PYRAZINONE DERIVATIVES AS INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES

The present invention relates to a compound of formula (I) as insulin secretion stimulators, wherein the compound of formula (I) has the structure: (see formula I) wherein n = 2; R1 is alkyl, alkenyl or alkynyl optionally substituted by one or more Y; R2 is hydrogen; R3 is hydrogen, halogen or aryl...

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Hauptverfasser: CHARON, CHRISTINE, ELBAWAB, SAMER, BOTTON, GERARD, KERGOAT, MICHELINE
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:The present invention relates to a compound of formula (I) as insulin secretion stimulators, wherein the compound of formula (I) has the structure: (see formula I) wherein n = 2; R1 is alkyl, alkenyl or alkynyl optionally substituted by one or more Y; R2 is hydrogen; R3 is hydrogen, halogen or aryl optionally substituted by one or more Y; R4 is: arylalkyl or aryloxyalkyl optionally substituted by one or more Y; or R4 is (see above formula) wherein: m = 1-6; R7 and R8 together constitute a heterocycle including one or more heteroatoms from N, O and S; Y is hydroxy, thio, halogen, cyano, trifluoromethoxy, trifluoromethyl, carboxy, carboxy methyl, carboxyethyl, alkyl, alkoxy, alkylamino, aryl, aryl sulfonylalkyl, aryloxy, arylalkoxy, amino, NR5R6, azido, nitro, guanidino, amidino, phosphono, oxo, carbamoyl, alkylsulfonyl, alkylsulfinyl or alkylthio, or two Y groups form a methylenedioxy; wherein R5 and R6 are independently hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl; wherein alkyl, aryl and heteroaryl groups are optionally substituted by one or more Y; or R5 and R6 together constitute a heterocycle including one or more heteroatoms from N, O and S; or a racemic form, tautomer, enantiomer, diastereomer, epimer or polymorph, or a mixture thereof, or a pharmaceutically acceptable salt thereof. La présente invention concerne des dérivés de pyrazinone de la formule (I), dans laquelle n, R1, R2, R3 et R4 sont tels que définis dans la revendication 1, comme stimulateurs de la sécrétion dinsuline. Linvention concerne également la préparation et lutilisation de ces dérivés de pyrazinone pour la prophylaxie et/ou le traitement du diabète et des pathologies associées.