149806-05-3

Upstream product

• 740841-42-3 6-bromonicotinoyl chloride 
• 1117-97-1 N,0-dimethylhydroxylamine 
• 6311-35-9 6-bromonicotinic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 

Downstream Products

• 416852-53-4 N-methoxy-N-methyl-6-(trifluoromethyl)pyridine-3-carboxamide 

Relevant academic research and scientific papers

NOVEL COMPOUNDS HAVING EFFECTS OF TREATING INFLAMMATORY DISEASE AS P38 MAP KINASE INHIBITOR

The present invention relates to novel compounds exhibiting anti-inflammatory activity. The compound of the present invention plays a critical role in the production of inflammatory prodrug (pro-inflammatory cytokines) and has an excellent inhibitory effe

Catalytic Enantioselective Pyridine N-Oxidation

The catalytic, enantioselective N-oxidation of substituted pyridines is described. The approach is predicated on a biomolecule-inspired catalytic cycle wherein high levels of asymmetric induction are provided by aspartic-acid-containing peptides as the aspartyl side chain shuttles between free acid and peracid forms. Desymmetrizations of bis(pyridine) substrates bearing a remote pro-stereogenic center substituted with a group capable of hydrogen bonding to the catalyst are demonstrated. Our approach presents a new entry into chiral pyridine frameworks in a heterocycle-rich molecular environment. Representative functionalizations of the enantioenriched pyridine N-oxides further document the utility of this approach. Demonstration of the asymmetric N-oxidation in two venerable drug-like scaffolds, Loratadine and Varenicline, show the likely generality of the method for highly variable and distinct chiral environments, while also revealing that the approach is applicable to both pyridines and 1,4-pyrazines.

PIPERIDINE COMPOUNDS AS PCSK9 INHIBITORS

One aspect of the invention relates to a series of new PCSK9 inhibitor compounds comprising piperidine ring structures, including compounds of formula (I) and/or pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating PCSK9 receptor related diseases comprising administration of one or more compounds of formula (I) or a pharmaceutically acceptable salt thereof.

Discovery of AZD6642, an inhibitor of 5-lipoxygenase activating protein (FLAP) for the treatment of inflammatory diseases

A drug discovery program in search of novel 5-lipoxygenase activating protein (FLAP) inhibitors focused on driving a reduction in lipophilicity with maintained or increased ligand lipophilic efficiency (LLE) compared to previously reported compounds led to the discovery of AZD6642 (15b). Introduction of a hydrophilic tetrahydrofuran (THF) ring at the stereogenic central carbon atom led to a significant shift in physicochemical property space. The structure-activity relationship exploration and optimization of DMPK properties leading to this compound are described in addition to pharmacokinetic analysis and an investigation of the pharmacokinetic (PK)-pharmacodynamic (PD) relationship based on ex vivo leukotriene B4 (LTB4) levels in dog. AZD6642 shows high specific potency and low lipophilicity, resulting in a selective and metabolically stable profile. On the basis of initial PK/PD relation measured, a low dose to human was predicted.

ALKYNE-BRIDGED HETERO-AROMATICS AND USES THEREOF

This invention relates to novel alkyne-bridged hetero-aromatics as described in the specification which are PDE10A inhibitors and useful for the treatment of neurological, psychiatric disorder, metabolic disorders, such as Schizophrenia, Parkinson's disea

Discovery of biphenylketones as dual modulators of inflammation and bone loss

Biphenylketones were identified as novel inhibitors of NFκB activation. Structure-activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50 = 0.8 μM), showed oral activity, and was able to compl