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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
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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
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：EP3945092A1
公开(公告)日：2022-02-02
申请号：EP20305860.7
申请日：2020-07-27
申请人： Etat Français représenté par la Direction Centrale Du Service de Santé des Armées , Centre National de la Recherche Scientifique , Universite de Rouen Normandie , Institut National Des Sciences Appliquées De Rouen
发明人： PROBST, Nicolas , BRAÏKI, Anissa , JEAN, Ludovic , RENARD, Pierre-Yves , DIAS, José , NACHON, Florian
IPC分类号： C07D401/06 , C07D401/14 , C07D409/06 , C07D417/06 , A61K31/44 , A61K31/425 , A61K31/433 , A61P25/00
摘要： The present invention relates to compounds for their use in the reactivation of butyrylcholinesterase. Such compounds are useful in the treatment or prevention of the intoxication with at least one organophosphorus nerve agent. The invention also relates to pharmaceutical compositions and kits comprising said compounds, and compounds per se.
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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
IPC分类号： C07D213/78 , C07D401/06 , C07D473/02 , C07D473/34 , A61K31/44 , A61K31/444 , A61K31/52 , A61K31/522 , A61P25/00
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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
IPC分类号： C07D213/74 , C07D401/12 , A61K31/4709 , A61P25/00
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公开(公告)号：EP4211129A1
公开(公告)日：2023-07-19
申请号：EP21773805.3
申请日：2021-09-10
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 , NIMMAKAYALA, Mallikarjuna Reddy , DIAS, José , NACHON, Florian , VOROS, Camille , RAZAFINDRAINIBE, Raymond Franck
IPC分类号： C07D405/06 , C07D409/06 , A61K31/4436 , A61P39/02 , C07D407/06 , C07D519/00
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公开(公告)号：EP3967681A1
公开(公告)日：2022-03-16
申请号：EP20306013.2
申请日：2020-09-11
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 , University Of Southampton
发明人： BAATI, Rachid , BROWN, Richard , DIAS, José , MARYAN-INSTONE, Alex , NACHON, Florian , YERRI, Jagadeesh
IPC分类号： C07D213/65 , C07D401/06 , A61K31/496 , A61K31/44 , A61P25/00 , A61P25/28 , A61P35/00
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; in the treatment of neurological diseases such as Alzheimer's disease; and/or in the treatment of cancer.-
公开(公告)号：EP3331859A1
公开(公告)日：2018-06-13
申请号：EP16747883.3
申请日：2016-07-29
IPC分类号： C07D213/74 , C07D401/12 , A61K31/4709 , A61P25/00
CPC分类号： C07D401/12 , C07D213/74
摘要： The present invention deals with novel compounds which are reactivators of human acetylcholinesterase, pharmaceutical compositions comprising said compounds, and their use in the treatment of a nervous and/or respiratory failure due to intoxication with at least one organophosphorous nerve agent such as warfare agents and pesticides. It also pertains to these compounds for use in the treatment of neurological diseases such as Alzheimer's disease.
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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
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.-
公开(公告)号：EP3696170A1
公开(公告)日：2020-08-19
申请号：EP19305185.1
申请日：2019-02-15
IPC分类号： C07D213/78 , C07D401/06 , C07D473/02 , C07D473/34 , A61K31/44 , A61K31/444 , A61K31/52 , A61K31/522 , A61P25/00
摘要： The present invention relates to a compound of formula (I), or one of its pharmaceutically acceptable salts:
wherein R1, R2 and -X-Y- have specific definitions.
It also relates to the use of such a compound as reactivator of acetylcholinesterase for treating organophosphorous nerve agents poisoning; and to a process for preparing it.
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