Processes for the synthesis and purification of glycoconjugate derivatives of cholic acid of formula (I) ##STR00001##
are provided herein.

Methods of making cholic acid derivatives, particularly ursodeoxycholic acid, tauroursodeoxycholic acid, 7-ketolithocholic acid, obeticholic acid, their carboxylate salts and carboxylate esters, and starting materials and intermediates therefor.

Methods of making cholic acid derivatives, particularly ursodeoxycholic acid, tauroursodeoxycholic acid, 7-ketolithocholic acid, obeticholic acid, their carboxylate salts and carboxylate esters, and starting materials and intermediates therefor.

The present invention relates to a novel metal complex, a method for producing same, and a method for producing a gamma-lactam compound using same, and the metal complex according to the present invention is used as a catalyst for producing a gamma-lactam compound and can efficiently produce a gamma-lactam compound with an excellent yield and excellent selectivity.

Compounds are provided according to Formula (A):

##STR00001##

and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1A, R.sup.1B, n, R.sup.2A, R.sup.2B, R.sup.3, and R.sup.4 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

The present invention relates to a method for preparing a modified hydrophobic excipient including the following steps: Step A. obtaining intermediate I or II from a hydrophobic natural compound with one to three hydroxyl groups or a hydrophobic synthetic compound with one to three hydroxyl groups and amino acid derivatives with amino protecting groups and different chain lengths acting as raw material; Step B. obtain intermediate III from an amino acid derivative and N-hydroxysuccinimide or 1-hydroxybenzotriazole acting as raw material and a dehydrating agent; and Step C. reacting the intermediate II and the intermediate III as raw material with an acid-binding agent under a dark condition to generate a modified hydrophobic excipient.

The present invention relates to a modified hydrophobic excipient having a molecular formula of:

##STR00001##

where R is a hydrophobic natural compound or a hydrophobic synthetic compound with one to three hydroxyl groups (n=1-3); and R1 is an α-amino protecting group, and R2 is an amino acid side chain, wherein, when m=0, R is reacted with an amino acid derivative with a protecting group by esterification to form a hydrophobic excipient carrying the amino acid derivative with a protecting group; or when m=1, R is firstly introduced with an amino acid linking arm of different chain lengths (l=1, 2, 4, 6) via an ester group, and then introduced with an amino acid derivative with a protecting group.

The present invention relates to a drug-loaded emulsion, comprising a modified hydrophobic excipient having the following formula, a hydrophobic drug and a surfactant:

##STR00001## where R is a hydrophobic natural compound or a hydrophobic synthetic compound with one to three hydroxyl groups (n=1-3); and R1 is an α-amino protecting group, and R2 is an amino acid side chain, wherein, when m=0, R is reacted with an amino acid derivative with a protecting group by esterification to form a hydrophobic excipient carrying the amino acid derivative with a protecting group; or when m=1, R is firstly introduced with an amino acid linking arm of different chain lengths (l=1, 2, 4, 6) via an ester group, and then introduced with an amino acid derivative with a protecting group.

3beta, 17beta disubstituted steroidal compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, are provided for the prevention and treatment of a variety of CNS-related conditions.

##STR00001##

Compounds of general formula (1):

##STR00001##

wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein;
are of use in the treatment and prevention of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease.