PMID

Data

Article Title

Organization

Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening.

University of California

Synthesis and assay of retro-a4ß1 integrin-targeting motifs.

University of Bologna

Orally available and efficaciousa4ß1/a4ß7 integrin inhibitors.

Elan Pharmaceuticals

Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists.

Ranbaxy Research Laboratories

Arylsulfonamide pyrimidines as VLA-4 antagonists.

Elan Pharmaceuticals

Identification of N-acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives and their orally active prodrug esters as dual-acting alpha4-beta1 and alpha4-beta7 receptor antagonists.

Hoffmann-La Roche

Identification of N-acyl 4-(3-pyridonyl)phenylalanine derivatives and their orally active prodrug esters as dual actinga4ß1 anda4ß7 receptor antagonists.

Hoffmann-La Roche

A novel, potent, and orally active VLA-4 antagonist with good aqueous solubility: trans-4-[1-[[2-(5-Fluoro-2-methylphenylamino)-7-fluoro-6-benzoxazolyl]acetyl]-(5S)-[methoxy(methyl)amino]methyl-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid.

Daiichi Sankyo

Identification of trans-4-[1-[[7-fluoro-2-(1-methyl-3-indolyl)-6-benzoxazolyl]acetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid as a potent, orally active VLA-4 antagonist.

Daiichi Sankyo

LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line.

Universit£

Modeling the molecular basis fora4ß1 integrin antagonism.

Ian Wark Laboratories

Combinatorial chemistry identifies high-affinity peptidomimetics against alpha4beta1 integrin for in vivo tumor imaging.

University of California

Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.

Merck Research Laboratories

Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid: an orally active, selective very late antigen-4 antagonist.

Daiichi Sankyo

Influence of acid surrogates toward potency of VLA-4 antagonist.

Merck Research Laboratories

Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.

Daiichi Pharmaceutical

2,3-Diphenylpropionic acids as potent VLA-4 antagonists.

Kaken Pharmaceutical

Identification of potent and novel alpha4beta1 antagonists using in silico screening.

Biogen

Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents.

Genentech

Dehydrophenylalanine derivatives as VLA-4 integrin antagonists.

Celltech R&D

Sulphonamide-based small molecule VLA-4 antagonists.

Molecumetics

N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.

Merck Research Laboratories

N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists.

Merck Research Laboratories

Identification of unique VLA-4 antagonists from a combinatorial library.

Merck Research Laboratories

N-acyl-L-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation.

Hoffmann-La Roche

N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.

Hoffmann-La Roche

N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists.

Celltech R&D

Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists.

Celltech R&D

N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists.

Merck Research Laboratories

Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists.

Pfizer

Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists.

Hoffmann-La Roche

Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists.

Celltech Chiroscience

N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.

Hoffmann-La Roche

Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.

Elan Pharmaceuticals

Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors.

Millennium Pharmaceuticals

Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists.

Johnson & Johnson Pharmaceutical Research & Development

Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.

Merck Research Laboratories

Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.

Genentech

Synthesis and biological activity of N-substituted aminocarbonyl-1,3-dioxolanes as VLA-4 antagonists.

New Drug Discovery Research

Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.

Merck Research Laboratories

Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.

Merck Research Laboratories

A novel and potent VLA-4 antagonist based on trans-4-substituted cyclohexanecarboxylic acid.

Daiichi Sankyo

Selectively targeting T- and B-cell lymphomas: a benzothiazole antagonist of alpha4beta1 integrin.

University of California Davis

Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist.

Daiichi Sankyo

Imidazopyridines as VLA-4 integrin antagonists.

Ucb Pharma

Synthetic study of VLA-4/VCAM-1 inhibitors: synthesis and structure-activity relationship of piperazinylphenylalanine derivatives.

Kyowa Hakko Kogyo

Highly constrained bicyclic VLA-4 antagonists.

Merck Research Laboratories

Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4.

Merck Research Laboratories

Amidines as amide bond replacements in VLA-4 antagonists.

Merck Research Laboratories

Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3.

Nerviano

Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.

Johnson & Johnson Pharmaceutical Research & Development

Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.

University of Nebraska Medical Center

N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists.

Merck Research Laboratories

Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores.

Genentech

N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.

Roche Research Center

N-aryl-prolyl-dipeptides as potent antagonists of VLA-4.

Merck Research Laboratories

N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.

Merck Research Laboratories

Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists.

Roche Research Center

Dual antagonists of ?5?1/?v?1 integrin for airway hyperresponsiveness.

University of California San Francisco

Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists.

Merck Research Laboratories

Squaric acid derivatives as VLA-4 integrin antagonists.

Celltech R&D

Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.

Merck Research Laboratories

The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.

Merck Research Laboratories

New ?-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins.

University of Bologna

The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.

Merck Research Laboratories

Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins.

Merck Research Laboratories

Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists.

Bayer

Design and synthesis of potent and selective inhibitors of integrin VLA-4.

Novartis Institute For Biomedical Research

The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.

Merck Research Laboratories

Design and synthesis of potent and selective alpha(4)beta(7) integrin antagonists.

Technische UniversitäT MüNchen

Insights into Protein-Ligand Interactions in Integrin Complexes: Advances in Structure Determinations.

Pliant Therapeutics

Small-molecule agents for the treatment of inflammatory bowel disease.

Gilead Sciences

Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors.

Millennium Pharmaceutical

The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic.

Roche Research Center

Cyclic thioether peptide mimetics as VCAM-VLA-4 antagonists.

Roche Research Center

Carbacyclic peptide mimetics as VCAM-VLA-4 antagonists.

Roche Research Center

Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.

Celltech Chiroscience

N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists.

Roche Research Center

Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.

Dupont Pharmaceuticals

Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.

Biogen

Could Dissecting the Molecular Framework of ?-Lactam Integrin Ligands Enhance Selectivity?

University of Bologna

Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.

Dupont Pharmaceuticals

Dehydro-?-proline Containing ?4?1 Integrin Antagonists: Stereochemical Recognition in Ligand-Receptor Interplay.

University of Bologna

Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists.

University of Bradford

Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.

Massachusetts General Hospital and Harvard Medical School

Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin.

University of California Davis

Small molecule inhibitors of integrin alpha2beta1.

University of Pennsylvania

Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists.

Daiichi Pharmaceutical

Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists.

Daiichi Pharmaceutical

Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent.

Johnson & Johnson Pharmaceutical

2,6-Quinolinyl derivatives as potent VLA-4 antagonists.

Ucb Pharma

Pyridone derivatives as potent and selective VLA-4 integrin antagonists.

Glaxosmithkline

Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists.

Glaxosmithkline

Structure-activity relationship studies of a series of peptidomimetic ligands for alpha(4) beta(1) integrin on Jurkat T-leukemia cells.

University of California Davis

Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists.

Johnson & Johnson Pharmaceutical

Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists.

Johnson & Johnson Pharmaceutical