304646-56-8

Upstream product

• 404-26-2 4-(trifluoroacetamido)benzoic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 407-25-0 trifluoroacetic anhydride 
• 619-45-4 4-methoxycarbonyl aniline 

Downstream Products

• 892878-68-1 methyl 4-[(2,2,2-trifluoroethyl)amino]benzoate 
• 71839-12-8 N-(n-butyl)-4-methoxycarbonylaniline 
• 1616681-26-5 methyl 4-(2-bromo-N-butylcyclopent-1-ene-1-carboxamido)benzoate 
• 1616681-28-7 methyl 4-(2-bromo-N-butylcyclohex-1-ene-1-carboxamido)benzoate 
• 1616681-30-1 methyl 4-(2-bromo-N-butylcyclohept-1-ene-1-carboxamido)benzoate 
• 1616681-32-3 methyl 4-(2-bromo-N-butylcyclooct-1-ene-1-carboxamido)benzoate 
• 1616680-38-6 N-phenyl-5-butyl-6-oxo-6,7,8,9,10,11-hexahydro-5H-cyclohepta[c]quinoline-2-carboxamide 
• 1616680-46-6 N-c-hexyl-5-butyl-6-oxo-6,7,8,9,10,11-hexahydro-5H-cyclohepta[c]quinoline-2-carboxamide 
• 892878-66-9 4-[(2,2,2-trifluoroethyl)amino]benzoic acid 

Relevant academic research and scientific papers

Structure-activity relationship study of non-steroidal NPC1L1 ligands identified through cell-based assay using pharmacological chaperone effect as a readout

Niemann-Pick type C1-like 1 (NPC1L1) is an intestinal cholesterol transporter that is known to be the target of the cholesterol absorption inhibitor ezetimibe. We previously discovered steroidal NPC1L1 ligands by using a novel cell-based assay that employs pharmacological chaperone effect as a readout. Those steroid derivatives bound to a site different from both the sterol-binding domain and the ezetimibe-binding site, implying that they may be a novel class of NPC1L1 inhibitors with a distinct mode of action. As an extension of that work, we aimed here to find non-steroidal NPC1L1 ligands, which may be better candidates for clinical application than steroidal ligands, by using the same assay to screen our focused library of ligands for liver X receptor (LXR), a nuclear receptor that recognizes oxysterols as endogenous ligands. Here we describe identification of a novel class of NPC1L1 ligands with a ring-fused quinolinone scaffold, and an analysis of the structure-activity relationships of their derivatives as NPC1L1 ligands.

HETEROCYCLIC ANTIVIRAL COMPOUNDS

Compounds having the formula I wherein A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re/sup

BICYCLIC COMPOUNDS USEFUL AS CATHEPSIN S INBHIBITORS

Compounds of formula (I), wherein R1, R2, R3, Ra and E are are defined within, and pharmaceutically acceptable salts, solvates, hydrates and N-oxides thereof having utility in the treatment of disorders mediated by cathepsin S.

CATHEPSIN S INHIBITORS

Compounds of the formula (I) where R1 is C1-C4 straight or branched alkyl, optionally substituted with up to three substituents selected from halo and hydroxy; R2 is halo, hydroxy, methyloxy, or C1-C2 alkyl, which alkyl is optionally substituted with up to three halogens or an hydroxy or a methyloxy; D is - C3-C7 alkylene-, thereby defining a cycloalkyl ring; E is -C(=O)-, -S(=O)m-, -NRdS(=O)m-, -NRaC(=O)-, -OC(=O)-, R3 is an optionally substituted carbocyclic or heterocyclic ring R10 is H, ORc, SRc or together with the gem H is =O or (ORc)2; Ra is independently selected from H, C1-C4 alkyl; have utility in the inhibition of cathepsin S and are thus useful pharmaceuticals against disorders such as autoimmune disorders and chronic pain.