The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 26912112 |
6 |
Synthesis, biological evaluation and molecular docking studies of 2-piperazin-1-yl-quinazolines as platelet aggregation inhibitors and ligands of integrinaIIbß3. |
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine |
| 26753814 |
7 |
Cyclic RGD peptidomimetics containing 4- and 5-amino-cyclopropane pipecolic acid (CPA) templates as dualaVß3 anda5ß1 integrin ligands. |
University Of Florence |
| 26367138 |
12 |
Design, Virtual Screening, and Synthesis of Antagonists ofaIIbß3 as Antiplatelet Agents. |
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine |
| 24949551 |
22 |
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
Philipps-Universit£T Marburg |
| 24973662 |
8 |
Targeting integrinsavß3 anda5ß1 with newß-lactam derivatives. |
University Of Bologna |
| 24654918 |
19 |
Pharmacophoric modifications lead to superpotentavß3 integrin ligands with suppresseda5ß1 activity. |
Technische Universit£T M£Nchen |
| 24412498 |
15 |
Synthesis and assay of retro-a4ß1 integrin-targeting motifs. |
University Of Bologna |
| 24095096 |
3 |
Synthesis and in vitro evaluation of a novel radioligand foravß3 integrin receptor imaging: [18F]FPPA-c(RGDfK). |
University Hospital Of Geneva |
| 23811088 |
26 |
Modulation ofavß3- anda5ß1-integrin-mediated adhesion by dehydro-ß-amino acids containing peptidomimetics. |
University Of Bologna |
| 23757209 |
10 |
Synthesis, biological evaluation, X-ray molecular structure and molecular docking studies of RGD mimetics containing 6-amino-2,3-dihydroisoindolin-1-one fragment as ligands of integrinaIIbß3. |
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine |
| 23644213 |
57 |
Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores. |
University Of Ljubljana |
| 23376251 |
32 |
Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism. |
University Of Ljubljana |
| 23362923 |
59 |
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypesa5ß1 andavß6: conformational control through flanking amino acids. |
Technische Universit£T M£Nchen |
| 20088512 |
4 |
One step radiosynthesis of 6-[(18)F]fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester ([(18)F]F-Py-TFP): a new prosthetic group for efficient labeling of biomolecules with fluorine-18. |
University Of Troms£ |
| 19959360 |
50 |
SAR of N-phenyl piperidine based oral integrin alpha5beta1 antagonists. |
Jerini |
| 19910191 |
46 |
Discovery of orally available integrin alpha5beta1 antagonists. |
Jerini |
| 8960563 |
12 |
Quantitative structure-activity relationship study of fibrinogen inhibitors, [[4-(4-amidinophenoxy)butanoyl]aspartyl]valine (FK633) derivatives, using a novel hydrophobic descriptor. |
Fujisawa Pharmaceutical |
| 10853647 |
63 |
Three-dimensional quantitative structure-activity relationship analyses of RGD mimetics as fibrinogen receptor antagonists. |
Kyoto University |
| | 9 |
Non-peptide fibrinogen receptor antagonists. 3. design and discovery of a centrally constrained inhibitor |
TBA |
| 21601452 |
2 |
Tetrazine-trans-cyclooctene ligation for the rapid construction of integrinavß3 targeted PET tracer based on a cyclic RGD peptide. |
University Of Delaware |
| 21349709 |
6 |
Exploring new near-infrared fluorescent disulfide-based cyclic RGD peptide analogs for potential integrin-targeted optical imaging. |
Washington University |
| 20888763 |
8 |
Synthesis and evaluation of bivalent, peptidomimetic antagonists of theavß3 integrins. |
The Methodist Hospital Research Institute |
| 17289386 |
10 |
Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics. |
Universit£ |
| 16982193 |
26 |
Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening. |
Chinese Academy Of Medical Sciences And Peking Union Medical College |
| 16854058 |
8 |
Discovery of small molecule integrin alphavbeta3 antagonists as novel anticancer agents. |
University Of Southern California |
| 16722662 |
2 |
Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior. |
University Of Naples Federico Ii |
| 16570923 |
8 |
Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors. |
Washington University |
| 15715477 |
3 |
Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery. |
University Of Southern California |
| 15369386 |
11 |
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis. |
Merck Research Laboratories |
| 15863341 |
33 |
Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids. |
Johnson & Johnson Pharmaceutical Research And Development |
| 15357963 |
16 |
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone. |
Merck Research Laboratories |
| 14521404 |
10 |
