The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27287367 |
36 |
Evaluation of bisbenzamidines as inhibitors for matriptase-2. |
University of Bonn |
27015008 |
51 |
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors. |
Bristol-Myers Squibb Research & Development |
26985294 |
114 |
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation. |
Southern Research |
27073051 |
71 |
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group. |
Bristol-Myers Squibb |
26732532 |
69 |
Active site-directed plasmin inhibitors: Extension on the P2 residue. |
Kobe Gakuin University |
26704266 |
80 |
Novel phenylalanine derived diamides as Factor XIa inhibitors. |
Bristol-Myers Squibb |
26421993 |
44 |
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors. |
Aurigene Discovery Technologies |
26367391 |
6 |
Phenylalanine and Phenylglycine Analogues as Arginine Mimetics in Dengue Protease Inhibitors. |
Heidelberg University |
26393374 |
34 |
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library. |
Queensland University of Technology |
26114810 |
8 |
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors. |
Southeast University |
26122211 |
3 |
Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate. |
Tokyo University of Pharmacy and Life Sciences |
25592713 |
37 |
Pyridine and pyridinone-based factor XIa inhibitors. |
Bristol-Myers Squibb |
26151189 |
56 |
Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors. |
TBA |
26005539 |
23 |
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety. |
Bristol-Myers Squibb |
25782055 |
9 |
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
Rempex Pharmaceuticals |
25881820 |
62 |
Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors. |
Bristol-Myers Squibb R & D |
25728130 |
79 |
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties. |
Bristol-Myers Squibb |
24951330 |
25 |
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties. |
Bristol-Myers Squibb |
25523211 |
18 |
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system. |
Astellas Pharma |
25438755 |
9 |
Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates. |
Astellas Pharma |
25405503 |
109 |
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity. |
Bristol-Myers Squibb |
25179681 |
81 |
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor. |
Chinese Academy of Sciences |
12565961 |
177 |
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors. |
Berlex Biosciences |
15887966 |
58 |
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring. |
Central Pharmaceutical Research Institute |
12904065 |
30 |
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide. |
Lg Life Sciences |
11170646 |
106 |
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa. |
Dupont Pharmaceuticals |
10794696 |
233 |
Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1. |
Universit£ |
9836616 |
92 |
Tetrahydro-isoquinoline-based factor Xa inhibitors. |
Boehringer Mannheim |
11858993 |
60 |
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds. |
Corvas International |
16759084 |
12 |
Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors. |
Peking University |
16137886 |
88 |
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization. |
Merck Research Laboratories |
15501047 |
75 |
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa. |
Merck |
15341970 |
59 |
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors. |
Eli Lilly |
15203158 |
84 |
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa. |
Merck |
12482415 |
30 |
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'. |
Merck Research Laboratories |
11960487 |
30 |
Structure-based design of novel potent nonpeptide thrombin inhibitors. |
Boehringer Ingelheim Pharma |
11689072 |
49 |
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator. |
Axys Pharmaceuticals |
11549459 |
5 |
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase. |
National Cancer Institute-Frederick |
11425524 |
62 |
Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality. |
Axys Pharmaceuticals |
11266160 |
57 |
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core. |
Dupont Pharmaceuticals |
11212109 |
14 |
The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase. |
Roche Discover Welwyn |
9873692 |
54 |
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa. |
Dupont Pharmaceuticals |
9873397 |
37 |
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors. |
3-Dimensional Pharmaceuticals |
9871573 |
15 |
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor. |
Biotech Research Institute |
9822554 |
14 |
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
9804697 |
61 |
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase. |
Northwestern University Medical School |
9484495 |
74 |
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa. |
Collegeville |