http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-3915983-A1

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filingDate 2020-05-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6cc391c1a2b4f6804585eac2480cc42e
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d980c45b9e9a33bed3139fddad929af9
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publicationDate 2021-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-3915983-A1
titleOfInvention Pyridine-thiazole-oxime and pyridine-oxazole-oxime derivatives as reactivators of organophosphorous nerve agent (opna)-inhibited human acetylcholinesterase for the treatment of nervous and/or respiratory failure after intoxication with opna
abstract The present invention relates to a compound of formula (I):wherein X is O or S; Y is -CH<sub>2</sub>-CH<sub>2</sub>-, -C=C- or -CH=CH-; Z is -CH<sub>2</sub>-; 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
priorityDate 2020-05-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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