C07J21/00

Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Inhibitors of CYP17A1

Compounds according to formula I or II are provided. Such compounds are useful in treating cancers, such as leukemia, colon cancer, breast cancer, or prostate cancer by beneficially inhibiting CYP17A1. Pharmaceutical compositions and methods including the compounds are also provided. ##STR00001##

ANTI-PARASITE COMPOUNDS

The present invention relates to compounds which are active against parasitic infections, such as protozoan parasite infections (including flagellate parasite infections, ciliate parasite infections, amoeba parasite infections and apicomplexan parasite infections) and helminth infections. The present invention also relates to compositions comprising the compounds, and methods of treating or preventing parasitic infections, such as protozoan parasite infections (including flagellate parasite infections, ciliate parasite infections, amoeba parasite infections and apicomplexan parasite infections) and helminth infections, using the compounds.

Process for the preparation of cortexolone 17α-propionate and new hydrated crystalline form thereof

The present invention is directed to a process for the preparation of cortexolone 17-propionate, comprising a hydrolysis reaction of an ortho-ester of formula (III) ##STR00001## in which R is a hydrogen atom or a methyl group, in the presence of a dilute solution of acetic acid. The present invention is also directed to a hydrated crystalline form of cortexolone 17-propionate obtained by such process.

Process for the preparation of 7 α-(methoxycarbonyl)-3-OXO-17alpha-pregn-4,9(11)-dien-21,17-carbolactone, a useful intermediate for the synthesis of molecules with pharmacological activity

An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. ##STR00001##
Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.

C-20 STEROID COMPOUNDS, COMPOSITIONS AND USES THEREOF TO TREAT TRAUMATIC BRAIN INJURY (TBI), INCLUDING CONCUSSIONS
20250206774 · 2025-06-26 ·

The present invention relates to C-20 steroid compounds, compositions and methods of use thereof to treat, minimize and/or prevent traumatic brain injury (TBI), including severe TBI, moderate TBI and mild TBI, including concussions.

C-20 STEROID COMPOUNDS, COMPOSITIONS AND USES THEREOF TO TREAT TRAUMATIC BRAIN INJURY (TBI), INCLUDING CONCUSSIONS
20250206774 · 2025-06-26 ·

The present invention relates to C-20 steroid compounds, compositions and methods of use thereof to treat, minimize and/or prevent traumatic brain injury (TBI), including severe TBI, moderate TBI and mild TBI, including concussions.

7-KETOLITHOCHOLIC ACID INTERMEDIATE, SYNTHESIS METHOD THEREFOR, AND APPLICATION THEREOF
20250206771 · 2025-06-26 ·

A synthesis method for a 7-ketolithocholic acid is prepared from a new intermediate I-1. According to the method, phytosterol degradation product bisnoralcohol is used as a starting material, and the 7-ketolithocholic acid or the intermediate thereof is obtained by means of an oxidation reaction, a Knoevenagel reaction (or wittig reaction), hydrogenation, a ketal protection reaction, an allylic oxidation reaction, ketal removal protection, and the hydrogenation.

NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF

Provided herein is a compound of Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.16b, R.sup.7a, R.sup.7a, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.11a, R.sup.22, R.sup.X, R.sup.Y and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.