Novel 1-phenylcycloalkanecarboxylic acid derivatives as potential anticonvulsant agents
摘要:
A series of analogues based on the anticonvulsant carbetapentane (1, 2-[2-(diethylamino)ethoxy]ethyl 1-phenyl-1-cyclopentylcarboxylate) was prepared as potential novel anticonvulsant drugs. Structure-activity relationships of analogues in which the ester function and cyclopentane moieties were modified have been investigated by evaluating their ability to prevent seizures in the rat maximal electroshock test. These compounds (11, ED50 = 16-mu-mol/kg; 12, ED50 = 86-mu-mol/kg, and 23, ED50 = 173-mu-mol/kg) were effective anticonvulsants. Compound 11, an alkyl ether derivative of 1, was more potent than the parent compound (ED50 = 48-mu-mol/kg) and also showed a 2-fold increase in potency compared to that of the prototypic anticonvulsant drug diphenylhydantoin.
[EN] NITROGEN-CONTAINING HETEROCYCLIC COMPOUND<br/>[FR] COMPOSÉ HÉTÉROCYCLIQUE CONTENANT DE L'AZOTE
申请人:TAKEDA PHARMACEUTICAL
公开号:WO2013018929A1
公开(公告)日:2013-02-07
The present invention provides a novel compound having a superior activity as an ERR-α modulator and useful as an agent for the prophylaxis or treatment of ERR-α associated diseases. The present invention relates to a compound represented by the formula (1) wherein each symbol is as defined in the specification, or a salt thereof.
The present invention provides a novel compound having a superior activity as an ERR-α modulator and useful as an agent for the prophylaxis or treatment of ERR-α associated diseases.
The present invention relates to a compound represented by the formula
wherein each symbol is as defined in the specification, or a salt thereof.