12-03-2020 дата публикации
Номер: US20200078374A1
Принадлежит:
The invention provides, in part, polyhydroxylated bile adds for treating biliary disorders, for example, biliary disorders arising out of cholestasis of portal hypertension. The invention also provides, in part, polyhydroxylated bile acids for stimulating bile flow. New compounds 2α,3α,7α,12α-tetrahydroxy-5β-cholanoic acid and 3α,4α,7α,12α-tetrahydroxy-5β-cholanoic acid are disclosed, uses thereof and synthesis thereof. 2. The method of wherein said compound is selected from the group consisting of a tetrahydroxylated bile acid and a pentahydroxylated bile acid claim 1 , or a derivative thereof.3. The method of wherein said tetrahydroxylated bile acid is selected from the group consisting of:a 3,6,7,12-tetrahydroxycholanoic acid,a 3,4,7,12-tetrahydroxycholanoic acid,a 1,3,7,12-tetrahydroxycholanoic acid,a 2,3,7,12-tetrahydroxycholanoic acid,a 3,7,16,24-tetrahydroxycholanoic acid, anda 3,7,15,24-tetrahydroxycholanoic acid,or a derivative thereof.4. The method of wherein said 3 claim 3 ,6 claim 3 ,7 claim 3 ,12-tetrahydroxycholanoic acid is selected from the group consisting of:a 3α,6α,7α,12α-tetrahydroxy-5β-cholan-24-oic acid,a 3α,6β,7α,12α-tetrahydroxy-5β-cholan-24-oic acid,a 3α,6α,7β,12α-tetrahydroxy-5β-cholan-24-oic acid,a 3α,6β,7β,12α-tetrahydroxy-5β-cholan-24-oic acid,a 3α,6α,7α,12β-tetrahydroxy-5β-cholan-24-oic acid,a 3α,6β,7α,12β-tetrahydroxy-5β-cholan-24-oic acid, anda 3α,6β,7β,12β-tetrahydroxy-5β-cholan-24-oic acid,or wherein said 2,3,7,12-tetrahydroxycholanic acid is a 2α,3α,7α,12α-tetrahydroxy-5β-cholanic acid,or wherein said a 3,4,7,12-tetrahydroxycholanic acid is a 3α,4α,7α,12α-tetrahydroxy-5β-cholanic acid,or a derivative thereof.5. The method of wherein said compound has a hydrophilicity greater than that of cholate claim 1 , or has a preferential affinity for MDRI when compared to BSEP claim 1 , or wherein said compound has a high affinity for MDR1 claim 1 , or wherein said compound is selected from the group consisting of a tauryl or glycyl conjugate ...
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