17704-74-4Relevant articles and documents
Imidazol-4-one and Imidazole-4-thione Compounds
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Page/Page column 16, (2010/05/13)
Imidazol-4-one or imidazole-4-thione compounds of formula (I): wherein X, R1, R2, R3, R4, R5, and R6 are defined herein. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.
QUINAZOLINE DERIVATIVES
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Page/Page column 199, (2008/06/13)
A quinazoline derivative of the formula (I) wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula (I), are useful in the treatment of hyperproliferative disorders such as a cancer.
Design and synthesis of dipeptide nitriles as reversible and potent cathepsin S inhibitors
Ward, Yancey D.,Thomson, David S.,Frye, Leah L.,Cywin, Charles L.,Morwick, Tina,Emmanuel, Michel J.,Zindell, Renée,McNeil, Daniel,Bekkali, Younes,Giradot, Marc,Hrapchak, Matt,DeTuri, Molly,Crane, Kathy,White, Della,Pav, Susan,Wang, Yong,Hao, Ming-Hong,Grygon, Christine A.,Labadia, Mark E.,Freeman, Dorothy M.,Davidson, Walter,Hopkins, Jerry L.,Brown, Maryanne L.,Spero, Denice M.
, p. 5471 - 5482 (2007/10/03)
The specificity of the immune response relies on processing of foreign proteins and presentation of antigenic peptides at the cell surface. Inhibition of antigen presentation, and the subsequent activation of T-cells, should, in theory, modulate the immune response. The cysteine protease Cathepsin S performs a fundamental step in antigen presentation and therefore represents an attractive target for inhibition. Herein, we report a series of potent and reversible Cathepsin S inhibitors based on dipeptide nitriles. These inhibitors show nanomolar inhibition of the target enzyme as well as cellular potency in a human B cell line. The first X-ray crystal structure of a reversible inhibitor cocrystallized with Cathepsin S is also reported.