858600-08-5

Upstream product

• 66572-55-2 6-methoxynicotinic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 26218-80-4 6-methoxy-nicotinic acid methyl ester 
• 33252-28-7 6-chloronicotinonitrile 
• 15871-85-9 6-methoxynicotinonitrile 
• 1117-97-1 N,0-dimethylhydroxylamine 

Downstream Products

• 213193-32-9 1‐(6‐methoxypyridin‐3‐yl)ethan‐1‐one 
• 862098-77-9 (4-bromo-2,5-difluorophenyl)[6-(methyloxy)-3-pyridinyl]methanone 
• 862098-73-5 (2,5-dibromo-3,6-difluorophenyl)[6-(methyloxy)-3-pyridinyl]methanone 
• 885229-42-5 1-(6-methoxypyridin-3-yl)propan-1-one 
• 1124-29-4 1-(6-hydroxypyridin-3-yl)ethanone 
• 31271-20-2 (+/)-1-benzyl-5-ethyl-2-piperidone 
• 32684-80-3 5-acetyl-1-benzylpyridin-2(1H)-one 
• 32401-36-8 (6-methoxypyridin-3-yl)(phenyl)methanone 
• 1296274-02-6 2-{[5-(4-bromobenzyl)pyridin-2-yl]oxy}ethanol 
• 1296274-01-5 (4-Bromophenyl)(6-methoxypyridin-3-yl)methanone 
• 202147-76-0 (4-fluorophenyl)(6-methoxypyridin-3-yl)methanone 

Relevant academic research and scientific papers

An investigation of structure‐activity relationships of azolylacryloyl derivatives yielded potent and long‐acting hemoglobin modulators for reversing erythrocyte sickling

Aromatic aldehydes that bind to sickle hemoglobin (HbS) to increase the protein oxygen affinity and/or directly inhibit HbS polymer formation to prevent the pathological hypoxia‐induced HbS polymerization and the subsequent erythrocyte sickling have for s

Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline

The ATP-synthase inhibitor bedaquiline is effective against drug-resistant tuberculosis but is extremely lipophilic (clogP 7.25) with a very long plasma half-life. Additionally, inhibition of potassium current through the cardiac hERG channel by bedaquiline, is associated with prolongation of the QT interval, necessitating cardiovascular monitoring. Analogues were prepared where the naphthalene C-unit was replaced with substituted pyridines to produce compounds with reduced lipophilicity, anticipating a reduction in half-life. While there was a direct correlation between in vitro inhibitory activity against M. tuberculosis (MIC90) and compound lipophilicity, potency only fell off sharply below a clogP of about 4.0, providing a useful lower bound for analogue design. The bulk of the compounds remained potent inhibitors of the hERG potassium channel, with notable exceptions where IC50 values were at least 5-fold higher than that of bedaquiline. Many of the compounds had desirably higher rates of clearance than bedaquiline, but this was associated with lower plasma exposures in mice, and similar or higher MICs resulted in lower AUC/MIC ratios than bedaquiline for most compounds. The two compounds with lower potency against hERG exhibited similar clearance to bedaquiline and excellent efficacy in vivo, suggesting further exploration of C-ring pyridyls is worthwhile.

ANTIBACTERIAL COMPOUNDS

The present invention relates to compounds of general formula (II),to compositions comprising these compounds and to methods of treating Enterobacteriaceae bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Enterobacteriaceae.

NITROGENATED HETEROCYCLIC COMPOUND

The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.

SELECTIVE OCTAHYDRO-CYCLOPENTA[C] PYRROLE NEGATIVE MODULATORS OF NR2B

Compounds that selectively negatively modulate NMDA receptors containing an NR1/NR2B subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed. Such diseases include, without limitation, neurological dysfunction such as Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, and seizure disorders; emotional disorders; depression; bipolar disorder; obsessive-compulsive disorder; and other anxiety disorders.

Synthesis and reduction reactions of pyridones and 5-acyl-2-methoxypyridines

The synthesis of a series of pyridones, from their 2-hydroxypyridine or 2-methoxypyridine precursors, is described, along with studies into their reductions to saturated heterocycles. A number of 5-acylpyridones were prepared and were evaluated as substrates for asymmetric transfer hydrogenation prior to conversion to saturated heterocycles. The enantioselective reduction of 5-acetyl-1-benzylpyrimidine-2,4(1H,3H)-dione is also described.

5-HYDROXYPYRIMIDINE-4-CARBOXAMIDE DERIVATIVE

The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by formula (1): [wherein, R1: formula (1A): [wherein, R4 and R5: H, halogen,

A new Knoevenagel-type synthesis of fully substituted γ- hydroxybutenolides

The synthesis of fully substituted γ-hydroxybutenolides is possible by a Knoevenagel-type ring condensation of α-methyleneketones and α-ketoesters under basic conditions. This novel transformation allowed the preparation of di-aryl/heteroaryl substituted hydroxyfuranones, such as 20 and 27, which are important intermediates for pyridazine fungicides. As it turned out, a whole range of different substituents, such as alkyl, cycloalkyl, aryl, heteroaryl and ester groups could be linked to the butenolide scaffold, demonstrating the broad scope of the novel cyclization.

SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS

Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

PYRAZOLE DERIVATIVES

A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.