées

发明人： BAATI, Rachid ,  DIAS, José ,  NACHON, Florian ,  RAZAFINDRAINIBE, Raymond Franck ,  NIMMAKAYALA, Mallikarjuna Reddy ,  VOROS, Camille

IPC分类号： C07D417/08 ,  C07D413/08 ,  C07D417/12 ,  A61K31/427 ,  A61K31/422 ,  A61K31/4439 ,  A61P39/00 ,  A61P39/02 ,  A61P25/28 ,  A61P35/00

公开(公告)号：EP3697769A1

公开(公告)日：2020-08-26

申请号：EP18785971.5

申请日：2018-10-17

申请人： Centre National de la Recherche Scientifique

发明人： BAATI, Rachid ,  YERRI, Jagadeesh ,  DIAS, José

IPC分类号： C07D401/06 ,  C07D405/06 ,  C07D519/00 ,  C07D213/53 ,  A61K31/44 ,  A61K31/4427 ,  A61P25/00 ,  A61P35/00 ,  A61P31/12

公开(公告)号：EP3071558A1

公开(公告)日：2016-09-28

申请号：EP14799803.3

申请日：2014-11-19

申请人： Université de Strasbourg ,  Commissariat à l'Energie Atomique et aux Energies Alternatives ,  Centre National de la Recherche Scientifique ,  Universite de Rouen ,  L'ETAT (MINISTÈRE DE LA DÉFENSE), REPRÉSENTÉ PAR LE DIRECTEUR CENTRAL DU SERVICE DE SANTÉ DES ARMÉES

发明人： BAATI, Rachid ,  KLIACHYNA, Maria ,  NUSSBAUM, Valentin ,  RENARD, Pierre-Yves ,  JEAN, Ludovic ,  WEIK, Martin ,  NACHON, Florian ,  TOUVREY, Mélanie ,  FRIEDEL, Mélanie ,  RENOU, Julien ,  VERDELET, Tristan ,  MERCEY, Guillaume ,  COLLETIER, Jacques-Philippe ,  SANSON, Benoît ,  SANTONI, Gianluca

IPC分类号： C07D401/12 ,  A61K31/473 ,  A61P25/00

CPC分类号： C07D401/12

摘要： The present invention deals with compounds of formula (I) which are novel uncharged reactivators of human acetylcholinesterase, pharmaceutical compositions comprising said compounds, and their use for reactivating human acetylcholinesterase inhibited by at least one organophosphorus nerve agent.

公开(公告)号：EP3967686A1

公开(公告)日：2022-03-16

申请号：EP20306011.6

申请日：2020-09-11

申请人： Centre national de la recherche scientifique ,  Université de Strasbourg ,  Etat Français, Service de Santé des Armées représenté par le délégué général de l'armement DGA/S2IE/SDSIE/BPI

发明人： BAATI, Rachid ,  NIMMAKAYALA, Mallikarjuna Reddy ,  DIAS, José ,  NACHON, Florian

IPC分类号： C07D401/06 ,  A61K31/501 ,  A61P39/02

摘要： The present invention relates to a compound of formula (I).

It also relates to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable support.
Finally, it relates to the use of such a compound as a medicine, preferably in the treatment of a nervous and/or respiratory failure due to intoxication with at least one organophosphorous nerve agent by reactivation of AChE; in the treatment of neurological diseases such as Alzheimer's disease; and/or in the treatment of cancer.