Compounds and methods of synthesizing oxysterols are provided. The compounds and methods provided allow the oxysterol to be safely produced at a high yield. The compounds and methods provided can produce the oxysterol in a stereoselective manner.

Disclosed herein are compounds having structural Formula (I), or salts thereof. These compounds are useful as sweet tasting agents and/or sweetness enhancers. Also disclosed are compositions comprising the present compounds and methods of increasing the sweet taste of ingestible compositions. Furthermore, methods for preparing the compounds are also disclosed.

An object of the present invention is to provide a separation medium and a separation method, ensuring high selectivity and good separation efficiency for specific steviol glycosides. The present invention is related to a separation medium in which polyethyleneimine is immobilized to porous particles of a (meth)acrylic polymer having a crosslinked structure and a hydroxyl group.

Provided are panaxdiol-type ginsenoside derivatives having structures as shown in formula I or formula II. Also provided are the uses thereof in the preparation of drugs for preventing and treating atherosclerosis. The panaxdiol-type ginsenoside derivatives have low cytotoxicities, can significantly reduce the percentages of the areas of atherosclerotic plaques in apoE−/− mice, can also effectively reduce the levels of low-density lipoprotein cholesterol and increase the levels of high-density lipoprotein cholesterol in serums of mice, and can significantly reduce the local TNF-α levels in the arteries of apoE−/− mice and have good anti-inflammatory effects; at a dose of 30 μM, the panaxdiol-type ginsenoside derivatives can significantly reduce the degrees of the formation of RAW264.7 cell-derived foam cells. In addition, the preparation methods for the panaxdiol-type ginsenoside derivatives are easy to operate and obtain high yields.

Provided are panaxdiol-type ginsenoside derivatives having structures as shown in formula I or formula II. Also provided are the uses thereof in the preparation of drugs for preventing and treating atherosclerosis. The panaxdiol-type ginsenoside derivatives have low cytotoxicities, can significantly reduce the percentages of the areas of atherosclerotic plaques in apoE−/− mice, can also effectively reduce the levels of low-density lipoprotein cholesterol and increase the levels of high-density lipoprotein cholesterol in serums of mice, and can significantly reduce the local TNF-α levels in the arteries of apoE−/− mice and have good anti-inflammatory effects; at a dose of 30 μM, the panaxdiol-type ginsenoside derivatives can significantly reduce the degrees of the formation of RAW264.7 cell-derived foam cells. In addition, the preparation methods for the panaxdiol-type ginsenoside derivatives are easy to operate and obtain high yields.

The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostrate Cancer (CRPC) and/or doubly resistant prostrate cancer, especially in individuals having prostrate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer. In some embodiments, GR inhibitors also have Androgen Receptors (AR) inhibitory activity and or administered in conjunction with AR Inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes. The present invention also provides systems for using such agents, for example to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer.

The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostrate Cancer (CRPC) and/or doubly resistant prostrate cancer, especially in individuals having prostrate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer. In some embodiments, GR inhibitors also have Androgen Receptors (AR) inhibitory activity and or administered in conjunction with AR Inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes. The present invention also provides systems for using such agents, for example to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer.

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):

##STR00001##

wherein: , R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein.

The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):

##STR00001##

wherein: , R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein.

The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.