449758-31-0Relevant academic research and scientific papers
Benzimidazole derivative and pharmaceutical purposes thereof
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Paragraph 0163-0166, (2019/10/29)
The invention discloses a benzimidazole derivative and pharmaceutical purposes thereof, and particularly discloses a benzimidazole derivative shown in a formula I and purposes of the benzimidazole derivative to preparation of drugs for treating and/or pre
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization
Deng, James Z.,McMasters, Daniel R.,Rabbat, Philippe M.A.,Williams, Peter D.,Coburn, Craig A.,Yan, Youwei,Kuo, Lawrence C.,Lewis, S. Dale,Lucas, Bobby J.,Krueger, Julie A.,Strulovici, Berta,Vacca, Joseph P.,Lyle, Terry A.,Burgey, Christopher S.
, p. 4411 - 4416 (2007/10/03)
Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin inhibitors, were utilized to transform a weak triazolopyrimidine lead into a series of potent oxazolop
DPP-IV INHIBITORS
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Page/Page column 48-49, (2010/02/14)
The invention relates to compounds of formula (I), Z-C(R1R 2)-C(R3NH2)-C(R4R5)-X-N(R 6R7), wherein Z, R1-7 and X have the meaning as cited in the description and the claims. Said compounds are useful as DPP-lV inhibitors. The invention also relates to the
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors
Young, Mary Beth,Barrow, James C.,Glass, Kristen L.,Lundell, George F.,Newton, Christina L.,Pellicore, Janetta M.,Rittle, Kenneth E.,Selnick, Harold G.,Stauffer, Kenneth J.,Vacca, Joseph P.,Williams, Peter D.,Bohn, Dennis,Clayton, Franklin C.,Cook, Jacquelynn J.,Krueger, Julie A.,Kuo, Lawrence C.,Lewis, S. Dale,Lucas, Bobby J.,McMasters, Daniel R.,Miller-Stein, Cynthia,Pietrak, Beth L.,Wallace, Audrey A.,White, Rebecca B.,Wong, Bradley,Yan, Youwei,Nantermet, Philippe G.
, p. 2995 - 3008 (2007/10/03)
In an effort to discover potent, clinically useful thrombin inhibitors, a rapid analogue synthetic approach was used to explore the P1 region. Various benzylamines were coupled to a pyridine/pyrazinone P2-P 3 template. One compound with an o-thiadiazole benzylic substitution was found to have a thrombin Ki of 0.84 nM. A study of ortho-substituted five-membered-ring heterocycles was undertaken and subsequently demonstrated that the o-triazole and tetrazole rings were optimal. Combination of these potent P1 aryl heterocycles with a variety of P2-P3 groups produced a compound with an extraordinary thrombin inhibitory activity of 1.4 pM. It is hoped that this potency enhancement in P1 will allow for more diversification in the P 2-P3 region to ultimately address additional pharmacological concerns.
Thrombin inhibitors
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Page 21, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.
Thrombin inhibitors
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: wherein R1 is, for example, hydrogen, Cl, or cyano, and R2 is, for example, hydrogen,
Thrombin inhibitors
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.
