147283-76-9Relevant articles and documents
A facile and efficient method for the synthesis of novel pyridone analogues by aminolysis of an ester under solvent-free conditions
Karis, N. David,Loughlin, Wendy A.,Jenkins, Ian D.
, p. 12303 - 12309 (2008/03/12)
A series of 15 pure novel N-alkylated pyridone derivatives have been synthesized in 73-96% yields on treatment of ethyl (2-pyridone)acetates with structurally diverse amines in an efficient aminolysis procedure under 'solvent-free' conditions.
Non-peptide αvβ3 antagonists. Part 6: Design and synthesis of αvβ3 antagonists containing a pyridone or pyrazinone central scaffold
Breslin, Michael J.,Duggan, Mark E.,Halczenko, Wasyl,Fernandez-Metzler, Carmen,Hunt, Cecilia A.,Leu, Chih-Tai,Merkle, Kara M.,Naylor-Olsen, Adel M.,Prueksaritanont, Thomayant,Stump, Gary,Wallace, Audrey,Rodan, Sevgi B.,Hutchinson, John H.
, p. 1809 - 1812 (2007/10/03)
Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the β-alanine 3-substituent produced compounds that are potent and selective αvβ3 antagonists and exhibit a range of physicochemical properties.
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors
Huang, Wenrong,Naughton, Mary Ann,Yang, Hua,Su, Ting,Dam, Suiko,Wong, Paul W.,Arfsten, Ann,Edwards, Susan,Sinha, Uma,Hollenbach, Stanley,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 723 - 728 (2007/10/03)
A series of novel transition state factor Xa inhibitors containing a variety of lactam ring systems as central templates was synthesized in an expedient manner and allowed for a great deal of structural variability. Among them, the piperazinone-based inhibitors were found to be not only active against factor Xa but also selective over thrombin. Optimization of the P4 moiety yielded several potent compounds with IC50 below 1 nM against factor Xa.
Selective factor Xa inhibitors
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Example 4, (2008/06/13)
Novel compounds of formula I: including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The co
Aromatic heterocyclic derivatives as enzyme inhibitors
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Page column 46-47, (2010/02/04)
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
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.
Aromatic heterocyclic derivatives as enzyme inhibitors
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, (2008/06/13)
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
AROMATIC HETEROCYCLIC DERIVATIVES AS ENZYME INHIBITORS
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, (2008/06/13)
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
AROMATIC HETEROCYCLIC DERIVATIVES AS ENZYME INHIBITORS
-
, (2008/06/13)
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors
Warner,Green,Gomes,Strimpler
, p. 3090 - 3099 (2007/10/02)
Human leukocyte elastase (HLE) is a serine protease produced by neutrophils that has been implicated in diseases such as amphysema and cystic fibrosis. An HLE inhibitor may have therapeutic value in these diseases. An active site model of HLE bound to a t
