1291779-91-3

Upstream product

• 92-67-1 4-phenylalanine 
• 3365-81-9 biphenyl-4-yl-methyl-amine 
• 347-37-5 2,2,2-trifluoro-4'-phenylacetanilide 
• 1291779-66-2 N-(biphenyl-4-yl)-N-methyl-2,2,2-trifluoro-acetamide 
• 220497-67-6 (1R,3S)-3-(9-fluorenylmethoxycarbonylamino)cyclopentanecarboxylic acid 

Relevant academic research and scientific papers

Discovery of BI 99179, a potent and selective inhibitor of type i fatty acid synthase with central exposure

Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool compound suitable for the in vivo validation of FAS as a therapeutic target. Optimisation yielded BI 99179 which is characterised by high potency, remarkably high selectivity and significant exposure (both peripheral and central) upon oral administration in rats.

CYCLOPENTANECARBOXAMIDE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE

The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, Rsup