C07D419/14

SMALL MOLECULE DEGRADERS OF HELIOS AND METODS OF USE

Disclosed are compounds and pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomers, or tautomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders associated with Helios and which may benefit from Helios degradation.

SMALL MOLECULE DEGRADERS OF HELIOS AND METODS OF USE

Disclosed are compounds and pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomers, or tautomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders associated with Helios and which may benefit from Helios degradation.

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
20230218632 · 2023-07-13 · ·

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).

Aryl hydrocarbon receptor modulators
11547698 · 2023-01-10 · ·

The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.

Aryl hydrocarbon receptor modulators
11547698 · 2023-01-10 · ·

The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.

NEW MACROCYCLIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

A compound of formula (I):

##STR00001##

wherein Z, Y.sub.1, Y.sub.2,

##STR00002##

R.sub.1 to R.sub.7 are as defined in the description, its optical isomers, and addition salts thereof with a pharmaceutically acceptable base.

Medicaments.

MOLECULES HAVING CERTAIN PESTICIDAL UTILITIES, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES RELATED THERETO

This disclosure relates to compounds having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such compounds and intermediates used in such processes, compositions containing such compounds, and processes of using such compounds against such pests. These compounds/molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses compounds having the following formula (“Formula One” and/or “Formula One-A”).

##STR00001##

MOLECULES HAVING CERTAIN PESTICIDAL UTILITIES, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES RELATED THERETO

This disclosure relates to compounds having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such compounds and intermediates used in such processes, compositions containing such compounds, and processes of using such compounds against such pests. These compounds/molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses compounds having the following formula (“Formula One” and/or “Formula One-A”).

##STR00001##