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ГЕТЕРОЦИКЛИЧЕСКИЕ АГОНИСТЫ РЕЦЕПТОРОВ ЖЕЛЧНЫХ КИСЛОТ TGR5, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
专利权人:
IVASHCHENKO ANDREJ ALEKSANDROVICH
发明人:
IVASHCHENKO ANDREJ ALEKSANDROVICH,Иващенко Андрей Александрович,SAVCHUK NIKOLAJ FILIPPOVICH,Савчук Николай Филиппович,TKACHENKO SERGEJ EVGENEVICH,Ткаченко Сергей Евгеньевич,KHVAT ALEKSANDR VIKTOROVICH
申请号:
RU2013108339/04
公开号:
RU0002543485C2
申请日:
2013.02.26
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of general formula I, or their racemic mixture, or their individual optic isomers, or pharmaceutically acceptable salts possessing the properties of TGR bile acid receptor agonist. The invention also refers to methods for preparing the compounds. In general formula I , X represents amino group RR"N, wherein the substitutes R and R" can be optionally identical, or represents hydrogen, C1-C6alkyl, C3-C6cycloalkyl substituted C1-C6alkyl, wherein the substitute is specified in phenyl or phenoxy, each of which can be substituted by halogen in turn, C1-C3alkyl, C1-C3alkoxy, phenyloxy, C3-C6cycloalkyl, 5-6-merous heteroaryl with 1 nitrogen atom aryl specified in phenyl optionally substituted by fluorine, C1-C3alkyl, C1-C3 alkoxy 5-6-merous heteroaryl with nitrogen atom as heteroatom C2-C4alkenyl, acyl specified in C1-C6alkylcarbonyl or C3-C6cycloalkylcarbonyl or substituted oxygroup, which represents hydroxy group, wherein hydrogen is substituted by C1-C6alkyl optionally substituted by hydroxy, di(C1-C3alkyl)amino, phenyl, which can be substituted by halogen in turn, C1-C3alkyl, C1-C3alkoxy C2-C4alkenyl and 5-6-merous heterocyclyl with nitrogen atom, or sulphur atom, or oxygen atom as heteroatom R1a and R1b represents hydrogen, C1-C3alkyl, or R1a and R1b together form methylene chain -(CH2)n-, wherein n=2-5 R1c and R1d represents hydrogen, C1-C3alkyl R2 represents acyl group specified in C1-C6alkylcarbonyl, wherein alkyl can be substituted by phenyl or phenoxy, each of which can be substituted by halogen in turn, C1-C3alkyl, C1-C3alkoxy C3-C6cycloalkylcarbonyl phenylcarbonyl, which can be substituted by halogen, C1-C3alkyl, C1-C3alkoxygroup, oxygroup, C1-C3alkylene dioxygroup 5-6-merous heteroarylcarbonyl with nitrogen atom, or oxygen atom, or sulphur atom as heteroatom, optionally substituted by carboxy, halogen or C1-C3alkoxycarbonyl, substituted aminocarbonyl group, wherein the substitute can be spe
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