Patent classifications
C07D209/34
COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
The present disclosure relates to a compound and a preparation method and application thereof, the compound having a chemical structure formula of:
##STR00001##
wherein M in the formula is selected from a group consisting of CF.sub.3 or CF.sub.2H, and R.sub.1, R.sub.2, and R.sub.3 are each independently selected from a group consisting of aryl, heteroaryl, and alkyl. The compound provided by the present disclosure can be used as a trifluoroethanolation reagent or difluoroethanolation reagent as synthetic intermediates of many organic compounds, and some of the compounds have pharmaceutical activity. The preparation steps of such compounds are simplified, with mild synthesis conditions and wide applicability of substrates.
Histone acetyltransferase activators and uses thereof
The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.
Histone acetyltransferase activators and uses thereof
The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.
NOVEL SULFONAMIDEUREA COMPOUNDS
The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R.sup.1 and R.sup.3 are each independently hydrogen or an optionally substituted hydrocarbyl group, or R.sup.1 and R.sup.3 together with the nitrogen atom to which they are attached may form a 3- to 12-membered optionally substituted cyclic group; and R.sup.2 is a cyclic group substituted at the position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
##STR00001##
Opioid receptor modulators and products and methods related thereto
Compounds are provided having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
Opioid receptor modulators and products and methods related thereto
Compounds are provided having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
METHODS AND MATERIALS FOR INCREASING OR MAINTAINING NICOTINAMIDE MONONUCLEOTIDE ADENYLYL TRANSFERASE-2 (NMNAT2) POLYPEPTIDE LEVELS
This document provides methods and materials for increasing or maintaining NMNAT2 polypeptide levels within cells. For example, compounds (e.g., organic compounds) having the ability to increase or maintain NMNAT2 polypeptide levels within cells, formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for increasing or maintain NMNAT2 polypeptide levels within cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in NMNAT2 polypeptide levels are provided (or for preventing said condition).
SMALL MOLECULE GRB2 STABILIZERS FOR RAS MAP KINASE INHIBITION
The present disclosure compounds of the formula (I-A) or (I), wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods for the use of said compounds and/or pharmaceutical compositions, such as in the treatment of cancer. The present disclosure also provides methods for the use of compounds of the formula (III), wherein the variables are defined herein.
##STR00001##
SMALL MOLECULE GRB2 STABILIZERS FOR RAS MAP KINASE INHIBITION
The present disclosure compounds of the formula (I-A) or (I), wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods for the use of said compounds and/or pharmaceutical compositions, such as in the treatment of cancer. The present disclosure also provides methods for the use of compounds of the formula (III), wherein the variables are defined herein.
##STR00001##
NEW ISOINDOLINONE SUBSTITUTED INDOLES AND DERIVATIVES AS RAS INHIBITORS
The present invention relates to new isoindolinone or isobenzofuranone substituted indoles and derivatives of formula (I) wherein the groups R.sup.1 to R.sup.7, R.sup.10 and n have the meanings given in the claims and specification, their use as inhibitors of RAS-family proteins and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
##STR00001##