141 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
8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.
F. Hoffmann-La Roche
Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors.
F. Hoffmann-La Roche
Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach.
F. Hoffmann-La Roche
3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.
F. Hoffmann-La Roche
6-Alkoxy-5-aryl-3-pyridinecarboxamides, a new series of bioavailable cannabinoid receptor type 1 (CB1) antagonists including peripherally selective compounds.
F. Hoffmann-La Roche
Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists.
F. Hoffmann-La Roche
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
F. Hoffmann-La Roche
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
F. Hoffmann-La Roche
Highly potent and selective cannabinoid receptor 2 agonists: initial hit optimization of an adamantyl hit series identified from high-through-put screening.
F. Hoffmann-La Roche
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
F. Hoffmann-La Roche
Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile salt export pump (Bsep) by troglitazone and trogl
F. Hoffmann-La Roche
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
F. Hoffmann-La Roche
Support vector machines classification of hERG liabilities based on atom types.
F. Hoffmann-La Roche
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
F. Hoffmann-La Roche
Carnitine palmitoyltransferase (CPT) modulators: a medicinal chemistry perspective on 35 years of research.
F. Hoffmann-La Roche
Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012.
F. Hoffmann-La Roche
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
Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts.
F. Hoffmann-La Roche
Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system.
F. Hoffmann-La Roche
Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.
F. Hoffmann-La Roche
Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.
F. Hoffmann-La Roche
5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
F. Hoffmann-La Roche
Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.
F. Hoffmann-La Roche
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
F. Hoffmann-La Roche
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: part 2. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
F. Hoffmann-La Roche
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.
F. Hoffmann-La Roche
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.
F. Hoffmann-La Roche
4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.
F. Hoffmann-La Roche
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
F. Hoffmann-La Roche
Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors.
F. Hoffmann-La Roche
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
F. Hoffmann-La Roche
Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
F. Hoffmann-La Roche
Structure-based design of beta-lactamase inhibitors. 2. Synthesis and evaluation of bridged sulfactams and oxamazins.
F. Hoffmann-La Roche
Design, synthesis, and evaluation of 2 beta-alkenyl penam sulfone acids as inhibitors of beta-lactamases.
F. Hoffmann-La Roche
Design and synthesis of potent and highly selective thrombin inhibitors.
F. Hoffmann-La Roche
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.
F. Hoffmann-La Roche
Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphatase.
F. Hoffmann-La Roche
Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties.
F. Hoffmann-La Roche
Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773).
F. Hoffmann-La Roche
Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia& diabetes.
F. Hoffmann-La Roche
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
F. Hoffmann-La Roche
Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.
F. Hoffmann-La Roche
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.
F. Hoffmann-La Roche
Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold.
F. Hoffmann-La Roche
Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.
F. Hoffmann-La Roche
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.
F. Hoffmann-La Roche
Piperidinyl-nicotinamides as potent and selective somatostatin receptor subtype 5 antagonists.
F. Hoffmann-La Roche
Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.
F. Hoffmann-La Roche
Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.
F. Hoffmann-La Roche
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.
F. Hoffmann-La Roche
Imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines as potent and highly selective GABAA alpha5 inverse agonists with potential for the treatment of cognitive dysfunction.
F. Hoffmann-La Roche
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors.
F. Hoffmann-La Roche
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
F. Hoffmann-La Roche
Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of type-2 diabetes.
F. Hoffmann-La Roche
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
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.
F. Hoffmann-La Roche
Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
F. Hoffmann-La Roche
Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers.
F. Hoffmann-La Roche
Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.
F. Hoffmann-La Roche
Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.
F. Hoffmann-La Roche
Allosteric FBPase inhibitors gain 10(5) times in potency when simultaneously binding two neighboring AMP sites.
F. Hoffmann-La Roche
From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.
F. Hoffmann-La Roche
Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.
F. Hoffmann-La Roche
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1.
F. Hoffmann-La Roche
A new class of histamine H3 receptor antagonists derived from ligand based design.
