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 |
10782685 |
9 |
Synthesis of a cyanopeptide-analogue with trypsin activating properties. |
Ernst-Moritz-Arndt-University |
28197309 |
40 |
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors. |
Global Blood Therapeutics |
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 |
26732532 |
69 |
Active site-directed plasmin inhibitors: Extension on the P2 residue. |
Kobe Gakuin University |
26421993 |
44 |
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors. |
Aurigene Discovery Technologies |
26393374 |
34 |
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library. |
Queensland University of Technology |
25592713 |
37 |
Pyridine and pyridinone-based factor XIa inhibitors. |
Bristol-Myers Squibb |
25987378 |
2 |
Inhibitors of melanogenesis in B16 melanoma 4A5 cells from flower buds of Lawsonia inermis (Henna). |
Kyoto Pharmaceutical University |
25921265 |
21 |
Novel type of plasmin inhibitors: providing insight into P4 moiety and alternative scaffold to pyrrolopyrimidine. |
Hiroshima International University |
25782055 |
9 |
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
Rempex Pharmaceuticals |
25728130 |
79 |
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties. |
Bristol-Myers Squibb |
24900876 |
56 |
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
Astrazeneca |
152812 |
69 |
Inhibition of four human serine proteases by substituted benzamidines. |
TBA |
660589 |
3 |
Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length. |
TBA |
24613052 |
69 |
Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin. |
Hiroshima International University |
24405333 |
69 |
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors. |
Bristol-Myers Squibb |
24175584 |
35 |
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor. |
Sanofi-Aventis R&D |
24135727 |
7 |
Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors. |
Emory University |
23899618 |
9 |
Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug. |
Lg Life Sciences |
23586812 |
38 |
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy. |
Ecole Polytechnique F�D�Rale De Lausanne Epfl |
23521080 |
6 |
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
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 |
16554154 |
9 |
Development of activity-based probes for trypsin-family serine proteases. |
Celera Genomics |
22882079 |
26 |
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase. |
Aarhus University |
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 |
22950366 |
6 |
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta. |
Hokkaido University |
22276953 |
63 |
A new strategy for the development of highly potent and selective plasmin inhibitors. |
Philipps University Marburg |
22366654 |
33 |
2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator. |
University of Louisville |
19861238 |
14 |
Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one. |
Takeda Pharmaceutical |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
15787457 |
3 |
Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera. |
Chiba University |
18164204 |
24 |
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors. |
Takeda Pharmaceutical |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
18077174 |
31 |
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. |
Takeda Pharmaceutical |
18054227 |
45 |
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors. |
Bristol-Myers Squibb Research and Development |
18052026 |
97 |
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties. |
University of Antwerp |
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 |
16517159 |
45 |
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. |
Abbott |
16250649 |
10 |
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library. |
Brown University |
15887966 |
58 |
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring. |
Central Pharmaceutical Research Institute |
15582437 |
2 |
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors. |
Central Pharmaceutical Research Institute |
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 |
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 |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
10579821 |
51 |
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency. |
Novartis Horsham Research Centre |
10479288 |
141 |
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa. |
Rh£Ne-Poulenc Rorer |
9836616 |
92 |
Tetrahydro-isoquinoline-based factor Xa inhibitors. |
Boehringer Mannheim |
9083470 |
9 |
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site. |
Merck Research Laboratories |
9357536 |
47 |
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position. |
Merck Research Laboratories |
9301673 |
234 |
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine. |
Klinikum Der Friedrich-Schiller-Universit£T Jena |
2231595 |
96 |
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
Abbott Laboratories |
12270173 |
23 |
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones. |
Universit£ |
10915051 |
43 |
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position. |
Novartis Horsham Research Centre |
| 22 |
Design and synthesis of conformationally constrained arginal thrombin inhibitors |
TBA |
| 48 |
DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORS |
TBA |
22285569 |
107 |
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA). |
University of Antwerp |
22041058 |
44 |
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors. |
Bristol-Myers Squibb |
