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 |
10206553 |
55 |
Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues. |
Sankyo |
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 |
28105278 |
10 |
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds. |
Mossakowski Medical Research Centre Polish Academy of Sciences |
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 |
23735006 |
17 |
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 |
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 |
7678430 |
23 |
Cyclic peptides as selective tachykinin antagonists. |
Merck Sharp and Dohme Research Laboratories |
11755367 |
38 |
First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants. |
Ucb Pharma |
| 6 |
Peptide azoles: A new class of biologically-active dipeptide mmetics. |
TBA |
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 |
10543877 |
25 |
Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides. |
Uppsala University |
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 |
7518002 |
38 |
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 |
7515443 |
79 |
Design and synthesis of side-chain conformationally restricted phenylalanines and their use for structure-activity studies on tachykinin NK-1 receptor. |
Universit£ |
7693945 |
6 |
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 |
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 |
1331460 |
54 |
Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. |
Glaxo Group Research |
1370695 |
27 |
Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles. |
Rochester |
1375965 |
47 |
Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists. |
Fujisawa Pharmaceutical |
1851847 |
22 |
Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists. |
Rochester |
2441057 |
22 |
Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors. |
TBA |
12127519 |
40 |
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 |
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 |
9873386 |
15 |
Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines. |
Yamanouchi Pharmaceutical |
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 |
| 31 |
An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345. |
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 |
20178322 |
22 |
Discovery of dipeptides with high affinity to the specific binding site for substance P1-7. |
Uppsala University |
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 |
| 14 |
3-Benzyloxy-2-phenylpiperidine NK1 antagonists: the influence of alpha methyl substitution |
TBA |
| 76 |
Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H1/NK1 receptor antagonist activity |
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 |
| 42 |
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists |
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 |
| 13 |
Alternative strategies towards the identification of chemical lead compounds by rational design |
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 |
| 23 |
Methionine replacements in biologically active peptides |
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 |
| 6 |
Application of the multipin peptide synthesis technique for peptide receptor binding studies: Substance P as A model system |
TBA |
| 1 |
A facile synthesis of the novel Neurokinin A antagonist SR 48968 |
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 |
| 1 |
Synthesis of RP-67,580, a new potent nonpeptide substance P antagonist |
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 |
18067242 |
6 |
Conformational comparisons of a series of tachykinin peptide analogs. |
Mississippi State University |
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 |
10937720 |
24 |
Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues. |
Sankyo |
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 |
31199640 |
50 |
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models. |
Astrazeneca |
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 |
31082225 |
26 |
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms. |
China Pharmaceutical University |
8759639 |
33 |
Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P. |
Hebrew University of Jerusalem |
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 |
26465170 |
87 |
Discovery of Novel Multifunctional Ligands with ?/? Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain. |
University of Arizona |
26212775 |
77 |
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities. |
University of Arizona |
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 |
7689652 |
6 |
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 |
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 |
15615542 |
52 |
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 |
8544174 |
19 |
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 |
7562907 |
33 |
New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists. |
Glaxo Wellcome Medicines Research Centre |
28710964 |
4 |
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 |
2433445 |
4 |
[pGlu6,Pro9]SP6-11, a selective agonist for the substance P P-receptor subtype. |
TBA |
2433443 |
9 |
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 |
29057060 |
100 |
Discovery of VU6005649, a CNS Penetrant mGlu |
Vanderbilt University |
29929882 |
7 |
An imidazole based H-Phe-Phe-NH |
Uppsala University |
1714957 |
12 |
Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity. |
Hebrew University of Jerusalem |
1694545 |
28 |
Potent and highly selective neurokinin antagonists. |
Glaxo Group Research |
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 |
1373191 |
15 |
Synthesis and substance P antagonist activity of naphthimidazolium derivatives. |
Rochester |
1282570 |
6 |
Discovery of a potent substance P antagonist: recognition of the key molecular determinant. |
Pfizer |
15831442 |
46 |
Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke. |
Taisho Pharmaceutical |
15131245 |
86 |
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization. |
Sanofi-Synthelabo Recherche |
12721338 |
61 |
N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties. |
Pudue Pharma Discovery Research |
12438541 |
27 |
SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization. |
Sanofi-SynthÉLabo Recherche |
12431845 |
84 |
Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder. |
Eli Lilly |
12206858 |
11 |
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist. |
Schering-Plough Research Institute |
11750183 |
29 |
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. |
Novartis Pharma |
11750180 |
139 |
Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. |
Eli Lilly |
11438309 |
51 |
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. |
Janssen Research Foundation |
11408556 |
2 |
Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors. |
Astrazeneca Pharmaceuticals |
11082453 |
77 |
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse. |
Abbott Laboratories |
9454810 |
72 |
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. |
Sanofi Recherche |
9225287 |
174 |
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. |
Roche Bioscience |
9190866 |
26 |
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist. |
Smithkline Beecham Pharmaceuticals |
8887981 |
72 |
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand. |
Abbott Laboratories |
8627566 |
53 |
In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist. |
Hoechst Marion Roussel |
8012715 |
38 |
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. |
Glaxo Group Research |
7830490 |
21 |
SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor. |
Sanofi Recherche |
7562491 |
10 |
Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity. |
Zeneca Pharmaceuticals |
7518514 |
46 |
(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization. |
Abbott Laboratories |
17516639 |
29 |
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. |
University of Arizona Tucson |
18266313 |
30 |
A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists. |
University of Arizona Tucson |