C07J7/00

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.

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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):

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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 areas 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.

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).

NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF

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

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and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein, and A is a heteroaryl ring system comprising 3 or 4 nitrogens 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.

NEUROACTIVE STERIODS, COMPOSITIONS, AND USES THEREOF

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

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and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein, and A is a heteroaryl ring system comprising 3 or 4 nitrogens 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.

Injectable suspension comprising 3-beta-hydroxy-5-alpha-pregnan-20-one, and a method for the manufacturing thereof

The present invention relates to aseptic suspensions, physically stable and injectable through a 25G needle or thinner, comprising crystalline, non-micronized 3-beta-hydroxy-5-alpha-pregnan-20-one particles, a mixture of acylglycerols and cholesterol, processes for preparing crystalline, non-micronized, 3-beta-hydroxy-5-alpha-pregnan-20-one suitable for such suspensions, as well as methods for manufacturing such suspensions.

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.

Method for preparing steroid derivative FXR agonist

The present invention falls within the field of pharmaceutical chemistry, and relates to a method for preparing a steroid derivative FXR agonist and relevant intermediates. In particular, the present invention relates to a method for preparing a compound of formula I, comprising reacting a compound of formula 8 with a compound of formula 9 to obtain a compound of formula 10, obtaining a compound of formula 11 from a reaction of the compound of formula 10, and obtaining the compound of formula I from a reaction of the compound of formula 11, as well as the intermediates used, the methods for preparing the intermediates and the use of the intermediates. The reaction conditions of the preparation method are mild, and some of the steps can convert multiple groups simultaneously, thereby effectively shortening the sequence of steps. The preparation method is suitable for industrialized production. ##STR00001##

Crystalline or amorphous form of steroid derivative FXR agonist, preparation method therefor and use thereof

Disclosed are a crystalline or amorphous form of steroid derivative FXR agonist (formula I), and a preparation method therefor, and a crystalline composition and pharmaceutical composition comprising the crystalline or amorphous form, and the use of same in the preparation of a drug for treating or preventing various conditions associated with FXR. ##STR00001##