224039-49-0

Upstream product

• 1710-98-1 p-tert-butyl benzoyl chloride 
• 224040-76-0 1-[4-(1,1-dimethylethyl)-phenyl]-2-(pyridin-4-yl)ethanone 
• 108-89-4 picoline 
• 224040-63-5 1-[4-(1,1-dimethylethyl)benzoyl]-2-methylaziridine 
• 17356-08-0 thiourea 

Downstream Products

• 284486-00-6 N-[4-[4-(1,1-dimethylethyl)phenyl]-5-(pyridin-4-yl)-1,3-thiazol-2-yl]-2-chloroacetamide hydrochloride 
• 224039-74-1 N-[4-(4-(1,1-dimethylethyl)phenyl)-5-(4-pyridyl)-1,3-thiazol-2-yl]propionamide 
• 224039-78-5 N-[4-(4-(1,1-dimethylethyl)phenyl)-5-(4-pyridyl)-1,3-thiazol-2-yl]isonicotinamide 

Relevant academic research and scientific papers

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

Thiazolopyrimidine compounds, its production and use

Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1is an optionally substitu

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.