Substituted benzylurea derivatives and medicine containing...

C - Chemistry – Metallurgy – 07 – C

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C07C 275/28 (2006.01) A61K 31/17 (2006.01) A61K 31/18 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) A61K 31/275 (2006.01) A61K 31/34 (2006.01) A61K 31/38 (2006.01) A61K 31/395 (2006.01) A61K 31/435 (2006.01) C07C 309/42 (2006.01) C07C 311/29 (2006.01) C07C 311/47 (2006.01) C07C 317/22 (2006.01) C07C 323/19 (2006.01) C07C 323/44 (2006.01) C07D 207/337 (2006.01) C07D 213/30 (2006.01) C07D 213/56 (2006.01) C07D 215/14 (2006.01) C07D 217/16 (2006.01) C07D 233/64 (2006.01) C07D 249/02 (2006.01) C07D 261/

Patent

CA 2218300

Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): <see fig. I> wherein R1 and R2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

L'invention porte sur des dérivés de substitution de benzylurée, représentés par la formule générale (1) <voir fig. I>, où R1 et R2 sont indépendamment H, un atome d'halogène, un alkyle ou un alcoxy, R3 est un phényle ou un groupe hétérocyclique avec substitution facultative, n est un entier de 1 à 6, et R4 est un groupe phényle avec substitution facultative; ou sur leurs sels; médicaments renfermant ces dérivés comme ingrédients actifs. Ces dérivés ou leurs sels inhibent fortement et uniquement l'ACAT dans les macrophages et sont donc utiles comme agents de prévention et de traitement pour l'athérosclérose.

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