380223-07-4Relevant academic research and scientific papers
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: Inhibition of interleukin-1β-converting enzyme
Laufersweiler, Michael C.,Wang, Yili,Soper, David L.,Suchanek, Maureen K.,Fancher, Amy N.,Lu, Wei,Wang, Richard L.,Oppong, Kofi A.,Ellis, Christopher D.,Baize, Mark W.,O'Neil, Steven V.,Wos, John A.,Demuth Jr., Thomas P.
, p. 4322 - 4326 (2007/10/03)
The application of a tricyclic pyrrolopyrimidinone scaffold for the synthesis of peptidomimetic inhibitors of interleukin-1β-converting enzyme (ICE) is reported. The synthesis of the tricyclic scaffold and conversion of it to a variety of target ICE inhib
Caspase inhibitors and uses thereof
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, (2008/06/13)
This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3 is independently selected from hydrogen or C16 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
