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

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

Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.

Genentech

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

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

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

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

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