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

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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.

Disclosed in the present disclosure is a method for preparing 16alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. In the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate is used as a starting material, and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis, so as to prepare 16alpha-hydroxyprednisolone. The method for preparing 16alpha-hydroxylprednisolone of the present disclosure can effectively control the generation of impurities in the reaction process by improving the disadvantages of traditional processes, and has a mild reaction process and a high overall conversion rate; and the method of the present disclosure has low requirements for a reaction device and low operation costs, is easy to operate, is suitable for industrial production, and has a good market prospect.

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

Disclosed in the present disclosure is a method for preparing 16alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. In the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate is used as a starting material, and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis, so as to prepare 16alpha-hydroxyprednisolone. The method for preparing 16alpha-hydroxylprednisolone of the present disclosure can effectively control the generation of impurities in the reaction process by improving the disadvantages of traditional processes, and has a mild reaction process and a high overall conversion rate; and the method of the present disclosure has low requirements for a reaction device and low operation costs, is easy to operate, is suitable for industrial production, and has a good market prospect.

The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 1713-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is —Si(R.sup.2).sub.3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is —Si(R.sup.2).sub.3.

Compounds are provided according to Formula (I):

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and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6a, and R.sup.6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

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Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, Y, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.5a, R.sup.5b, R.sup.6a, R.sup.6b, R.sup.7, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

##STR00001##

The present invention generally relates to new compounds for therapeutic uses. In particular, this disclosure relates to novel tetracyclic compounds useful for treatment of cancer, especially castration resistant prostate cancer. Pharmaceutical composition matters and methods for treating a cancer patient by administering therapeutically effective amounts of such compound alone or together with other therapeutics are within the scope of this disclosure.

The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.