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 R'R"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 specified in C1-C6alkyl optionally substituted by C1-C3alkoxycarbonyl, halogen, 5-6-merous heteroaryl together with nitrogen atom, or oxygen atom or nitrogen atom as heteroatom; C3-C6cycloalkyl; phenyl optionally substituted by halogen, C1-C3alkyl, C1-C3alkoxy, C1-C3alkoxycarbonyl, C1-C3alkylenedioxygroup; 5-6-merous heteroarym with nitrogen atom, or oxygen atom or nitrogen atom as heteroatom optionally substituted by carboxy, C1-C3alkoxycarbonyl; aminocarbonyl group substituted by C1-C3alkyl; sulphonyl group specified in alkylsuphonyl optionally substituted by hydroxyl group, cyano group, phenyl, which is optionally substituted by C1-C3alkyl, halogen, C1-C3alkoxy group; henylsulphonyl oprtionally substituted by C1-C3alkyl, halogen, C1-C3alkoxy group, cyano group, C1-C3alkylene dioxygroup, or 5-6-merous heteroarylsulphonyl with nitrogen atom, or sulphur atom, or oxygen atom as heteroatom optionally substituted by halogen, C1-C3alkyl, C1-C3alkoxy group; R3 represents hydrogen.
EFFECT: compounds can be used for preparing the pharmaceutical composition applicable in treating or preventing metabolic diseases, such as diabetes, obesity, diabetic obesity, metabolic syndrome, hypercholesterolemia, dislipidemia.
14 cl, 17 dwg, 8 tbl, 16 ex
| Title | Year | Author | Number |
|---|---|---|---|
| ANELLATED 9-HYDROXY-1,8-DIOXO-1,3,4,8-TETRAHYDRO-2H-PYRIDO[1,2-A]PYRAZINE-7-CARBOXAMIDES - INTEGRASE INHIBITORS, METHODS FOR PREPARING AND USING THEREOF | 2019 |
|
RU2717101C1 |
| SUBSTITUTED 3,4,12,12A-TETRAHYDRO-1H-[1,4]OXAZINO[3,4-C]PYRIDO[2,1-F][1,2,4]TRIAZINE-6,8-DIONE, PHARMACEUTICAL COMPOSITION, METHODS FOR PRODUCTION AND USE THEREOF | 2019 |
|
RU2720305C1 |
| HETEROCYCLIC INHIBITORS OF Hh-SYGNAL CASCADE, BASED ON THEM MEDICINAL COMPOSITIONS AND METHOD OF TREATING DISEASES INDUCED BY ABBARANT ACTIVITY OF Hh-SIGNAL SYSTEM | 2007 |
|
RU2364597C1 |
| INCRETIN SECRETAGOGUES, METHODS FOR PREPARING AND APPLYING THEM | 2011 |
|
RU2456287C1 |
| ANTI-RNA VIRAL, INCLUDING ANTI-CORONAVIRUS AGENT - SUBSTITUTED QUINOXALINE, PHARMACEUTICAL COMPOSITION AND APPLICATIONS | 2020 |
|
RU2744429C1 |
| SUBSTITUTED PYRIDO[4',3':5,6]PYRANO[2,3-d]PYRIMIDINES AND COMBINATORY LIBRARY | 2004 |
|
RU2269538C1 |
| 2-ALKYLAMINO-3-ARYLSULPHONYLCYCLOALKANO [e OR d]PYRAZOLO[1,5-a] PYRIMIDINES SEROTONIN 5-HT RECEPTOR ANTAGONISTS, METHODS FOR MAKING AND APPLYING THEREOF | 2008 |
|
RU2377244C1 |
| (3-ARYLSULPHONYL QUINOLIN-8-YL-DIALKYL-AMINES - SELECTIVE SEROTONIN 5-HT RECEPTOR ANTAGONISTS, METHODS FOR PRODUCTION AND USE THEREOF | 2012 |
|
RU2500672C1 |
| HEPATITIS B (HBV) INHIBITOR | 2017 |
|
RU2666727C1 |
| MEDICATION, REDUCING DESIRE FOR ALCOHOL, PHARMACEUTICAL COMPOSITION AND METHODS OF ITS OBTAINING, MEDICATION AND TREATMENT METHOD | 2008 |
|
RU2401831C2 |
