The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula I

##STR00001##

wherein each substituent is independently selected from; R.sub.1 is H or CH.sub.3; R.sub.2 is C.sub.1-C.sub.6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R.sub.1 and R.sub.2 combine to form saturated, unsaturated C.sub.3-C.sub.6 cyclic or heterocyclic ring; R.sub.3 and R.sub.4 are same or different and each independently represents H or halogen; R.sub.5 is —OH or —OCOR wherein R represents H or C.sub.1-C.sub.6 linear, branched or cyclic alkyl group that may be substituted.

Provided are certain polymorphic forms of vamorolone as well as pharmaceutical compositions and methods for their use.

Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.

The present invention relates to certain cortexolone derivatives of formula (I)

##STR00001##

and the use of the same as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of the pharmaceutical compositions as antitumor medicinal products.

The present invention is directed to a process for the preparation of cortexolone 17α-propionate, comprising a hydrolysis reaction of an ortho-ester of formula (III)

##STR00001## in which R is a hydrogen atom or a methyl group, in the presence of a dilute solution of acetic acid.

The present invention is also directed to a hydrated crystalline form of cortexolone 17α-propionate obtained by such process.

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.

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

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.

An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

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.