384830-06-2

Upstream product

• 384830-00-6 3-[1-(tert-butyl-dimethyl-silanyl)-2-carboxy-4-oxo-azetidin-3-ylmethyl]-piperidine-1-carboxylic acid tert-butyl ester 
• 384830-02-8 (R)-3-((2S,3R)-2-Benzyloxycarbonyl-4-oxo-azetidin-3-ylmethyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 384829-99-6 (S)-3-iodomethylpiperidine-1-carboxylic acid tert-butyl ester 
• 191599-51-6 ethyl (S)-1-[(tert-butoxy)carbonyl]piperidine-3-carboxylate 
• 37675-18-6 (S)-(+)-nipecotic acid ethyl ester 
• 152120-55-3 N,N-bis(benzyloxycarbonyl)-1H-pyrazole-1-carboxamidine 
• 140695-84-7 tert-butyl (3S)-3-(hydroxymethyl)piperidine-1-carboxylate 
• 253177-37-6 4-(6-phenyl-hexanoyl)-piperazine-1-carbonyl chloride 
• 384830-05-1 (2S,3R)-3-((R)-1-{Benzyloxycarbonylamino-[(E)-benzyloxycarbonylimino]-methyl}-piperidin-3-ylmethyl)-4-oxo-azetidine-2-carboxylic acid benzyl ester 
• 384830-01-7 (R)-3-((2S,3R)-2-Carboxy-4-oxo-azetidin-3-ylmethyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 384830-03-9 (2S,3R)-4-Oxo-3-(R)-1-piperidin-3-ylmethyl-azetidine-2-carboxylic acid benzyl ester 

Relevant academic research and scientific papers

Synthesis of potent and highly selective inhibitors of human tryptase

The serine protease tryptase has been implicated in allergic and inflammatory diseases and associated with asthma. The synthesis and SAR of a series of N1-activated-4-carboxy azetidinones are described, resulting in identification of BMS-363131 (2) as a potent inhibitor of human tryptase (IC503000-fold) for tryptase versus related serine proteases including trypsin.

Beta lactam compounds and their use as inhibitors of tryptase

Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.