148 articles for RR Wexler
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
Nonpeptide angiotensin II receptor antagonists: the discovery of a series of N-(biphenylylmethyl)imidazoles as potent, orally active antihypertensives.
E. I. Du Pont De Nemours
Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.
Bristol-Myers Squibb
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.
Bristol-Myers Squibb R & D
Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.
Bristol-Myers Squibb Research & Development
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Bristol-Myers Squibb R & D
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.
Bristol-Myers Squibb Research & Development
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
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
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
Bristol-Myers Squibb
Discovery of 4-aryl-7-hydroxyindoline-based P2Y1 antagonists as novel antiplatelet agents.
Bristol-Myers Squibb Research
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.
Bristol-Myers Squibb
Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.
Bristol-Myers Squibb Research and Development
Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.
Bristol-Myers Squibb
2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.
Bristol-Myers Squibb
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors.
Bristol-Myers Squibb
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.
Bristol-Myers Squibb R & D
Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.
Bristol-Myers Squibb
Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.
Bristol-Myers Squibb
Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.
Bristol-Myers Squibb R & D
Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.
Bristol-Myers Squibb Pharmaceutical Research Institute
2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.
Bristol-Myers Squibb
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.
Bristol-Myers Squibb
Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.
Bristol-Myers Squibb R & D
Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.
Bristol-Myers Squibb Research and Development
Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
Bristol-Myers Squibb
Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors.
Bristol-Myers Squibb
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
Bristol-Myers Squibb Research and Development
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bristol-Myers Squibb Research and 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
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
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
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
Dupont Pharmaceuticals
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.
Dupont Pharmaceuticals
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
Dupont Pharmaceuticals
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.
Dupont Pharmaceuticals
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Dupont Pharmaceuticals
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: heterocyclic bioisosteres for the urea group in DuP 128
TBA
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing heterocyclic groups bioisosteric for an imidazole
Dupont Pharmaceuticals
Balanced angiotensin II receptor antagonists. III. The effects of substitution at the imidazole 5-position.
TBA
Balanced angiotensin II receptor antagonists. II.1,2 4-aminomethyl- and acylaminomethylimidazoles
TBA
Balanced angiotensin II receptor antagonists. I. The effects of biphenyl “ortho”-substitution on AT1/AT2 affinities
TBA
Potent imidazole angiotensinII antagonists: acyl sulfonamides and acyl sulfamides as tetrazole replacements
TBA
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
Bristol-Myers Squibb
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Bristol-Myers Squibb
Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis.
Bristol Myers Squibb
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure.
Bristol Myers Squibb
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bristol-Myers Squibb
Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors.
Bristol Myers Squibb
Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Bristol-Myers Squibb Research & Early Development
Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists.
Bristol Myers Squibb Research and Development
Design and preparation of N-linked hydroxypyridine-based APJ agonists.
Bristol-Myers Squibb Research & Early Development
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Pharmaceutical Research Institute
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.
Bristol-Myers Squibb Pharmaceutical Research Institute
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
Bristol Myers Squibb
Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO).
Bristol-Myers Squibb
Identification of 6-hydroxy-5-phenyl sulfonylpyrimidin-4(1H)-one APJ receptor agonists.
Bristol-Myers Squibb
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.
Bristol-Myers Squibb
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Bristol-Myers Squibb
Discovery and structure activity relationships of 7-benzyl triazolopyridines as stable, selective, and reversible inhibitors of myeloperoxidase.
Bristol Myers Squibb
Potent P1' biphenylmethyl substituted aggrecanase inhibitors.
Bristol-Myers Squibb Pharma
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors.
Bristol Myers Squibb
Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.
Bristol Myers Squibb
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Dupont Pharmaceuticals
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
Dupont Pharmaceuticals
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Bristol Myers Squibb
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.
Bristol-Myers Squibb Research and Development
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.
Dupont Pharmaceuticals
Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.
Bristol-Myers Squibb
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.
Dupont Pharmaceuticals
Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor.
Bristol-Myers Squibb
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.
Dupont Pharmaceuticals
Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Bristol-Myers Squibb Research & Development
Benzothiazole-based compounds as potent endothelial lipase inhibitors.
Bristol-Myers Squibb
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.
Dupont Pharmaceuticals
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.
Bristol-Myers Squibb
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.
Dupont Pharmaceuticals
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
Dupont Pharmaceuticals
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.
Dupont Pharmaceuticals
Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
Bristol-Myers Squibb
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.
Dupont Pharmaceuticals
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
Potent Triazolopyridine Myeloperoxidase Inhibitors.
Bristol-Myers Squibb Research and Development
Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.
Bristol-Myers Squibb
Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo.
TBA
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
Discovery of novel P1 groups for coagulation factor VIIa inhibition using fragment-based screening.
Bristol-Myers Squibb
A novel series of selective, non-peptide inhibitors of angiotensin II binding to the AT2 site.
Dupont Pharmaceuticals
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.
Dupont Pharmaceuticals
Balanced AT1/AT2 receptor antagonists. 4. XR510 and related 5-(3-amidopropanoyl)imidazoles possessing equal affinity for the AT1 and AT2 receptors.
Dupont Pharmaceuticals
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Bristol-Myers Squibb
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor.
Bristol-Myers Squibb
Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.
Bristol-Myers Squibb
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
4-cyano-benzyl carbamimidoylcarbamate derivatives and their use as AOC3 inhibitors
Boehringer Ingelheim International
Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists
Rugen Holdings (Cayman)
Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
Boehringer Ingelheim International
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.
Faculte De Medecine Et De Pharmacie
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
Hebrew University of Jerusalem
Structure-activity relationship of HIV-1 protease inhibitors containing AHPBA. Part III: Modification of P2 site.
Sankyo