FIELD: chemistry.
SUBSTANCE: invention relates to 1,5-benzothiazepine derivatives of formula (I). In formula (I): each of R1 and R2 is independently C1-4 alkyl; R3 is independently selected from the group consisting of hydrogen, halogen, hydroxy, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, cyano, nitro, amino, N-(C1-4 alkyl) amino, N, N-di(C1-4 alkyl)amino and N-(aryl-C1-4alkyl)amino; n is integer 1, 2 or 3; R4 is selected from the group consisting of hydrogen, halogen, hydroxy, cyano, C1-4 alkyl, C3-6 cycloalkyl, C1-4 alkoxy, C3-6 cycloalkyloxy, C1-4 alkylthio, C3-6 cycloalkylthio, amino, N-(C1-4 alkyl) amino and N, N-di(C1-4 alkyl) amino; and each of R5A, R5B, R5C and R5D is independently selected from the group consisting of hydrogen, halogen, hydroxy, amino, C1-4 alkyl and C1-4 alkoxy; or a pharmaceutically acceptable salt thereof, provided that the compound is not racemic 3-((7-bromo-3-butyl-3-ethyl-1,1-dioxide-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepine-8-yl)oxy)propanoic acid. Invention also relates to a pharmaceutical composition containing said compounds and to use of said compounds as a medicinal agent.
EFFECT: disclosed compounds are bile acid modulators having activity of inhibiting apical sodium-dependent bile acid transporter (ASBT) and/or hepatic bile acid transport (LBAT) and can be used in the treatment of cardiovascular diseases, disorders of fatty acid metabolism and glucose utilization, gastrointestinal diseases, and liver diseases.
14 cl, 8 tbl, 52 ex
| Title | Year | Author | Number |
|---|---|---|---|
| BENZOTHIA(DI)AZEPINES AND THEIR USE AS BILE ACID MODULATORS | 2019 |
|
RU2785867C2 |
| BENZOTHIADIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACIDS MODULATORS | 2020 |
|
RU2814570C2 |
| BICYCLIC TETRAHYDROTHIAZEPINE DERIVATIVES USEFUL FOR TREATING NEOPLASTIC AND/OR INFECTIOUS DISEASES | 2016 |
|
RU2730524C2 |
| 1,5-BENZOTHIAZEPINES AND EMPLOYMENT THEREOF AS ANTIHYPERLIPIDEMIC DRUGS | 2001 |
|
RU2302414C2 |
| ORTHO-SUBSTITUTED DERIVATIVES OF BENZOIC ACID, METHOD AND INTERMEDIATE COMPOUNDS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND USING | 2003 |
|
RU2288912C2 |
| BENZOIC ACID DERIVATIVES AS PPAR α AND PPAR λ MODULATORS | 2003 |
|
RU2339613C2 |
| 1,4-BENZOTHIAZEPINE-1,1-DIOXIDE, PHARMACEUTICAL COMPOSITION DECREASING BLOOD LIPID LEVEL, METHOD OF TREATMENT OF MAMMAL CLINICAL STATE, METHOD OF SYNTHESIS OF COMPOUND | 1995 |
|
RU2156245C2 |
| MENIN-MLL INTERACTION INHIBITORS | 2017 |
|
RU2799820C2 |
| 5-OXA-2-AZASPIRO[3.4]OCTANE DERIVATIVES AS M4 AGONISTS | 2020 |
|
RU2820477C1 |
| DERIVATIVES OF SUBSTITUTED PHENYLPROPIONIC ACID AS AGONISTS OF HUMAN ALPHA-RECEPTORS ACTIVATED BY PEROXISOME PROLIFERATOR (PPARα), METHOD AND INTERMEDIATE COMPOUNDS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF, THEIR USING AND METHODS FOR TREATMENT OF DYSLIPIDEMIA IN DIABETES MELLITUS TYPE 2 | 2002 |
|
RU2303031C2 |
