SAVCHUK NIKOLAJ FILIPPOVICH,Савчук Николай Филиппович (RU),TKACHENKO SERGEJ EVGENEVICH,Ткаченко Сергей Евгеньевич (US),NAZARENKOV DENIS EVGENEVICH,Назаренков Денис Евгеньевич (US)
申请号：
RU2011120084/04
公开号：
RU0002456287C1
申请日:
2011.05.20
申请国别(地区):
RU
年份:
2012
代理人:
摘要：
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new compounds of general formula 1, or their pharmaceutically acceptable salts showing the properties of incretin secretagogues, preferentially the properties of a bile acid receptor TGR5 agonist. The compounds are applicable for treating metabolic diseases associated with glucose metabolism, such as diabetes, obesity, metabolic syndrome, etc. In formula 1 R1, R2 and R3 independently represent a cyclic system substitute specified in: hydrogen, C1-C3alkyl, halogen, a trifluoromethyl group, C1-C3alkoxy, a cyano group, a trifluoromethoxy group an amino group substituted by C1-C3alkyl or two radicals R3, found at carbon neighbours in a benzene ring, together with the benzene ring bound therewith form 3,4-methylene dioxyphenyl R4 represents hydrogen, C1-C5alkyl, a carboxyl group, C1-C3alkoxycarbonyl or an amide group CONHR5 R5 is an optionally substituted by C1-C3alkyl, C5-C6cycloalkyl optionally substituted by phenyl, benzyl, pyridyl X and Y represent two hydrogen atoms or an oxygen atom, provided Y=O, then X=2H, provided Y=2H, then X=O or X=Y=2H the sign (N) shows the possibility of bioisosteric substitution of the benzene ring by the pyridine, pyrimidine, pyridazine, triazine or pyrazine ones.EFFECT: preparing the pharmaceutical composition and the combined drugs with the use of the compounds of formula 1 or the based pharmaceutical composition and a protein kinase DPP-IV inhibitor specified in Vildagliptin or Sitagliptin, and/or an endogenous bile acid or mied bile acid secretagogues.53 cl, 7 dwg, 8 exИзобретение относится к новым соединениям общей формулы 1 или их фармацевтически приемлемым солям, обладающим свойствами стимуляторов секреции инкретиновых гормонов, предпочтительно свойствами агониста рецепторов желчных кислот TGR5. Изобретение также относится к способам их получения, фармацевтическим композициям и комбинированным лекарственным средствам с использованием соединений формулы 1 или фармацевтич
