The present disclosure relates generally to therapeutic agents that may be useful as modulators of Integrated Stress Response (ISR) pathway.

Provided are 1,4-diphenyl-1H-imidazole and 2,4-diphenylthiazole derivatives having a structure represented by Formula I, a preparation method therefor and uses thereof: ##STR00001##
wherein R.sub.1 is any one of H, OH, and OCH.sub.3, R.sub.2 is any one of H, NO.sub.2, CH.sub.3, CF.sub.3, SO.sub.2CH.sub.3, COOCH.sub.3, or CONHCH.sub.3, R.sub.3 is any one of H, NO.sub.2, OCH.sub.3, or CF.sub.3, R.sub.4 is selected from H, CF.sub.3, or Cl, R.sub.5 is any one of H, Cl, CF.sub.3, or NHCH.sub.3, and R.sub.6 is any one of OCF.sub.3, CF.sub.3, or CN; V is either C or N, W is either CH or N, X is a C atom, Y is either CH or N, and Z is either CH or S. This compound can be used in preparation of anti-inflammatory adjuvants, TLR1 or TLR2 agonists, and anti-tumor agents and for regulating the activity activation level of TLR1 and TLR2 alkaline phosphatases in vitro and in vivo.

Provided are 1,4-diphenyl-1H-imidazole and 2,4-diphenylthiazole derivatives having a structure represented by Formula I, a preparation method therefor and uses thereof: ##STR00001##
wherein R.sub.1 is any one of H, OH, and OCH.sub.3, R.sub.2 is any one of H, NO.sub.2, CH.sub.3, CF.sub.3, SO.sub.2CH.sub.3, COOCH.sub.3, or CONHCH.sub.3, R.sub.3 is any one of H, NO.sub.2, OCH.sub.3, or CF.sub.3, R.sub.4 is selected from H, CF.sub.3, or Cl, R.sub.5 is any one of H, Cl, CF.sub.3, or NHCH.sub.3, and R.sub.6 is any one of OCF.sub.3, CF.sub.3, or CN; V is either C or N, W is either CH or N, X is a C atom, Y is either CH or N, and Z is either CH or S. This compound can be used in preparation of anti-inflammatory adjuvants, TLR1 or TLR2 agonists, and anti-tumor agents and for regulating the activity activation level of TLR1 and TLR2 alkaline phosphatases in vitro and in vivo.

This invention provides compounds, for example, of Formulae (A)-(H) and (J)-(AA) and pharmaceutically acceptable salts, solvates, esters, amides, and prodrugs thereof. The invention further provides pharmaceutical compositions comprising a compound of the invention, and a pharmaceutically acceptable carrier or vehicle. The compounds and compositions disclosed herein are useful for treating or preventing various diseases and conditions, for example liver disease such as liver fibrosis, fatty liver disease, non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH), and kidney diseases such as acute kidney injury (AKI).

The present invention relates to novel biologically active compounds, in particular dicarboxylic acid bisamide derivatives of general formula I:

##STR00001##

or pharmaceutically acceptable salts thereof, which are able to form complexes with or chelate metal ions. The invention also relates to the use of said compounds as an agent for the prevention and/or treatment of cardiovascular, viral, cancer, neurodegenerative and inflammatory diseases, diabetes, age-related diseases, diseases caused by microbial toxins, alcoholism and alcoholic cirrhosis, anaemia, porphyria cutanea tarda, and transition metal salt poisoning. The present invention also relates to novel methods for preparing dicarboxylic acid bisamide derivatives of general formula I.

The present invention relates to novel biologically active compounds, in particular dicarboxylic acid bisamide derivatives of general formula I:

##STR00001##

or pharmaceutically acceptable salts thereof, which are able to form complexes with or chelate metal ions. The invention also relates to the use of said compounds as an agent for the prevention and/or treatment of cardiovascular, viral, cancer, neurodegenerative and inflammatory diseases, diabetes, age-related diseases, diseases caused by microbial toxins, alcoholism and alcoholic cirrhosis, anaemia, porphyria cutanea tarda, and transition metal salt poisoning. The present invention also relates to novel methods for preparing dicarboxylic acid bisamide derivatives of general formula I.

Described herein are novel γ- and δ-propargyl carboxylic acids and esters. The novel compositions are antagonists of CSE and may be used to modulate of the activity of the carotid body, therefore providing therapeutic benefits for sleep-related breathing disorders and related conditions.

The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.

##STR00001##

Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.

Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.