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BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS FOR USE THEREOF
专利权人:
INK.;ENANTA FARMASYUTIKALS
发明人:
VENG Gotsyan (US),ВЭНГ Гоцян (US),OR Yat Sun (US),ОР Ят Сун (US),SHEN Zhujchao (US),ШЕНЬ Жуйчао (US),LUN Tszyan (US),ЛУН Цзян (US),DAJ Pen (US),ДАЙ Пэн (US),SIN Syuechao (US),СИН Сюэчао (US),KHE Tszin
申请号:
RU2017120970
公开号:
RU0002707280C2
申请日:
2015.11.27
申请国别(地区):
RU
年份:
2019
代理人:
摘要:
FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to a compound represented by formula I, or a pharmaceutically acceptable salt thereof. In the IRa formula is hydrogen or -C1-C8 alkyl; Rb is selected from a group consisting of: 1) -C(O)NR'10R'11; 2) -C(O)NHSO2R1; and 3) -SO2R1; R1 is selected from a group consisting of: 1) -C1-C8 alkyl, unsubstituted or substituted with halogen, phenyl, carboxyl or hydroxyl; 2) -C3-C8 cycloalkyl, unsubstituted or substituted C1-C6 alkyl or halogen; bicyclo[2.2.1]heptane or 2-oxo-7,7-dimethylbicyclo[2.2.1]heptane; 3) phenyl unsubstituted or substituted with halogen, C1-C6 alkyl, halogen-C1-C6 alkyl, hydroxy-C1-C6 alkyl, C1-C6 alkoxy, halogen-C1-C6 alkoxy, piperidinyl, di(C1-C6 alkyl)amine, C3-C8 cycloalkyl, C3-C8 cycloalkyl substituted with halogen-C1-C6 alkyl, phenyl, carboxy, C1-C6 alkyloxycarbonyl, methoxycarbonyl-C1-C6 alkyl, 2-methylthiazol-4-yl, 4-methylthiazol-2-yl, isoxazol-5-yl, 2-methyloxazol-5-yl or 1,3,4-oxadiazol-2-yl; 1,3-benzodioxole; 1,4-benzodioxane; indane; naphthyl or 1,2,3,4-tetrahydronaphthalene; 4) 6-member heterocycloalkyl, in which two ring heteroatoms are selected from N, O and S, substituted with one or two groups selected from C1-C6 alkyl, oxo, C1-C6 alkylcarbonyl or 3-azabicyclo [3.1.0] hexane; 2-oxo-7-azaspiro[3.5]nonane or 6-azaspiro[2.5]octane; 5) five- or six-membered heteroaryl, in which one or two ring heteroatoms are selected from S and N, unsubstituted or substituted with C1-C6 alkyl, phenyl; 2,3-dihydroindole, substituted with acetyl, or quinoline, and 6) -NR10R11; R2 is hydrogen; m is selected from 0, 1, 2 and 3; R3 is hydrogen or hydroxyl; R4 is hydrogen; R5 and R6 are independently selected from hydrogen or a protecting group for a hydroxy group selected from tert-butyldimethylsilyl, acetyl and N-methylcarbamoyl; R7 is selected from -C1-C8 alkyl; R10 and R11 each is independently selected from hydrogen and -C1-C8 alkyl, or R10 and R11, taken together with the nitrogen atom to which
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