Patent classifications
C07J9/005
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.G are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
##STR00001##
Enzyme compositions, steroid derivatives, enzyme inhibitors, and methods of making same for pharmaceutical applications
The present disclosure provides for a synthetic strategy to incorporate a C12α-hydroxy group from the methylene (—CH2-) in a steroid backbone, combining synthetic chemistry and enzymology techniques to develop a selective inhibitor for cytochrome P450 8B1, and developing a selective P450 8B1 inhibitor, which can be used as a tool to study P450 8B1 and treat health issues.
Crystalline form of obeticholic acid and preparation method therefor
The present invention relates to a new crystalline form of obeticholic acid and a preparation method therefor. In particular, the present invention relates to crystal form E of obeticholic acid and a preparation method therefor. The crystalline form is very stable, and the solvent residue is low, and the crystalline form is suitable for industrial production. Obeticholic acid has the following structure: ##STR00001##
Crystalline form of obeticholic acid and preparation method therefor
The present invention relates to a new crystalline form of obeticholic acid and a preparation method therefor. In particular, the present invention relates to crystal form E of obeticholic acid and a preparation method therefor. The crystalline form is very stable, and the solvent residue is low, and the crystalline form is suitable for industrial production. Obeticholic acid has the following structure: ##STR00001##
Methods for preparing bile acids
The present disclosure provides methods of preparing cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, and novel and useful synthetic intermediates, for example, as described for methods 1, 1A, 1B, 2, 3, 3A, and 4. The method can start with a plant derived steroid as a starting material, such as dehydroepiandrosterone (DHEA) or Acetyl-dehydroepiandrosterone (Ac-DHEA). Also provided are pharmaceutical or cosmetic compositions and uses thereof, which comprise one or more of cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, which is of high purity, for example, free of animal derived impurities.
3,3 DISUBSTITUTED 19-NOR PREGNANE COMPOUNDS, COMPOSITIONS, AND USES THEREOF
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III):
##STR00001##
where R.sup.1, R.sup.2, R.sup.3, R.sup.3′, R.sup.4, R.sup.6a, R.sup.6a, R.sup.11a, and R.sup.11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3′ R.sup.4, R.sup.5, R.sup.6, and R.sup.G are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
##STR00001##
INOTODIOL ESTER DERIVATIVE PRECURSOR DRUG
The present disclosure relates to an ester derivative prodrug of inotodiol and use thereof. The prodrug not only has increased solubility with respect to an inorganic solvent and an organic solvent, but also has improved stability, and thus can be used in the treatment of various inflammatory diseases, including inflammatory diseases or allergic diseases.
TGR5 modulators and methods of use thereof
The application relates to compounds of formula A: ##STR00001##
or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein X, Y, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.5a, R.sup.5b, R.sup.6a, R.sup.6b, R.sup.7, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
##STR00001##