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 |
28105277 |
33 |
Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors. |
Bristol-Myers Squibb |
27994741 |
48 |
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors. |
Bristol-Myers Squibb R & D |
27612545 |
37 |
Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors. |
Bristol-Myers Squibb Research & Development |
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 |
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 |
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 |
24951330 |
25 |
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties. |
Bristol-Myers Squibb |
24405333 |
69 |
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors. |
Bristol-Myers Squibb |
24418773 |
61 |
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia. |
Astrazeneca |
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 |
23124211 |
22 |
Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element. |
Zydus Research Centre |
22276953 |
63 |
A new strategy for the development of highly potent and selective plasmin inhibitors. |
Philipps University Marburg |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University Of Florida |
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 |
10479288 |
141 |
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa. |
Rh£Ne-Poulenc Rorer |
9301673 |
234 |
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine. |
Klinikum Der Friedrich-Schiller-Universit£T Jena |
| 24 |
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor |
TBA |
22041058 |
44 |
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors. |
Bristol-Myers Squibb |
21035339 |
16 |
Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa. |
Université |
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 |
19541481 |
57 |
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb |
19297154 |
88 |
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. |
Millennium Pharmaceuticals |
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 |
17420122 |
18 |
Selective and dual action orally active inhibitors of thrombin and factor Xa. |
Glaxosmithkline |
16913694 |
46 |
Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders. |
Institut De Recherches Servier |
16725321 |
13 |
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors. |
Celera Genomics |
16213711 |
37 |
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15080981 |
72 |
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors. |
Millennium Pharmaceuticals |
15013007 |
319 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity. |
Millennium Pharmaceuticals |
15013006 |
69 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs. |
Millennium Pharmaceuticals |
14980671 |
78 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors. |
Millennium Pharmaceuticals |
14980670 |
107 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs. |
Millennium Pharmaceuticals |
14698147 |
60 |
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
12639567 |
135 |
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors. |
Millennium Pharmaceuticals |
12039584 |
59 |
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors. |
Millennium Pharmaceuticals |
12039583 |
140 |
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides. |
Millennium Pharmaceuticals |
11960487 |
30 |
Structure-based design of novel potent nonpeptide thrombin inhibitors. |
Boehringer Ingelheim Pharma |
11958994 |
31 |
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors. |
Aventis Pharmaceuticals |
11677132 |
65 |
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors. |
Cor Therapeutics |
11063603 |
53 |
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors. |
Pfizer |
10937736 |
35 |
Nonbenzamidine compounds as selective factor Xa inhibitors. |
Aventis Pharmaceuticals |
10698439 |
68 |
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa. |
Rhone-Poulenc Rorer |
10509929 |
116 |
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors. |
RhôNe-Poulenc Rorer |
9784099 |
84 |
Design of benzamidine-type inhibitors of factor Xa. |
Institut FüR Biochemie |
28460818 |
29 |
Neutral macrocyclic factor VIIa inhibitors. |
Bristol-Myers Squibb Research And Development |
| 18 |
Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles |
Hacettepe University |