C07D213/79

NOVEL LUMINESCENT LANTHANIDE CHELATE REPORTERS, BIOSPECIFIC BINDING REACTANTS LABELLED WITH NOVEL LUMINESCENT LANTHANIDE CHELATE REPORTERS AND THEIR USE
20220315609 · 2022-10-06 ·

The present invention relates to novel luminescent lanthanide chelate reporters which are formed from two to three separate lanthanide chelate moieties covalently conjugated to each other to act as an unique labelling reactant, and which can be attached to a biospecific reactant and used in various assays.

INHIBITORS OF PHOSPHOLIPID SYNTHESIS AND METHODS OF USE

Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome, hyperlipidemia, infection and inflammation.

INHIBITORS OF PHOSPHOLIPID SYNTHESIS AND METHODS OF USE

Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome, hyperlipidemia, infection and inflammation.

HETEROCYCLE CONTAINING STAT INHIBITORS AND COMPOSITIONS

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for the inhibition of Signal Transducer and Activator of Transcription 5a and 5b (STAT5). Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as, for example, breast cancer and pancreatic cancer.

Modulators of mas-related G-protein receptor X4 and related products and methods

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

Modulators of mas-related G-protein receptor X4 and related products and methods

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

LANTHIONINE SYNTHETASE C-LIKE 2-BASED THERAPEUTICS

Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.

LANTHIONINE SYNTHETASE C-LIKE 2-BASED THERAPEUTICS

Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.

INHIBITORS OF HISTONE DEMETHYLASES

Compounds of the form in which Q is selected from —COOH—CH═NR.sup.12, —W, —CH.sub.2NHR.sup.13, —CH=0 and —CH(OR.sup.17).sub.2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.

##STR00001##

INHIBITORS OF HISTONE DEMETHYLASES

Compounds of the form in which Q is selected from —COOH—CH═NR.sup.12, —W, —CH.sub.2NHR.sup.13, —CH=0 and —CH(OR.sup.17).sub.2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.

##STR00001##