C07D277/36

cGAS ANTAGONIST COMPOUNDS

Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

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.

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.

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.

PYRROLIDINE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING BETA-AMYLOID OR TAU PROTEIN-ASSOCIATED DISEASES CONTAINING SAME

Provided are: a novel pyrrolidine derivative or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing same and having the effects of inhibiting beta-amyloid and/or tau protein aggregation, and/or breaking down beta-amyloid and/or tau protein aggregates, and/or preventing and/or treating beta-amyloid and/or tau protein-associated diseases.

PYRROLIDINE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING BETA-AMYLOID OR TAU PROTEIN-ASSOCIATED DISEASES CONTAINING SAME

Provided are: a novel pyrrolidine derivative or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing same and having the effects of inhibiting beta-amyloid and/or tau protein aggregation, and/or breaking down beta-amyloid and/or tau protein aggregates, and/or preventing and/or treating beta-amyloid and/or tau protein-associated diseases.

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##

CGAS antagonist compounds

Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.