PMID

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Article Title

Organization

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

Highly constrained bicyclic VLA-4 antagonists.

Merck Research Laboratories

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

Biogen