226395-87-5Relevant articles and documents
OPTICAL AGENTS FOR IMAGING AND VISUALIZATION OF MATRIX METALLOPROTEINASE ENZYMES
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, (2013/03/28)
The invention relates generally to optical agents for biomedical applications including imaging, visualization, phototherapy and diagnostic monitoring of cells and tissue expressing MMPs and/or tissues associated with the expression of MMPs. In some embodiments, for example, optical agents of the present invention selectively bind to, or otherwise preferentially associate with, a target tissue expressing one or more MMPs, and function to couple electromagnetic radiation into and/or out of the target tissue, for example via optical absorption, fluorescence, scattering and/or optoacoustic processes.
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl Sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease
Becker, Daniel P.,Barta, Thomas E.,Bedell, Louis J.,Boehm, Terri L.,Bond, Brian R.,Carroll, Jeffery,Carron, Chris P.,Decrescenzo, Gary A.,Easton, Alan M.,Freskos, John N.,Funckes-Shippy, Chris L.,Heron, Marcia,Hockerman, Susan,Howard, Carol Pearcy,Kiefer, James R.,Li, Madeleine H.,Mathis, Karl J.,McDonald, Joseph J.,Mehta, Pramod P.,Munie, Grace E.,Sunyer, Teresa,Swearingen, Craig A.,Villamil, Clara I.,Welsch, Dean,Williams, Jennifer M.,Yu, Ying,Yao, Jun
experimental part, p. 6653 - 6680 (2010/11/18)
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMPs-2,-9, and-13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. α-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while α-piperidine and α-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9i (SC-77774), respectively, were identified as backup compounds.