C07J41/0088

Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof

The present invention provides compounds of Formula I, ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

Small molecules active against gram-negative bacteria

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

STEROIDS AND PROTEIN-CONJUGATES THEREOF
20210040144 · 2021-02-11 ·

Described herein are protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.

COMPOUNDS FOR TREATING NEURODEGENERATIVE DISORDERS

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

##STR00001##

Process for preparation of sulfonylurea bile acid derivatives

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.

METHODS FOR MODULATION OF LIPOPROTEIN LIPASE AND APOLIPOPROTEIN C2 EXPRESSION AND/OR ACTIVITY IN THE TREATMENT OF PERIPHERAL AND CENTRAL NERVOUS SYSTEM TISSUE DISEASE STATES
20210024568 · 2021-01-28 ·

Methods for modulating lipoprotein lipase (LPL) and Apoliprotein C2 (ApoC2) expression and/or activity in the treatment of peripheral and central nervous system tissue disease states with C-6 substituted estradiol derivatives are presented herein.

HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF
20210024572 · 2021-01-28 ·

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.

##STR00001##

Small molecules active against gram-negative bacteria

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

INHIBITORS OF GLUCOCORTICOID RECEPTOR

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.

INHIBITORS OF GLUCOCORTICOID RECEPTOR

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.