100 articles for thisTarget
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Synthesis and evaluation of imidazo[1,5-a]pyrazines as corticotropin releasing hormone receptor ligands.
Dupont Pharmaceuticals
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
Dupont Pharmaceuticals
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
Dupont Pharmaceuticals
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.
Dupont Pharmaceuticals
4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.
Dupont Pharmaceuticals
Corticotropin-releasing hormone receptor antagonists: framework design and synthesis guided by ligand conformational studies.
Dupont Pharmaceuticals
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.
Dupont Pharmaceuticals
Discovery of an orally active series of isoxazoline glycoprotein IIb/IIIa antagonists.
Dupont Pharmaceuticals
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
Dupont Pharmaceuticals
Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition.
Dupont Pharmaceuticals
Novel piperidine sigma receptor ligands as potential antipsychotic drugs.
Dupont Pharmaceuticals
Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz.
Dupont Pharmaceuticals
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Dupont Pharmaceuticals
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
Dupont Pharmaceuticals
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.
Dupont Pharmaceuticals
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-alpha production.
Dupont Pharmaceuticals
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Dupont Pharmaceuticals
Novel 4,4-bis(trifluoromethyl) imidazolines as stereospecific and orally active acyl coa: Cholesterol acyltransferase (ACAT) inhibitors and antihypercholesterolemic agents
Dupont Pharmaceuticals
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing two heterocyclic head groups
Dupont Pharmaceuticals
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing heterocyclic groups bioisosteric for an imidazole
Dupont Pharmaceuticals
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Dupont Pharmaceuticals
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
Dupont Pharmaceuticals
Glutamyl-gamma-boronate inhibitors of bacterial Glu-tRNA(Gln) amidotransferase.
Dupont Pharmaceuticals
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.
Dupont Pharmaceuticals
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.
Dupont Pharmaceuticals
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.
Dupont Pharmaceuticals
Alpha-ketoamides, alpha-ketoesters and alpha-diketones as HCV NS3 protease inhibitors.
Dupont Pharmaceuticals
Selection of a potent inhibitor of trihydroxynaphthalene reductase by sorting disease control data.
Dupont Pharmaceuticals
Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.
Dupont Pharmaceuticals
Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents.
Dupont Pharmaceuticals
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.
Dupont Pharmaceuticals
P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors.
Dupont Pharmaceuticals
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
Dupont Pharmaceuticals
Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.
Dupont Pharmaceuticals
4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists.
Dupont Pharmaceuticals
Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
Dupont Pharmaceuticals
Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.
Dupont Pharmaceuticals
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.
Dupont Pharmaceuticals
Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.
Dupont Pharmaceuticals
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
Dupont Pharmaceuticals
Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.
Dupont Pharmaceuticals
Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines.
Dupont Pharmaceuticals
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.
Dupont Pharmaceuticals
Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents.
Dupont Pharmaceuticals
Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.
Dupont Pharmaceuticals
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.
Dupont Pharmaceuticals
Structure-based design and synthesis of a series of hydroxamic acids with a quaternary-hydroxy group in P1 as inhibitors of matrix metalloproteinases.
Dupont Pharmaceuticals
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
Dupont Pharmaceuticals
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.
Dupont Pharmaceuticals
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups.
Dupont Pharmaceuticals
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Dupont Pharmaceuticals
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.
Dupont Pharmaceuticals
Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production.
Dupont Pharmaceuticals
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.
Dupont Pharmaceuticals
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Dupont Pharmaceuticals
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Dupont Pharmaceuticals
The solution conformation of (D)Phe-Pro-containing peptides: implications on the activity of Ac-(D)Phe-Pro-boroArg-OH, a potent thrombin inhibitor.
Dupont Pharmaceuticals
A novel series of selective, non-peptide inhibitors of angiotensin II binding to the AT2 site.
Dupont Pharmaceuticals
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.
Dupont Pharmaceuticals
Heteroaryl-fused 2-phenylisothiazolone inhibitors of cartilage breakdown.
Dupont Pharmaceuticals
Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
Dupont Pharmaceuticals
Balanced AT1/AT2 receptor antagonists. 4. XR510 and related 5-(3-amidopropanoyl)imidazoles possessing equal affinity for the AT1 and AT2 receptors.
Dupont Pharmaceuticals
Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity.
Dupont Pharmaceuticals
Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis.
Dupont Pharmaceuticals
N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists
Ogeda
Subunit selective NMDA receptor potentiators for the treatment of neurological conditions
Emory University
Compositions, methods, and systems for the synthesis and use of imaging agents
Lantheus Medical Imaging
Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
Sanofi
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Merck Research Laboratories
Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.
Bristol-Myers Squibb
Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere.
Glaxo Group Research
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships.
Glaxo Group Research
Synthesis of novel, potent, diol-based HIV-1 protease inhibitors via intermolecular pinacol homocoupling of (2S)-2-benzyloxymethyl-4-phenylbutanal.
Stockholm University