Patent classifications
C07D235/12
Substituted imidazole salt compounds, preparation method thereof, pharmaceutical composition thereof and application thereof
Disclosed in the invention are a type of compounds having aldolase selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for inhibiting triglyceride and cholesterol synthesis, for reducing fatty acid synthesis, for preventing and/or treating obesity and type II diabetes, for preventing and/or treating tumor, for preventing and/or treating Parkinson's disease, for preventing and/or treating Alzheimer's disease or for prolonging the lifespan of mammals: ##STR00001##
Substituted imidazole salt compounds, preparation method thereof, pharmaceutical composition thereof and application thereof
Disclosed in the invention are a type of compounds having aldolase selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for inhibiting triglyceride and cholesterol synthesis, for reducing fatty acid synthesis, for preventing and/or treating obesity and type II diabetes, for preventing and/or treating tumor, for preventing and/or treating Parkinson's disease, for preventing and/or treating Alzheimer's disease or for prolonging the lifespan of mammals: ##STR00001##
Methods of synthesizing substituted purine compounds
The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
Methods of synthesizing substituted purine compounds
The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
Process and method for reducing metal corrosion in water
This disclosure relates to compositions and methods of reducing corrosion using benzimidazoles. The method may include adding a benzimidazole and a halogen to an aqueous system that is in contact with a metal surface. The halogen may be bromine, iodine, or any combination thereof. In some cases, adding the halogen may be optional depending on the substituents on the benzimidazole ring. Compositions are also disclosed that include a benzimidazole, optionally a halogen depending on the substituents on the benzimidazole ring, and optionally a halogen stabilizer.
Process and method for reducing metal corrosion in water
This disclosure relates to compositions and methods of reducing corrosion using benzimidazoles. The method may include adding a benzimidazole and a halogen to an aqueous system that is in contact with a metal surface. The halogen may be bromine, iodine, or any combination thereof. In some cases, adding the halogen may be optional depending on the substituents on the benzimidazole ring. Compositions are also disclosed that include a benzimidazole, optionally a halogen depending on the substituents on the benzimidazole ring, and optionally a halogen stabilizer.
Benzimidazole Derivatives as Modulators of Retinoid-Related Orphan Receptor Gamma (RORy) and Pharmaceutical Use Thereof
The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders.
##STR00001##
Benzimidazole Derivatives as Modulators of Retinoid-Related Orphan Receptor Gamma (RORy) and Pharmaceutical Use Thereof
The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders.
##STR00001##
SUBSTITUTED IMIDAZOLE SALT COMPOUNDS, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION THEREOF AND APPLICATION THEREOF
Disclosed in the invention are a type of compounds having aldolase selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for inhibiting triglyceride and cholesterol synthesis, for reducing fatty acid synthesis, for preventing and/or treating obesity and type II diabetes, for preventing and/or treating tumor, for preventing and/or treating Parkinson's disease, for preventing and/or treating Alzheimer's disease or for prolonging the lifespan of mammals:
##STR00001##
SUBSTITUTED IMIDAZOLE SALT COMPOUNDS, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION THEREOF AND APPLICATION THEREOF
Disclosed in the invention are a type of compounds having aldolase selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for inhibiting triglyceride and cholesterol synthesis, for reducing fatty acid synthesis, for preventing and/or treating obesity and type II diabetes, for preventing and/or treating tumor, for preventing and/or treating Parkinson's disease, for preventing and/or treating Alzheimer's disease or for prolonging the lifespan of mammals:
##STR00001##