F. Hoffmann-La Roche
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
F. Hoffmann-La Roche
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
F. Hoffmann-La Roche
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
F. Hoffmann-La Roche
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
F. Hoffmann-La Roche
Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.
F. Hoffmann-La Roche
Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.
F. Hoffmann-La Roche
Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists.
F. Hoffmann-La Roche
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
F. Hoffmann-La Roche
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
F. Hoffmann-La Roche
Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
F. Hoffmann-La Roche
Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.
F. Hoffmann-La Roche
Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.
F. Hoffmann-La Roche
Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor.
F. Hoffmann-La Roche
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
F. Hoffmann-La Roche
Novel and potent NPY5 receptor antagonists derived from virtual screening and iterative parallel chemistry design.
F. Hoffmann-La Roche
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
F. Hoffmann-La Roche
Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists.
F. Hoffmann-La Roche
1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.
F. Hoffmann-La Roche
Novel dihydrofolate reductase inhibitors. Structure-based versus diversity-based library design and high-throughput synthesis and screening.
F. Hoffmann-La Roche
4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
F. Hoffmann-La Roche
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
F. Hoffmann-La Roche
Synthesis of triazole-Tethered pyrrolidine libraries: novel ECE inhibitors.
F. Hoffmann-La Roche
Design of Potent and Druglike Nonphenolic Inhibitors for Catechol O-Methyltransferase Derived from a Fragment Screening Approach Targeting the S-Adenosyl-l-methionine Pocket.
F. Hoffmann-La Roche
Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist.
F. Hoffmann-La Roche
2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as potent and selective peptide deformylase inhibitors.
F. Hoffmann-La Roche
Stepwise Design of γ-Secretase Modulators with an Advanced Profile by Judicious Coordinated Structural Replacements and an Unconventional Phenyl Ring Bioisostere.
F. Hoffmann-La Roche
Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.
F. Hoffmann-La Roche
Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.
F. Hoffmann-La Roche
Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.
F. Hoffmann-La Roche
Piperidine-renin inhibitors compounds with improved physicochemical properties.
F. Hoffmann-La Roche
Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.
F. Hoffmann-La Roche
Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 ( SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA).
F. Hoffmann-La Roche
Structure-based design of beta-lactamase inhibitors. 1. Synthesis and evaluation of bridged monobactams.
F. Hoffmann-La Roche
Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase.
F. Hoffmann-La Roche
Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines.
F. Hoffmann-La Roche
Substituted 2-oxo-azepane derivatives are potent, orally active gamma-secretase inhibitors.
F. Hoffmann-La Roche
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.
F. Hoffmann-La Roche
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.
F. Hoffmann-La Roche
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
F. Hoffmann-La Roche
Discovery of a Novel Class of Survival Motor Neuron 2 Splicing Modifiers for the Treatment of Spinal Muscular Atrophy.
F. Hoffmann-La Roche
Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof
Shanghai Yingli Pharmaceutical
Compound having ERK kinase inhibitory activity and use thereof
Shanghai Haihe Pharmaceutical
3-substituted piperidine compounds for Cbl-b inhibition, and use thereof
Nurix Therapeutics
Functionalized pyrano[2,3-D]pyrimidin-7-one derivatives and methods for their preparation and use
The Texas A&M University System
β- and γ-diketones and γ-hydroxyketones as Wnt/β-catenin signaling pathway activators
Samumed
Heterocyclic-imidazole compounds, pharmaceutical compositions thereof, preparation method therefor and use thereof
Shanghai Huilun Life Science & Technology
PXD101 analogs with L-phenylglycine-containing branched cap as histone deacetylase inhibitors.
Shandong University
Synthesis and structure-activity relationship of the isoindolinyl benzisoxazolpiperidines as potent, selective, and orally active human dopamine D4 receptor antagonists.
Aventis Pharmaceuticals
Synthesis and structure-activity relationships of dehydroaltenusin derivatives as selective DNA polymerase alpha inhibitors.
Kyoto Prefectural University
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase.
Anadys Pharmaceuticals
Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood.
Wyeth Research
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.
Gsk
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.
Biocryst Pharmaceuticals
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design.
Biocryst Pharmaceuticals