Novel antimicrobial compounds against drug targets such as Eskape pathogens, Leishmania donovani, Mycobacterium tuberculosis, Clostridium difficile, Naegleria fowleri, and cancer are presented herein.

The present disclosure relates to synthetic methods for preparing a 9-alpha-substituted or a 9-beta-substituted steroid-like compound. In particular, the disclosure relates to methods for generating a steroidal C9-C10 bond and establishing stereochemistry at C9 in such compounds. The methods provide high levels of stereoselection in the C9-C10 bond forming process. Compounds synthesized by such methods can be used as nuclear hormone receptor modulators.

The present disclosure relates to synthetic methods for preparing a 9-alpha-substituted or a 9-beta-substituted steroid-like compound. In particular, the disclosure relates to methods for generating a steroidal C9-C10 bond and establishing stereochemistry at C9 in such compounds. The methods provide high levels of stereoselection in the C9-C10 bond forming process. Compounds synthesized by such methods can be used as nuclear hormone receptor modulators.

The present disclosure is generally directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof, for use as, for example, modulators for GABA type-A receptors. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

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.

Novel antimicrobial compounds against drug targets such as Eskape pathogens, Leishmania donovani, Mycobacterium tuberculosis, Clostridium difficile, Naegleria fowleri, and cancer are presented herein.

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

(3,9,10,13,14,17,20S,22E)-Ergosta-5,7,22-trien-3-ol. A method for preparing the same by drying a fruiting body of Cordyceps militaris, grinding the fruiting body to yield ultrafine powders; boiling and extracting the ultrafine powders, centrifuging and collecting a precipitate. A method for treating a tumor by administering to a patient in need of treating a tumor (3,9,10,13,14,17,20S,22E)-ergosta-5,7,22-trien-3-ol.

The present invention relates to ent-19-Norprogesterone, 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.