Patent classifications
C07J9/00
C17, C20, AND C21 SUBSTITUTED NEUROACTIVE STEROIDS AND THEIR METHODS OF USE
Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
METHOD FOR PREPARING CHOLESTEROL, DERIVATIVE THEREOF, AND ANALOG THEREOF
The present invention relates to the field of pharmaceutical chemistry, and specifically to a method for preparing cholesterol, a derivative thereof, and an analog thereof. The derivative of cholesterol comprises, but is not limited to, 7-dehydrocholesterol, 25-hydroxycholesterol, 25-hydroxy-7-dehydrocholesterol, and ergosterol. In the present invention, a compound represented by formula I can be prepared by means of a microbial transformation using phytosterols as a raw material, followed by preparing cholesterol, the derivative thereof, and the analog thereof.
METHOD FOR PREPARING CHOLESTEROL, DERIVATIVE THEREOF, AND ANALOG THEREOF
The present invention relates to the field of pharmaceutical chemistry, and specifically to a method for preparing cholesterol, a derivative thereof, and an analog thereof. The derivative of cholesterol comprises, but is not limited to, 7-dehydrocholesterol, 25-hydroxycholesterol, 25-hydroxy-7-dehydrocholesterol, and ergosterol. In the present invention, a compound represented by formula I can be prepared by means of a microbial transformation using phytosterols as a raw material, followed by preparing cholesterol, the derivative thereof, and the analog thereof.
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.
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (III):
##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.2, R.sup.3, R.sup.5, and n are as defined herein, and at least one hydrogen is replaced with a deuterium. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (III):
##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.2, R.sup.3, R.sup.5, and n are as defined herein, and at least one hydrogen is replaced with a deuterium. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
COMPOUND WITH ANTI-SPORE ACTIVITY AND PHARMACEUTICAL COMPOSITION THEREOF
The present disclosure provides a compound represented by formula (I), or a salt or a stereoisomer thereof. The compound is capable of effectively inhibiting germination of Clostridium difficile spores with a significant bacteriostatic activity. The compound has an excellent prospect for use in preparation of a drug for preventing and/or treating a C. difficile-caused infectious disease, recurrence of the C. difficile-caused infectious disease, or a complication of the C. difficile-caused infectious disease.
COMPOUND WITH ANTI-SPORE ACTIVITY AND PHARMACEUTICAL COMPOSITION THEREOF
The present disclosure provides a compound represented by formula (I), or a salt or a stereoisomer thereof. The compound is capable of effectively inhibiting germination of Clostridium difficile spores with a significant bacteriostatic activity. The compound has an excellent prospect for use in preparation of a drug for preventing and/or treating a C. difficile-caused infectious disease, recurrence of the C. difficile-caused infectious disease, or a complication of the C. difficile-caused infectious disease.
METHODS FOR IMPROVED PRODUCTION OF VITAMINS D2 AND D3
It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.
METHODS FOR IMPROVED PRODUCTION OF VITAMINS D2 AND D3
It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.