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 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16a-methyl-3-oxoandrosta-1,4-diene-17β-carbothioate, which is equally potent to but safer than fluticasone, is among those provided. Another compound of particular interest is 2-hydroxyethyl 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16β-methyl-3-oxoandrosta-1,4-diene-17β-carboxylate.

Provided in the present invention are a 3-hydroxyl-5-pregnane-20-one derivative as shown in formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the derivative or the pharmaceutically acceptable salt thereof. The derivative or the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising the above-mentioned derivative or salt of the present invention can be used to prepare a drug for treating a disease caused by abnormalities in the central nervous system.

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Provided in the present invention are a 3-hydroxyl-5-pregnane-20-one derivative as shown in formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the derivative or the pharmaceutically acceptable salt thereof. The derivative or the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising the above-mentioned derivative or salt of the present invention can be used to prepare a drug for treating a disease caused by abnormalities in the central nervous system.

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The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.

Compositions and methods for preparing OXY133 polymorphs Form C to Form I are provided. The methods include subjecting a slurry of OXY133 to conditions sufficient to convert OXY133 to the OXY133 polymorph Form C, polymorph Form D, polymorph Form E, polymorph Form F, polymorph Form G, polymorph Form H, polymorph Form I or a mixture thereof. A polymorph of OXY133 is also provided and that polymorph can be polymorph Form C, polymorph Form D, polymorph Form E, polymorph Form F, polymorph Form G, polymorph Form H, polymorph Form I or a mixture thereof. Pharmaceutical compositions including OXY133 polymorphs are also provided.

Disclosed is a use of 5α-androstane-3β,5,6β-triol, an analogue, a deuterated derivative, and a pharmaceutically acceptable salt thereof in manufacture of a medicament for the treatment of hemorrhagic stroke in a patient. The hemorrhagic stroke is intracerebral hemorrhage or subarachnoid hemorrhage.

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

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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 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.

The invention relates to the last step of a synthetic process, in which Nomegestrol-acetate of formula (I) is synthesized from 17α-acetoxy-6-methylene-19-norpregn-4-ene-3,20-dione of formula (II) in the presence of Pd/C catalyst and acetic acid in hot ethanolic solution. ##STR00001##

Disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery. In particular, disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery based on ratios of steroids in samples obtained from the pregnant female.