115 articles for thisTarget
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4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures.
Daiichi Sankyo
Identification of a novel hormone sensitive lipase inhibitor with a reduced potential of reactive metabolites formation.
Daiichi Sankyo
Identification of a novel boronic acid as a potent, selective, and orally active hormone sensitive lipase inhibitor.
Daiichi Sankyo
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.
Daiichi Sankyo
Optimization of 3-aryl-3-ethoxypropanoic acids and discovery of the potent GPR40 agonist DS-1558.
Daiichi Sankyo
Absorption, elimination, and metabolism of CS-1036, a novela-amylase inhibitor in rats and monkeys, and the relationship between gastrointestinal distribution and suppression of glucose absorption.
Daiichi Sankyo
Discovery of DS-5272 as a promising candidate: A potent and orally active p53-MDM2 interaction inhibitor.
Daiichi Sankyo
Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P1 agonists.
Daiichi Sankyo
Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach.
Daiichi Sankyo
Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists.
Daiichi Sankyo
Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration.
Daiichi Sankyo
Synthesis and optimization of novel (3S,5R)-5-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)piperidine-3-carboxamides as orally active renin inhibitors.
Daiichi Sankyo
Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes.
Daiichi Sankyo
Lead optimization of 5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxyhexanamides to reduce a cardiac safety issue: discovery of DS-8108b, an orally active renin inhibitor.
Daiichi Sankyo
Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties.
Daiichi Sankyo
A novel, potent, and orally active VLA-4 antagonist with good aqueous solubility: trans-4-[1-[[2-(5-Fluoro-2-methylphenylamino)-7-fluoro-6-benzoxazolyl]acetyl]-(5S)-[methoxy(methyl)amino]methyl-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid.
Daiichi Sankyo
Identification of trans-4-[1-[[7-fluoro-2-(1-methyl-3-indolyl)-6-benzoxazolyl]acetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid as a potent, orally active VLA-4 antagonist.
Daiichi Sankyo
Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid: an orally active, selective very late antigen-4 antagonist.
Daiichi Sankyo
Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors.
Daiichi Sankyo
Design, synthesis and evaluation of novel zwitterionic compounds as PPARa/¿ dual agonists (1).
Daiichi Sankyo
Discovery of novel dihydroimidazothiazole derivatives as p53-MDM2 protein-protein interaction inhibitors: synthesis, biological evaluation and structure-activity relationships.
Daiichi Sankyo
Discovery and optimization of novel fatty acid transport protein 1 (FATP1) inhibitors.
Daiichi Sankyo
Design and optimization of novel (2S,4S,5S)-5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxy-2-isopropylhexanamides as renin inhibitors.
Daiichi Sankyo
Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPAR¿ modulators.
Daiichi Sankyo
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P3-sparing S1P1 agonists.
Daiichi Sankyo
Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.
Daiichi Sankyo
Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.
Daiichi Sankyo
Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
Daiichi Sankyo
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
Daiichi Sankyo
Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPAR¿ partial agonists.
Daiichi Sankyo
Orally active zwitterionic factor Xa inhibitors with long duration of action.
Daiichi Sankyo
Discovery of atrop fixed alkoxy-aminobenzhydrol derivatives: novel, highly potent and orally efficacious squalene synthase inhibitors.
Daiichi Sankyo
Discovery of imidazo[1,2-b]pyridazines as IKKß inhibitors. Part 3: exploration of effective compounds in arthritis models.
Daiichi Sankyo
Discovery of novel SCD1 inhibitors: 5-alkyl-4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4'-piperidine] analogs.
Daiichi Sankyo
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors.
Daiichi Sankyo
Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors.
Daiichi Sankyo
Discovery of imidazo[1,2-b]pyridazines as IKKß inhibitors. Part 2: improvement of potency in vitro and in vivo.
Daiichi Sankyo
Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1'-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-3,4-dihydrospiro[chromene-2,4'-piperidine] analogs.
Daiichi Sankyo
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.
Daiichi Sankyo
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.
Daiichi Sankyo
A prodrug approach towards the development of tricyclic-based FBPase inhibitors.
Daiichi Sankyo
Structure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors.
Daiichi Sankyo
Novel spiropiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 1'-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-5-(trifluoromethyl)-3,4-dihydrospiro[chromene-2,4'-piperidine].
Daiichi Sankyo
Novel benzoylpiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-ylethyl)amide and its plasma triglyceride-lowering effects in Zucker fatty rats.
Daiichi Sankyo
Synthesis, SAR, and X-ray structure of tricyclic compounds as potent FBPase inhibitors.
