The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28085275 |
53 |
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker. |
Bristol-Myers Squibb |
27994741 |
48 |
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors. |
Bristol-Myers Squibb R & D |
27455395 |
66 |
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex. |
Bristol-Myers Squibb R & D |
27073051 |
71 |
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group. |
Bristol-Myers Squibb |
26871940 |
7 |
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program. |
Merck Research Laboratories |
26704266 |
80 |
Novel phenylalanine derived diamides as Factor XIa inhibitors. |
Bristol-Myers Squibb |
26318999 |
70 |
Development of a novel tricyclic class of potent and selective FIXa inhibitors. |
Merck Research Laboratories |
25978966 |
65 |
Development of a novel class of potent and selective FIXa inhibitors. |
Merck Research Laboratories |
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 |
25937013 |
40 |
Rapid development of two factor IXa inhibitors from hit to lead. |
Merck Research Laboratories |
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 |
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 |
23294255 |
114 |
Development of new cyclic plasmin inhibitors with excellent potency and selectivity. |
Philipps University Marburg |
16644215 |
52 |
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors. |
Celera Genomics |
22770607 |
54 |
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold. |
Virginia Commonwealth University |
20121198 |
63 |
Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis. |
Trigen |
18054227 |
45 |
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors. |
Bristol-Myers Squibb Research and Development |
14640539 |
112 |
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1). |
Pharmaceutical Research Institute |
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 |
20650636 |
118 |
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate. |
F. Hoffmann-La Roche |
20355714 |
26 |
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor. |
Takeda Pharmaceutical |
20121197 |
148 |
Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors. |
Trigen |
18674905 |
58 |
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination. |
Chugai Pharmaceutical |
16487703 |
4 |
Discovery of novel hydroxy pyrazole based factor IXa inhibitor. |
Celera Genomics |
16213711 |
37 |
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
32527459 |
67 |
Discovery of hydroxy pyrimidine Factor IXa inhibitors. |
Merck |
32340773 |
110 |
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants. |
Merck |
32551603 |
185 |
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach. |
Novartis Institutes For Biomedical Research |
27434175 |
54 |
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold. |
The University of Queensland |
27347787 |
32 |
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability. |
Astrazeneca |
31445854 |
43 |
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability. |
Bristol-Myers Squibb |
30446438 |
36 |
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors. |
China Pharmaceutical University |
30520638 |
54 |
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma. |
The University of Queensland |
31833761 |
32 |
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups. |
Bristol-Myers Squibb |
31563807 |
63 |
Discovery of novel, potent, isosteviol-based antithrombotic agents. |
Peking University |
29072911 |
16 |
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs. |
University of Nottingham |
29501396 |
59 |
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors. |
Bristol-Myers Squibb |
29477075 |
3 |
Precise structures of fucosylated glycosaminoglycan and its oligosaccharides as novel intrinsic factor Xase inhibitors. |
Chinese Academy of Sciences |
27976897 |
39 |
Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics. |
Virginia Commonwealth University |
29077405 |
63 |
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212). |
Bristol-Myers Squibb |
28408226 |
51 |
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors. |
Mochida Pharmaceutical |
28110961 |
26 |
Synthesis, characterization and biological evaluation of novel chalcone sulfonamide hybrids as potent intestinal alkaline phosphatase inhibitors. |
Comsats Institute of Information Technology |
8788495 |
7 |
GR127935: a potent and selective 5-HT1D receptor antagonist. |
Glaxo Research and Development |
19884013 |
98 |
5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity. |
Wyeth Research |
19842661 |
140 |
Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases. |
Abbott Laboratories |
19699645 |
12 |
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase. |
Northern Kentucky University |
19428244 |
60 |
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics. |
Gsk |