C07D307/66

Inhibitors of Beta-Hydroxylase for Treatment of Cancer
20180009798 · 2018-01-11 ·

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

Inhibitors of Beta-Hydroxylase for Treatment of Cancer
20180009798 · 2018-01-11 ·

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

Organic electroluminescent element, compound for use in the element, and light emitting device, display device, and illumination device using the element

The disclosure relates to organic electroluminescent elements, compounds for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): ##STR00001##
where R.sup.1 to R.sup.3 and R.sup.6 to R.sup.8 each independently represents a hydrogen atom, which may be a deuterium atom, or a substituent with a Hammett substituent constant σ.sub.p value of −0.15 or more, R.sup.5, R.sup.9 and R.sup.10 each independently represents a hydrogen atom or a substituent, L.sup.1 represents a divalent linking group, DG.sup.1 represents a donor group, and n1 represents 1 or 2, and where R.sup.1 to R.sup.3, R.sup.5 to R.sup.10, L.sup.1, and DG.sup.1 are not bound to each other to form a ring.

Organic electroluminescent element, compound for use in the element, and light emitting device, display device, and illumination device using the element

The disclosure relates to organic electroluminescent elements, compounds for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): ##STR00001##
where R.sup.1 to R.sup.3 and R.sup.6 to R.sup.8 each independently represents a hydrogen atom, which may be a deuterium atom, or a substituent with a Hammett substituent constant σ.sub.p value of −0.15 or more, R.sup.5, R.sup.9 and R.sup.10 each independently represents a hydrogen atom or a substituent, L.sup.1 represents a divalent linking group, DG.sup.1 represents a donor group, and n1 represents 1 or 2, and where R.sup.1 to R.sup.3, R.sup.5 to R.sup.10, L.sup.1, and DG.sup.1 are not bound to each other to form a ring.

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.

Sulphonyl urea derivatives as NLRP3 inflammasome modulators

The present disclosure relates to compounds of Formula (I): ##STR00001##
and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

Sulphonyl urea derivatives as NLRP3 inflammasome modulators

The present disclosure relates to compounds of Formula (I): ##STR00001##
and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

PANTETHENOYLCYSTEINE DERIVATIVES AND USES THEREOF

The present disclosure relates to compounds of Formula (I) or (II): (Formulae (I), (II)), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.

##STR00001##

PANTETHENOYLCYSTEINE DERIVATIVES AND USES THEREOF

The present disclosure relates to compounds of Formula (I) or (II): (Formulae (I), (II)), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.

##STR00001##

ANDROGEN RECEPTOR MODULATORS AND METHODS FOR USE AS PROTEOLYSIS TARGETING CHIMERA LIGANDS
20230078913 · 2023-03-16 ·

The present invention relates to bifunctional Proteolysis Targeting Chimeric ligands (Protac compounds) comprising a ligase modulator/binder and a molecule that binds to a protein target of interest, and methods of treating various diseases and conditions with the Protac compounds, including diseases associated with androgen receptors.