Process for preparation of sulfonylurea bile acid derivatives

    公开(公告)号:US10584145B2

    公开(公告)日:2020-03-10

    申请号:US15826233

    申请日:2017-11-29

    Abstract: The present invention relates to processes for preparing a compound of Formula I: or a pharmaceutically acceptable salt or solvate thereof. These compounds and pharmaceutical compositions are useful as FXR or TGR5 modulators. Specifically, the present invention relates to bile acid derivatives and methods for their preparation and use. The present invention relates to a process for the preparation of a compound (II) and its salts and derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of FXR and TGR5 modulators. The present invention also relates to a process for the preparation of a compound (III) and its diethylamine salt.

    Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof

    公开(公告)号:US10253018B2

    公开(公告)日:2019-04-09

    申请号:US15988763

    申请日:2018-05-24

    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, ester, stereoisomer, tautomer, solvate, hydrate, or combination thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).

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