C07J9/00

OXYSTEROLS AND METHODS OF USE THEREOF

Compounds are provided according to Formula (I) 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, 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##

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##

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##

PROCESS FOR THE PURIFICATION OF PHYTOSTEROL
20220340615 · 2022-10-27 ·

A process for purification of phytosterols, said process comprising, a. providing a liquid mixture comprising a phytosterol, lower alcohol, wherein the lower alcohol is present in an amount of from 25 to 800% by weight, based on the amount of phytosterol; b. cooling the mixture to form phytosterol crystals, wherein the crystals are formed at a temperature of from of from 10° C. to 75° C., preferably 15° C. to 50° C., more preferably 20° C. to 45° C., even more preferably 25° C. to 35° C. c. separating the phytosterol crystals from the remainder of the mixture by filtration; d. subjecting the phytosterol crystals to washing with a solvent system comprising at least one polar aprotic solvent to obtain purified phytosterol; e. optionally repeating step (d); f. drying the washed phytosterol crystals; g. optionally melting and drying in molted state to remove traces of remaining solvent; and h. optionally subjecting to a particle-forming process to obtain solid sterol particles.

PROCESS FOR THE PURIFICATION OF PHYTOSTEROL
20220340615 · 2022-10-27 ·

A process for purification of phytosterols, said process comprising, a. providing a liquid mixture comprising a phytosterol, lower alcohol, wherein the lower alcohol is present in an amount of from 25 to 800% by weight, based on the amount of phytosterol; b. cooling the mixture to form phytosterol crystals, wherein the crystals are formed at a temperature of from of from 10° C. to 75° C., preferably 15° C. to 50° C., more preferably 20° C. to 45° C., even more preferably 25° C. to 35° C. c. separating the phytosterol crystals from the remainder of the mixture by filtration; d. subjecting the phytosterol crystals to washing with a solvent system comprising at least one polar aprotic solvent to obtain purified phytosterol; e. optionally repeating step (d); f. drying the washed phytosterol crystals; g. optionally melting and drying in molted state to remove traces of remaining solvent; and h. optionally subjecting to a particle-forming process to obtain solid sterol particles.

PROCESS FOR THE PRODUCTION AND PURIFICATION OF STEROLS

The presently claimed invention relates to a process for the production and purification of sterols from oil distillates or oil distillation residues, in particular from the latter. Specifically, the presently claimed invention relates to a process for obtaining sterols in a pure form with reduced impurity and improved color.

Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): ##STR00001##
wherein: custom character, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): ##STR00001##
wherein: custom character, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

METHOD FOR MANUFACTURING PHOSPHONATE ESTERS AND METHOD FOR MANUFACTURING PHOSPHATE ESTERS
20230130333 · 2023-04-27 ·

The present invention provides a method for efficiently manufacturing a phosphonate ester by phosphonylating an alcohol under mild conditions, and a method for manufacturing a phosphate ester. In the method for manufacturing a phosphonate ester of the present invention, a compound represented by the formula (1) is reacted with a compound represented by the formula (2) in the presence of a zinc catalyst to obtain a compound represented by the formula (3).

##STR00001##

X represents an organic group. R.sup.1 represents an alkyl group. R.sup.2 represents an organic group.

Isotopically labeled bile acid derivatives

The present application relates to isotopically labeled compounds of Formula I and methods of preparation and use thereof. ##STR00001##