234 articles for thisTarget

---

The following articles (labelled with PubMed ID or TBD) are for your review

PMID	Data	Article Title	Organization
12372504	15	Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands.	F. Hoffmann-La Roche
12182851	15	Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.	F. Hoffmann-La Roche
27876250	60	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
26713106	59	Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.	Vrije Universiteit Brussel
26988801	55	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
26048800	55	Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.	Bristol-Myers Squibb
25738882	210	Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).	Euroscreen
25494650	8	CNS drug design: balancing physicochemical properties for optimal brain exposure.	Eli Lilly
25544687	60	Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.	Vrije Universiteit Brussel
24881566	140	Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).	Glaxosmithkline
25516784	12	Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues.	Uppsala University
24900878	40	Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.	Universit£
12565946	51	Discovery of orally bioavailable NK1 receptor antagonists.	Ucb Pharma
24507922	20	Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.	Bristol-Myers Squibb
24374277	41	Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.	Universit£
24900633	11	Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.	Amgen
24075145	17	Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.	Glaxosmithkline
23899615	18	Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.	University of Arizona
23808489	11	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
23582449	20	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
23466604	36	Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.	Universit£
23403082	28	Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.	Broad Institute of Mit and Harvard
23477943	51	Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.	Bristol-Myers Squibb
23253443	135	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
23281966	8	Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.	Astrazeneca
7473572	28	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
12372532	45	Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.	Ucb Pharma
21974957	27	Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.	Glaxosmithkline
19963378	11	Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.	Glaxosmithkline
19388677	10	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
19473027	21	Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.	National Institute of Neuroscienc
9733486	91	Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.	Washington University
11755367	38	First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants.	Ucb Pharma
22574973	36	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
21413808	170	Synopsis of some recent tactical application of bioisosteres in drug design.	Bristol-Myers Squibb Pharmaceutical Research and Development
21421318	25	Non-peptide NK1 receptor ligands based on the 4-phenylpyridine moiety.	Universit£
20875743	90	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
20684563	176	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
20188553	66	Tetrahydroindolizinone NK1 antagonists.	Merck Research Laboratories
20560643	71	Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.	University of Arizona
16562853	22	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
18248994	16	Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.	Merck Research Laboratories
17407815	27	Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.	Janssen-Cilag
16950620	36	N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.	Merck Sharp & Dohme Research Laboratories
16220969	219	Designed multiple ligands. An emerging drug discovery paradigm.	Organon Laboratories
15481976	17	Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.	Philipps-Universit£T Marburg
12190319	15	Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.	Astrazeneca Pharmaceuticals
11708932	7	An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.	Merck
11585444	295	From hit to lead. Analyzing structure-profile relationships.	Universities of Lille
10691681	17	Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.	Clinical Research Institute of Montr£Al
11052787	24	Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.	University of Pennsylvania
10090788	75	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
9784098	8	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
9703462	98	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
8648606	72	Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.	Cambridge University Forvie Site
8691440	22	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
8691422	25	2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.	Smithkline Beecham
7699709	22	Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.	Merck Sharp & Dohme Research Laboratories
8388471	28	Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs.	Institut De Recherches Servier
11266174	51	Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.	Novartis Institute For Medical Sciences
11591520	6	Discovery of novel, orally active dual NK1/NK2 antagonists.	Astrazeneca Pharmaceuticals
9871670	13	Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.	Pfizer
9871768	7	Asymmetric synthesis of Boc-N-methyl-p-benzoyl-phenylalanine. Preparation of a photoreactive antagonist of substance P.	Universit£
9871763	35	High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.	Merck Sharp Laboratory
	52	Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity	TBA
	66	Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds	TBA
	8	2,3-Substituted 2-azanorbornanes as polar -turn mimetics	TBA
	22	The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists	TBA
	1	Synthesis of RPR 100893, prototype of a new series of potent and selective non peptide NK1 antagonists : the triarylperhydroisoindolols.	TBA
	24	The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design	TBA
22189275	26	Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.	Takeda Pharmaceutical
21944973	31	Design, structure-activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor antagonists.	Takeda Pharmaceutical
21937153	46	Recent progress in synthesis and bioactivity studies of indolizines.	University of Botswana
21925887	10	Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.	University of Arizona
