Patent classifications
C07J41/0088
NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF
Provided herein is a compound of Formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7a, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.11a, R.sup.22, R.sup.X, R.sup.Y and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
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.
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.
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.
Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes
The invention relates to a process for preparing a compound of general formula (Ia): wherein R.sup.2, Y, R.sup.4 and R.sup.5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.
COMPOUNDS FOR TREATING NEAR VISION DISORDERS
Cataract and presbyopia affect billions of people worldwide. Described herein are new compounds and methods of treating and preventing these diseases.
Cellular signalling inhibitors, their formulations and methods thereof
The present disclosure relates generally to Cellular Signalling inhibitors of compound of Formula I, compositions and formulations comprising the same, methods, processes, and uses thereof. In particular, the present disclosure provides CSF-1R inhibitors demonstrating sustained inhibition of CSF/CSF1R signalling pathway with decreased toxicity. The present disclosure also provides supramolecular combinatorial therapeutics, wherein a CSF-1R inhibitor is combined with one or more of a chemotherapeutic agent, a kinase inhibitor, and an immunoregulator, each of which is optionally conjugated with a lipid. The present disclosure also provides a method for treating cancer, allergy, Systemic lupus erythematosus, nephritis, Chronic Obstructive Pulmonary Disease, and abnormal macrophage functions or any combinations thereof. ##STR00001##
PROCESS FOR PREPARATION OF SULFONYLUREA BILE ACID DERIVATIVES
The present invention relates to processes for preparing a compound of Formula I:
##STR00001##
or a pharmaceutically acceptable salt or solvate thereof, and intermediates of use in said processes.
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.
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.