1007346-42-0Relevant academic research and scientific papers
MAP4K4 INHIBITORS
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Paragraph 00204; 00205, (2019/05/02)
This invention relates to pyrrolopyrimidine comprising compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these pyrrolopyrimidine comprising compounds, f
Substituted Benzo-Imidazo-Pyrido-Diazepine Compounds
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Page/Page column 138, (2012/05/07)
The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
7-Fluoroindazoles as potent and selective inhibitors of factor Xa
Lee, Yu-Kai,Parks, Daniel J.,Lu, Tianbao,Thieu, Tho V.,Markotan, Thomas,Pan, Wenxi,McComsey, David F.,Milkiewicz, Karen L.,Crysler, Carl S.,Ninan, Nisha,Abad, Marta C.,Giardino, Edward C.,Maryanoff, Bruce E.,Damiano, Bruce P.,Player, Mark R.
, p. 282 - 297 (2008/09/17)
We have developed a novel series of potent and selective factor Xa inhibitors that employ a key 7-fluoroindazolyl moiety. The 7-fluoro group on the indazole scaffold replaces the carbonyl group of an amide that is found in previously reported factor Xa inhibitors. The structure of a factor Xa cocrystal containing 7-fluoroindazole 51a showed the 7-fluoro atom hydrogen-bonding with the N-H of Gly216 (2.9 ?) in the peptide backbone. Thus, the 7-fluoroindazolyl moiety not only occupied the same space as the carbonyl group of an amide found in prior factor Xa inhibitors but also maintained a hydrogen bond interaction with the protein's β-sheet domain. The structure-activity relationship for this series was consistent with this finding, as the factor Xa inhibitory potencies were about 60-fold greater (ΔΔG ≈ 2.4 kcal/mol) for the 7-fluoroindazoles 25a and 25c versus the corresponding indazoles 25b and 25d. Highly convergent synthesis of these factor Xa inhibitors is also described.
