393842-97-2

Upstream product

• 393842-94-9 1-(1-benzyloxycarbonylmethyl)-3-(S)-t-butoxycarbonylaminoperhydroazepin-2-one 
• 393842-95-0 (3-amino-2-oxo-azepan-1-yl)-acetic acid benzyl ester 
• 179686-45-4 3-(S)-tert-butoxycarbonylamino-4,5,6,7-tetrahydroazepin-2-one 
• 393842-96-1 {3-[(biphenyl-4-carbonyl)-amino]-2-oxo-azepan-1-yl}-acetic acid benzyl ester 

Downstream Products

• 393842-98-3 [3-(2-{3-[(biphenyl-4-carbonyl)-amino]-2-oxo-azepan-1-yl}-acetylamino)-benzyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Synthesis of potent and selective 2-azepanone inhibitors of human tryptase

The serine protease tryptase has been associated with a broad range of allergic and inflammatory diseases and, in particular, has been implicated as a critical mediator of asthma. The inhibition of tryptase therefore has the potential to be a valuable therapy for asthma. The synthesis, employing solution phase parallel methods, and SAR of a series of novel 2-azepanone tryptase inhibitors are presented. A member of this series, 8t, was identified as a potent inhibitor of human tryptase (IC50=38 nM) with selectivity ≤330-fold versus related serine proteases (trypsin, plasmin, uPA, tPA, APC, alpha-thrombin, and FXa).

Lactam compounds and their use as inhibitors of serine proteases and method

Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R4is ?R7O— or R8 and R1, R2, R3, R5, R6, R7, and R8, are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.