850786-98-0Relevant articles and documents
BICYCLIC PIPERAZINE COMPOUND AND USE THEREOF
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Page/Page column 59-60, (2010/11/08)
The present invention provides a compound represented by the formula: wherein R1 is an acyl group, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, a sulfur atom or the like, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors
Zask, Arie,Kaplan, Joshua,Du, XueMei,MacEwan, Gloria,Sandanayaka, Vincent,Eudy, Nancy,Levin, Jeremy,Jin, Guixian,Xu, Jun,Cummons, Terri,Barone, Dauphine,Ayral-Kaloustian, Semiramis,Skotnicki, Jerauld
, p. 1641 - 1645 (2007/10/03)
Potent and selective TACE and MMP inhibitors utilizing the diazepine and thiazepine ring systems were synthesized and evaluated for biological activity in in vitro and in vivo models of TNF-α release. Oral activity in the mouse LPS model of TNF-α release