C07J75/00

Method for preparing substituted 3,7-dihydroxy steroids
09994608 · 2018-06-12 · ·

The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17-ethynyl-androst-5-ene-3,7,17-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.

Method for preparing substituted 3,7-dihydroxy steroids
09994608 · 2018-06-12 · ·

The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17-ethynyl-androst-5-ene-3,7,17-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.

METHOD FOR PREPARING SUBSTITUTED 3,7-DIHYDROXY STEROIDS
20180079775 · 2018-03-22 ·

The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S, 10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17-ethynyl-androst-5-ene-3, 7, 17-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.

METHOD FOR FULLY AUTOMATED SYNTHESIS OF 16Beta-18F-FLUORO-5Alpha-DIHYDROTESTOSTERONE (18F-FDHT)

The automated synthesis of clinically relevant amounts of 16-.sup.18F-fluoro-5-dihydrotestosterone (.sup.18F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 295%. The specific activity was 4.6 Ci/mol (170 GBq/mol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated .sup.18F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.

Compositions and methods for treating CNS disorders

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia. ##STR00001##

Compositions and methods for treating CNS disorders

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia. ##STR00001##

METHODS FOR ASSEMBLY OF TETRACYCLIC COMPOUNDS BY STEREOSELECTIVE C9-C10 BOND FORMATION
20240400607 · 2024-12-05 ·

The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

Solvolysis of biomass to produce aqueous and organic products

The present invention provides processes for deconstructing biomass to produce aqueous and organic products using a solvent produced in a bioreforming reaction.

Method of using supercritical fluid technology to separate and purify functional components of Antrodia camphorata

A method of using supercritical fluid technology to separate and purify the functional components of Antrodia cinnamomea is described. Triterpenoids and polysaccharides of Antrodia cinnamomea are extracted from a fractionation tank containing extract of Antrodia cinnamomea and supercritical solvent at a set temperature and pressure. The extracted functional components and supercritical solvent are then continuously fed into three separating tanks at a set temperature and a pressure below that of the aforesaid pressure to obtain various functional components of triterpenoids and polysaccharides from the Antrodia cinnamomea feed in each separating tank.

SOLVOLYSIS OF BIOMASS TO PRODUCE AQUEOUS AND ORGANIC PRODUCTS

The present invention provides processes for deconstructing biomass to produce aqueous and organic products using a solvent produced in a bioreforming reaction.