C07J43/00

NEUROACTIVE STEROIDS AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
20230118577 · 2023-04-20 ·

The invention of this disclosure is directed to a neuroactive steroid (NAS) of a novel structure. This invention is also directed to a pharmaceutical composition comprising the neuroactive steroid (NAS) and salts thereof. The pharmaceutical composition can be used for preventing and/or treating CNS conditions or diseases related to GABA-modulation, such as depression, bipolar disorder, dementia, Huntington's disease, Parkinson's disease, etc. This invention is further directed to a method for treating a CNS disorder in a subject in need thereof.

Compound for treating clostridium difficile

The invention relates to compounds, compositions and polymers comprising a first component adapted to promote germination of Clostridium difficile (C. diff) and a second component which acts as an antimicrobial agent. Said compounds, compositions and polymers are useful for destroying C. diff where conventional antimicrobial agents are unsuccessful. The compositions can be formulated as coating or materials which actively destroy C. diff which come into contact with it. The germination promotion is induced by bile salts. The invention also relates to the use of such materials as a treatment for C. diff associated diseases and toxic megacolon.

Steroid derivative regulators, method for preparing the same, and uses thereof

Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA .sub.A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description. ##STR00001##

SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE CONJUGATES

Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Described herein are neuroactive steroids of the Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein custom-character, 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.

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 purifying crude rocuronium bromide

A method for purifying crude rocuronium bromide includes removing the residual solvent in crude rocuronium bromide by vacuum microwave drying or fluidized drying to meet medicinal requirements. High-quality rocuronium bromide can be obtained by the method of the present application. The method makes the large-scale industrial production of rocuronium bromide easy to realize, and can also avoid or reduce the use of diethyl ether which is a flammable and explosive solvent. In addition, the equipment used requires less expense and occupies less space.

p53 MODULATORS AND USES THEREOF
20230145782 · 2023-05-11 ·

Described herein, inter alia, are p53 modulator compounds and methods of using the same. In an aspect is provided a p53 protein covalently bonded to a compound described herein. In an aspect is provided a pharmaceutical composition including a compound described herein and a pharmaceutically acceptable excipient. In an aspect is provided a method of treating cancer in a subject in need of such treatment, including administering to the subject an effective amount of a compound described herein.

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.

PRODRUGS OF FULVESTRANT

The present invention relates to Fulvestrant prodrugs and process for the preparation thereof. The present disclosure also relates to pharmaceutical composition of Fulvestrant prodrugs and method of treatment using the same.