5515-15-1

Upstream product

• 5515-11-7 2-[hydroxy(4-nitrophenyl)methylene]malononitrile 
• 77-78-1 dimethyl sulfate 
• 46700-35-0 (4-nitro-benzoyl)-malononitrile 
• 67-56-1 methanol 
• 122-04-3 4-nitro-benzoyl chloride 

Downstream Products

• 81067-03-0 2-Amino-4-methoxy-6-(4-nitro-phenyl)-pyrimidine-5-carbonitrile 
• 180903-11-1 5-amino-1-tert-butyl-3-(4-nitrophenyl)-1H-pyrazole-4-carbonitrile 
• 192512-78-0 C₁₆H₁₀N₆O₄ 
• 594983-83-2 5-amino-1-methyl-3-(4-nitrophenyl)-1H-pyrazole-4-carbonitrile 
• 42754-63-2 3-amino-5-(4-nitro-phenyl)-1⁽²⁾H-pyrazole-4-carbonitrile 
• 1446247-08-0 3-(4-nitrophenyl)-5-({[(3-pyrrolidin-1-ylpropyl)amino]carbonyl}amino)isothiazol-4-carboxamide 
• 1446247-10-4 3-(4-aminophenyl)-5-({[(3-pyrrolidin-1-ylpropyl)amino]carbonyl}amino)isothiazol-4-carboxamide 
• 1446247-11-5 3-[4-({[(4-methylphenyl)amino]carbonyl}amino)phenyl]-5-({[(3-pyrrolidin-1-ylpropyl)amino]carbonyl}amino)isothiazol-4-carboxamide 
• 605661-26-5 2-[amino(4-nitrophenyl)methylene]malononitrile 
• 909028-96-2 3-amino-3-(4-nitrophenyl)-2-thioformamidoacrylonitrile 
• 1446247-91-1 C₂₄H₂₆N₆O₅S 
• 1446247-90-0 C₁₆H₁₇N₅O₆S 
• 605661-28-7 5-amino-3-(4-nitrophenyl)isothiazole-4-carbonitrile 
• 1446247-75-1 phenyl [4-cyano-3-(4-nitrophenyl)isothiazol-5-yl]carbamate 

Relevant academic research and scientific papers

3-PHENYL-5-UREIDOISOTHIAZOLE-4-CARBOXIMIDE AND 3-AMINO-5-PHENYLISOTHIAZOLE DERIVATIVES AS KINASE INHIBITORS

This invention is directed to a compound of Formula I Formula I or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, n, X1, X2, L1, and L2 are as defined herein.

FUSED RING HETEROARYL KINASE INHIBITORS

Provided herein are fused ring heteroaryl compounds useful in a variety of methods, including reducing the activity of certain kinases and treating certain disease states.

Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR

We have described the synthesis, enzyme inhibitory activity, structure-activity relationships, and proposed binding mode of a novel series of pyrrole derivatives as lymphocyte-specific kinase (Lck) inhibitors. The most potent analogs exhibited good enzyme inhibitory activity (IC50s 10 nM) for Lck kinase inhibition.

A small molecule inhibitor selective for a variant ATP-binding site of the chaperonin GroEL

The chaperonin GroEL is a megadalton-sized molecular machine that plays an essential role in the bacterial cell assisting protein folding to the native state through actions requiring ATP binding and hydrolysis. A combination of medicinal chemistry and genetics has been employed to generate an orthogonal pair, a small molecule that selectively inhibits ATPase activity of a GroEL ATP-binding pocket variant. An initial screen of kinase-directed inhibitors identified an active pyrazolo-pyrimidine scaffold that was iteratively modified and screened against a collective of GroEL nucleotide pocket variants to identify a cyclopentyl carboxamide derivative, EC3016, that specifically inhibits ATPase activity and protein folding by the GroEL mutant, I493C, involving a side chain positioned near the base of ATP. This orthogonal pair will enable in vitro studies of the action of ATP in triggering activation of GroEL-mediated protein folding and might enable further studies of GroEL action in vivo. The approach originated for studying kinases by Shokat and his colleagues may thus also be used to study large macromolecular machines.

CHEMICAL COMPOUNDS

Pyrazole derivatives are described herein. The described invention also includes methods of making such pyrazole derivatives as well as methods of using the same in the treatment of diseases.

One-pot synthesis of tetrasubstituted pyrazoles - Proof of regiochemistry

1-Alkyl-5-amino-3-aryl-4-cyanopyrazoles, useful intermediates for fused heterocyclic systems, are synthesised by a one-pot three-step procedure from acid chlorides, malononitrile and alkylhydrazines. The regiochemistry of the hydrazine incorporation was p