368426-67-9Relevant articles and documents
NOVEL SUBSTITUTED NITROGEN-CONTAINING HETEROBICYCLES AND USE THEREOF AS FACTOR XA INHIBITORS
-
Page/Page column 153, (2008/06/13)
The invention relates to novel substituted nitrogen-containing heterobicycles of general formula (I), wherein B, X1 to X3, and R1 to R5 are defined as indicated in claim 1, the tautomers, enantiomers, diastereom
Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates
Cui, Jingrong Jean,Araldi, Gian-Luca,Reiner, John E.,Reddy, Komandla Malla,Kemp, Scott J.,Ho, Jonathan Z.,Siev, Daniel V.,Mamedova, Lala,Gibson, Tony S.,Gaudette, John A.,Minami, Nathaniel K.,Anderson, Susanne M.,Bradbury, Annette E.,Nolan, Thomas G.,Semple
, p. 2925 - 2930 (2007/10/03)
Novel, potent, and highly selective classes of thrombin inhibitors were identified, which resulted from judicious combination of P4-aromatics and P2-P3-heterocyclic dipeptide surrogates with weakly basic (calcd pKa ~non-basic - 8.6) bicyclic P1-arginine mimics. The design, synthesis, and biological activity of achiral, non-covalent, orally bioavailable inhibitors NC1-NC44 featuring P1-indazoles, benzimidazoles, indoles, benzotriazoles, and aminobenzisoxazoles is disclosed.