Docking studies on alphavbeta3 integrin ligands: pharmacophore refinement and implications for drug design. |
Technische Universit£T M£Nchen |
| 11020288 |
13 |
Nonpeptide alpha(v)beta(3) antagonists. 1. Transformation of a potent, integrin-selective alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist. |
Merck Research Laboratories |
| 8893849 |
10 |
Synthesis and solution conformation of cyclo[RGDRGD]: a cyclic peptide with selectivity for the alpha V beta 3 receptor. |
Texas A&M University |
| 7650686 |
3 |
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist. |
Merck Research Laboratories |
| 15013021 |
10 |
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives. |
Merck Research Laboratories |
| 12643914 |
40 |
Biphenyls as potent vitronectin receptor antagonists. Part 2: biphenylalanine ureas. |
Bayer |
| 14643310 |
6 |
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint. |
Merck Research Laboratories |
| 12419389 |
13 |
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements. |
Merck Research Laboratories |
| 11755355 |
32 |
Biphenyls as potent vitronectin receptor antagonists. |
Bayer |
| 12161158 |
11 |
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics. |
Merck Research Laboratories |
| 11992781 |
31 |
Synthesis of highly potent and selective hetaryl ureas as integrin alpha(V)beta3-receptor antagonists. |
Basf |
| 11738567 |
16 |
Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements. |
Merck Research Laboratories |
| 11738566 |
20 |
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide. |
Merck Research Laboratories |
| 9873697 |
15 |
Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model. |
Smithkline Beecham Pharmaceuticals |
| 23140358 |
28 |
Synthesis and biological evaluation (in vitro and in vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrinaVß3. |
Universit£ |
| 22959246 |
24 |
Camptothecins in tumor homing via an RGD sequence mimetic. |
Sigma-Tau Industrie Farmaceutiche Riunite |
| 22871580 |
6 |
Near-infrared fluorescent divalent RGD ligand for integrinavß3-targeted optical imaging. |
Washington University |
| 22621422 |
2 |
¹²5I-radiolabeled morpholine-containing arginine-glycine-aspartate (RGD) ligand ofavß3 integrin as a molecular imaging probe for angiogenesis. |
University Of Florence |
| 22575869 |
61 |
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 1. |
Astrazeneca |
| 22572578 |
124 |
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 2. |
Astrazeneca |
| 20055426 |
30 |
Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics. |
Universita Degli Studi Di Bologna |
| 19860432 |
42 |
alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers. |
Universite Catholique De Louvain |
| 18343671 |
8 |
Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands. |
Department Of Organic Chemistry Ugo Schiff University Of Firenze Via Della Lastruccia 13 |
| 18303826 |
48 |
Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues. |
Universit£ |
| 18068982 |
20 |
Design and synthesis of novel potent and selective integrin alphanubeta3 antagonists--novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates. |
Basf |
| 17184884 |
16 |
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design. |
Johnson & Johnson Pharmaceutical Research And Development |
| 16919941 |
8 |
Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists. |
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine |
| 16302808 |
28 |
Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders. |
Universit£ |
| 16134928 |
34 |
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. |
The Scripps Research Institute |
| 15857114 |
11 |
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities. |
University Of Ljubljana |
| 15482918 |
10 |
Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid. |
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine |
| 15357991 |
20 |
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands. |
3-Dimensional Pharmaceuticals |
| 12139455 |
78 |
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents. |
Genentech |
| 11543674 |
3 |
Determination of the binding specificity of an integral membrane protein by saturation transfer difference NMR: RGD peptide ligands binding to integrin alphaIIbbeta3. |
University Of Hamburg |
| 10999999 |
83 |
Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
Cor Therapeutics |
| 9622548 |
8 |
Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes. |
3-Dimensional Pharmaceuticals |
| 9207948 |
65 |
Discovery of an orally active series of isoxazoline glycoprotein IIb/IIIa antagonists. |
Dupont Pharmaceuticals |
| 9191954 |
9 |
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists. |
