C07J7/00

Process for the preparation of allopregnanolone

A method for the purification of allopregnanolone is disclosed. Allopregnanolone prepared from isopregnanolone contains impurities such as triphenylphosphine oxide and other unknown impurities. To remove these impurities and purify allopregnanolone, the allopregananolone is dissolved in acetonitrile, and crystallized from the acetonitrile. The resulting crystallized allopregnanolone may then be re-crystallized from acetonitrile to further purify the allopregnanolone.

COMPOUNDS HAVING ANTI-INFLAMMATORY AND ANTI-OXIDANT ACTIVITY
20200199170 · 2020-06-25 ·

The present invention relates to new compounds of formula (1) wherein R is C(O)CH.sub.2OH or CH(OH)CH.sub.2OH; R.sub.1, is O or OH; R.sub.2 is H or OH; R.sub.3 is H or C.sub.1-C.sub.4alkyl; R.sub.4 is H or C.sub.1C.sub.4alkyl. These compounds are obtained by a process using at least one bacterium belonging to the Actinobacteria class, preferably belonging to the Rhodococcus genus. Thanks to their antiinflammatory and anti-oxidant properties, the compounds of the invention can be advantageously used in the treatment of inflammatory diseases, autoimmune diseases and of diseases in need of a joined anti-inflammatory and anti-oxidant activity.

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CRYSTALLINE SOLVATE FORMS OF A PHARMACEUTICAL

Described herein are solid state 17-ethynylandrost-5-ene-3,7,17-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17-ethynylandrost-5-ene-3,7,17-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.

POTENT SOFT ANTI-INFLAMMATORY CORTICOSTEROID COMPOUNDS AND USES THEREOF
20200181191 · 2020-06-11 ·

Potent soft corticosteroid pharmaceutical compositions comprising them and method for use as anti-inflammatory agents. Also, a method for softening fluticasone propionate and similar corticosteroids to arrive at potent but safer alternatives. The compound 5-fluoromethyl 17-dichloroacetoxy-6,9-difluoro-11-hydroxy-16a-methyl-3-oxoandrosta-1,4-diene-17-carbothioate, which is equally potent to but safer than fluticasone, is among those provided. Another compound of particular interest is 2-hydroxyethyl 17-dichloroacetoxy-6,9-difluoro-11-hydroxy-16-methyl-3-oxoandrosta-1,4-diene-17-carboxylate.

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.

19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF

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

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and pharmaceutically acceptable salts thereof; wherein custom-character, 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.

19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF

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

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and pharmaceutically acceptable salts thereof; wherein custom-character, 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.

ENZYMATIC PROCESS FOR OBTAINING 17 ALPHA-MONOESTERS OF CORTEXOLONE AND/OR ITS 9,11-DEHYDRODERIVATIVES
20200155572 · 2020-05-21 · ·

The present invention refers to a new enzymatic process for obtaining 17-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17-propionate and 9,11-dehydro-cortexolone 17-butanoate.

NON-HORMONAL STEROID MODULATORS OF NF-KAPPA BETA FOR TREATMENT OF DISEASE

The present invention relates to compounds and methods which may be useful as treatments of diseases.

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 -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.