A method of forming a probe, wherein the method includes converting cholenic acid into a compound with a terminal alkyne group, wherein the converting the cholenic acid comprises using a sequence, wherein the sequence comprises synthesizing a THP-protection group, LiAlH4 reduction, Dess-Martin oxidation, and Seyferth-Gilbert-Bestmann homologation. The method additionally includes forming A-Chol by removing the THP-protection. Further, the method includes forming PhA-Chol from the compound with the terminal alkyne group via a palladiumcatalyzed Sonogashira reaction. Additionally, the method includes forming PhDY Chol from the compound with the terminal alkyne group via a coppercatalyzed Cadiot-Chodkiewicz reaction.

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.

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.

The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.

The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.

The present invention relates to a crystalline form Of (E)-methyl 6-((3S,8S,9S,10R,13S,14S,17R)-3-(((5S,6R)-5-acetoxy -6-(acetoxytnethyl)-5,6-dihydro-2H-pyran-2-yl)oxy)-10,13 -dimethyl-2,3,4,7,8,9,10.11,12,13,14,15,16,17-tetradecahydro -1H-cyclopenta [a]phenanthrene-17-yl)hept-5-enoate and a blood vessel leak blocker comprising the same. The novel crystalline form has high purity, excellent stability, excellent long-term storage and pharmaceutical stability, and can be used as a vascular leakage blocker, so it is very advantageous in producing high-quality drug substances.

The present invention relates to a crystalline form Of (E)-methyl 6-((3S,8S,9S,10R,13S,14S,17R)-3-(((5S,6R)-5-acetoxy -6-(acetoxytnethyl)-5,6-dihydro-2H-pyran-2-yl)oxy)-10,13 -dimethyl-2,3,4,7,8,9,10.11,12,13,14,15,16,17-tetradecahydro -1H-cyclopenta [a]phenanthrene-17-yl)hept-5-enoate and a blood vessel leak blocker comprising the same. The novel crystalline form has high purity, excellent stability, excellent long-term storage and pharmaceutical stability, and can be used as a vascular leakage blocker, so it is very advantageous in producing high-quality drug substances.

Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Described herein are processable compositions comprising at least one moiety that is processable in its free form. Also described herein are compositions and methods for the treatment of ocular diseases or disorders including glaucoma, blepharitis, ocular inflammation, diabetic macular edema, posterior inflammation, anterior inflammation, macular degeneration (e.g., wet macular degeneration (AMD) or dry AMD), post-cataract surgery, and retinal vein occlusion. Said compositions and methods comprise steroids and prostaglandins which demonstrate anti-inflammatory activity, intraocular pressure (IOP) lowering, and/or other desirable activities. Injection of said compositions in the eye provides therapeutic benefit to patients suffering from ocular disorders.