21944858 |
12 |
Identification of novel plasmin inhibitors possessing nitrile moiety as warhead. |
Hiroshima International University |
21741839 |
83 |
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT. |
Philipps University Marburg |
21168329 |
47 |
New furin inhibitors based on weakly basic amidinohydrazones. |
Philipps University Marburg |
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 |
20405925 |
5 |
Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020. |
University of Basel |
20355714 |
26 |
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor. |
Takeda Pharmaceutical |
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 |
20038105 |
50 |
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics. |
Philipps University Marburg |
19703768 |
63 |
Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). |
Berlex Biosciences |
19541481 |
57 |
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb |
| 15 |
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moiety |
TBA |
| 37 |
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors |
TBA |
| 25 |
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates |
TBA |
| 78 |
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors |
TBA |
| 61 |
(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors |
TBA |
| 13 |
Characterization of LY806303 as a potent and selective inhibitor of thrombin |
TBA |
19297158 |
30 |
Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR. |
Millennium Pharmaceuticals |
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 |
19250826 |
100 |
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors. |
The Medicines Company (Leipzig) |
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 |
19036586 |
128 |
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors. |
Curacyte Discovery |
18507371 |
24 |
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors. |
Takeda Pharmaceutical |
17935298 |
3 |
Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens. |
University of ZüRich |
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 |
16970403 |
74 |
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position. |
University of Antwerp |
16725321 |
13 |
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors. |
Celera Genomics |
16540315 |
23 |
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors. |
Mochida Pharmaceutical |
16460935 |
39 |
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s. |
Johnson & Johnson Pharmaceutical Research and Development |
16213711 |
37 |
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15801822 |
28 |
9-hydroxyazafluorenes and their use in thrombin inhibitors. |
Merck Research Laboratories |
15582418 |
103 |
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties. |
Abbott Laboratories |
15341970 |
59 |
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors. |
Eli Lilly |
15149680 |
58 |
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. |
Pfizer |
15149645 |
92 |
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors. |
Abbott Laboratories |
15115382 |
16 |
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator. |
University of Antwerp |
15013007 |
319 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity. |
Millennium Pharmaceuticals |
14711304 |
117 |
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution. |
Abbott Laboratories |
14698147 |
60 |
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
12824021 |
39 |
Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents. |
Boehringer Ingelheim Pharma |
12824020 |
31 |
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives. |
Boehringer Ingelheim Pharma |
12668020 |
29 |
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. |
3-Dimensional Pharmaceuticals |
12639567 |
135 |
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors. |
Millennium Pharmaceuticals |
12372529 |
21 |
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12113833 |
183 |
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors. |
Celera |
12113832 |
120 |
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors. |
Celera |
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 |
11844691 |
107 |
4-amidinobenzylamine-based inhibitors of urokinase. |
Universitat Jena |
11755350 |
31 |
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines. |
Pfizer |
11755349 |
24 |
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines. |
Pfizer |
11677132 |
65 |
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors. |
Cor Therapeutics |
11527709 |
19 |
Optimization of a screening lead for factor VIIa/TF. |
Axys Pharmaceuticals |
11495587 |
198 |
Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa. |
Axys Pharmaceuticals |
11459634 |
94 |
Development of potent and selective factor Xa inhibitors. |
Axys Pharmaceuticals |
11425539 |
23 |
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. |
Shionogi |
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 |
11378359 |
57 |
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors. |
3-Dimensional Pharmaceuticals |
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 |
32150407 |
27 |
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases. |
Qpex Biopharma |
11206478 |
18 |
Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor. |
Institute of Molecular and Cell Biology |
11078187 |
36 |
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors. |
Shionogi |
11063603 |
53 |
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors. |
Pfizer |
11055356 |
236 |
Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity. |
