612840-83-2

Upstream product

• 612840-97-8 2-(4-chloro-phenyl)-3-ethyl-pent-4-enoic acid (S)-1-phenyl-ethylamine salt 
• 612840-80-9 (4-chloro-phenyl)-acetic acid pent-2-enyl ester 

Downstream Products

• 888490-62-8 (S)-1-[(2S,3R)-2-(4-Chloro-phenyl)-3-ethyl-pent-4-enoyl]-piperidine-2-carboxylic acid methylamide 
• 612840-95-6 2(S)-(4-chloro-phenyl)-3(R)-ethyl-1-morpholin-4-yl-pent-4-en-1-one 

Relevant academic research and scientific papers

A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors

The structural features contributing to the different pharmacokinetic properties of the TACE/MMP inhibitors TNF484 and TrocadeTM were analyzed using an in vivo cassette-dosing approach in rats. This enabled us to identify a new lead compound with excellent pharmacokinetic properties, but weaker activity on the biological targets. Directed structural modifications maintained oral bioavailability and restored biological activity, leading to a novel compound almost equipotent to TNF484 in vivo, but with a more than tenfold higher oral bioavailability.

HYDROXAMIC ACID DERIVATIVES

Novel hydroxamic acid derivatives, e.g., of formula (I), wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimm