The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 9873531 |
3 |
Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening. |
University of California |
| 24412498 |
15 |
Synthesis and assay of retro-a4ß1 integrin-targeting motifs. |
University of Bologna |
| 23777782 |
107 |
Orally available and efficaciousa4ß1/a4ß7 integrin inhibitors. |
Elan Pharmaceuticals |
| 23312947 |
22 |
Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists. |
Ranbaxy Research Laboratories |
| 23562062 |
4 |
Arylsulfonamide pyrimidines as VLA-4 antagonists. |
Elan Pharmaceuticals |
| 23312474 |
36 |
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 |
| 23312471 |
31 |
Identification of N-acyl 4-(3-pyridonyl)phenylalanine derivatives and their orally active prodrug esters as dual actinga4ß1 anda4ß7 receptor antagonists. |
Hoffmann-La Roche |
| 23218775 |
38 |
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 |
| 22261021 |
33 |
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 |
| 22101134 |
9 |
LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line. |
Universit£ |
| 21889349 |
20 |
Modeling the molecular basis fora4ß1 integrin antagonism. |
Ian Wark Laboratories |
| 16767086 |
2 |
Combinatorial chemistry identifies high-affinity peptidomimetics against alpha4beta1 integrin for in vivo tumor imaging. |
University of California |
| 19713111 |
31 |
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 |
| 19891440 |
57 |
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 |
| 16039122 |
9 |
Influence of acid surrogates toward potency of VLA-4 antagonist. |
Merck Research Laboratories |
| 15582407 |
20 |
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist. |
Daiichi Pharmaceutical |
| 15582442 |
36 |
2,3-Diphenylpropionic acids as potent VLA-4 antagonists. |
Kaken Pharmaceutical |
| 12086484 |
13 |
Identification of potent and novel alpha4beta1 antagonists using in silico screening. |
Biogen |
| 9341911 |
133 |
Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents. |
Genentech |
| 12617895 |
30 |
Dehydrophenylalanine derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 14552799 |
14 |
Sulphonamide-based small molecule VLA-4 antagonists. |
Molecumetics |
| 12749892 |
42 |
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists. |
Merck Research Laboratories |
| 11858990 |
20 |
N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists. |
Merck Research Laboratories |
| 11844701 |
5 |
Identification of unique VLA-4 antagonists from a combinatorial library. |
Merck Research Laboratories |
| 11755339 |
33 |
N-acyl-L-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation. |
Hoffmann-La Roche |
| 12161162 |
69 |
N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Hoffmann-La Roche |
| 12039570 |
51 |
N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 12039569 |
36 |
Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 12031328 |
21 |
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 11551757 |
29 |
Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists. |
Pfizer |
| 11140722 |
24 |
Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists. |
Hoffmann-La Roche |
| 10853676 |
13 |
Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists. |
Celltech Chiroscience |
| 10782674 |
50 |
N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Hoffmann-La Roche |
| 21316228 |
28 |
Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model. |
Elan Pharmaceuticals |
| 18331794 |
20 |
Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors. |
Millennium Pharmaceuticals |
| 18226905 |
60 |
Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 18242984 |
6 |
Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists. |
Merck Research Laboratories |
| 12139455 |
78 |
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents. |
Genentech |
| 20705461 |
38 |
Synthesis and biological activity of N-substituted aminocarbonyl-1,3-dioxolanes as VLA-4 antagonists. |
New Drug Discovery Research |
| 20022493 |
35 |
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 19441819 |
17 |
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 |
| 19124247 |
9 |
A novel and potent VLA-4 antagonist based on trans-4-substituted cyclohexanecarboxylic acid. |
Daiichi Sankyo |
| 19072684 |
11 |
Selectively targeting T- and B-cell lymphomas: a benzothiazole antagonist of alpha4beta1 integrin. |
University of California Davis |
| 18952443 |
26 |
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 |
| 18539454 |
47 |
Imidazopyridines as VLA-4 integrin antagonists. |
Ucb Pharma |
| 18160288 |
31 |
Synthetic study of VLA-4/VCAM-1 inhibitors: synthesis and structure-activity relationship of piperazinylphenylalanine derivatives. |
Kyowa Hakko Kogyo |
| 17118652 |
15 |
Highly constrained bicyclic VLA-4 antagonists. |
Merck Research Laboratories |
| 15081035 |
24 |