Axys Pharmaceuticals |
11055355 |
72 |
Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors. |
Axys Pharmaceuticals |
11055344 |
37 |
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties. |
Corvas International |
11012033 |
8 |
Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and HT29 cell lines. |
Kobe Gakuin University |
10937736 |
35 |
Nonbenzamidine compounds as selective factor Xa inhibitors. |
Aventis Pharmaceuticals |
10915052 |
20 |
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors. |
Novartis Horsham Research Centre |
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 |
10853674 |
32 |
Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors. |
Corvas International |
27347787 |
32 |
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability. |
Astrazeneca |
27280436 |
304 |
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines. |
Philipps University Marburg |
10782677 |
73 |
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa. |
Corvas International |
30707839 |
63 |
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides. |
Chinese Academy of Sciences |
10698439 |
68 |
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa. |
Rhone-Poulenc Rorer |
31679971 |
44 |
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease. |
University of Wollongong |
10617091 |
73 |
Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates. |
Corvas International |
10560742 |
85 |
3-Amidinophenylalanine-based inhibitors of urokinase. |
UniversitäT Jena |
10509929 |
116 |
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors. |
RhôNe-Poulenc Rorer |
10508448 |
11 |
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites. |
Brown University |
10498211 |
42 |
Novel benzo-fused lactam scaffolds as factor Xa inhibitors. |
Corvas International |
31445854 |
43 |
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability. |
Bristol-Myers Squibb |
10425106 |
12 |
4-Heterocyclohexanone-based inhibitors of the serine protease plasmin. |
Brown University |
10328293 |
23 |
The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore. |
Novartis Horsham Research Centre |
10230630 |
36 |
Thrombin inhibitors based on a propargylglycine template. |
Biotech Research Institute |
10206557 |
36 |
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals. |
Corvas International |
30520638 |
54 |
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma. |
The University of Queensland |
9873692 |
54 |
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa. |
Dupont Pharmaceuticals |
9873569 |
16 |
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates. |
Corvas International |
9873397 |
37 |
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors. |
3-Dimensional Pharmaceuticals |
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 |
31658420 |
98 |
Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding. |
Philipps University Marburg |
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 |
9784099 |
84 |
Design of benzamidine-type inhibitors of factor Xa. |
Institut FüR Biochemie |
9703466 |
35 |
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position. |
Merck Research Laboratories |
30613336 |
32 |
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II. |
The University of Queensland |
9171866 |
12 |
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy. |
Merck Research Laboratories |
27009905 |
22 |
Plasmin inhibitors with hydrophobic amino acid-based linker between hydantoin moiety and benzimidazole scaffold enhance inhibitory activity. |
Hiroshima International 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) |
26536069 |
89 |
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor. |
Aarhus University |
8426361 |
111 |
Highly selective tripeptide thrombin inhibitors. |
Eli Lilly |
8423602 |
15 |
Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
8035417 |
23 |
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
7739010 |
118 |
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. |
Thrombosis Research Institute |
7473571 |
90 |
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions. |
Eli Lilly |
9722497 |
2 |
Aeruginosin 103-A, a thrombin inhibitor from the cyanobacterium Microcystis viridis. |
The University of Tokyo |
9644086 |
1 |
Dehydroradiosumin, a trypsin inhibitor from the cyanobacterium Anabaena cylindrica. |
The University of Tokyo |
6219223 |
94 |
Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. |
TBA |
11170666 |
6 |
Isolation and structure determination of nostocyclopeptides A1 and A2 from the terrestrial cyanobacterium Nostoc sp. ATCC53789. |
University of Hawaii At Manoa |
30201291 |
27 |
Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis. |
Abdulaziz University For Health Sciences |
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 |
30130401 |
71 |
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer. |
University of Wollongong |
28045523 |
35 |
Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold. |
The University of Queensland |
27976897 |
39 |
Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics. |
Virginia Commonwealth University |
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 |
1447734 |
29 |
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases. |
University of Illinois |
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 |
9802391 |
31 |
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4. |
Uppsala University |
24058293 |
12 |
Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors. |
Durham University |