1268522-40-2

Upstream product

• 42754-59-6 2-(1-Methoxy-2-phenylethylidene)malononitrile 
• 1380347-94-3 5-amino-3-benzyl-1-methyl-1H-pyrazole-4-carbonitrile 

Downstream Products

• 1380347-95-4 3-benzyl-1-methyl-5-nitro-1H-pyrazole-4-carboxylic acid 
• 1380347-96-5 (3-benzyl-1-methyl-5-nitro-1H-pyrazol-4-yl)methanol 
• 1380347-97-6 3-benzyl-4-(bromomethyl)-1-methyl-5-nitro-1H-pyrazole 
• 1380347-98-7 tert-butyl 3-(3-benzyl-1-methyl-5-nitro-1H-pyrazol-4-yl)-N-(diphenylmethylene)-L-alaninate 
• 1380348-03-7 2,2,2-trifluoroethyl 3-(3-benzyl-1-methyl-5-nitro-1H-pyrazol-4-yl)-N-(tert-butoxycarbonyl)-L-alaninate 
• 1380347-92-1 (5S)-5-amino-3-benzyl-7-hydroxy-1-methyl-1,4,5,7-tetrahydro-6H-pyrazolo[34-b]pyridin-6-one 
• 1380481-73-1 C₁₄H₁₆N₄O₄ 
• 1380348-01-5 3-(3-benzyl-1-methyl-5-nitro-1H-pyrazol-4-yl)-N-(tert-butoxycarbonyl)-L-alanine 
• 1380348-05-9 PF-04859989 

Relevant academic research and scientific papers

SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS NADPH OXIDASE INHIBITORS

The present application relates to substituted fused heteroaryl and heterocyclic compounds, useful as nicotinamide adenine dinucleotide phosphate oxidase inhibitors (NADPH oxidase inhibitors), processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by NADPH oxidase. (Formula I)

PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency

The structure-based design, synthesis, and biological evaluation of a new pyrazole series of irreversible KAT II inhibitors are described herein. The modification of the inhibitor scaffold of 1 and 2 from a dihydroquinolinone core to a tetrahydropyrazolopyridinone core led to discovery of a new series of potent KAT II inhibitors with excellent physicochemical properties. Compound 20 is the most potent and lipophilically efficient of these new pyrazole analogs, with a kinact/Ki value of 112,000 M-1 s -1 and lipophilic efficiency (LipE) of 8.53. The X-ray crystal structure of 20 with KAT II demonstrates key features that contribute to this remarkable potency and binding efficiency.

KAT II INHIBITORS

Compounds of Formula I: (I) wherein X, Y, Z, R 1, R 2, R 3, R 4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive 5 deficits associated