C07J7/009

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.

Compositions and methods for treating CNS disorders

Described herein are neuroactive steroids of the Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof; wherein custom character, A, R.sup.1, R.sup.2, and R.sup.3 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, e.g., for treating a subject suffering from a disease or disorder described herein.

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 inflammatiom or a respiratory disease (e.g., asthma).

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.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Provided herein are compounds of Formula (I-I): and pharmaceutically acceptable alts thereof; wherein p, R.sup.1, R.sup.3a, R.sup.2a, R.sup.11a, R.sup.11b, R.sup.6a, and R.sup.6b are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-X) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

##STR00001##

Methods of treating certain depressive disorders and delirium tremens

The disclosure provides a method of treating a patient having postpartum depression, premenstrual dysphoric disorder, menopausal depression, or delirium tremens comprising administering an effective amount of an injectable neurosteroid formulation to the patient. In certain embodiments the injectable neurosteroid formulation is an injectable ganaxolone formulation. Two types of injectable neurosteroid formulations may be used in the disclosed methods. The first such formulation is an injectable formulation containing ganaxolone and sulfobutyl ether β-cyclodextrin in a 1:1 inclusion complex. The second such formulation is an injectable neurosteroid formulation comprising a neurosteroid, preferably ganaxolone, but which may be a neurosteroid selected from allopregnanolone, ganaxolone, alphaxalone, alphadolone, hydroxydione, minaxolone, pregnanolone, tetrahydrocorticosterone, and combinations of the foregoing; a surface stabilizer selected from hydroxyl ethyl starch, dextran, and povidone; and a surfactant.

STEROID DERIVATIVE REGULATORS, METHOD FOR PREPARING THE SAME, AND USES THEREOF
20210139530 · 2021-05-13 ·

Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound of formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator the of GABA.sub.A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description.

##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 agent 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 dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

PRODRUGS OF NEUROACTIVE STEROIDS
20230416298 · 2023-12-28 ·

The present application relates to novel compounds that are prodrugs of brexanolone, ganaxolone and zuranolone, pharmaceutical compositions comprising one or more compounds disclosed herein and salts thereof, and a pharmaceutically acceptable excipient, and use of the compounds disclosed herein and salts thereof for treating diseases or conditions related to GABA.sub.A receptor function, such as major depression disorder (MDD) and postpartum depression (PPD), in mammals and especially in humans.

PROCESS FOR PREPARING HIGH PURITIY ALLOPREGNANOLONE AND INTERMEDIATES THEREOF

The invention relates to an efficient and industrially applicable process for the preparation and purification of allopregnanolone and intermediates thereof without the assistance of column chromatography.