06-08-2020 дата публикации
Номер: US20200247768A1
Принадлежит:
The invention relates to 1,5-benzothiazepine 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. 2. A compound according to claim 1 , wherein Ris n-butyl.3. A compound according to claim 1 , wherein Ris n-butyl.4. A compound according to claim 1 , wherein Ris ethyl.5. A compound according to claim 1 , wherein Ris independently selected from the group consisting of hydrogen claim 1 , halogen claim 1 , hydroxy claim 1 , amino claim 1 , cyano claim 1 , Chaloalkyl claim 1 , Calkoxy and Chaloalkoxy.6. A compound according to claim 1 , wherein Ris selected from the group consisting of halogen claim 1 , hydroxy claim 1 , cyano claim 1 , Calkyl claim 1 , Calkoxy claim 1 , Calkylthio claim 1 , amino claim 1 , N—(Calkyl)amino and N claim 1 ,N-di(Calkyl)amino.7. A compound according to claim 1 , wherein Rand Rare each independently selected from the group consisting of hydrogen claim 1 , halogen and hydroxy claim 1 , amino claim 1 , methyl and methoxy.8. A compound according to claim 1 , selected from the group consisting of:(S)-3-((7-bromo-3-butyl-3-ethyl-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)propanoic acid;(R)-3-((7-bromo-3-butyl-3-ethyl-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)propanoic acid;3-((7-bromo-3,3-dibutyl-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)propanoic acid;3-((3-butyl-7-chloro-3-ethyl-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)propanoic acid;(S)-3-((3-butyl-7-chloro-3-ethyl-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl)oxy)propanoic acid ...
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