199296-29-2Relevant academic research and scientific papers
Kilogram scale synthesis of the pyrazinone acetic acid core of an orally efficacious thrombin inhibitor
Fleitz, Fred J.,Lyle, Terry A.,Zheng, Nan,Armstrong III, Joseph D.,Volante
, p. 3171 - 3180 (2000)
A multi-kilogram scale synthesis of the orally efficacious thrombin inhibitor 1 has been achieved via construction of the pyrazinone core from an unsymmetric oxalic diamide. Key features include judicious choice of reagents to minimize side products, a ke
MASP-2 INHIBITORS AND METHODS OF USE
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Paragraph 2830-2831, (2019/12/24)
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
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:
Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-monocyclic arginine surrogates
Reiner, John E.,Siev, Daniel V.,Araldi, Gian-Luca,Cui, Jingrong Jean,Ho, Jonathan Z.,Reddy, Komandla Malla,Mamedova, Lala,Vu, Phong H.,Lee, Kuen-Shan S.,Minami, Nathaniel K.,Gibson, Tony S.,Anderson, Susanne M.,Bradbury, Annette E.,Nolan, Thomas G.,Semple, J. Edward
, p. 1203 - 1208 (2007/10/03)
Investigations on P2-P3-heterocyclic dipeptide surrogates directed towards identification of an orally bioavailable thrombin inhibitor led us to pursue novel classes of achiral, non-covalent P1-arginine derivatives. The design, synthesis, and biological activity of inhibitors NC1-NC30 that feature three classes of monocyclic P1-arginine surrogates will be disclosed: (1) (hetero)aromatic amidines, amines and hydroxyamidines, (2) 2-aminopyrazines, and (3) 2-aminopyrimidines and 2-aminotetrahydropyrimidines.
PYRAZINONE 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: STR1 for example: STR2
Efficacious, orally bioavailable thrombin inhibitors based on 3- aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates
Sanderson, Philip E. J.,Lyle, Terry A.,Cutrona, Kellie J.,Dyer, Dona L.,Dorsey, Bruce D.,McDonough, Colleen M.,Naylor-Olsen, Adel M.,Chen, I.-Wu,Chen, Zhongguo,Cook, Jacquelynn J.,Cooper, Carolyn M.,Gardell, Stephen J.,Hare, Timothy R.,Krueger, Julie A.,Lewis, S. Dale,Lin, Jiunn H.,Lucas Jr., Bobby J.,Lyle, Elizabeth A.,Lynch Jr., Joseph J.,Stranieri, Maria T.,Vastag, Kari,Yan, Youwei,Shafer, Jules A.,Vacca, Joseph P.
, p. 4466 - 4474 (2007/10/03)
We have addressed the key deficiency of noncovalent pyridinone acetamide thrombin inhibitor L-374,087 (1), namely, its modest half-lives in animals, by making a chemically stable 3-alkylaminopyrazinone bioisostere for its 3- sulfonylaminopyridinone core.
