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US 2017/0290814 A1Published application
Methods of treatment of cholestasis and fibrosis
AssigneeGenfit
InventorsMATHIEU DUBERNET, ROBERT WALCZAK, PHILIPPE DELATAILLE
Life of this patent
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Abstract
The present invention relates compounds useful and their use for treating cholestatic and fibrotic diseases.
Claims13
A method of treating a cholestatic or fibrotic disorder comprising administering a compound of formula (I), or a pharmaceutically acceptable salt thereof, to a subject having a cholestatic or fibrotic disorder:
- wherein
- R1 represents a hydrogen atom, a deuterium atom, a halogen atom, a (C6-C14)aryl group, a heterocyclic group, a (C3-C14)cycloalkyl group, a (C1-C6)alkyl group, a sulfonyl group, a sulfoxyde group, a (C1-C6)alkylcarbonyl group, a (C1-C6)alkyloxy, a carboxylic group, a carboxylate group, a nitro group, an amino group, a (C1-C6)alkylamino group, an amido group, a (C1-C6)alkylamido group, a (C1-C6)dialkylamido group;
- R2 represents a hydrogen atom, a deuterium atom, a nitro group, a (C6-C14)aryl group, a heterocyclic group, a halogen atom, a (C1-C6)alkyl group, a (C3-C14)cycloalkyl group, a (C2-C6)alkynyl group, a (C1-C6)alkyloxy group, a (C1-C6)alkylthio group, a (C1-C6)alkylcarbonyl group, a (C1-C6)alkylcarbonylamino group, a (C6-C14)arylcarbonylamino group, a carboxylic or carboxylate group, an amido group, a (C1-C6)alkylamido group, a (C1-C6)dialkylamido group, a NH2 group, a (C1-C6)alkylamino group;
- or R1 and R2, together with the carbon atoms to which they are attached, form a substituted or unsubstituted 5- to 8-membered cycloalkyl, heterocyclic and aryl group;
- R3, R4, R5, R6, and R7, identical or different, represent a hydrogen atom, a deuterium atom, a halogen atom, a hydroxyl group, a (C1-C6)alkylcarbonyl group, a (C1-C6)alkyl group, a (C1-C6)alkyloxy group, a (C1-C6)alkylthio group, a (C1-C6)alkylcarbonyloxy group, a (C6-C14)aryloxy group, a (C6-C14)aryl group, a heterocyclic group, a (C3-C14)cycloalkyl group, a nitro group, a sulfonylaminoalkyle group, a NH2 group, an amino(C1-C6)alkyl group, a (C1-C6)alkylcarbonylamino group, a carboxylic group, a carboxylate group, or a R9 group;
- R9 represents a O—R8 group or an amino acid selected from the group consisting of alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine, or a moiety of formula (A):
- wherein R′ represents a alkyl, alkenyl, alkynyl group, cycloalkyl group, cycloalkylalkyl group, cycloalkylalkenyl group, cycloalkenyl group, a cycloalkenylalkyl group, a cycloalkenylalkenyl group, a cycloalkenylalkynyl group;
- R″ and R′″, independently, represent hydrogen atom, an alkyl group, or a nitrogen protecting group;
- R8 is a hydrogen atom, a deuterium atom, a glucuronidyl group, or a
- group wherein, R8a, R8b and R8c, identical or different, represent a hydrogen atom or a deuterium atom;
- with the proviso that compound of formula (I) is not NTZ or TZ.
8 more elements
Dependencies are inferred from the claim text.