Benzothiadiazepine compounds and their use as bile acid modulators
AssigneeAlbireo AB
InventorsPer-Göran Gillberg, Jan Mattsson, Ingemar Starke, Santosh S. Kulkarni
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Abstract
The invention relates to 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
Claims20
A compound of formula (I-b)
- or a pharmaceutically acceptable salt thereof,
- wherein
- R2 is methyl, ethyl, n-propyl or n-butyl;
- R3 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, hydroxy, cyano, trifluoromethyl, methoxy, and trifluoromethoxy;
- R4 is selected from the group consisting of fluoro, chloro, bromo, hydroxy, cyano, methoxy, ethoxy, methylthio, ethylthio and dimethylamino;
- and
- R5A is selected from the group consisting of hydrogen, halogen, hydroxy, amino and methyl.
A compound:
- 3-((3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydrobenzo-1,2,5-thiadiazepin-8-yl)oxy) propanoic acid, or a pharmaceutically acceptable salt thereof.
A compound:
- (R)-3-((3-butyl-3-ethyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy) propanoic acid, or a pharmaceutically acceptable salt thereof.
A compound:
- 3-((3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy)-2-hydroxypropanoic acid, or a pharmaceutically acceptable salt thereof.
A compound:
- (R)-3-((3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy)-2-hydroxypropanoic acid, or a pharmaceutically acceptable salt thereof.
A compound:
- 3-((3-butyl-7-(dimethylamino)-3-ethyl-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy) propanoic acid, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.