Merck Research Laboratories |
| 7608903 |
29 |
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists. |
Searle Research & Development |
| 7837237 |
37 |
Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation. |
R. W. Johnson Pharmaceutical Research Institute |
| 1479591 |
8 |
Potent inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Asp-carboxylate of RGDX mimetics and the platelet GP IIb-IIIa receptor. |
Searle Research & Development |
| 1597855 |
194 |
Cyclic RGD peptide analogues as antiplatelet antithrombotics. |
Genentech |
| 10673106 |
28 |
RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements. |
Hoechst Marion Roussel |
| | 10 |
Synthesis, evaluation and Tc-99m complexation of a hydrazinonicotinyl conjugate of a GP IIb/IIIa antagonist cyclic peptide for the detection of deep vein thrombosis |
TBA |
| | 18 |
Design, synthesis, and evaluation of fibrinogen inhibitors, -(p-amidinophenoxy) alkanoylaspartic acid derivatives |
TBA |
| | 3 |
Preparation and Properties of a fibrinogen receptor antagonist containing the Arg-Gly-Asp sequence and nitroxide radicals |
TBA |
| 22185640 |
15 |
Tailoring of integrin ligands: probing the charge capability of the metal ion-dependent adhesion site. |
Technische Universit£T M£Nchen |
| 22365562 |
154 |
Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold. |
University Of Ljubljana |
| 21852128 |
11 |
RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor. |
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine |
| 21344906 |
54 |
Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry. |
The University Of Tokyo |
| 20951038 |
3 |
Small molecule inhibitors of hantavirus infection. |
University Of New Mexico School Of Medicine |
| 20809642 |
28 |
Click-chemistry-derived triazole ligands of arginine-glycine-aspartate (RGD) integrins with a broad capacity to inhibit adhesion of melanoma cells and both in vitro and in vivo angiogenesis. |
University Of Florence |
| 20218623 |
68 |
Emerging targets in osteoporosis disease modification. |
Amgen |
| 19942441 |
47 |
Novel tumor-targeted RGD peptide-camptothecin conjugates: synthesis and biological evaluation. |
Istituto Di Ricerche Chimiche E Biochimiche G. Ronzoni |
| | 12 |
Beta-amino acid derivatives as orally active non-peptide fibrinogen receptor antagonists |
TBA |
| | 41 |
Dihydroisoquinolone RGD mimics. Exploration of the aspartate isostere |
TBA |
| | 24 |
Tetrahydrothienopyridine derivatives as novel GPIIb/IIIa antagonists |
TBA |
| | 18 |
Nonpeptide GPIIb/IIIa inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation |
TBA |
| | 17 |
Structure-activity relationships in 3-oxo-1,4-benzodiazepine-2-acetic acid GPIIb/IIIa antagonists. The 2-benzazepine series |
TBA |
| | 54 |
Solid-phase parallel synthesis applied to lead optimization: Discovery of potent analogues of the GPIIb/IIIa antagonist RWJ-50042 |
TBA |
| | 17 |
Non-peptide fibrinogen receptor antagonists based upon a 4-substituted piperidine scaffold |
TBA |
| | 12 |
Platelet glycoprotein IIb–IIIa receptor (GPIIb–IIIa) antagonists derived from amidinoindoles |
TBA |
| | 13 |
Non-peptide glycoprotein IIb/IIIa inhibitors. 6. Design and synthesis of rigid, centrally constrained non-peptide fibrinogen receptor antagonists |
TBA |
| | 11 |
Synthesis and antiplatelet activity of DMP 757 analogs |
TBA |
| | 2 |
Design, synthesis and SAR of RGD peptide hybrids as highly efficient inhibitors of platelet aggregation |
TBA |
| | 1 |
Adamantane and Nipecotic Acid Derivatives as Novel β-Turn Mimics |
TBA |
| | 17 |
Fibrinogen receptor antagonists containing a gamma-lactam Gly-Asp isostere |
TBA |
| 17973471 |
24 |
Multiple N-methylation by a designed approach enhances receptor selectivity. |
Technische UniversitäT MüNchen |
| 17910915 |
19 |
Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides. |
Bayer Healthcare |
| 17869121 |
32 |
Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds. |
Università |
| 17616113 |
63 |
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists. |
Jerini |
| 17399986 |
114 |
R-isomers of Arg-Gly-Asp (RGD) mimics as potent alphavbeta3 inhibitors. |
Pfizer |
| 17387018 |
74 |
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization. |
Pfizer |
| 16621534 |
87 |
Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists. |
Pfizer |
| 16509596 |
29 |
Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior. |
Istituto Di Ricerche Chimiche E Biochimiche G. Ronzoni |
| 16303301 |
44 |
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties. |
Pfizer |
| 16298127 |
80 |
Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists. |
Pfizer |
