C07J41/00

NEUROACTIVE STEROIDS AND THEIR METHODS OF USE

Provided herein is a compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein 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.11a, R.sup.11b, R.sup.15a, R.sup.15b, R.sup.16a, R.sup.16b, R.sup.18, R.sup.19, R.sup.20a, R.sup.20b, X, A, Z, q, u, r, s, t, m, 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.

##STR00001##

Enhanced sensitivity for analysis of ketosteroid compounds using mass spectrometry

The present disclosure provides methods and composition involving increased sensitivity of compounds using mass spectrometry. In one embodiment, a method of increasing the sensitivity for detection of a carbonyl group-containing compound by mass spectrometry can comprise derivatizing the carbonyl group-containing compound with an O-substituted hydroxylamine thereby producing an oxime, resulting in enhanced sensitivity of detection by mass spectrometry, as compared to the underivatized carbonyl group-containing compound. Additionally, a method for assaying a carbonyl group-containing compound can comprise reacting the carbonyl group-containing compound in a sample with an O-substituted hydroxylamine to produce an oxime and performing analysis with mass spectrometric detection of the oxime by a mass spectrometry instrument. Further, an assay for a ketosteroid can comprise a derivatized ketosteroid produced by reacting the ketosteroid with an O-substituted hydroxylamine to produce an oxime and a mass spectrometry instrument for performing mass spectrometric analysis on the derivatized ketosteroid.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and custom-character 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.

##STR00001##

PROCESS PER PREPARING (3a,5a)-20-OXOPREGNAN-3-YL GLYCYL-L-VALINATE HYDROCHLORIDE

The present invention refers to a process for the preparation of (3α,5α)-20-oxopregnan-3-yl glycyl-L-valinate hydrochloride, a compound having the formula I reported below:

##STR00001##

FORMULATIONS FOR THE DELIVERY OF ACTIVE AGENTS TO INSECTS, PLANTS, AND PLANT PATHOGENS

The present disclosure is directed to formulations comprising (1) at least one formulation transport agent, (2) at least one complexing agent, and (3) at least one active agent that modulates one or more traits of a target insect, plant, or plant pathogen. The present disclosure is also directed to methods of delivering such formulations to the target organism, as well as to formulation transport agents used to prepare such formulations.

NOVEL DRUG DELIVERY CONJUGATED MOIETY FOR ORAL ADMINISTRATION OF DRUG UNSUITABLE FOR ORAL ADMINISTRATION AND PREPARATION METHOD THEREOF

The present invention provides a novel drug delivery conjugated moiety for oral administration of a drug that is not suitable for oral administration or a pharmaceutically acceptable salt thereof. When the drug delivery conjugated moiety of the present invention or a pharmaceutically acceptable salt thereof is combined with a drug, which is not suitable for oral administration, and is administered orally, it exhibits an excellent absorption rate without decreasing the biological activities of the drug. Moreover, the drug delivery conjugated moiety of the present invention or a pharmaceutically acceptable salt thereof can be easily prepared in a few steps, which is very advantageous in terms of mass production.

Progesterone phosphate analogs and uses related thereto

This disclosure relates to progesterone phophate derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation such as those resulting from traumatic brain injury or stroke.

METHODS OF MAKING CHOLIC ACID DERIVATIVES AND STARTING MATERIALS THEREFOR

Methods of making cholic acid derivatives, particularly ursodeoxycholic acid, tauroursodeoxycholic acid, 7-ketolithocholic acid, obeticholic acid, their carboxylate salts and carboxylate esters, and starting materials and intermediates therefor.

Natural product analogs including an anti-inflammatory cyanoenone pharmacore and methods of use

This invention provides novel compounds comprising the following anti-inflammatory pharmacore: ##STR00001##
wherein X, R.sub.1 and R.sub.2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Thionyl tetrafluoride modified compounds and uses

Thionyl tetrafluoride gas reacts efficiently with primary amines to form reactive iminosulfur oxydifluoride compounds. These dual S.sup.VI—F loaded iminosulfur oxydifluoride compounds, in turn, readily react with secondary amines or aryloxy silyl ethers (ArO—SiR.sub.3), yielding the corresponding fused heteroatom-linked substrates. Iminosulfur oxyfluoride polymers also are provided by disclosed methods.