6576-06-3

Upstream product

• 108-89-4 picoline 
• 94-30-4 ethyl 4-methoxybenzoate 
• 874-90-8 4-methoxybenzonitrile 
• 6580-93-4 4-<2-Hydroxy-2-(p-methoxyphenyl)ethyl>pyridine 
• 303162-29-0 (4-methoxyphenyl)(2-methylaziridin-1-yl)methanone 
• 94-00-8 4-pyridinecarboxylic acid phenyl ester 
• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 100-07-2 4-methoxy-benzoyl chloride 

Downstream Products

• 171001-11-9 (R*,S*)-1-(4-methoxyphenyl)-1-phenyl-2-(4-pyridinyl)ethanol 
• 171000-98-9 (E)-1-(4-hydroxyphenyl)-1-phenyl-2-(4-pyridinyl)ethene 
• 97422-32-7 [4-(4-methoxyphenyl)-5-(4-pyridyl)-1,3-thiazol-2-yl]amine 

Relevant academic research and scientific papers

THERAPEUTIC METHODS AND COMPOUNDS

The invention provides a compound of formula I: (I) or a pharmaceutically acceptable salt thereof, wherein R1-R5 Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful to treat malaria.

Catalytic α-Arylation of Ketones with Heteroaromatic Esters

Heteroaromatic esters were found to be applicable as an arylating agent for the Pd-catalyzed α-arylation of ketones in a decarbonylative fashion. The use of our in-house ligand, dcypt, enabled this unique bond formation. Considering the ubiquity and low cost of aromatic esters, the present work will allow for rapid access to valuable α-aryl carbonyl compounds.

Continuous-Flow Synthesis of 2 H -Azirines and Their Diastereoselective Transformation to Aziridines

Using continuous-flow techniques, a small collection of 2H-azirines was prepared from oxime precursors via mesylation and base-promoted cyclisation. The 2H-azirines were either isolated after in-line purification or derivatised into a selection of 2-subst

Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as selective adenosine A3 antagonists

To investigate the potency of an adenosine A3 receptor (A 3AR) antagonist as an anti-asthmatic drug, a novel series of 4-phenyl-5-pyridyl-1,3-thiazole derivatives was synthesized and evaluated in human adenosine A1, A

Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as p38 MAP kinase inhibitors

A novel series of 4-phenyl-5-pyridyl-1,3-thiazole analogues possessing potent in vitro inhibitory activity against p38 mitogen-activated protein kinase and the release of tumor necrosis factor-α (TNF-α) from human monocytic THP-1 cells stimulated by lipopolysaccharide has been identified. Subsequent structure-activity relationship (SAR) studies and optimization for absorption, distribution, metabolism, and elimination (ADME) profiles led to the identification of compounds 7g and 10b as orally active lead candidates that block the in vivo production of proinflammatory cytokine (TNF-α). In pharmacokinetic studies, compound 10b showed good oral administration in mice and demonstrated significant in vivo anti-inflammatory activity in an anti-collagen monoclonal antibody-induced arthritis mouse model (minimum effective dose (MED)=30 mg/kg). Further elucidation of this class of compounds may provide novel anti-inflammatory agents, such as anti-rheumatoid arthritis drugs.

MEDICINAL COMPOSITIONS

The present invention relates to an agent for the prophylaxis or treatment of pain, an agent for suppressing activation of osteoclast, and an inhibitor of osteoclast formation, which contains a p38 MAP kinase inhibitor and/or a TNF-α production inhibitor.

Adenosine A3 receptor antagonists

A pharmaceutical composition for antagonizing adenosine at adenosine A3receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.

Derivatives of 4-styrylpyridines: Synthesis, estrogen receptor binding affinity, and photophysical properties

In order to develop novel ligands for the estrogen receptor (ER) that might have high binding affinity and fluorescence properties suitable for assaying ER levels in cells, we have prepared a series of substituted 4'- hydroxyl-styrylpyridines and phenylethylpyridines and studied their optical spectroscopy and receptor binding properties. Several derivatives that contain alkyl substituents on the internal ethene or ethane carbons were prepared. While most of these compounds have only modest affinity for ER, one fluorescent analog, (E)-l-(4-hydroxyphenyl)-1-phenyl-2-(4-pyridinyl)ethene (13), has reasonably good binding affinity for ER and shows long wavelength fluorescence emission that is sensitive to solvent polarity and pH. This compound may prove to be a useful probe for detecting ER in cells.

Novel piperidine σ receptor ligands as potential antipsychotic drugs

σ receptor ligands represent a new class of potential antipsychotic drugs. This paper presents the structure-activity relationships leading to novel disubstituted piperidine σ ligands, which have little or no affinity for dopamine D2 receptors. Selectivity for σ sites over dopamine D2 or serotonin 5-HT2 receptors appears to be governed by the chemical nature of the piperidine nitrogen substituent, its distance from the basic nitrogen, and its orientation relative to the other piperidine substituent. Several of these compounds have good oral potency in some animal models used to evaluate potential antipsychotic drugs. The N-cyclopropylmethyl ketones and ethers (e.g. 6i (DuP 734), 6q, 18a, and 18n) have the best in vivo potency. Compounds 6i (DuP 734) and 6q did not cause catalepsy in the rat, even at very high doses. On the basis of the pharmacology profiles of these σ ligands, we propose these compounds may be effective antipsychotic drugs, which do not induce extrapyramidal side effects or tardive dyskinesia.

Rate-equilibrium relationships for the deprotonation of 4-phenacylpyridines and 4-phenacylpyridinium cations

Substituent effects upon the equilibria and kinetics of enolate ion formation from eight 4-(X-phenacyl)pyridines (5), eight 1-methyl-4-(X-phenacyl)pyridinium cations (6), five 1-benzyl-4-(X-phenacyl)pyridinium cations (7), and eight 1-(X-benzyl)-4-phenacy