1159982-72-5

Upstream product

• 1572-10-7 3⁽⁵⁾-phenylpyrazol-5⁽³⁾-amine 
• 1663-67-8 malonoyl dichloride 

Downstream Products

• 1232223-03-8 5-chloro-7-morpholin-4-yl-2-phenylpyrazolo[1,5-a]pyrimidine 
• 1232224-10-0 5-Chloro-2-phenyl-7-thiazolidin-3-yl-pyrazolo[1,5-a]pyrimidine 
• 1232224-20-2 5-Chloro-7-[1-(2-hydroxyethyl)-piperazin-4-yl]-2-phenyl-pyrazolo[1,5-a]-pyrimidine 
• 1232223-96-9 5-Chloro-7-(3-hydroxy-azetidin-1-yl)-2-phenyl-pyrazolo[1,5-a]pyrimidine 
• 1232224-00-8 7-(4-tert-butoxy-carbonyl-piperazin-1-yl)-5-chloro-2-phenyl-pyrazolo[1,5-a]pyrimidine 
• 1232220-11-9 N-(3-methylbenzylidene)-N'-(2-phenyl-7-morpholin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)hydrazine 
• 1232220-13-1 N-(1H-indol-3-yl-methylidene)-N'-(7-morpholin-4-yl-2-phenyl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232220-23-3 N-benzylidene-N'-(7-morpholin-4-yl-2-phenyl-pyrazolo-[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232224-02-0 N-[7-(4-Tert-butoxy-carbonyl-piperazin-1-yl)-2-phenyl-pyrazolo[1,5-a]-pyrimidin-5-yl]-N'-(3-methyl-benzylidene)-hydrazine 
• 1232221-00-9 N-(3-methyl-benzylidene)-N'-(2-phenyl-7-thiazolidin-3-yl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232223-60-7 (7-morpholin-4-yl-2-phenyl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232221-42-9 N-(2-methyl-1H-indol-7-yl-methylidene)-N'-(7-morpholin-4-yl-2-phenyl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232221-48-5 N-(2-methyl-benzofuran-7-yl-methylidene)-N'-(7-morpholin-4-yl-2-phenyl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 
• 1232221-52-1 N-(1H-indol-4-yl-methylidene)-N'-(7-morpholin-4-yl-2-phenyl-pyrazolo[1,5-a]pyrimidin-5-yl)-hydrazine 

Relevant academic research and scientific papers

Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201

Interleukin-12 (IL-12) and IL-23 are proinflammatory cytokines and therapeutic targets for inflammatory and autoimmune diseases, including inflammatory bowel diseases, psoriasis, rheumatoid arthritis, and multiple sclerosis. We describe the discovery of APY0201, a unique small molecular IL-12/23 production inhibitor, from activated macrophages and monocytes, and demonstrate ameliorated inflammation in an experimental model of colitis. Through a chemical proteomics approach using a highly sensitive direct nanoflow LC-MS/MS system and bait compounds equipped with the FLAG epitope associated regulator of PIKfyve (ArPIKfyve) was detected. Further study identified its associated protein phosphoinositide kinase, FYVE finger-containing (PIKfyve), as the target protein of APY0201, which was characterized as a potent, highly selective, ATP-competitive PIKfyve inhibitor that interrupts the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P2. These results elucidate the function of PIKfyve kinase in the IL-12/23 production pathway and in IL-12/23-driven inflammatory disease pathologies to provide a compelling rationale for targeting PIKfyve kinase in inflammatory and autoimmune diseases.

PYRAZOLO-PYRIMIDINE COMPOUNDS

The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.