Patent classifications
C07J41/00
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.
Methods for onapristone synthesis dehydration and deprotection
Methods and systems for making onapristone (ONA) using acidic hydrolysis and dehydration with sulfuric acid in an alcoholic solution are provided.
CONJUGATED NEUROACTIVE STEROID COMPOSITIONS AND METHODS OF USE
The present disclosure provides modified neuroactive steroids. The modified neuroactive steroids may comprise, consist of, or consist essentially of a therapeutic agent and/or a modifying moiety. The modified neuroactive steroid can have modified characteristics as compared to native neuroactive steroids that do not include a modifying moiety and/or therapeutic agent. The modified neuroactive steroid may be, for example, modified pregnenolone, pregnenolone metabolites, allopregnanolone, and/or allopregnanolone metabolites. The modified neuroactive steroids can be used to treat, prevent and/or ameliorating a phenotypic state of interest in a subject.
Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid
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.
BILE ACID-GCPII INHIBITOR CONJUGATES TO TREAT INFLAMMATORY DISEASES, INCLUDING INFLAMMATORY BOWEL DISEASE (IBD)
GCPII inhibitors comprising 2-(phosphonomethyl) pentanedioic acid (2-PMPA) conjugated to a bile acid and their use for treating a disease or condition associated with elevated levels of GCPII, including inflammatory bowel disease.
Isotopically labeled bile acid derivatives
The present application relates to isotopically labeled compounds of Formula I and methods of preparation and use thereof. ##STR00001##
Therapeutic DNP derivatives and methods using same
The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.
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##
HUMAN AMINOSTEROL ENT-03 COMPOUNDS, RELATED COMPOSITIONS COMPRISING THE SAME, AND METHODS OF USING THE SAME
The present application relates generally to novel aminosterol compounds, compositions comprising the same, and methods of making and using the novel aminosterol compounds and compositions.
6-SUBSTITUTED, 22-CYANO HYODEOXYCHOLANIC ANALOGUES AND USES THEREOF
The present invention relates to compounds of formula (I), to pharmaceutical compositions thereof and to their uses, in particular in the treatment and/or prevention of GPBAR1 mediated diseases.
##STR00001##