Novel 1,3-dialkylurea derivatives having a hydroxyl group

Details Novel 1,3-dialkylurea derivatives having a hydroxyl group Novel 1,3-dialkylurea derivatives having a hydroxyl group

C - Chemistry, Metallurgy

07

C

C07C 275/24 (2006.01) A61K 31/17 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) A61K 31/33 (2006.01) C07C 323/59 (2006.01) C07D 209/20 (2006.01) C07D 233/64 (2006.01) C07D 317/60 (2006.01)

Patent

CA 2180021

A compound represented by general formula (I) and salts thereof, wherein R1 and R4 represent carboxyl optionally converted into an ester, amide or hydroxamate group; R2 represents lower alkyl or phenyl lower alkyl; and R3 represents hydrogen, lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, hydroxy lower alkyl, mercapto lower alkyl, carboxy lower alkyl, lower alkoxycarbonyl lower alkyl, imidazolyl lower alkyl, indolyl lower alkyl, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted naphthyl or optionally substituted naphthyl lower alkyl. The compound has an inhibitory effect on endopeptidase 24.11 and being useful as a remedy for cardiovascular diseases such as cardiac insufficiency and hypertension, kidney diseases such as renal insufficiency, gastrointestinal disorders such as diarrhea and gastric hyperacidity, endocrine/metabolic diseases such as obesity, and autoimmune diseases such as rheumatism, and as an analgesic agent for muscular pain, hemicrania, etc.

Cette invention se rapporte à un composé représenté par la formule générale (I) et à des sels de ce composé. Dans cette formule, R?1¿ et R?4¿ représentent carboxyle éventuellement converti en un groupe ester, amide ou hydroxamate; R?2¿ représente alkyle inférieur ou phényle alkyle inférieur; et R?3¿ représente hydrogène, alkyle inférieur, amino alkyle inférieur, alkylamino inférieur alkyle inférieur, hydroxy alkyle inférieur, mercapto alkyle inférieur, carboxy alkyle inférieur, alcoxycarbonyle inférieur alkyle inférieur, imidazolyle alkyle inférieur, indolyle alkyle inférieur, phényle éventuellement substitué, phényle alkyle inférieur éventuellement substitué, naphtyle éventuellement substitué ou naphtyle alkyle inférieur éventuellement substitué. Ce composé possède un effet inhibiteur sur l'endopeptidase 24.11 et il est par conséquent utile comme médicament contre les troubles cardio-vasculaires, tels que l'insuffisance cardiaque et l'hypertension, contre les maladies du foie, telles que l'insuffisance rénale, contre les troubles gastro-intestinaux, tels que la diarrhée et l'hyperacidité gastrique, contre les maladies endocrines/métaboliques telles que l'obésité, et contre les maladies auto-immunes, telles que les rhumatismes, et également comme agent analgésique contre les douleurs musculaires, l'hémicranie, etc.

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