Patent classifications
C07J21/006
Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
Described herein are steroids of Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
Steroid 6.7.Beta.-Epoxides as Chemical Intermediates
The invention relates to a process for preparing a compound of general formula (Ia):
##STR00001##
wherein R.sup.2, Y, R.sup.4 and R.sup.5 are as defined herein. The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.
NOVEL CYTOTOXIC AGENTS THAT PREFERENTIALLY TARGET LEUKEMIA INHIBITORY FACTOR (LIF) FOR THE TREATMENT OF MALIGNANCIES AND AS NEW CONTRACEPTIVE AGENTS
Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.
METHOD FOR PREPARING A FARNESOID X RECEPTOR AGONIST
The invention relates to a process for preparing a compound of formula (I)
##STR00001##
in particular obeticholic acid and intermediates suitable for its synthesis.
Neuroactive steroids, compositions, and uses thereof
Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. ##STR00001##
Method for fully automated synthesis of 16β-18F-fluoro-5α-dihydrotestosterone (18F-FDHT)
The automated synthesis of clinically relevant amounts of 16-.sup.18F-fluoro-5-dihydrotestosterone (.sup.18F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 295%. The specific activity was 4.6 Ci/mol (170 GBq/mol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated .sup.18F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.
Cytotoxic agents that preferentially target leukemia inhibitory factor (LIF) for the treatment of malignancies and as new contraceptive agents
Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.
PROGESTERONE ANTAGONISTS
Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.
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.