110 articles for GD Hartman
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.
Merck Research Laboratories
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Merck Research Laboratories
Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase.
Merck Research Laboratories
Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).
Merck Research Laboratories
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Merck Research Laboratories
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.
Merck Research Laboratories
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
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist.
Merck Research Laboratories
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.
Merck Research Laboratories
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
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.
Merck Research Laboratories
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
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
Merck Research Laboratories
Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.
TBA
Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.
TBA
Discovery of selective glucocorticoid receptor modulator MK-5932.
Merck Research Laboratories
Quinolizidinone carboxylic acids as CNS penetrant, selective m1 allosteric muscarinic receptor modulators.
TBA
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates.
Merck Research Laboratories
Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity.
Merck Research Laboratories
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.
Merck Research Laboratories
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Merck Research Laboratories
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Merck
Proline bis-amides as potent dual orexin receptor antagonists.
Merck Research Laboratories
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.
Merck Research Laboratories
Rapid assembly of diverse and potent allosteric Akt inhibitors.
Merck Research Laboratories
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Merck
Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
Merck And
Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.
Merck Research Laboratories
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.
Merck Research Laboratories
4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.
Merck Research Laboratories
New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides.
Merck Sharp and Dohme Research Laboratories
Tricyclic imidazole antagonists of the Neuropeptide S Receptor.
Merck Research Laboratories
Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold.
Merck Research Laboratories
Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3).
Merck Research Laboratories
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
Merck Research Laboratories
Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.
Merck Research Laboratories
Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.
Merck Research Laboratories
Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy.
Merck Research Laboratories
Pyridyl amides as potent inhibitors of T-type calcium channels.
Merck Research Laboratories
Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Merck Research Laboratories
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Merck Research Laboratories
Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Merck Research Laboratories
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.
Merck Research Laboratories
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Merck Research Laboratories
Nonpeptide GPIIb/IIIa inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation
TBA
Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3).
Merck Research Laboratories
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
Merck
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors.
Merck Research Laboratories
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
Merck Research Laboratories
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Merck Research Laboratories
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
Merck Research Laboratories
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
Merck Research Laboratories
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Merck Research Laboratories
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Merck
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Merck Research Laboratories
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.
Merck Research Laboratories
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Merck Research Laboratories
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
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
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.
Merck Research Laboratories
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Merck Research Laboratories
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Merck Research Laboratories
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.
Merck Research Laboratories
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
SAR studies in the sulfonyl carboxamide class of HBV capsid assembly modulators.
Novira Therapeutics
Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.
Merck Research Laboratories
Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.
Merck Research Laboratories
2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Merck Research Laboratories
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp.
Merck Research Laboratories
Synthesis and Evaluation of 5-Fluoro-2-aryloxazolo[5,4-b]pyridines as β-Amyloid PET Ligands and Identification of MK-3328.
Merck Research Laboratories
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Merck
3-Hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors. 7. Modification of the hexahydronaphthalene moiety of simvastatin: 5-oxygenated and 5-oxa derivatives.
Merck Sharp & Dohme Research Laboratories
Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors.
Merck Research Laboratories
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors.
Merck Research Laboratories
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.
Merck Research Laboratories
Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof
Jiangsu Hengrui Medicine
Structure-activity relationships of a new family of steroidal aromatase inhibitors. 1. Synthesis and evaluation of a series of analogs related to 19-[(methylthio)methyl]androstenedione (RU54115).
Centre De Recherche De Roussel Uclaf
1,2,5,6-tetra-O-benzyl-D-mannitol derivatives as novel HIV protease inhibitors.
Pharmacor
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.
Merck Research Laboratories
Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.
Merck Research Laboratories
Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.
University of Auckland
Energetics of heme binding to native and denatured states of cytochrome b562.
University of Illinois
Equilibrium thermodynamics of a physiologically-relevant heme-protein complex.
University of North Carolina at Chapel Hill
Calorimetric investigation of ethidium and netropsin binding to chicken erythrocyte chromatin.
Universite De Liege