Novel ureido - and amido-pyrazolone derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 231/50 (2006.01) A61K 31/4152 (2006.01) A61K 31/4155 (2006.01) A61P 1/00 (2006.01) A61P 25/04 (2006.01) C07D 403/12 (2006.01)

Patent

CA 2527194

The present invention provides compounds of formula (I); wherein each of R1 to R4 is independently selected from hydrogen, a halogen, a substituted or unsubstituted cyclic and heterocyclic moiety, substituted or unsubstituted, linear or branched alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, alkenyl, alkenyloxy, alkenylcarbonyl, alkenyloxycarbonyl, alkynyl, alkynyloxy, alkynylcarbonyl, alkynyloxycarbonyl, aryl, benzyl, arlyoxy, arylcarbonyl, aryloxycarbonyl and sulphur equivalents of said oxy, carbonyl and oxycarbonyl moieties, and A is NH, or (CH2)n, where n is preferably 0, 1 or 2. The invention also relates to methods for preparing the compounds and their uses as CCK receptor ligands and CCK antagonists.

La présente invention se rapporte à des composés représentés par la formule (I), dans laquelle : R¿1?, R¿2, ?R¿3? et R¿4 ?sont chacun indépendamment sélectionnés parmi hydrogène, un halogène, une fraction cyclique et hétérocyclique substituée ou non substituée, alkyle, alkyloxy, alkylcarbonyle, alkyloxycarbonyle, alcényle, alcényloxy, alcénylcarbonyle, alcényloxycarbonyle, alcynyle, alcynyloxy, alcynylcarbonyle, alcynyloxycarbonyle, aryle, benzyle, aryloxy, arylcarbonyle, aryloxycarbonyle, linéaires ou ramifiés et substitués ou non substitués, et des équivalents sulfurés desdites fractions oxy, carbonyle et oxycarbonyle ; et A représente NH, ou (CH¿2?)¿n?, n étant de préférence égal à 0, 1 ou 2. L'invention concerne également des procédés permettant de préparer lesdits composés, ainsi que leur utilisation comme ligands des récepteurs CCK et comme antagonistes de la CCK.

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