C07D223/12

Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof

The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.

Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof

The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.

HISTONE DEACETYLASE INHIBITORS
20190382342 · 2019-12-19 ·

Provided herein are compounds and methods for inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

HISTONE DEACETYLASE INHIBITORS
20190382342 · 2019-12-19 ·

Provided herein are compounds and methods for inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES AND DISORDERS

The present disclosure relates to compounds that are capable of inhibiting PRMT8 and/or upregulating SirT1. The disclosure further relates to methods of treating neurodegenerative diseases and disorders (e.g., Alzheimer's disease).

COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES AND DISORDERS

The present disclosure relates to compounds that are capable of inhibiting PRMT8 and/or upregulating SirT1. The disclosure further relates to methods of treating neurodegenerative diseases and disorders (e.g., Alzheimer's disease).

Oxalic amide ligands, and uses thereof in copper-catalyzed coupling reaction of aryl halides

The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of CN, CO and CS bonds. ##STR00001##

Oxalic amide ligands, and uses thereof in copper-catalyzed coupling reaction of aryl halides

The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of CN, CO and CS bonds. ##STR00001##

Prodrugs of Chlorokynurenines
20190308934 · 2019-10-10 ·

The present disclosure relates to prodrugs of 7-chlorokynurenic acid. In certain embodiments, the prodrugs include those having the structure of any one of formula (I)-(VIII), wherein R.sup.1-R.sup.13, monomer 1, monomer 2, and linker are defined herein. Also provided are methods of preparing and using these prodrugs.

##STR00001## ##STR00002##

Prodrugs of Chlorokynurenines
20190308934 · 2019-10-10 ·

The present disclosure relates to prodrugs of 7-chlorokynurenic acid. In certain embodiments, the prodrugs include those having the structure of any one of formula (I)-(VIII), wherein R.sup.1-R.sup.13, monomer 1, monomer 2, and linker are defined herein. Also provided are methods of preparing and using these prodrugs.

##STR00001## ##STR00002##