Abstract: Compounds of general formula (I) or general formula (II):— wherein R1, P1, P2, Q, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
Abstract: The present invention relates to a process for preparing a compound of formula I, wherein R1 is Pg1 or P1?; P1? is CO-hydrocarbyl; P2 is CH2, O or N-Pg2; and Pg1 and Pg2 are each independently nitrogen protecting groups; (i) reacting a compound of formula II with a dioxirane to form an epoxide of formula III; where X is selected from CN, CH2N3, CH2NH-Pg2, ONH-Pg2, NHNH-Pg2, N(Pg2)NH-Pg2; (ii) converting a compound of formula III to a compound of formula I
Type:
Application
Filed:
February 8, 2008
Publication date:
January 1, 2009
Applicant:
Amura Therapeutics Ltd.
Inventors:
Martin Quibell, Yikang Wang, James Nally, John Paul Watts, Virendar Kumar Agrawal, Michael Standen
Abstract: Compounds of general formula (I) or general formula (II) wherein R1, P1, P2, Q, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.