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4. |
Merck Research Laboratories |
| 15081033 |
21 |
Amidines as amide bond replacements in VLA-4 antagonists. |
Merck Research Laboratories |
| 14741263 |
67 |
Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3. |
Nerviano |
| 14741249 |
21 |
Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 12617914 |
116 |
N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists. |
Merck Research Laboratories |
| 12270174 |
34 |
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores. |
Genentech |
| 12161161 |
94 |
N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Roche Research Center |
| 12127538 |
26 |
N-aryl-prolyl-dipeptides as potent antagonists of VLA-4. |
Merck Research Laboratories |
| 12127523 |
22 |
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 12039589 |
6 |
Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists. |
Roche Research Center |
| 12031329 |
110 |
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists. |
Merck Research Laboratories |
| 11909715 |
73 |
Squaric acid derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 11844689 |
51 |
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 11844683 |
31 |
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists. |
Merck Research Laboratories |
| 11755344 |
47 |
The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists. |
Merck Research Laboratories |
| 11755338 |
24 |
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins. |
Merck Research Laboratories |
| 11714601 |
9 |
Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists. |
Bayer |
| 11677134 |
42 |
Design and synthesis of potent and selective inhibitors of integrin VLA-4. |
Novartis Institute For Biomedical Research |
| 11591507 |
79 |
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 11472212 |
6 |
Design and synthesis of potent and selective alpha(4)beta(7) integrin antagonists. |
Technische UniversitäT MüNchen |
| 31999923 |
16 |
Insights into Protein-Ligand Interactions in Integrin Complexes: Advances in Structure Determinations. |
Pliant Therapeutics |
| 31266686 |
7 |
Small-molecule agents for the treatment of inflammatory bowel disease. |
Gilead Sciences |
| 10915035 |
16 |
Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors. |
Millennium Pharmaceutical |
| 10866374 |
11 |
The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic. |
Roche Research Center |
| 10866373 |
8 |
Cyclic thioether peptide mimetics as VCAM-VLA-4 antagonists. |
Roche Research Center |
| 10866372 |
7 |
Carbacyclic peptide mimetics as VCAM-VLA-4 antagonists. |
Roche Research Center |
| 10853677 |
34 |
Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists. |
Celltech Chiroscience |
| 10782673 |
6 |
N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists. |
Roche Research Center |
| 10197962 |
13 |
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action. |
Dupont Pharmaceuticals |
| 10072689 |
39 |
Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses. |
Biogen |
| 31670514 |
45 |
Could Dissecting the Molecular Framework of ?-Lactam Integrin Ligands Enhance Selectivity? |
University of Bologna |
| 9016328 |
19 |
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists. |
Dupont Pharmaceuticals |
| 26101577 |
15 |
Dehydro-?-proline Containing ?4?1 Integrin Antagonists: Stereochemical Recognition in Ligand-Receptor Interplay. |
University of Bologna |
| 24568695 |
76 |
Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists. |
University of Bradford |
| 23899692 |
10 |
Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. |
Massachusetts General Hospital and Harvard Medical School |
| 17948981 |
10 |
Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin. |
University of California Davis |
| 17915848 |
48 |
Small molecule inhibitors of integrin alpha2beta1. |
University of Pennsylvania |
| 16377201 |
24 |
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists. |
Daiichi Pharmaceutical |
| 17194595 |
18 |
Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists. |
Daiichi Pharmaceutical |
| 16495061 |
8 |
Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent. |
Johnson & Johnson Pharmaceutical |
| 17035017 |
25 |
2,6-Quinolinyl derivatives as potent VLA-4 antagonists. |
Ucb Pharma |
| 16455247 |
15 |
Pyridone derivatives as potent and selective VLA-4 integrin antagonists. |
Glaxosmithkline |
| 16931004 |
29 |
Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists. |
Glaxosmithkline |
| 17041919 |
51 |
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 |
| 16112583 |
74 |
Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists. |
Johnson & Johnson Pharmaceutical |
| 16722660 |
60 |
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists. |
Johnson & Johnson Pharmaceutical |
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