Daiichi Sankyo
Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide.
Daiichi Sankyo
Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part II: Identification of 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide and its biological evaluation.
Daiichi Sankyo
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.
Daiichi Sankyo
A novel and potent VLA-4 antagonist based on trans-4-substituted cyclohexanecarboxylic acid.
Daiichi Sankyo
Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist.
Daiichi Sankyo
Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors.
Daiichi Sankyo
Lead optimization of pyrido[2,3-d][1]benzazepin-6-one derivatives leading to the discovery of a potent, selective, and orally available human parathyroid hormone receptor 1 (hPTHR1) antagonist (DS69910557).
Daiichi Sankyo
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring.
Daiichi Sankyo
Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
Daiichi Sankyo
Discovery of 3-amino-4-{(3S)-3-[(2-ethoxyethoxy)methyl]piperidin-1-yl}thieno[2,3-b]pyridine-2-carboxamide (DS96432529): A potent and orally active bone anabolic agent.
Daiichi Sankyo
4-Pyridone-3-carboxylic acid as a benzoic acid bioisostere: Design, synthesis, and evaluation of EP300/CBP histone acetyltransferase inhibitors.
Daiichi Sankyo
Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition.
Daiichi Sankyo
A novel [5.2.1]bicyclic amine is a potent analgesic without µ opioid activity.
Daiichi Sankyo
Discovery of novel histone lysine methyltransferase G9a/GLP (EHMT2/1) inhibitors: Design, synthesis, and structure-activity relationships of 2,4-diamino-6-methylpyrimidines.
Daiichi Sankyo
Discovery of DS42450411 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4-aminopyrimidine derivatives.
Daiichi Sankyo
Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity.
Daiichi Sankyo
Structure-Activity Relationship Studies of 3- or 4-Pyridine Derivatives of DS-6930.
Daiichi Sankyo
Discovery of novel, potent, and orally bioavailable pyrido[2,3-d][1]benzazepin-6-one antagonists for parathyroid hormone receptor 1.
Daiichi Sankyo
Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A.
Daiichi Sankyo
Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold.
Daiichi Sankyo
Synthesis and biological evaluation of novel imidazol-1-ylacetic acid derivatives as non-brain penetrant bombesin receptor subtype-3 (BRS-3) agonists.
Daiichi Sankyo
Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity.
Daiichi Sankyo
Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity.
Daiichi Sankyo
Discovery of novel PTHR1 antagonists: Design, synthesis, and structure activity relationships.
Daiichi Sankyo
Discovery of novel pyridazine derivatives as glucose transporter type 4 (GLUT4) translocation activators.
Daiichi Sankyo
Discovery of a Potent, Selective, and Orally Available MTHFD2 Inhibitor (DS18561882) with in Vivo Antitumor Activity.
Daiichi Sankyo
Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.
Daiichi Sankyo
Lead optimization of novel p53-MDM2 interaction inhibitors possessing dihydroimidazothiazole scaffold.
Daiichi Sankyo
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
Daiichi Sankyo
Potent in vitro activity of tomopenem (CS-023) against methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa.
Daiichi Sankyo
Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity.
Daiichi Sankyo
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of cyclin D1-CDK4: synthesis, biological evaluation and structure-activity relationships. Part 2.
Daiichi Sankyo
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
Daiichi Sankyo
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: synthesis, biological evaluation, and structure-activity relationships.
Daiichi Sankyo
Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
Daiichi Sankyo
Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
Daiichi Sankyo
Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).
Daiichi Sankyo
Design, synthesis, and pharmacological evaluation of a novel series of hormone sensitive lipase inhibitor.
Daiichi Sankyo
Tricyclic compounds as glycogen synthase kinase 3 (GSK3) inhibitors and uses thereof
The Broad Institute
Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase
University Of Texas
Pyrazolopyridine derivative having GLP-1 receptor agonist effect
Chugai Seiyaku Kabushiki Kaisha
Two amino acid residues confer different binding affinities of Abelson family kinase SRC homology 2 domains for phosphorylated cortactin.
Yale University
Pyrazolopyridine, pyrarolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo.
Eli Lilly
Selective alpha-2 adrenoceptor blockade by SK&F 86466: in vitro characterization of receptor selectivity.
Smith Kline & French Laboratories
Evidence for two types of binding of 3H-gaba and 3H-muscimol in rat cerebral cortex and cerebellum.
TBA
Disruption of protein-membrane binding and identification of small-molecule inhibitors of coagulation factor VIII.
University of Washington
Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation.
University of Marburg