Patent classifications
C07D515/04
NRF2-ACTIVATING COMPOUND
A compound having Nrf2-activating action is provided. The compound is represented by formula (I), a salt of the compound, or a solvate of the compound or salt:
##STR00001##
wherein R.sup.1a and R.sup.1b are identical or different and represent a hydrogen atom, an alkyl group, or a halogen atom; R.sup.2 represents an optionally substituted group derived from a heterocycle, and the heterocycle represents thiophene, furan, pyrrole, thiazole, or a fused ring including any of these heterocycles; R.sup.4 and R.sup.5 are identical or different and represent a hydrogen atom or an optionally substituted alkyl group, or R.sup.4 and R.sup.5 bind with each other to form —NH—CH—N—; R.sup.6 represents an optionally substituted alkyl group; A.sup.1, A.sup.2, A.sup.3, and A.sup.4 are identical or different and represent CH or N wherein the number of N is 1 or less; and Z represents a hydrogen atom or a halogen atom.
NRF2-ACTIVATING COMPOUND
A compound having Nrf2-activating action is provided. The compound is represented by formula (I), a salt of the compound, or a solvate of the compound or salt:
##STR00001##
wherein R.sup.1a and R.sup.1b are identical or different and represent a hydrogen atom, an alkyl group, or a halogen atom; R.sup.2 represents an optionally substituted group derived from a heterocycle, and the heterocycle represents thiophene, furan, pyrrole, thiazole, or a fused ring including any of these heterocycles; R.sup.4 and R.sup.5 are identical or different and represent a hydrogen atom or an optionally substituted alkyl group, or R.sup.4 and R.sup.5 bind with each other to form —NH—CH—N—; R.sup.6 represents an optionally substituted alkyl group; A.sup.1, A.sup.2, A.sup.3, and A.sup.4 are identical or different and represent CH or N wherein the number of N is 1 or less; and Z represents a hydrogen atom or a halogen atom.
CYCLIC SULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF
The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof).
CYCLIC SULFONAMIDE DERIVATIVES AS TRAP1 MODULATORS AND USES THEREOF
The present disclosure provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“TNF”) receptor associated protein 1 (“TRAP1”) modulators (e.g., TRAP1 activators). The provided compounds may also rescue the activity in PTEN-induced kinase 1 (“PINK1”) loss of function contexts. The provided compounds may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof).
Bicylic compound acting as an inhibitor
A bicyclic compound acting as a RORγ inhibitor. Provided are a compound of formula (I) or a pharmaceutically acceptable salt thereof, the compound having a structure as represented by formula (I-A) or formula (I-B). The provided compound of formula (I-A) or formula (I-B) or pharmaceutically acceptable salt thereof has good RORγ inhibitory activities, being expected to be used for treating diseases mediated by RORγ receptors in a mammal. ##STR00001##
INHIBITORS OF HEPATITIS B VIRUS
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing the compounds.
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
##STR00001##
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
##STR00001##
Tricyclic inhibitors of Hepatitis B virus
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing the compounds.
Ataxia Telengiectasia And RAD3-Related (ATR) Inhibitors And Methods Of Their Use
The disclosure is directed to compounds and compositions that inhibit Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase and methods of their use.