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

The invention relates to compounds of formula (I), their method of synthesis as well as their use to treat neurodegenerative disorders.

The present invention relates to compounds of Formulas 3-6, ##STR00001##
where R.sub.4 PG.sub.1 and PG.sub.2 are defined as disclosed herein. These compounds are useful as intermediates in processes for preparing a compound of Formula I: ##STR00002##
where R.sub.1 is defined as disclosed herein.

There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis.

##STR00001##

The present invention relates to processes for preparing compounds of Formula (I) and Formula (II): ##STR00001## These compounds are useful as FXR or TGR5 modulators. The present invention also relates to processes for the preparation of the compounds of Formula (III), Formula (IV), Formula (V), and Formula (VI), ##STR00002## The present invention also relates to a process for the preparation of compounds (VII), (VIII) and (IX), ##STR00003##

Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.

Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e. g., such for inducing sedation and/or anesthesia.

##STR00001##

Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory disease.

What is described is a method of synthesis of the compound of formula 1A,

##STR00001## or a salt thereof, wherein R.sub.3 is a linear or branched alkene of 1, 2, 3, 4, 5 or 6 carbons; R.sub.4 and R.sub.5 are the same or different, each a hydrogen, or a linear or branched alkyl of 1, 2, 3, 4, 5 or 6 carbons; and L.sub.3 is a bond or an alkane of 1, 2, 3, 4, 5 or 6 carbons.

A highly effective synthetic route to produce donor-acceptor azetines through the highly enantioselective [3+1]-cycloaddition of silyl-protected enoldiazoacetates with aza-ylides using chiral copper(I) catalysis is provided. In one embodiment, the 2-azetidine cycloaddition products undergo generation of 3-azetidinones by reactions with nucleophiles that produce a broad spectrum of peptide products by the retro-Claisen reaction provided by facile strain with high efficacy and complete retention of enantiopurity. This ring opening reaction uncovers a new methodology for the attachment of chiral peptide units to a variety of amines and alcohols, and tolerates a broad scope of nucleophiles including naturally occurring amines, alcohols, amino acids, and other nitrogen based nucleophiles.