PREPARATION, USES AND SOLID FORMS OF OBETICHOLIC ACID

To provide preparation, uses and solid forms of obeticholic acid.SOLUTION: The present invention relates to obeticholic acid shown in the figure or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for treatment or prevention of an FXR mediated d...

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Bibliographische Detailangaben
Hauptverfasser:	FIONA DUBAS-FISHER, EMMA SHARP, ALEX EBERLIN, GROSS RALF, POULSEN HEIDI WAENERLUND, MELISSA REWOLINSKI, ANDRE STEINER, EMILIE JOLIBOIS
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS STEROIDS
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Beschreibung
Zusammenfassung:	To provide preparation, uses and solid forms of obeticholic acid.SOLUTION: The present invention relates to obeticholic acid shown in the figure or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for treatment or prevention of an FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to crystals and synthetic processes of 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、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、オベチコール酸の結晶及び合成プロセスに関する。【選択図】図５