21807525	30	3-benzhydryl-4-piperidones as novel neurokinin-1 receptor antagonists and their efficient synthesis.	Takeda Pharmaceutical
21413804	21	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
21366266	66	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
21376585	120	Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.	Euroscreen
21292483	67	Identification of a new series of non-peptidic NK3 receptor antagonists.	H. Lundbeck
21229983	19	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
20850972	11	Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.	F. Hoffmann-La Roche
20846861	20	Discovery of a series of potent, orally activea,a-disubstituted piperidine NK(1) antagonists.	Merck Research Laboratories
20729082	59	Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.	Merck Research Laboratories
20813948	63	Spiroindolones, a potent compound class for the treatment of malaria.	Swiss Tropical and Public Health Institute
20617791	70	Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.	University of Arizona
20430616	36	Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.	F. Hoffmann-La Roche
20153964	44	Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.	Merck Research Laboratories
19963374	68	Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.	Pfizer
19762245	69	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
19817444	45	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
7517439	2	Spiroquinazoline, a Novel Substance P Inhibitor with a New Carbon Skeleton, Isolated from Aspergillus flavipes	TBA
7528269	2	1'-(2-Phenyl-ethylene)-ditryptophenaline, a New Dimeric Diketopiperazine from Aspergillus flavus	TBA
	9	Studies on the active conformation of the NK1 antagonist CGP 49823. Part 21. Fluoro-olefin analogs of tertiary amide rotamers.	TBA
	6	Studies on the active conformation of NK1 antagonist CGP 49823. Part 1. Synthesis of conformationally restricted analogs.	TBA
	10	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
	21	Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamides	TBA
	10	1,4-Benzodiazepin-2-one derived neurokinin-1 receptor antagonists	TBA
	11	Nonpeptide bradykinin antagonist analogs based on a model of a Sterling-Winthrop nonpeptide bradykinin antagonist overlapped with cyclic hexapeptide bradykinin antagonist peptides	TBA
	41	Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors	TBA
	18	SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 21. synthesis of CGP 49823	TBA
	8	The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptors	TBA
	48	SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist	TBA
	24	Linear amides as substance P antagonists	TBA
	17	1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channel	TBA
	13	Structure-activity studies of the natural product substance P antagonist win 64821	TBA
	17	Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitution	TBA
	15	Phenyl-glycinol based NK1 receptor antagonists — towards the minimum pharmacophore	TBA
	4	Spiro-piperidine non-peptide neurokinin-1 receptor antagonists	TBA
	17	4,4-Diphenyl-7-perhydrothiapyrano[3,4-c]pyrrolone, a new series of substance P receptors antagonists	TBA
	15	1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists	TBA
	12	Quinuclidine-based NK1 antagonists, the role of the benzhydryl	TBA
	6	N-alkyl quinuclidinium substance P antagonists	TBA
	11	2-Aryl-1-azabicyclo[2.2.2]octanes as novel nonpeptide substance P antagonists	TBA
	4	Perhydrothiopyranopyrroles derivatives : A novel series of potent and selective nonpeptide NK1 antagonists.	TBA
	7	The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanes	TBA
	3	Gem-disubstituted amino-ether based substance p antagonists	TBA
	6	Piperidine-ether based hNK1 antagonists 1: Determination of the relative and absolute stereochemical requirements	TBA
	9	Acyclic NK1 antagonists: Replacements for the benzhydryl group.	TBA
	6	Morpholine-based substance P antagonists: assessment of the 3-point binding model	TBA
	24	Acyclic NK-1 antagonists: 2-benzhydryl-2-aminoethyl ethers	TBA
	2	Articulating a pharmacophore driven synthetic strategy: Discovery of a potent substance P antagonist	TBA
	4	Quinuclidine based NK-1 antagonists 2: determination of the absolute stereochemical requirements	TBA
	17	Quinuclidine-based NK-1 antagonists I: 3-benzyloxy-1-azabicyclo[2.2.2]octanes	TBA
	5	Nuclear variations of quinuclidine substance P antagonists: 2-diphenylmethyl-1-azabicyclo[3.2.2]nonan-3-amines	TBA
	20	1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.	TBA
	2	Conformationally restricted analogs of CP-99,994: synthesis of a spirocyclic amine	TBA
	5	Preparation and radiolabelling of CP-96,345, the first non-peptide substance P antagonist	TBA
19354254	24	Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.	Merck Research Laboratories
18829330	1	Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.	The University of Tokyo
18821747	45	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
18640044	24	Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.	Pfizer
18640038	74	Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.	Amgen
18570365	29	The many roles for fluorine in medicinal chemistry.	Merck Research Laboratories
18554914	17	Design, synthesis, and structure-affinity relationship studies in NK1 receptor ligands based on azole-fused quinolinecarboxamide moieties.	Università
18547807	19	Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.	Schering-Plough Research Institute
17967540	3	Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist.	Pfizer
17919904	5	Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety.	Pfizer
17723300	55	Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.	Merck Research Laboratories
17637506	33	The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.	Merck
16950617	50	N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.	Merck Sharp & Dohme Research Laboratories
16884289	26	Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.	Merck Research Laboratories
16831551	31	Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.	Merck Research Laboratories
16824752	42	Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.	Merck Research Laboratories
16722655	28	Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.	Pfizer
16698264	37	Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.	Merck Research Laboratories
16682196	19	Cyclobutane derivatives as potent NK1 selective antagonists.	Schering-Plough Research Institute
