C07D215/38

Histone methyltransferase inhibitors
11713299 · 2023-08-01 · ·

The present disclosure provides compounds of Formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. ##STR00001##
where R.sup.1, alk, R.sup.2, Z.sup.1, Z.sup.2, X, R.sup.3, R.sup.4, B, a, and b are as described herein.

Histone methyltransferase inhibitors
11713299 · 2023-08-01 · ·

The present disclosure provides compounds of Formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. ##STR00001##
where R.sup.1, alk, R.sup.2, Z.sup.1, Z.sup.2, X, R.sup.3, R.sup.4, B, a, and b are as described herein.

QUINOLINONE DERIVATIVES AS METHIONINE ADENOSYLTRANSFERASE 2A INHIBITORS
20230227409 · 2023-07-20 ·

Disclosed herein are certain quinolinone derivatives of Formula (A) that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.

##STR00001##

QUINOLINONE DERIVATIVES AS METHIONINE ADENOSYLTRANSFERASE 2A INHIBITORS
20230227409 · 2023-07-20 ·

Disclosed herein are certain quinolinone derivatives of Formula (A) that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.

##STR00001##

TETRAHYDROQUINOLINE DERIVATIVES AND A PROCESS OF PREPARATION THEREOF

The present disclosure provides tetrahydroquinoline derivatives of Formula (I)

##STR00001##

wherein X.sub.1 and X.sub.2 each, independently, are oxygen or sulphur; R.sub.1 is a lower alkoxy, or an optionally substituted aryl group; R.sub.2 is selected from a group consisting of hydrogen, lower alkyl, haloalkyl, or an amino group; R.sub.3 and R.sub.4 each, independently, are hydrogen, or lower alkyl groups; and R5 and R6 are optionally substituted aryl groups. The present disclosure also provides a method for making the compound of Formula (I).

TETRAHYDROQUINOLINE DERIVATIVES AND A PROCESS OF PREPARATION THEREOF

The present disclosure provides tetrahydroquinoline derivatives of Formula (I)

##STR00001##

wherein X.sub.1 and X.sub.2 each, independently, are oxygen or sulphur; R.sub.1 is a lower alkoxy, or an optionally substituted aryl group; R.sub.2 is selected from a group consisting of hydrogen, lower alkyl, haloalkyl, or an amino group; R.sub.3 and R.sub.4 each, independently, are hydrogen, or lower alkyl groups; and R5 and R6 are optionally substituted aryl groups. The present disclosure also provides a method for making the compound of Formula (I).

SELECTIVE NEURONAL NITRIC OXIDE SYNTHASE INHIBITORS
20220411377 · 2022-12-29 ·

Disclosed are 7-phenyl-2-aminoquinoline compounds that are shown to inhibit the biological activity of neuronal nitric oxide synthases (nNOSs). Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject in need thereof. Because the disclosed compounds are shown to inhibit the activity of neuronal nitric oxide synthases (nNOSs), the disclosed compounds and pharmaceutical compositions may be utilized in methods for treating a subject having or at risk for developing a disease or disorder that is associated with nNOS activity including neurological diseases and disorders.

SELECTIVE NEURONAL NITRIC OXIDE SYNTHASE INHIBITORS
20220411377 · 2022-12-29 ·

Disclosed are 7-phenyl-2-aminoquinoline compounds that are shown to inhibit the biological activity of neuronal nitric oxide synthases (nNOSs). Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject in need thereof. Because the disclosed compounds are shown to inhibit the activity of neuronal nitric oxide synthases (nNOSs), the disclosed compounds and pharmaceutical compositions may be utilized in methods for treating a subject having or at risk for developing a disease or disorder that is associated with nNOS activity including neurological diseases and disorders.

COMPOUNDS AND METHODS FOR MODULATING RNA FUNCTION

The present invention provides compounds, compositions thereof, and methods of using the same.

COMPOUNDS AND METHODS FOR MODULATING RNA FUNCTION

The present invention provides compounds, compositions thereof, and methods of using the same.