91 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.
Bristol-Myers Squibb
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Bristol-Myers Squibb
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Bristol-Myers Squibb
Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.
Institute For Infection Research
Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.
Bristol-Myers Squibb R & D
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.
Bristol-Myers Squibb
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.
Bristol-Myers Squibb
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
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
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.
Bristol-Myers Squibb Research & Development
Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.
Bristol-Myers Squibb
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Celera Genomics
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.
Virginia Commonwealth University
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
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
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.
Berlex Biosciences
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
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.
Pharmacia
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
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.
Pharmacia
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.
University of Montreal
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.
Technical University of Denmark
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
Preparation of L-proline based aeruginosin 298-A analogs: optimization of the P1-moiety.
University of New Orleans
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors
TBA
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
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.
Chugai Pharmaceutical
Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea.
Griffith University
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
Johnson & Johnson Pharmaceutical Research and Development
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bristol-Myers Squibb
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.
Pfizer
Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Verseon
Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and Perspectives.
Hefei University of Technology
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.
Celera
Factor VIIa inhibitors: a prodrug strategy to improve oral bioavailability.
Celera Genomics
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.
Celera
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs.
Northwest University
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa.
Pfizer
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
Kalvista Pharmaceuticals
Potent Cyclic Peptide Inhibitors of FXIIa Discovered by mRNA Display with Genetic Code Reprogramming.
The University of Sydney
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.
Aventis Pharma Deutschland
Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment.
Shenyang Pharmaceutical University
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.
Pharmacia
Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo.
Genentech
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.
Aventis Pharma Deutschland
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.
Senju Pharmaceutical
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.
Axys Pharmaceuticals
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Merck
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
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Bristol Myers Squibb
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.
Molecumetics
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.
China Pharmaceutical University
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Bristol-Myers Squibb
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Bristol-Myers Squibb
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.
Dupont Pharmaceuticals
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)
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Bicycle Therapeutics
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Bristol-Myers Squibb
Neutral macrocyclic factor VIIa inhibitors.
Bristol-Myers Squibb Research and Development
Substituted spiropyrido[1,2-a]pyrazine derivative and medicinal use thereof as HIV integrase inhibitor
Japan Tobacco
Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
Vtv Therapeutics
Azabicyclo derivatives, process for preparation thereof and medical use thereof
Shanghai Haiyan Pharmaceutical Technology
Pyrrolopyrimidine derivatives as NR2B NMDA receptor antagonists
Rugen Holdings (Cayman)
Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists
Rugen Holdings (Cayman)
Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine.
Memorial Sloan-Kettering Cancer Center
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1.
Bristol-Myers Squibb Pharmaceutical Research Institute
Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.
Hong Kong University of Science and Technology
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines.
Wyeth-Ayerst Research
Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.
Gilead Sciences
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.
Biocryst Pharmaceuticals
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design.
Biocryst Pharmaceuticals