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 |
27073051 |
71 |
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group. |
Bristol-Myers Squibb |
26704266 |
80 |
Novel phenylalanine derived diamides as Factor XIa inhibitors. |
Bristol-Myers Squibb |
25592713 |
37 |
Pyridine and pyridinone-based factor XIa inhibitors. |
Bristol-Myers Squibb |
26005539 |
23 |
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety. |
Bristol-Myers Squibb |
25990761 |
66 |
Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin. |
Institute For Infection Research |
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 |
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 |
24102612 |
105 |
Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity. |
University of Bari &Quot;Aldo Moro&Quot |
23927973 |
41 |
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold. |
Bristol-Myers Squibb Research & Development |
23478148 |
10 |
Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
23602442 |
28 |
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility. |
Bristol-Myers Squibb |
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 |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
17588746 |
103 |
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa. |
Bristol-Myers Squibb |
15837303 |
52 |
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors. |
Berlex Biosciences |
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 |
12954057 |
113 |
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors. |
Pharmacia |
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 |
12824035 |
39 |
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors. |
Pharmacia |
12270173 |
23 |
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones. |
Universit£ |
22041058 |
44 |
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors. |
Bristol-Myers Squibb |
21641796 |
30 |
Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors. |
Technical University of Denmark |
20102150 |
35 |
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif. |
Johnson & Johnson Pharmaceutical Research and Development |
19447619 |
3 |
Preparation of L-proline based aeruginosin 298-A analogs: optimization of the P1-moiety. |
University of New Orleans |
| 37 |
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors |
TBA |
19128974 |
28 |
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
Daiichi Sankyo |
18674905 |
58 |
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination. |
Chugai Pharmaceutical |
15332844 |
8 |
Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea. |
Griffith University |
18159923 |
24 |
7-fluoroindazoles as potent and selective inhibitors of factor Xa. |
Johnson & Johnson Pharmaceutical Research and Development |
17643988 |
92 |
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications. |
Bristol-Myers Squibb |
17566736 |
60 |
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa. |
Pfizer |
16714109 |
40 |
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles. |
Celera |
16650987 |
10 |
Efforts toward oral bioavailability in factor VIIa inhibitors. |
Celera |
16458507 |
2 |
Factor VIIa inhibitors: a prodrug strategy to improve oral bioavailability. |
Celera Genomics |
16257204 |
37 |
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation. |
Celera |
16213711 |
37 |
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15913999 |
8 |
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa. |
Pfizer |
15203149 |
72 |
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition. |
Aventis Pharma Deutschland |
14552766 |
12 |
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex. |
Pharmacia |
12699744 |
15 |
Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo. |
Genentech |
12668013 |
42 |
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors. |
Aventis Pharma Deutschland |
12593666 |
30 |
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. |
Senju Pharmaceutical |
12270169 |
13 |
Albumin affinity tags increase peptide half-life in vivo. |
Genentech |
11689072 |
49 |
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator. |
Axys Pharmaceuticals |
11527709 |
19 |
Optimization of a screening lead for factor VIIa/TF. |
Axys Pharmaceuticals |
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 |
32456431 |
24 |
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species. |
Bristol Myers Squibb |
31445854 |
43 |
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability. |
Bristol-Myers Squibb |
10212122 |
35 |
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors. |
Molecumetics |
30446438 |
36 |
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors. |
China Pharmaceutical University |
9873692 |
54 |
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa. |
Dupont Pharmaceuticals |
29400967 |
136 |
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
Bristol-Myers Squibb |
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 |
9871540 |
100 |
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors. |
Dupont Pharmaceuticals |
31563807 |
63 |
Discovery of novel, potent, isosteviol-based antithrombotic agents. |
Peking University |
26575094 |
60 |
Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
University of Antwerp (Ua) |
29501396 |
59 |
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors. |
Bristol-Myers Squibb |
28780160 |
14 |
Macrocyclic factor XIa inhibitors. |
Bristol-Myers Squibb |
29517911 |
87 |
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema. |
Bicycle Therapeutics |
29077405 |
63 |
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212). |
Bristol-Myers Squibb |
28460818 |
29 |
Neutral macrocyclic factor VIIa inhibitors. |
Bristol-Myers Squibb Research and Development |
9802391 |
31 |
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4. |
Uppsala University |
9195867 |
15 |
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D. |
University of California Berkeley |
20383151 |
2 |
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. |
Dana-Farber Cancer Institute |
19648931 |
16 |
Design, synthesis and selection of DNA-encoded small-molecule libraries. |
Praecis Pharmaceuticals |
19305397 |
22 |
Molecular docking and ligand specificity in fragment-based inhibitor discovery. |
University of California San Francisco |
19699645 |
12 |
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase. |
Northern Kentucky University |