| 15974570 |
30 |
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists. |
Università |
| 15745815 |
7 |
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics. |
Merck Research Laboratories |
| 15715463 |
16 |
Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core. |
Johnson And Johnson Pharmaceutical Research & Development |
| 15501072 |
58 |
1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability. |
Johnson & Johnson Pharmaceutical Research & Development |
| 15380233 |
46 |
Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins. |
Johnson & Johnson Pharmaceutical Research And Development |
| 15125957 |
23 |
N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists. |
Amgen |
| 15109653 |
30 |
Discovery of a potent and selective alpha v beta 3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model. |
Dainippon Pharmaceutical |
| 15056002 |
112 |
Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. |
Millennium Pharmaceuticals |
| 15006384 |
179 |
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists. |
Pfizer |
| 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 |
| 14698164 |
39 |
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds. |
Pharmaceutical Research Institute |
| 14640540 |
18 |
Molecular model of the alpha(IIb)beta(3) integrin. |
Merck Research Laboratories |
| 14561098 |
8 |
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. |
Merck Research Laboratories |
| 12729670 |
49 |
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold. |
Merck Research Laboratories |
| 12668017 |
17 |
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists. |
Glaxosmithkline |
| 12565960 |
33 |
Thiophene-based vitronectin receptor antagonists. |
Shire Biochem |
| 12565923 |
6 |
Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors. |
Leiden University |
| 12482416 |
52 |
Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones. |
Basf |
| 12477347 |
16 |
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin. |
Merck Research Laboratories |
| 12392735 |
30 |
Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists. |
Institut De Recherches Servier |
| 11909727 |
35 |
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes. |
Cor Therapeutics |
| 11855984 |
102 |
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins. |
Merck |
| 11814816 |
30 |
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective alpha(V)beta(3) antagonists. |
Knoll |
| 11714601 |
9 |
Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists. |
Bayer |
| 11551763 |
25 |
1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists. |
The R. W. Johnson Pharmaceutical Research Institute |
| 11454469 |
95 |
alpha(v)beta(3) Antagonists based on a central thiophene scaffold. |
Aventis Pharma Deutschland |
| 11392540 |
23 |
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 2: design of potent antagonists containing the 3-azaspiro[5.5]undecanes. |
Cor Therapeutics |
| 11392539 |
34 |
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 1: design of potent and specific 3,9-diazaspiro[5.5]undecanes. |
Cor Therapeutics |
| 11384239 |
82 |
Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective alphavbeta3 integrin antagonists. |
Technische UniversitäT MüNchen |
| 11327582 |
23 |
2-Acylimino-3H-thiazoline derivatives: a novel template for platelet GPIIb/IIIa receptor antagonists. |
Taisho Pharmaceutical |
| 11312916 |
2 |
Discovery of an orally active non-peptide fibrinogen receptor antagonist based on the hydantoin scaffold. |
Aventis Pharma |
| 10987423 |
83 |
Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors. |
Merck Research Laboratories |
| 10853677 |
34 |
Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists. |
Celltech Chiroscience |
| 10743945 |
21 |
Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists. |
Dupont Pharmaceuticals |
| 10714506 |
13 |
Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere. |
Eli Lilly |
| 10633037 |
88 |
Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3). |
Dupont Pharmaceuticals |
| 10633036 |
79 |
Isoxazolines as potent antagonists of the integrin alpha(v)beta(3). |
Dupont Pharmaceuticals |
| 10633035 |
20 |
Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic. |
Smithkline Beecham Pharmaceuticals |
| 10602710 |
51 |
Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308. |
The R. W. Johnson Pharmaceutical Research Institute |
| 10579850 |
15 |
Fused bicyclic Gly-Asp beta-turn mimics with specific affinity for GPIIb-IIIa. |
Eli Lilly |
| 10447947 |
14 |
N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists. |
Technische UniversitäT MüNchen |
| 10406646 |
15 |
