16759-48-1

Upstream product

• 7170-01-6 3-methyl-1H-[1,2,4]triazole 
• 350-46-9 4-Fluoronitrobenzene 
• 100-01-6 4-nitro-aniline 
• 122-51-0 orthoformic acid triethyl ester 

Downstream Products

• 52739-51-2 4-(3-methyl-1H-1,2,4-triazol-1-yl)aniline 
• 1361391-64-1 4-(3-methyl-1H-1,2,4-triazol-1-yl)phenol 
• 1361391-62-9 2-(4-(5-ethylpyrimidin-2-yloxy)cyclohexyl)-4-((4-(3-methyl-1H-1,2,4-triazol-1-yl)phenoxy)methyl)thiazole 
• 1255700-86-7 (R)-4-methyl-N-(4-(3-methyl-1H-1,2,4-triazol-1-yl)phenyl)-2-phenyl-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine 

Relevant academic research and scientific papers

CATHEPSIN K INHIBITOR AND APPLICATION THEREOF

The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.

HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES

Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.

Multicomponent synthesis of 1-aryl 1,2,4-triazoles

A multicomponent (single reactor) process for the synthesis of 1-aryl 1,2,4-triazoles was explored and developed. This transformation prepared the 1,2,4-triazole directly from anilines, amino pyridines, and pyrimidines. The reaction scope was explored with 21 different substrates, and the position of the nitrogen atoms in the newly formed ring was established by 15N labeling and NMR spectroscopy.

CYCLOHEXANE ANALOGUES AS GPR119 AGONISTS

This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.

NEW COMPOUNDS MODULATING GAMMA-SECRETASE AND THEIR USE IN THE TREATMENT OF ALPHA BETA RELATED PATHOLOGIES, SUCH AS ALZHEIMER'S DISEASE

The present invention relates to novel compounds of formulae (I) and (II) and therapeutically acceptable salts thereof, their pharmaceutical compositions processes for making them and their use in therapeutic methods for treatment and/or prevention of var

Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors

Given the significant body of data supporting an essential role for c-jun-N-terminal kinase (JNK) in neurodegenerative disorders, we set out to develop highly selective JNK inhibitors with good cell potency and good brain penetration properties. The structure-activity relationships (SAR) around a series of aminopyrimidines were evaluated utilizing biochemical and cell-based assays to measure JNK inhibition and brain penetration in mice. Microsomal stability in three species, P450 inhibition, inhibition of generation of reactive oxygen species (ROS), and pharmacokinetics in rats were also measured. Compounds 9g, 9i, 9j, and 9l had greater than 135-fold selectivity over p38, and cell-based IC50 values 50 = 0.8 nM for inhibition of ROS and had good pharmacokinetic properties in rats along with a brain-to-plasma ratio of 0.75. These results suggest that biaryl substituted aminopyrimidines represented by compound 9l may serve as the first small molecule inhibitors to test efficacy of JNK inhibitors in neurodegenerative disorders. 2009 American Chemical Society.

SUBSTITUTED PYRIMIDINYL-AMINES AS PROTEIN KINASE INHIBITORS

The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.