C07D263/46

Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer

Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: ##STR00001##
wherein W, X, Y, Z, x, R.sup.1, R.sup.2, R.sup.3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

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.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

Compounds and compositions for treating conditions associated with NLRP activity
11597706 · 2023-03-07 · ·

In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured: Formulae (I) and (II), wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein. ##STR00001##

Compounds and compositions for treating conditions associated with NLRP activity
11597706 · 2023-03-07 · ·

In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured: Formulae (I) and (II), wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein. ##STR00001##

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

STACKED ORGANIC ELECTROLUMINESCENT DEVICE

Provided is a stacked organic electroluminescence device. At least one light-emitting unit of the stacked organic electroluminescent device includes an organic layer including a specific combination of a P-type material with a deep LUMO energy level and a hole transporting material with a deep HOMO energy level. Meanwhile, a P-type material is used as the buffer layer of the charge generation layer between the light-emitting units. The device can offer better device performance and more simplified fabrication process. Further provided is a display assembly including the device.

SMALL MOLECULE INHIBITORS OF ONCOGENIC CHD1L WITH PRECLINICAL ACTIVITY AGAINST COLORECTAL CANCER

Treatment of CHD1L-driven cancers, including TCF transcription-driven cancers and EMT-driven cancers using CHD1L inhibitors. Small molecule inhibitors of CHDL1 which inhibit CHD1L ATPase and inhibit CHD1L-dependent TCF-transcription have been identified. CHD1L inhibitors prevent the TCF-complex from binding to Wnt response elements and promoter sites. More specifically, CHD1L inhibitors induce the reversion of EMT. CHD1L inhibitors are useful in the treatment of various cancers and particularly CRC and m-CRC. The CHD1L-driven cancer is among others, CRC, breast cancer, glioma, liver cancer, lung cancer or gastrointestinal (GI) cancers. CHD1L inhibitors of formulas I and XX and salts thereof as defined herein are provided as well as pharmaceutical compositions containing CHD1L inhibitors. Synergistic combinations of CHD1L inhibitors with other antineoplastic agents are also described.