Patent classifications
C07J7/00
Neuroactive steroids, compositions, and uses thereof
Described herein are steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6, and Z 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.
PROCESS FOR PREPARING (3alpha,5alpha)-3-HYDROXY-3-METHYL-PREGNAN-20-ONE (GANAXOLONE)
The present invention refers to a process for preparing (3α,5α)-hydroxy-3-methyl-pregnan-20-one, a compound also known as Ganaxolone, having the formula below: (I):
##STR00001##
NEUROACTIVE STEROIDS SUBSTITUTED IN POSITION 10 WITH A CYCLIC GROUP FOR USE IN THE TREATMENT OF CNS DISORDERS
Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein n, R.sup.19, R.sup.5, R.sup.3a, R.sup.6a, R.sup.6b, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.17b, R.sup.15a, R.sup.15b, R.sup.16a and R.sup.16b 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.
##STR00001##
C19 scaffolds and steroids and methods of use and manufacture thereof
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.
3,3 DISUBSTITUTED 19-NOR PREGNANE COMPOUNDS, COMPOSITIONS, AND USES THEREOF
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III):
##STR00001##
where R.sup.1, R.sup.2, R.sup.3, R.sup.3′, R.sup.4, R.sup.6a, R.sup.6a, R.sup.11a, and R.sup.11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.
Compositions and methods for treating CNS disorders
Described herein are neuroactive steroids of the Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof; wherein , A, R.sup.1, R.sup.2, R.sup.3a, R.sup.4a, R.sup.4b, R.sup.5, R.sup.7a, and R.sup.7b 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.
C7, C12, AND C16 SUBSTITUTED NEUROACTIVE STEROIDS AND THEIR METHODS OF USE
Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.12, R.sup.16, R.sup.17, R.sup.19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
##STR00001##
Processes for the preparation of ortho-allylated hydroxy aryl compounds
The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I). ##STR00001##
Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof
The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic gent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, Meibomian gland dysfuntion or skin inflammation or a respiratory disease (e.g., asthma).
ENZYMATIC PROCESS FOR OBTAINING 17 ALPHA-MONOESTERS OF CORTEXOLONE AND/OR ITS 9,11-DEHYDRODERIVATIVES
The present invention refers to a new enzymatic process for obtaining 17α-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17α,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17α-propionate and 9,11-dehydro-cortexolone 17α-butanoate.