BONGARTZ Zhan-P'er Andre Mark (BE),БОНГАРТЗ Жан-Пьер Андре Марк (BE),LINDERS Joannes Teodorus Marija (BE),ЛИНДЕРС Йоаннес Теодорус Мария (BE),MERPUL Liven (BE),МЕРПУЛ Ливен (BE),VAN LOMMEN Gi Rozalija,BONGARTZ ZHAN-PER ANDRE MARK,БОНГАРТЗ Жан-Пьер Андре Марк,LINDERS JOANNES TEODORUS MARIJA,ЛИНДЕРС Йоаннес Теодорус Мария,MERPUL LIVEN,МЕРПУЛ Ливен,VAN LOMMEN GI ROZALIJA EHGEN,ВАН ЛОММЕН Ги Розалия Эг
申请号：
RU2009148320/04
公开号：
RU0002470017C2
申请日:
2008.06.06
申请国别(地区):
RU
年份:
2012
代理人:
摘要：
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to DGAT inhibitor of formula (I), its N-oxide, pharmaceutically acceptable salt and solvate, based on it pharmaceutical composition and its application for treatment of diseases, mediated by DGAT activity, such as obesity and diabetes. In general formula (I) A represents CH or N； X represents -C (=O)-C(=O)； -O-C(=O)-； -NRX-C(=O)-； -Z1-C(O)-； -Z1-NRx-C(O)-； -C(O)-Z1-； -NRx-C(O)-Z1-； -S(=O)p-； -NRX-C(=S) -； Y represents NRx-C(=O)-Z2-； -NRx-C(=O)-Z2-NRy-； -NR*-C(=O)-Z2-NRy-C(=O)-； -NRx-C(=O)-Z2-NRy-C(=O)-O-； -NRx-C(O)-Z2-O-； -NRx-C(=O)-Z2-O-C(=O)-； -NRx-C(=O)-Z2-C(=O)-O-； -NRx-C(=O)-Z2-C(=O)-NRy-； -NRx-C(=O)-Z2-NRy-C(=O)-NRy-, -C(<；))-Z2-； -C(=O)-NRx-Z2-； -C(=O)-NRx-Z2-O-； R1 represents C1-12alkyl, optionally substituted with cyano, C1-4alkyloxy, C1-4alkyloxy C1-4alkyloxy, C3-6cycloalkyl or aryl； C2-6alkenyl, C2-6alkinyl； C3-6cycloalkyl； adamantanyl； aryl1； aryl1C1-6alkyl； Het1； or HetC1-6alkyl, on condition that when Y represents -NRxC(=O)-Z2-； -NRx-C(=O)-Z2-NRy； -NRx-C(=O)-Z2-C(=O)-NRy-, -C(=O)Z2-； -NRx-C(=O)-Z2-NRy-C(=O)-NRy-； -C(=O)-NRx-Z2-； -C(=O)-NRx-O-Z2- or -C(=O)-NRx-Z2-NRy-； then R1 can also represent hydrogen； R2 represents R3； R3 represents phenyl, naphthalenyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle, containing 1 or 2 N atoms, where each of said cycles can optionally be substituted with, at least, one substituent, in particular, one-five substituents, said substituents represent halogen, C1-6alkyl, optionally substituted with hydroxy, polyhalogen C1-6alkyl, C1-6alkylthio, polyhalogen-C1-6alkyloxy, carboxyl, hydroxyl, C1-6alkylcarbonyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, nitro, R5R4N-C(=O)-； R5R4N-C1-6alkyl； HetC1-4alkyl, Het-C(=O)-C1-4alkyl, Het-C(=O)-； R8 represents hydrogen, halogen, C1-4alkyl, substituted with hydroxyl Values of other radicals are given in invention formula.EFFECT: obtaining pharmaceutical composition for treatment of diseases, mediated by DGAT activity,
