The present application provides a compound of formula I:

##STR00001##

or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1-R.sup.10, m, n, p, and are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.

The present invention relates to compounds having cholane scaffolds of formula (I), ##STR00001##
said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBARI mediated diseases.

The present invention relates to new and improved processes for the preparation of deoxycholic acid (DCA) and pharmaceutically acceptable salts thereof, as well as to novel intermediates useful for the preparation of DCA and pharmaceutically acceptable salts thereof. The starting compounds are steroids, sterols or fermented phytosterols of vegetable origin, being of formula SM: ##STR00001##

A process for the preparation of obeticholic acid and derivatives thereof by: (a) hydrogenation of the double bond and reductive opening of the epoxide of a compound of formula (II) or a salt or solvate thereof ##STR00001## to obtain a compound of formula (IIIa) and/or (IIIb), or salts or solvates thereof ##STR00002## and (b) conversion of a compound of formula (IIIa) and/or a compound of formula (IIIb), or a salt or solvate thereof, into a compound of formula (I), or a salt or solvate thereof ##STR00003##

5-cholesten, 3(3, 25-diol, disulfate (25HCDS) has been found to be an authentic PPAR.sub.γ agonist and LXR antagonist, and is used for the therapy of lipid disorders and inflammatory diseases, including without limitation fatty liver, inflammatory bowel, and atherosclerotic disease.

The present invention relates to methods and novel intermediates useful in the preparation of a compound of formula (A) ##STR00001##
or a pharmaceutically acceptable salt thereof, comprising converting the aldehyde of a compound of formula (B) with a reducing agent to prepare a compound of formula (C) ##STR00002##
and converting the compound of formula (C) with a sulfating reagent to prepare a compound of formula (A). An objective of the present invention is to provide methods of preparing bile acid derivatives and novel intermediates. A use of the methods and intermediates described relates to the synthesis of bile acid derivatives which activate both FXR and TGR5.

The present invention relates to fulvestrant prodrugs of formula II and process for the preparation thereof. The present disclosure also relates to pharmaceutical composition of fulvestrant prodrugs and method of treatment using the same.

##STR00001##

The present disclosure relates to methods and novel intermediates useful in the preparation of a compound of formula I ##STR00001## or pharmaceutically acceptable salt, hydrate, solvate or amino acid, sulfate or glucuronide conjugate, or prodrug thereof, comprising the step of reacting a compound of formula I-4 with a halogenating reagent to provide a compound of formula I-5a ##STR00002##

In an aspect, the disclosure pertains to inhibitors of ANGPTL4; synthesis methods for making disclosed compounds; pharmaceutical compositions comprising disclosed compounds; methods of treating disorders of uncontrolled cellular proliferation, e.g., a cancer; and methods of treating a disease associated with an ANGPTL4 dysfunction using disclosed compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

In an aspect, the disclosure pertains to inhibitors of ANGPTL4; synthesis methods for making disclosed compounds; pharmaceutical compositions comprising disclosed compounds; methods of treating disorders of uncontrolled cellular proliferation, e.g., a cancer; and methods of treating a disease associated with an ANGPTL4 dysfunction using disclosed compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.