74 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.
Merck Sharp and Dohme Research Laboratories
Novel 5-HT3 antagonists: indol-3-ylspiro(azabicycloalkane-3,5'(4'H)-oxazoles).
Merck Sharp and Dohme Research Laboratories
Spiropiperidines as high-affinity, selective sigma ligands.
Merck Sharp and Dohme Research Laboratories
Benz[f]isoquinoline analogues as high-affinity sigma ligands.
Merck Sharp and Dohme Research Laboratories
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.
Merck Sharp and Dohme Research Laboratories
Cyclic peptides as selective tachykinin antagonists.
Merck Sharp and Dohme Research Laboratories
2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.
Merck Sharp and Dohme Research Laboratories
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Merck Sharp and Dohme Research Laboratories
Current and novel approaches to the drug treatment of schizophrenia.
Merck Sharp and Dohme Research Laboratories
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.
Merck Sharp and Dohme Research Laboratories
Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.
Merck Sharp and Dohme Research Laboratories
HIV protease: a novel chemotherapeutic target for AIDS.
Merck Sharp and Dohme 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
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics.
Merck Sharp and Dohme Research Laboratories
Phosphinic acid inhibitors of D-alanyl-D-alanine ligase.
Merck Sharp and Dohme Research Laboratories
Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.
Merck Sharp and Dohme Research Laboratories
Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.
Merck Sharp and Dohme Research Laboratories
3-Substituted gem-cyclohexane sulfone based gamma-secretase inhibitors for Alzheimer's disease: conformational analysis and biological activity.
Merck Sharp and Dohme Research Laboratories
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.
Merck Sharp and Dohme Research Laboratories
NK1 antagonists based on seven membered lactam scaffolds.
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.
Merck Sharp and Dohme Research Laboratories
8-Fluoroimidazo[1,2-a]pyridine: synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA A receptor.
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Merck Sharp and Dohme Research Laboratories
Sarcosine based indandione hGlyT1 inhibitors.
Merck Sharp and Dohme Research Laboratories
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
Merck Sharp and Dohme Research Laboratories
Cyclic sulfamide gamma-secretase inhibitors.
Merck Sharp and Dohme Research Laboratories
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
Merck Sharp and Dohme Research Laboratories
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.
Merck Sharp and Dohme Research Laboratories
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
Merck Sharp and Dohme Research Laboratories
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Merck Sharp and Dohme Research Laboratories
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.
Merck Sharp and Dohme Research Laboratories
2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.
Merck Sharp and Dohme Research Laboratories
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Merck Sharp and Dohme Research Laboratories
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.
Merck Sharp and Dohme Research Laboratories
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
Merck Sharp and Dohme Research Laboratories
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
Merck Sharp and Dohme Research Laboratories
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
Merck Sharp and Dohme Research Laboratories
Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.
Merck Sharp and Dohme Research Laboratories
Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.
Merck Sharp and Dohme Research Laboratories
High affinity phenylglycinol-based NK1 receptor antagonists.
Merck Sharp and Dohme Research Laboratories
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.
Merck Sharp and Dohme Research Laboratories
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.
Merck Sharp and Dohme Research Laboratories
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
Merck Sharp and Dohme Research Laboratories
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
Merck Sharp and Dohme Research Laboratories
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Merck Sharp and Dohme Research Laboratories
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.
Merck Sharp and Dohme Research Laboratories
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Merck Sharp and Dohme Research Laboratories
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
Merck Sharp and Dohme Research Laboratories
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
Merck Sharp and Dohme Research Laboratories
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
Merck Sharp and Dohme Research Laboratories
3-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors.
Merck Sharp and Dohme Research Laboratories
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
Merck Sharp and Dohme Research Laboratories
Identification of 3,5-dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as novel high-affinity glycine site N-methyl-D-aspartate antagonists.
Merck Sharp and Dohme Research Laboratories
4,4-Disubstituted piperidines: a new class of NK1 antagonist.
Merck Sharp and Dohme Research Laboratories
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
Merck Sharp and Dohme Research Laboratories
Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.
Merck Sharp and Dohme Research Laboratories
Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.
Merck Sharp and Dohme Research Laboratories
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.
Merck Sharp and Dohme Research Laboratories
Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors.
Merck Sharp and Dohme Research Laboratories
Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane.
Merck Sharp and Dohme Research Laboratories
Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors.
Merck Sharp and Dohme Research Laboratories
4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.
Merck Sharp and Dohme Research Laboratories
Cyclosporin analogues for preventing or treating hepatitis C infection
Enanta Pharmaceuticals
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.
Purdue University