Patent classifications
C07D231/56
Inhibitors of NLRP3 inflammasome
The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging; wherein the inhibitors of NLRP3 inflammasomes are compounds of Formula VII: ##STR00001##
or a pharmaceutically acceptable salt thereof.
SULPHONAMIDES AS METHIONINE METABOLIC PATHWAY INHIBITORS
The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.
METHOD FOR CONTROLLING SOYBEAN RUST FUNGUS RESISTANT TO QoI FUNGICIDES
The present invention provides a method for controlling a soybean rust fungus having an amino acid substitution of F129L in a mitochondrial cytochrome b protein. A compound represented by formula (I)
##STR00001##
[wherein: X.sup.1 represents —C(H)═ or the like; X.sup.2 represents —C(O)OCH.sub.3 or the like; Y.sup.1 represents —C(R.sup.4)═ or the like; Y.sup.2 represents —C(R.sup.5)═ or the like; R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 each represent a C1-C4 alkyl group or the like; and E represents a C1-C6 chain hydrocarbon group or the like]
can be used for controlling a soybean rust fungus having an amino acid substitution of F129L in a mitochondrial cytochrome b protein.
2H-INDAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
This invention relates to 2H-indazole Derivatives of formula (I′), or pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, capable of modulating the activity of IRAK4. The invention further provides a method of manufacturing compounds of the invention, and methods for their therapeutic use. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including inflammatory disease, autoimmune disease, cancer, cardiovascular disease, a disease of the central nervous system, disease of the skin, an ophthalmic disease and condition, and a bone disease.
##STR00001##
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.
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.
NOVEL PYRAZOLE DERIVATIVES
The Present invention provides a novel pyrazole derivative compound represented by Chemical formula 1, a stereoisomer thereof, a solvate thereof, an isotopic variant thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
##STR00001##
(In the above, A, B and R, and the like are the same as defined in the description of the invention.)
4-AMINOBUT-2-ENAMIDE DERIVATIVES AND SALTS THEREOF
The present invention provides an antitumor agent comprising a compound or a pharmaceutically acceptable salt thereof that covalently binds to GTP-bound KRASG12C as an active ingredient.
COMBINED USE OF SODIUM TRANS-[TETRACHLORIDOBIS(1H-INDAZOLE)RUTHENATE(III)] AND ETOMOXIR FOR TREATING CANCERS
Methods are provided for treating a cancer in a human patient in need thereof, comprising administering an effective amount of sodium trans-[tetrachloridobis(1H-indazole)ruthenate(III)] and a effective amount of etomoxir.
INHIBITORS OF HIF-2ALPHA
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.