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 relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.
本发明涉及公式III和V的化合物,这些化合物可用作药物制剂,特别是作为自噬抑制剂。
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
申请人:MATSUMOTO Shigemitsu
公开号:US20130072467A1
公开(公告)日:2013-03-21
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.