Patent classifications
C07J1/0011
HUMAN GHRELIN O-ACYLTRANSFERASE INHIBITORS
A class of cyanosteroid compounds that efficiently inhibit ghrelin acylation by ghrelin O-acyltransferase. The compounds have a steroid scaffold with ,-unsaturated ketone in the A ring position such an -cyanoenone. Exemplary compounds include (5S,8S,9S,10S,13S,14S)-10,13-dimethyl-3-oxo-4,5,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthrene-2-carbonitrile.
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 neuroactive steroids of the Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof; wherein R.sup.1a and R.sup.1b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof; wherein , A, R.sup.1, R.sup.2, R.sup.3a, R.sup.4a, R.sup.4b, R.sup.5, R.sup.7a, and R.sup.7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
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.
A TRIFLUOROMETHYL THIANTHRENIUM COMPOUND, PROCESS FOR PREPARING THE SAME AND THE USE THEREOF
The present inventions refers a novel trifluoromethyl thianthrenium compound referred to as TT-CF.sub.3.sup.+X.sup.?, a process for preparing the same and the use thereof for trifluoromethylating organic compounds.
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.
QUANTITATIVE PROFILING OF PROGESTERONE METABOLITES FOR THE PREDICTION OF SPONTANEOUS PRETERM DELIVERY
Disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery. In particular, disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery based on ratios of steroids in samples obtained from the pregnant female.
METHODS FOR THE PURIFICATION OF DEOXYCHOLIC ACID
Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12--hydroxysteroids from -9,11-ene, 11-keto or 11-hydroxy--steroids. This invention is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.
C-HALOGEN BOND FORMATION
Methods of halogenating a carbon containing compound having an sp3 CH bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative CH fluorination of a carbon containing compound having an sp3 CH bond are provided. The halogenated products of the methods are provided.