C07D267/16

Imaging histone deacetylases with a radiotracer using positron emission tomography

Disclosed herein are histone deacetylase imaging agents for positron emission tomography and related imaging methods using the histone deacetylase imaging agents. The histone deacetylase imaging agents may be a compound of formula (I): wherein R.sup.1 is a moiety including a positron emitter; R.sup.2 represents hydrogen, or substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and n is an integer selected from 0 or 1. In one version of the compound of formula (I), R.sup.1 is a moiety including an adamantyl group. ##STR00001##

Ring closing synthesis of macrocyclic MCL-1 inhibitor intermediates

Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof. ##STR00001##

Ring closing synthesis of macrocyclic MCL-1 inhibitor intermediates

Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof. ##STR00001##

Tricyclic compounds with OMA1/OPA1 modulatory properties

Tricyclic compounds, and in particular novel dibenzoxazepin derivates are disclosed herein, which were quite surprisingly found as having OMA1 and/or OPA1 modulatory properties. Compounds of present invention may provide useful for the treatment of certain conditions and diseases, which are amenable to OMA1 and/or OPA1-modulatory therapies. Such conditions may include conditions and diseases prevalent in the elderly, including cancer. Pharmaceutical compositions comprising compounds of present invention may be combined with other treatments or further comprise other pharmaceutically active ingredients.

Tricyclic compounds with OMA1/OPA1 modulatory properties

Tricyclic compounds, and in particular novel dibenzoxazepin derivates are disclosed herein, which were quite surprisingly found as having OMA1 and/or OPA1 modulatory properties. Compounds of present invention may provide useful for the treatment of certain conditions and diseases, which are amenable to OMA1 and/or OPA1-modulatory therapies. Such conditions may include conditions and diseases prevalent in the elderly, including cancer. Pharmaceutical compositions comprising compounds of present invention may be combined with other treatments or further comprise other pharmaceutically active ingredients.

Imaging histone deacetylases with a radiotracer using positron emission tomography

Disclosed herein are histone deacetylase imaging agents for positron emission tomography and related imaging methods using the histone deacetylase imaging agents. The histone deacetylase imaging agents may be a compound of formula (I): ##STR00001##
wherein R.sup.1 is a moiety including a positron emitter; R.sup.2 represents hydrogen, or substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and n is an integer selected from 0 or 1. In one version of the compound of formula (I), R.sup.1 is a moiety including an adamantyl group.

Imaging histone deacetylases with a radiotracer using positron emission tomography

Disclosed herein are histone deacetylase imaging agents for positron emission tomography and related imaging methods using the histone deacetylase imaging agents. The histone deacetylase imaging agents may be a compound of formula (I): ##STR00001##
wherein R.sup.1 is a moiety including a positron emitter; R.sup.2 represents hydrogen, or substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and n is an integer selected from 0 or 1. In one version of the compound of formula (I), R.sup.1 is a moiety including an adamantyl group.