201006-25-9Relevant academic research and scientific papers
INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES
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, (2016/09/26)
The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.
Inhibitors of HGFA, matriptase, and hepsin serine proteases: A nonkinase strategy to block cell signaling in cancer
Han, Zhenfu,Harris, Peter K. W.,Jones, Darin E.,Chugani, Ryan,Kim, Tommy,Agarwal, Manjula,Shen, Wei,Wildman, Scott A.,Janetka, James W.
, p. 1219 - 1224 (2015/04/27)
Hepatocyte growth factor activators (HGFA), matriptase, and hepsin are S1 family trypsin-like serine proteases. These proteases proteolytically cleave the single-chain zymogen precursors, pro-HGF (hepatocyte growth factor), and pro-MSP (macrophage stimula
Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants
Lin, Jian,Deng, Hongfeng,Jin, Lei,Pandey, Pramod,Quinn, Jesse,Cantin, Susan,Rynkiewicz, Michael J.,Gorga, Joan C.,Bibbins, Frank,Celatka, Cassandra A.,Nagafuji, Pamela,Bannister, Thomas D.,Meyers, Harold V.,Babine, Robert E.,Hayward, Neil J.,Weaver, David,Benjamin, Howard,Stassen, Frans,Abdel-Meguid, Sherin S.,Strickler, James E.
, p. 7781 - 7791 (2007/10/03)
Human coagulation factor XIa (FXIa), a serine protease activated by site-specific cleavage of factor XI by thrombin, FXIIa, or autoactivation, is a critical enzyme in the amplification phase of the coagulation cascade. To investigate the potential of FXIa
Process for the preparation of chiral keto-heterocycles of basic amino acids
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, (2008/06/13)
A process for the preparation of novel keto heterocycle derivatives of basic natural and unnatural amino acids which affords products of high enantiomeric excess where a metalated heterocycle is reacted with N,O-dialkyl amide of an amino acid containing arylsulphonamide protected side chain amine in high chemical and optical yield as well as the novel compounds obtained by the process.
Pyrrolo[1,2-a]pyrazine-1,4-dione serine protease inhibitors
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, (2008/06/13)
PCT No. PCT/US97/09832 Sec. 371 Date Oct. 27, 1998 Sec. 102(e) Date Oct. 27, 1998 PCT Filed Jun. 10, 1997 PCT Pub. No. WO97/48706 PCT Pub. Date Dec. 24, 1997This invention relates to pyrrolo[1,2-a]pyrazine-1,4-diones of general formula: wherein B is carbonyl or methylene, R2, R4, R5, and R6 are hydrogen, alkyl, or substituted alkyl, A is a basic group, and Q is hydrogen or a keto heterocycle group. The compounds are inhibitors of serine proteases, typically thrombin, Factor Xa, and Factor VIIa, and are useful for treating and preventing thrombotic disorders.
