C07J13/005

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, and R.sup.3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. ##STR00001##

Methods for Preparing Bile Acids
20220009957 · 2022-01-13 ·

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.

Methods for preparing bile acids
11161872 · 2021-11-02 · ·

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.

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##

Process for the preparation of 3β-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene

A process for the synthesis of β-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (6). ##STR00001##

NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF

3beta, 17beta disubstituted steroidal compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, are provided for the prevention and treatment of a variety of CNS-related conditions.

##STR00001##

Neuroactive steroids and methods of use thereof

Compounds are provided according to Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6a, and R.sup.6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.

PROCESS FOR THE PREPARATION OF 3beta-HYDROXY-17-(1H-BENZIMIDAZOL-1-YL)ANDROSTA-5,16-DIENE

A process for the synthesis of β-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula 6).

##STR00001##

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, and R.sup.3 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 production of estetrol intermediates
11053274 · 2021-07-06 · ·

The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P.sup.1 and P.sup.2 are each independently a protecting group selected from R.sup.2—Si—R.sup.3R.sup.4, or R.sup.1CO—, wherein R.sup.1 is a group selected from C.sub.1-6alkyl or C.sub.3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently a group selected from C.sub.1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I). ##STR00001##