303 articles for thisTarget
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Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands.
F. Hoffmann-La Roche
Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.
F. Hoffmann-La Roche
Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues.
Sankyo
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds.
Mossakowski Medical Research Centre Polish Academy of Sciences
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.
Vrije Universiteit Brussel
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.
Bristol-Myers Squibb
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
Euroscreen
CNS drug design: balancing physicochemical properties for optimal brain exposure.
Eli Lilly
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.
Vrije Universiteit Brussel
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues.
Uppsala University
Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.
University of Montreal
Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.
Bristol-Myers Squibb
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.
University of Montreal
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.
Amgen
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Glaxosmithkline
Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.
University of Arizona
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Merck Research Laboratories
Constrained H-Phe-Phe-NH2 analogues with high affinity to the substance P 1-7 binding site and with improved metabolic stability and cell permeability.
Uppsala University
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
University of Siena
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
Broad Institute of Mit and Harvard
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Bristol-Myers Squibb
Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.
Bristol-Myers Squibb Research and Development
Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.
Astrazeneca
Quantitative structure-activity relationships (QSARs) of N-terminus fragments of NK1 tachykinin antagonists: a comparison of classical QSARs and three-dimensional QSARs from similarity matrices.
Cambridge University Forvie Site
Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.
Ucb Pharma
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.
Glaxosmithkline
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
Glaxosmithkline
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
Glaxosmithkline
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
National Institute of Neuroscienc
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.
Washington University
Cyclic peptides as selective tachykinin antagonists.
Merck Sharp and Dohme Research Laboratories
First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants.
Ucb Pharma
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonists.
F. Hoffmann-La Roche
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
Non-peptide NK1 receptor ligands based on the 4-phenylpyridine moiety.
University of Siena
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Tom'S of Maine
Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.
Merck Research Laboratories
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Janssen-Cilag
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.
Merck Sharp & Dohme Research Laboratories
Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.
Philipps-Universit£T Marburg
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
Astrazeneca Pharmaceuticals
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
Merck
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.
Clinical Research Institute of Montr£Al
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
University of Pennsylvania
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).
Smithkline Beecham
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.
Uppsala University
Axially chiral N-benzyl-N,7-dimethyl-5-phenyl-1, 7-naphthyridine-6-carboxamide derivatives as tachykinin NK1 receptor antagonists: determination of the absolute stereochemical requirements.
Takeda Chemical Industries
2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.
Novartis Institute For Medical Sciences
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
Cambridge University Forvie Site
Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.
University of Pennsylvania
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.
Smithkline Beecham
Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.
Merck Sharp & Dohme Research Laboratories
Studies on neurokinin antagonists. 4. Synthesis and structure-activity relationships of novel dipeptide substance P antagonists: N2-[(4R)-4-hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl]-N- methyl-N-(phenylmethyl)-3-(2-naphthyl)-L-alaninamide and its related compounds.
Fujisawa Pharmaceutical
Design and synthesis of side-chain conformationally restricted phenylalanines and their use for structure-activity studies on tachykinin NK-1 receptor.
Pierre and Marie Curie University
Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand.
Pfizer
Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs.
Institut De Recherches Servier
Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.
Glaxo Group Research
Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles.
Rochester
Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists.
Fujisawa Pharmaceutical
Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors.
TBA
Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.
The Schering Plough Research Institute
Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.
Novartis Institute For Medical Sciences
Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.
Pfizer
Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.
Yamanouchi Pharmaceutical
Asymmetric synthesis of Boc-N-methyl-p-benzoyl-phenylalanine. Preparation of a photoreactive antagonist of substance P.
Pierre and Marie Curie University
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
Merck Sharp Laboratory
Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity
TBA
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds
TBA
The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists
TBA
Synthesis of RPR 100893, prototype of a new series of potent and selective non peptide NK1 antagonists : the triarylperhydroisoindolols.
TBA
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design
TBA
Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.
Takeda Pharmaceutical
Design, structure-activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor antagonists.
Takeda Pharmaceutical
Recent progress in synthesis and bioactivity studies of indolizines.
University of Botswana
Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.
University of Arizona
3-benzhydryl-4-piperidones as novel neurokinin-1 receptor antagonists and their efficient synthesis.
Takeda Pharmaceutical
Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.
Vrije Universiteit Brussel
Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
University of Arizona
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.
Euroscreen
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Glaxosmithkline
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.
F. Hoffmann-La Roche
Discovery of a series of potent, orally activea,a-disubstituted piperidine NK(1) antagonists.
Merck Research Laboratories
Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.
Merck Research Laboratories
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
University of Arizona
Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.
F. Hoffmann-La Roche
Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.
