101 articles for thisTarget
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Article Title
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Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening.
University of California
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.
University of Louvain
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
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
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-(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
Synthetic study of VLA-4/VCAM-1 inhibitors: synthesis and structure-activity relationship of piperazinylphenylalanine derivatives.
Kyowa Hakko Kogyo
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-(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 α5β1/αvβ1 integrin for airway hyperresponsiveness.
University of California San Francisco
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists.
Merck Research Laboratories
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 β-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
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
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 β-Lactam Integrin Ligands Enhance Selectivity?
University of Bologna
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
Dehydro-β-proline Containing α4β1 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
Imide and acylurea derivatives as modulators of the glucocorticoid receptor
Bristol-Myers Squibb
Isoindoline derivatives for use in the treatment of a viral infection
Viiv Healthcare
Aza-phenalene-3-ketone derivative, preparation method thereof, and its application as PARP inhibitor
Suzhou Kangrun Pharmaceuticals
Histone deacetylase inhibitors and compositions and methods of use thereof
Chdi Foundation
Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
Sk Biopharmaceuticals
Compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, preparation method thereof and pharmaceutical use thereof
Shenyang Sunshine Pharmaceutical