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DERIVES DE PYRAZINONE COMME STIMULATEURS DE LA SECRETION D'INSULINE, LEURS PROCEDES D'OBTENTION ET LEUR UTILISATION POUR LE TRAITEMENT DU DIABETE
专利权人:
MERCK PATENT GMBH
发明人:
BOTTON, GERARD,KERGOAT, MICHELINE,CHARON, CHRISTINE,ELBAWAB, SAMER
申请号:
CA2717753
公开号:
CA2717753C
申请日:
2009.01.15
申请国别(地区):
CA
年份:
2016
代理人:
摘要:
The present invention relates to a compound of formula (I) as insulinsecretion 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 oneor more Y; R2is hydrogen; R3 is hydrogen, halogen or aryl optionally substituted by one ormore Y; R4is: arylalkyl or aryloxyalkyl optionally substituted by one or more Y; or R4is(see above formula)wherein: m = 1-6; R7 and R8 together constitute a heterocycle including one ormoreheteroatoms from N, O and S; Y is hydroxy, thio, halogen, cyano,trifluoromethoxy,trifluoromethyl, carboxy, carboxy methyl, carboxyethyl, alkyl, alkoxy,alkylamino, aryl, arylsulfonylalkyl, aryloxy, arylalkoxy, amino, NR5R6, azido, nitro, guanidino,amidino,phosphono, oxo, carbamoyl, alkylsulfonyl, alkylsulfinyl or alkylthio, or two Ygroups forma methylenedioxy; wherein R5 and R6 are independently hydrogen, alkyl, aryl,arylalkyl,heteroaryl, heteroarylalkyl; wherein alkyl, aryl and heteroaryl groups areoptionallysubstituted by one or more Y; or R5 and R6 together constitute a heterocycleincludingone or more heteroatoms from N, O and S; or a racemic form, tautomer,enantiomer,diastereomer, epimer or polymorph, or a mixture thereof, or a pharmaceuticallyacceptable salt thereof.
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