Merck Research Laboratories
Discovery of dipeptides with high affinity to the specific binding site for substance P1-7.
Uppsala University
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.
Pfizer
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
University of Arizona
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.
F. Hoffmann-La Roche
Spiroquinazoline, a Novel Substance P Inhibitor with a New Carbon Skeleton, Isolated from Aspergillus flavipes
TBA
1'-(2-Phenyl-ethylene)-ditryptophenaline, a New Dimeric Diketopiperazine from Aspergillus flavus
TBA
Studies on the active conformation of the NK1 antagonist CGP 49823. Part 21. Fluoro-olefin analogs of tertiary amide rotamers.
TBA
Studies on the active conformation of NK1 antagonist CGP 49823. Part 1. Synthesis of conformationally restricted analogs.
TBA
Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H1/NK1 receptor antagonist activity
TBA
The dipeptide neurokinin-1 receptor antagonist S19752 is a potent and long-acting inhibitor of bronchoconstriction when administered by aerosol to the guinea pig in vivo
TBA
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
TBA
Nonpeptide bradykinin antagonist analogs based on a model of a Sterling-Winthrop nonpeptide bradykinin antagonist overlapped with cyclic hexapeptide bradykinin antagonist peptides
TBA
Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors
TBA
The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptors
TBA
SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist
TBA
1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channel
TBA
4,4-Diphenyl-7-perhydrothiapyrano[3,4-c]pyrrolone, a new series of substance P receptors antagonists
TBA
1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists
TBA
Perhydrothiopyranopyrroles derivatives : A novel series of potent and selective nonpeptide NK1 antagonists.
TBA
Alternative strategies towards the identification of chemical lead compounds by rational design
TBA
The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanes
TBA
Piperidine-ether based hNK1 antagonists 1: Determination of the relative and absolute stereochemical requirements
TBA
Articulating a pharmacophore driven synthetic strategy: Discovery of a potent substance P antagonist
TBA
Quinuclidine based NK-1 antagonists 2: determination of the absolute stereochemical requirements
TBA
Nuclear variations of quinuclidine substance P antagonists: 2-diphenylmethyl-1-azabicyclo[3.2.2]nonan-3-amines
TBA
Application of the multipin peptide synthesis technique for peptide receptor binding studies: Substance P as A model system
TBA
1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.
TBA
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Merck Research Laboratories
Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.
The University of Tokyo
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
University of Arizona
Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.
Pfizer
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.
Amgen
Design, synthesis, and structure-affinity relationship studies in NK1 receptor ligands based on azole-fused quinolinecarboxamide moieties.
Università
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
Schering-Plough Research Institute
Conformational comparisons of a series of tachykinin peptide analogs.
Mississippi State University
Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist.
Pfizer
Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety.
Pfizer
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Merck Research Laboratories
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Merck
Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design.
Vrije Universiteit Brussel
Geminal Diheteroatomic Motifs: Some Applications of Acetals, Ketals, and Their Sulfur and Nitrogen Homologues in Medicinal Chemistry and Drug Design.
Bristol Myers Squibb Research and Early Development
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.
Merck Sharp & Dohme Research Laboratories
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
Merck Research Laboratories
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Merck Research Laboratories
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Merck Research Laboratories
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Merck Research Laboratories
Cyclobutane derivatives as potent NK1 selective antagonists.
Schering-Plough Research Institute
Diarylacetylene piperidinyl amides as novel anxiolytics.
Johnson & Johnson Pharmaceutical Research and Development
NK1 antagonists based on seven membered lactam scaffolds.
Merck Sharp and Dohme Research Laboratories
1-Phenyl-8-azabicyclo[3.2.1]octane ethers: a novel series of neurokinin (NK1) antagonists.
Merck Sharp & Dohme Research Laboratories
Novel lactam NK1 antagonists with anti-emetic activity.
Merck Sharp & Dohme Research Laboratories
Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
F. Hoffmann-La Roche
Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.
Merck Sharp & Dohme Research Laboratories
The Design and Optimization of Monomeric Multitarget Peptides for the Treatment of Multifactorial Diseases.
China Pharmaceutical University
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
Schering-Plough Research Institute
Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption.
Pfizer
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
Merck
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
Universidad De Sevilla
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.
Astrazeneca Pharmaceuticals
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
Medicines For Malaria Venture
Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.
University of Pennsylvania
Improving NK1R-targeted gene delivery of stearyl-antimicrobial peptide CAMEL by conjugating it with substance P.
Lanzhou University
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.
Schering-Plough Research Institute
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.
Merck Sharp & Dohme Research Laboratories
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.
Merck Sharp and Dohme Research Laboratories
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.
Schering-Plough Research Institute
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.
