Patent classifications
C07J1/0022
Method for preparing 7alpha-methyl-19-aldehyde-4-androstene-3,17-dione by electrocatalytic oxidation
The present invention relates to a method for preparing 7α-methyl-19-aldehyde-4-androstene-3,17-dione by electrocatalytic oxidation. The method specifically includes: adopting an H-shaped electrolytic cell for reaction, in an anode chamber, using a metal oxide catalyst as a working electrode, using 7α-methyl-17,19-dihydroxy-4-androstene-3-one as a reaction substrate, and dissolving it in a mixed solvent to be used as an anolyte, and adding nitroxide radicals to be used as a medium; and in a cathode chamber, using a platinum sheet as a counter electrode, using a weakly alkaline solution as a catholyte, carrying out an electrocatalytic oxidation reaction in a constant temperature water bath, adding an organic solvent at the end of the reaction for extraction to obtain an organic extract liquor, and taking an organic layer and carrying out distilling under a reduced pressure to obtain 7α-methyl-19-aldehyde-4-androstene-3,17-dione.
Androstane Derivatives with Activity as Pure or Predominantly Pure Stimulators of SERCA2a for the Treatment of Heart Failure.
Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na.sup.+/K.sup.+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.
##STR00001##
Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof
The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. ##STR00001##
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 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.
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.
DIETARY SUPPLEMENTS FOR MUSCLE GROWTH AND STRENGTH
A compound is provided for oral administration of dehydroepiandrosterone (DHEA) derivatives to a human so as to improve at least one of adrenal hormonal balance, improved immune system function, reduction of adipose tissue, skeletal muscle growth, reduction of abdominal bloating, improved recovery from training, increased strength, and increased endurance. The compound includes a first portion comprised of any one of 3a-enanthoxy-5a-androstan-17-one, 3b-undecyloxy-5a-androstan-17-one, and 3b-hydroxy-androstane-3b-ol-one. A second portion of the compound is comprised of 6,7-dihydrogergamottin. A third portion is comprised of piperine, and a fourth portion is comprised of any one or more of rice flour, gelatin, magnesium stearate, and silica. The compound preferably is administered in capsule form one or two times in a 24-hour period.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein (II), 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.
##STR00001##
Stable isotope-labeled compounds
Provided are a novel internal standard useful in the measurement of androgens, a method capable of measuring the androgen in a highly selective and highly sensitive (accurate) manner using liquid chromatography mass spectrometry with simplified pretreatments, and a method for diagnosis of a disease using the androgen measurement method. The novel stable isotope-labeled compound is synthesized by performing reduction reaction in a specific solvent. An androgen is measured using this novel stable isotope-labeled compound as an IS.
Method for Fluoroalkylation of Enamines
The invention discloses a method for fluoroalkylation of enamines with a fluoro alkyl halide in the presence of a base.