21384-46-3

Upstream product

• 122-01-0 4-chloro-benzoyl chloride 
• 75-55-8 2-Methylaziridine 

Downstream Products

• 58158-45-5 1-(4-chlorophenyl)-2-(pyridin-4-yl)ethanone 
• 365428-07-5 2-(2-tert-butoxycarbonylaminopyridin-4-yl)-1-(4-chlorophenyl)ethanone 
• 896738-38-8 N-{4-[2-(4-chlorophenyl)imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl}benzamide 
• 896737-64-7 4-[2-(4-chlorophenyl)imidazo[1,2-b]pyridazin-3-yl]pyridin-2-amine 
• 896737-60-3 4-[6-chloro-2-(4-chlorophenyl)imidazo[1, 2-b]pyridazin-3-yl]pyridin-2-amine 
• 365428-30-4 2-(2-aminopyridin-4-yl)-2-bromo-1-(4-chlorophenyl)ethanone hydrobromide 
• 224038-60-2 [4-(4-chlorophenyl)-5-(4-pyridyl)-1,3-thiazol-2-yl]amine 
• 65296-14-2 5-methyl-2-(4-chlorophenyl)-4,5-dihydrooxazole 
• 1335199-97-7 2-(4-chlorophenyl)-4-methyl-4,5-dihydrooxazole 

Relevant academic research and scientific papers

Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors

We identified novel potent inhibitors of p38 MAP kinase using structure-based design strategy. X-ray crystallography showed that when p38 MAP kinase is complexed with TAK-715 (1) in a co-crystal structure, Phe169 adopts two conformations, where one intera

Phosphine-catalyzed heine reaction

Aziridines are important synthetic intermediates which readily undergo ring-opening reactions. It is demonstrated that electron-rich phosphines are efficient catalysts for the regioselective rearrangement of N-acylaziridines to oxazolines. The reactions o

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.

CONCOMITANT DRUGS

The present invention relates to a pharmaceutical agent containing one or more kinds of a p38 MAP kinase inhibitor and/or a TNF-α production inhibitor and one or more kinds of drugs selected from the group consisting of (1) a non-steroidal antiinflammator

JNK INHIBITOR

The present invention relates to a c-Jun N-terminal kinase inhibitor containing an azole compound (I) substituted by a nitrogen-containing aromatic group having substituent(s)(except a compound represented by the formula: ) or a salt thereof or a prodrug thereof.

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.

p38MAP KINASE INHIBITORS

A 1,3-thiazole compound substituted at the 5-position by a pyridyl group optionally having substituent(s) has a superior p38 MAP kinase inhibitory activity and TNF-α production inhibitory activity.