Merck Sharp & Dohme Research Laboratories
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.
Merck Sharp & Dohme Research Laboratories
Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.
Schering-Plough Research Institute
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Pharmazeutisches Institut Der UniversitäT Freiburg
Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.
Schering-Plough Research Institute
Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionamides.
Novartis Pharma
2-Aryl indole NK(1) antagonists: optimisation of the amide substituent.
Merck Sharp & Dohme Research Laboratories
Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.
Cambridge University Forvie Site
Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.
Eli Lilly
2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.
Merck Sharp and Dohme Research Laboratories
2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.
The Neuroscience Research Centre
Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994.
Laboratoire De Chimie ThéRapeutique Associé
Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.
Schering-Plough Research Institute
Multiple-conformation and protonation-state representation in 4D-QSAR: the neurokinin-1 receptor system.
Biographics Laboratory 3R
Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.
Schering-Plough Research Institute
The design and synthesis of novel NK1/NK2 dual antagonists.
Schering-Plough Research Institute
Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.
Sankyo
N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide: an orally active neurokinin NK1/NK2 antagonist.
Novartis Pharma
Solution structures in SDS micelles and functional activity at the bullfrog substance P receptor of ranatachykinin peptides.
Marshall University School of Medicine and Huntington Va Medical Center
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
Merck Research Laboratories
Axially chiral 1,7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK(1) receptor antagonists: synthesis, antagonistic activity, and effects on bladder functions.
Takeda Chemical Industries
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
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
Astrazeneca
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
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
Merck Research Laboratories
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.
University of Pennsylvania
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.
Smithkline Beecham S.P.A. Milano
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
China Pharmaceutical University
Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P.
Hebrew University of Jerusalem
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
Merck Sharp and Dohme Research Laboratories
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Merck Research Laboratories
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
Eli Lilly
Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.
University of Arizona
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
University of Arizona
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
Merck Sharp and Dohme Research Laboratories
4,4-Disubstituted piperidines: a new class of NK1 antagonist.
Merck Sharp and Dohme Research Laboratories
Studies on neurokinin antagonists. 3. Design and structure-activity relationships of new branched tripeptides N alpha-(substituted L-aspartyl, L-ornithyl, or L-lysyl)-N-methyl-N-(phenylmethyl)-L-phenylalaninamides as substance P antagonists.
Fujisawa Pharmaceutical
Novel, potent, and orally active substance P antagonists: synthesis and antagonist activity of N-benzylcarboxamide derivatives of pyrido[3,4-b]pyridine.
Takeda Chemical Industries
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
Merck Sharp & Dohme Research Laboratories
Importance of parallel vectors and"hydrophobic collapse" of the aligned aromatic rings: discovery of a potent substance P antagonist.
Pfizer
Comparison of the conformation of active and nonactive backbone cyclic analogs of substance P as a tool to elucidate features of the bioactive conformation: NMR and molecular dynamics in DMSO and water.
Technische UniversitäT MüNchen
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
Merck Sharp and Dohme Research Laboratories
Structure determination, pharmacological evaluation, and structure-activity studies of a new cyclic peptide substance P antagonist containing the new amino acid 3-prenyl-beta-hydroxytyrosine, isolated from Aspergillus flavipes.
Sterling Winthrop Pharmaceuticals Research Division
Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.
Merck Sharp and Dohme Research Laboratories
Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.
Menarini Ricerche
Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity.
Gsk
New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists.
Glaxo Wellcome Medicines Research Centre
Design, synthesis and biological studies of a library of NK1-Receptor Ligands Based on a 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyran core: Switch from antagonist to agonist effect by chemical modification.
Universidad De Sevilla
Antagonists of substance P. Further modifications of substance P antagonists obtained by replacing either positions 7, 9 or 7, 8 and 11 of SP with D-amino acid residues.
TBA
Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity.
Hebrew University of Jerusalem
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
Pfizer
Synthesis and substance P antagonist activity of naphthimidazolium derivatives.
Rochester
Discovery of a potent substance P antagonist: recognition of the key molecular determinant.
Pfizer
NOVEL SUBSTITUTED PYRAZINE-CARBOXAMIDE DERIVATIVES
Boehringer Ingelheim International
Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency.
Yale University
Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
Boehringer Ingelheim International
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity
University of North Carolina At Chapel Hill
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives
Idorsia Pharmaceuticals
Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
Viiv Healthcare UK (NO.5)
Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
Albany Molecular Research
Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
Incyte
Thiophene derivative as SGLT2 inhibitor and pharmaceutical composition comprising same
Green Cross
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.
Gsk
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Kochi Medical School
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Merck Research Laboratories
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
University of Tampere