C07D233/84

METHODS AND MATERIALS FOR INHIBITING NF-kB ACTIVITY
20230041576 · 2023-02-09 ·

This document provides compounds that are inhibitors of NF-κB activity, as well as the methods of using such compounds for treating diseases and conditions such as cancer, inflammatory conditions, or autoimmune diseases.

NOVEL HEADGROUP LIPID COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

The disclosure features novel lipids and compositions involving the same. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

COMPOSITION FOR SLEEP IMPROVEMENT COMPRISING ERGOTHIONEINE OR SALT THEREOF

The present invention aims to provide a composition for sleep improvement, which contains a highly safe substance as an active ingredient, and a method of improving sleep. The present invention relates to, for example, a composition for sleep improvement, which contains L-ergothioneine or a salt thereof as an active ingredient.

ACLY inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

SUBSTITUTED IMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS

The invention provides substituted imidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.

Use of ergothioneine for extending lifespan or improving healthspan

Among others, the present invention provides novel methods for extending lifespan or improving healthspan in a mammal, which include administration to the mammal of a composition containing a therapeutically effective amount of ergothioneine, or a pharmaceutically acceptable salt, acid, ester, analog or derivative thereof.

Compounds

The present invention relates to compounds of formula (I), wherein Q is selected from O or S; R.sup.1 is a 5- or 6-membered heteroaryl group consisting of one or more carbon atoms, and one or more nitrogen and/or oxygen atoms, and substituted with a monovalent, optionally substituted cycloalkyl, cycloalkenyl or heterocyclic group, wherein the 5- or 6-membered heteroaryl group of R.sup.1 may optionally be further substituted; R.sup.2 is an α,α′-substituted cyclic group which may optionally be further substituted; R.sup.3 and R.sup.4 are each independently hydrogen, halogen, —OH, —NH.sub.2, —CN, —R.sup.5, —OR.sup.5, —NHR.sup.5 or —N(R.sup.5).sub.2; or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R.sup.5 is independently an optionally substituted C.sub.1-C.sub.4 alkyl group. 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##

Compounds

The present invention relates to compounds of formula (I), wherein Q is selected from O or S; R.sup.1 is a 5- or 6-membered heteroaryl group consisting of one or more carbon atoms, and one or more nitrogen and/or oxygen atoms, and substituted with a monovalent, optionally substituted cycloalkyl, cycloalkenyl or heterocyclic group, wherein the 5- or 6-membered heteroaryl group of R.sup.1 may optionally be further substituted; R.sup.2 is an α,α′-substituted cyclic group which may optionally be further substituted; R.sup.3 and R.sup.4 are each independently hydrogen, halogen, —OH, —NH.sub.2, —CN, —R.sup.5, —OR.sup.5, —NHR.sup.5 or —N(R.sup.5).sub.2; or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R.sup.5 is independently an optionally substituted C.sub.1-C.sub.4 alkyl group. 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##

ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE

The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.

ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE

The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.