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model. |
Smithkline Beecham Pharmaceuticals |
| 10406645 |
36 |
Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics. |
Smithkline Beecham Pharmaceuticals |
| 10395482 |
40 |
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation. |
Merck Research Laboratories |
| 10230615 |
60 |
Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds. |
Dupont Pharmaceuticals |
| 10206551 |
15 |
Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors. |
Merck Research Laboratories |
| 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 |
| 10052962 |
21 |
Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists. |
Smithkline Beecham Pharmaceuticals |
| 10021912 |
32 |
Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate. |
Dupont Pharmaceuticals |
| 9873696 |
80 |
Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists. |
Smithkline Beecham Pharmaceuticals |
| 9767641 |
11 |
New platelet fibrinogen receptor glycoprotein IIb-IIIa antagonists: orally active series of N-alkylated amidines with a 6,6-bicyclic template. |
Mitsui Pharmaceuticals |
| 9651154 |
54 |
Design of a new class of orally active fibrinogen receptor antagonists. |
RhôNe-Poulenc Rorer |
| 9632368 |
30 |
GPIIb/IIIa integrin antagonists with the new conformational restriction unit, trisubstituted beta-amino acid derivatives, and a substituted benzamidine structure. |
Nippon Steel |
| 9484499 |
94 |
Novel non-peptide fibrinogen receptor antagonists. 1. Synthesis and glycoprotein IIb-IIIa antagonistic activities of 1,3,4-trisubstituted 2-oxopiperazine derivatives incorporating side-chain functions of the RGDF peptide. |
Takeda Chemical Industries |
| 9435900 |
89 |
Fibrinogen receptor (GPIIb-IIIa) antagonists derived from 5,6-bicyclic templates. Amidinoindoles, amidinoindazoles, and amidinobenzofurans containing the N-alpha-sulfonamide carboxylic acid function as potent platelet aggregation inhibitors. |
Cor Therapeutics |
| 9341914 |
15 |
New orally active non-peptide fibrinogen receptor (GpIIb-IIIa) antagonists: identification of ethyl 3-[N-[4-[4-[amino[(ethoxycarbonyl) imino]methyl]phenyl]-1,3-thiazol-2-yl]-N-[1-[(ethoxycarbonyl)methyl]pip erid -4-yl]amino]propionate (SR 121787) as a potent and long-acting antithrombotic agent. |
Sanofi Recherche |
| 9288166 |
74 |
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists. |
Eli Lilly |
| 9240343 |
28 |
Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists. |
Smithkline Beecham Pharmaceuticals |
| 9207949 |
26 |
Non-peptide RGD surrogates which mimic a Gly-Asp beta-turn: potent antagonists of platelet glycoprotein IIb-IIIa. |
Eli Lilly |
| 9057858 |
23 |
From peptide to non-peptide. 3. Atropisomeric GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus. |
Genentech |
| 9016328 |
19 |
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists. |
Dupont Pharmaceuticals |
| 8960544 |
10 |
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists. |
Smithkline Beecham Pharmaceuticals |
| 8759635 |
16 |
Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines. |
F. Hoffmann-La Roche |
| 8667355 |
2 |
Discovery of an orally active non-peptide fibrinogen receptor antagonist. |
Hoechst |
| 8145226 |
45 |
Conformationally constrained peptides and semipeptides derived from RGD as potent inhibitors of the platelet fibrinogen receptor and platelet aggregation. |
Smithkline Beecham Pharmaceuticals Research And Development |
| 8057299 |
66 |
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp. |
Merck Research Laboratories |
| 7837245 |
4 |
Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore. |
Smithkline Beecham Pharmaceuticals |
| 7752183 |
22 |
Design and evaluation of nonpeptide fibrinogen gamma-chain based GPIIb/IIIa antagonists. |
R. W. Johnson Pharmaceutical Research Institute |
| 7507165 |
139 |
Design and synthesis of novel cyclic RGD-containing peptides as highly potent and selective integrin alpha IIb beta 3 antagonists. |
Telios Pharmaceuticals |
| 1920361 |
52 |
Development of a small RGD peptide fibrinogen receptor antagonist with potent antiaggregatory activity in vitro. |
Smithkline Beecham Pharmaceuticals Research And Development |
| 1469694 |
22 |
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors. |
Merck Research Laboratories |
| 1433204 |
10 |
Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists. |
Smithkline Beecham Pharmaceuticals |
| 1433203 |
20 |
Investigation of conformational specificity at GPIIb/IIIa: evaluation of conformationally constrained RGD peptides. |
Smithkline Beecham Pharmaceuticals |
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