C07J43/003

ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

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.

IMMUNE CELL MODULATORS
20230119606 · 2023-04-20 ·

Disclosed are immune cell-selective small molecule compounds that modulate certain immune cell-specific receptors and enzymes, and methods of their synthesis and use to treat proliferative disorders.

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.

Phosphonium Compound, Reagent Kit for Derivatization, Mass Spectrometric Method, and Method for Producing Phosphonium Compound

Provided is a phosphonium compound represented by Formula (I):

##STR00001##

in Formula (I), R.sup.1, R.sup.2, and R.sup.3 are independently from each other, an alkyl group or an aryl group, the alkyl group is a substituted or unsubstituted, linear or branched alkyl group having 1 to 20 carbon atoms or a substituted or unsubstituted cyclic alkyl group having 5 to 20 carbon atoms, the aryl group is a substituted or unsubstituted aryl group having 6 to 20 carbon atoms; X is a reactive group having a hydrazide group, a halide group, a pseudohalide group, or a thioester group; and Y.sup.− is an anion having a total charge of −1, or Y.sup.− is absence.

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.