Succinamic acid compound, production method thereof and use...

Details Succinamic acid compound, production method thereof and use... Succinamic acid compound, production method thereof and use...

C - Chemistry, Metallurgy

07

D

C07D 277/64 (2006.01) A61K 31/425 (2006.01)

Patent

CA 2171756

Provision of a succinamic acid compound of the formula (1) Image (1) wherein R1 is an alkyl or a lower alkenyl and R2 is an optionally esterified carboxyl, a pharmaceutically acceptable salt thereof, an agent for the prophylaxis and/or treatment of the complications of diabetes, comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, an aldose reductase inhibitor comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, and a method for producing the succinamic acid compound or a pharmaceutically acceptable salt thereof. The novel succinamic acid compounds of the formula (1) of the present invention and pharmaceutically acceptable salts thereof have a strong aldose reductase inhibitory activity in mammals such as human, and show superior safety. Hence, they are useful as pharmaceutical agents for the treatment of the complications of diabetes such as faulty union of corneal injury, cataract, neurosis, retinopathy and nephropathy, in particular, cataract and neurosis. According to the production method of the present invention, efficient production of such useful compounds of the present invention can be provided. 2 8

Sont décrits un nouveau composé d'acide succinamique représenté par la formule générale (1), ou bien un sel pharmaceutiquement acceptable de celui-ci; un agent prophylactique et/ou un remède contre les complications du diabète renfermant ce composé ou ce sel comme principe actif; un inhibiteur d'aldose-réductase contenant ce composé ou ce sel comme principe actif; et un procédé pour produire ce composé ou ce sel. Dans la formule (1), R<1> représente alkyle ou alcényle inférieur, et R<2> représente carboxyle qui peut être estérifié. Le composé décrit (1) et son sel possèdent une puissante activité inhibitrice de l'aldose-réductase sur les mammifères, et notamment l'homme, ainsi qu'une excellente innocuité, et sont par conséquent utiles comme remède pour le traitement des complications du diabète, telles que la rupture d'une cicatrisation de lésion cornéenne, la cataracte, la névrose, la rétinopathie et la néphropathie, notamment la cataracte et la névrose. Le procédé décrit permet de produire efficacement lesdits composés.

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