16580201	4	Diarylacetylene piperidinyl amides as novel anxiolytics.	Johnson & Johnson Pharmaceutical Research and Development
16574413	28	NK1 antagonists based on seven membered lactam scaffolds.	Merck Sharp and Dohme Research Laboratories
16413782	20	1-Phenyl-8-azabicyclo[3.2.1]octane ethers: a novel series of neurokinin (NK1) antagonists.	Merck Sharp & Dohme Research Laboratories
16384700	24	Novel lactam NK1 antagonists with anti-emetic activity.	Merck Sharp & Dohme Research Laboratories
16332435	38	Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.	F. Hoffmann-La Roche
16307878	25	Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.	Merck Sharp & Dohme Research Laboratories
16290143	18	Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.	Schering-Plough Research Institute
16039119	35	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
14998319	22	A non-peptide NK1 receptor agonist showing subpicomolar affinity.	Università
14736234	11	Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.	Astrazeneca Pharmaceuticals
12723949	9	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
12372524	74	Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.	Schering-Plough Research Institute
12217362	10	Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.	Merck Sharp & Dohme Research Laboratories
12182850	19	Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.	Merck Sharp and Dohme Research Laboratories
12161132	102	Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.	Schering-Plough Research Institute
12127505	28	Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists.	Novartis Pharma
12067555	31	4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.	Merck Sharp & Dohme Research Laboratories
12067554	27	4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.	Merck Sharp & Dohme Research Laboratories
11859013	93	Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.	Schering-Plough Research Institute
11784148	81	Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.	Pharmazeutisches Institut Der UniversitäT Freiburg
11755340	94	Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.	Schering-Plough Research Institute
11714615	22	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
11714604	19	2-Aryl indole NK(1) antagonists: optimisation of the amide substituent.	Merck Sharp & Dohme Research Laboratories
11428921	9	Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.	Cambridge University Forvie Site
11425527	16	Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.	Eli Lilly
11354385	27	2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.	Merck Sharp and Dohme Research Laboratories
11354384	27	2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.	The Neuroscience Research Centre
11266164	3	Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994.	Laboratoire De Chimie ThéRapeutique Associé
11229755	66	Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.	Schering-Plough Research Institute
11087566	69	Multiple-conformation and protonation-state representation in 4D-QSAR: the neurokinin-1 receptor system.	Biographics Laboratory 3R
11055350	58	Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.	Schering-Plough Research Institute
11055349	19	The design and synthesis of novel NK1/NK2 dual antagonists.	Schering-Plough Research Institute
10888334	10	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
10794691	8	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
10737756	1	Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.	Merck Research Laboratories
10508446	12	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
9873524	37	L-tryptophan urea amides as NK1/NK2 dual antagonists.	Merck Research Laboratories
9873446	12	Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.	Merck Sharp and Dohme Research Laboratories
9873445	41	Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.	Merck Sharp and Dohme Research Laboratories
9871627	20	High affinity phenylglycinol-based NK1 receptor antagonists.	Merck Sharp and Dohme Research Laboratories
9804702	37	4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.	Merck Sharp and Dohme Research Laboratories
9804700	10	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
9554871	43	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
9191956	51	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
8709125	11	N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.	Merck Sharp and Dohme Research Laboratories
8627597	17	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
8576917	79	3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.	Eli Lilly
8393115	11	N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.	Merck Sharp and Dohme Research Laboratories
7731011	5	4,4-Disubstituted piperidines: a new class of NK1 antagonist.	Merck Sharp and Dohme Research Laboratories
7543579	46	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
7535362	39	Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.	Merck Sharp & Dohme Research Laboratories
7527861	3	Importance of parallel vectors and"hydrophobic collapse" of the aligned aromatic rings: discovery of a potent substance P antagonist.	Pfizer
7520943	16	Aza-tricyclic substance P antagonists.	Pfizer
7518522	12	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
7513763	92	Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.	Merck Sharp and Dohme Research Laboratories
7508512	21	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
7490729	62	Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.	Merck Sharp and Dohme Research Laboratories
1378901	18	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
1282570	6	Discovery of a potent substance P antagonist: recognition of the key molecular determinant.	Pfizer
23031230	5	Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases.	Universit?? Degli Studi Di Siena
23792961	10	Site-specific inhibitory mechanism for amyloid ß42 aggregation by catechol-type flavonoids targeting the Lys residues.	Kyoto University
26833890	18	Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.	Yogi Vemana University
26469307	7	Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.	University of Leipzig
17112725	3	Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.	Merck Research Laboratories
17064063	18	Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.	Abbott Laboratories
10891109	19	Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.	Palacky University
10406636	6	Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors.	Gilead Sciences