PREPARATION, USES AND SOLID FORMS OF OBETICHOLIC ACID

PROBLEM TO BE SOLVED: To provide preparation, use and solid form of obeticholic acid.SOLUTION: The invention relates to obeticholic acid of the formula or a pharmaceutically acceptable salt, solvate, amino acid conjugate thereof. Obeticholic acid is useful for treating or preventing a FXR mediated d...

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Main Authors FIONA DUBAS-FISHER, EMMA SHARP, ALEX EBERLIN, GROSS RALF, POULSEN HEIDI WAENERLUND, MELISSA REWOLINSKI, ANDRE STEINER, EMILIE JOLIBOIS
Format Patent
LanguageEnglish
Japanese
Published 08.11.2018
Subjects
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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Summary:PROBLEM TO BE SOLVED: To provide preparation, use and solid form of obeticholic acid.SOLUTION: The invention relates to obeticholic acid of the formula or a pharmaceutically acceptable salt, solvate, amino acid conjugate thereof. Obeticholic acid is useful for treating or preventing a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for lowering HDL cholesterol, for lowering triglyceride in a mammal, or for inhibiting fibrosis. The invention also relates to a process for synthesizing obeticholic acid.SELECTED DRAWING: Figure 5 【課題】オベチコール酸の調製、使用および固体形態の提供。【解決手段】本発明は、オベチコール酸：またはその薬学的に許容される塩、溶媒和物もしくはアミノ酸結合体に関する。オベチコール酸は、ＦＸＲにより媒介される疾患または状態、心臓血管疾患または胆汁うっ滞性肝臓疾患の治療または予防に有用であり、かつＨＤＬコレステロールを減少させること、哺乳動物においてトリグリセリドを低下させること、または線維症の阻害に、有用である。本発明はまた、オベチコール酸を合成するプロセスに関する。【選択図】図５
Bibliography:Application Number: JP20180137552