1037082-29-3Relevant academic research and scientific papers
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex
Zhang, Xiaojun,Glunz, Peter W.,Johnson, James A.,Jiang, Wen,Jacutin-Porte, Swanee,Ladziata, Vladimir,Zou, Yan,Phillips, Monique S.,Wurtz, Nicholas R.,Parkhurst, Brandon,Rendina, Alan R.,Harper, Timothy M.,Cheney, Daniel L.,Luettgen, Joseph M.,Wong, Pancras C.,Seiffert, Dietmar,Wexler, Ruth R.,Priestley, E. Scott
supporting information, p. 7125 - 7137 (2016/08/24)
Inhibitors of the tissue factor (TF)/factor VIIa complex (TF-FVIIa) are promising novel anticoagulants which show excellent efficacy and minimal bleeding in preclinical models. Starting with an aminoisoquinoline P1-based macrocyclic inhibitor, optimizatio
Synthesis and P1′ SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors
Ladziata, Vladimir (Uladzimir),Glunz, Peter W.,Zou, Yan,Zhang, Xiaojun,Jiang, Wen,Jacutin-Porte, Swanee,Cheney, Daniel L.,Wei, Anzhi,Luettgen, Joseph M.,Harper, Timothy M.,Wong, Pancras C.,Seiffert, Dietmar,Wexler, Ruth R.,Priestley, E. Scott
, p. 5051 - 5057 (2016/10/05)
Selective tissue factor-factor VIIa complex (TF-FVIIa) inhibitors are viewed as promising compounds for treating thrombotic disease. In this contribution, we describe multifaceted exploratory SAR studies of S1′-binding moieties within a macrocyclic chemotype aimed at replacing cyclopropyl sulfone P1′ group. Over the course of the optimization efforts, the 1-(1H-tetrazol-5-yl)cyclopropane P1′ substituent emerged as an improved alternative, offering increased metabolic stability and lower clearance, while maintaining excellent potency and selectivity.
PYRIMIDOPYRIMIDINONES USEFUL AS WEE-1 KINASE INHIBITORS
-
Page/Page column 304, (2015/07/07)
The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.
MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
-
Page/Page column 106, (2008/12/07)
The present invention relates generally to novel macrocycles of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
