BENZODIOXOLE DERIVATIVE AND PREPARATION METHOD AND USE THEREOF

• Main Authors: LIU, LIFEI, ZHONG, JINQING, GONG, YONGXIANG, ZHU, QIFENG, BAI, HUA, ZHAO, XUYANG, LIU, XIAOYU, ZHENG, XIAOHE
• Format: Patent
• Language: English; French
• Published: 05.05.2020
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Provided in the present invention are benzodioxole derivatives and preparation methods thereof. These compounds represented by formula (I) or pharmaceutically acceptable salts thereof have acetylcholinesterase inhibitory activity, so can be used in the treatment or prevention of Alzheimer's disease: R1 and R2 are independently selected from the group consisting of hydrogen, methyl and ethyl; or R1 and R2 together form =O; or R1 and R2 together with the carbon atom connecting them form a 3-membered carbon ring. A is selected from the group consisting of phenyl, R3-substituted phenyl, pyridinyl, R4-substituted pyridinyl, pyrimidinyl, R5-substituted pyrimidinyl, pyrrolyl, R6-substituted pyrrolyl, pyridazinyl, R7-substituted pyridazinyl, pyrazolyl, and R8-substituted pyrazolyl. R3 to R7 each independently is selected from the group consisting of halogen, (C1¨C3) alkyl, (C2¨C3) alkenyl, (C3¨C4) cycloalkyl, (C1¨C3) alkoxy, trifluoromethyl and cyano. le is selected from the group consisting of (C1¨C3) alkyl, (C2¨C3) alkenyl and (C3¨C4) cycloalkyl. (see above formula) La présente invention porte sur de nouveaux dérivés de benzodioxole et sur leur procédé de préparation. Ces composés de formule (I) ou leurs sels pharmaceutiquement acceptables ont une activité d'inhibition de l'acétylcholine estérase, de sorte qu'ils peuvent être utilisés dans le traitement ou la prévention de la maladie d'Alzheimer. R1, R2 et A dans la formule (I) sont tels que définis dans la description.