204 articles for thisTarget
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Article Title
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Isolation and structure of SCH 351633: a novel hepatitis C virus (HCV) NS3 protease inhibitor from the fungus Penicillium griseofulvum.
Schering-Plough Research Institute
HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein.
Schering-Plough Research Institute
Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.
Schering-Plough Research Institute
The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein.
Schering-Plough Research Institute
Cholesterol interaction with the daunorubicin binding site of P-glycoprotein.
Schering-Plough Research Institute
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
Schering-Plough Research Institute
Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein.
Schering-Plough Research Institute
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
Schering-Plough Research Institute
Interaction of common azole antifungals with P glycoprotein.
Schering-Plough Research Institute
Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists.
Schering-Plough Research Institute
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
Schering-Plough Research Institute
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.
Schering-Plough Research Institute
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Schering-Plough Research Institute
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.
Schering-Plough Research Institute
Discovery of novel orally active ureido NPY Y5 receptor antagonists.
Schering-Plough Research Institute
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.
Schering-Plough Research Institute
Novel steroidal saponins, Sch 725737 and Sch 725739, from a marine starfish, Novodinia antillensis.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Schering-Plough Research Institute
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
Schering-Plough Research Institute
Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design.
Schering-Plough Research Institute
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.
Schering-Plough Research Institute
Condensed aromatic peptide family of microbial metabolites, inhibitors of CD28-CD80 interactions.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
Schering-Plough Research Institute
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious¿-secretase modulators in vivo.
Schering-Plough Research Institute
Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Schering-Plough Research Institute
Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists.
Schering-Plough Research Institute
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.
Schering-Plough Research Institute
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
Schering-Plough Research Institute
New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.
Schering-Plough Research Institute
Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists.
Schering-Plough Research Institute
Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.
Schering-Plough Research Institute
Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists.
Schering-Plough Research Institute
Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
Schering-Plough Research Institute
The discovery of azepane sulfonamides as potent 11beta-HSD1 inhibitors.
Schering-Plough Research Institute
Discovery of orally active 3-pyridinyl-tropane as a potent nociceptin receptor agonist for the management of cough.
Schering-Plough Research Institute
Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors.
Schering-Plough Research Institute
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Schering-Plough Research Institute
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.
Schering-Plough Research Institute
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
Schering-Plough Research Institute
Spiro-piperidine azetidinones as potent TRPV1 antagonists.
Schering-Plough Research Institute
Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines.
Schering-Plough Research Institute
Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough.
Schering-Plough Research Institute
Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.
Schering-Plough Research Institute
Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists.
Schering-Plough Research Institute
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
Schering-Plough Research Institute
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.
Schering-Plough Research Institute
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Schering-Plough Research Institute
Chemokine receptor CCR-5 inhibitors produced by Chaetomium globosum.
Schering-Plough Research Institute
Isolation and structure elucidation of Sch 642305, a novel bacterial DNA primase inhibitor produced by Penicillium verrucosum.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.
Schering-Plough Research Institute
3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.
Schering-Plough Research Institute
Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.
Schering-Plough Research Institute
Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Schering-Plough Research Institute
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.
Schering-Plough Research Institute
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Schering-Plough Research Institute
Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists.
Schering-Plough Research Institute
Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.
Schering-Plough Research Institute
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Schering-Plough Research Institute
Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists.
Schering-Plough Research Institute
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.
Schering-Plough Research Institute
SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: taming hERG.
Schering-Plough Research Institute
Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.
Schering-Plough Research Institute
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.
Schering-Plough Research Institute
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
Schering-Plough Research Institute
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.
Schering-Plough Research Institute
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists.
Schering-Plough Research Institute
Metabolism-based identification of a potent thrombin receptor antagonist.
Schering-Plough Research Institute
Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.
Schering-Plough Research Institute
Himbacine derived thrombin receptor (PAR-1) antagonists: structure-activity relationship of the lactone ring.
Schering-Plough Research Institute
Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.
Schering-Plough Research Institute
Modification of the clozapine structure by parallel synthesis.
Schering-Plough Research Institute
Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.
Schering-Plough Research Institute
P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease.
Schering-Plough Research Institute
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists.
Schering-Plough Research Institute
Cyclobutane derivatives as potent NK1 selective antagonists.
Schering-Plough Research Institute
Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas.
Schering-Plough Research Institute
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.
Schering-Plough Research Institute
Enhanced FTase activity achieved via piperazine interaction with catalytic zinc.
Schering-Plough Research Institute
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
Schering-Plough Research Institute
Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists.
Schering-Plough Research Institute
Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease.
Schering-Plough Research Institute
Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents.
Schering-Plough Research Institute
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
Schering-Plough Research Institute
Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease.
Schering-Plough Research Institute
Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.
Schering-Plough Research Institute
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1.
Schering-Plough Research Institute
The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: antagonists versus agonists.
Schering-Plough Research Institute
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Schering-Plough Research Institute
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
Schering-Plough Research Institute
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.
Schering-Plough Research Institute
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.
Schering-Plough Research Institute
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Schering-Plough Research Institute
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.
Schering-Plough Research Institute
Three new compounds from the plant Lippia alva as inhibitors of chemokine receptor 5 (CCR5).
Schering-Plough Research Institute
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.
Schering-Plough Research Institute
Non-peptidic small-molecule inhibitors of the single-chain hepatitis C virus NS3 protease/NS4A cofactor complex discovered by structure-based NMR screening.
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagoni
Schering-Plough Research Institute
Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists.
Schering-Plough Research Institute
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.
Schering-Plough Research Institute
Application of the lambda-dynamics method to evaluate the relative binding free energies of inhibitors to HCV protease.
Schering-Plough Research Institute
Two antiviral compounds from the plant Stylogne cauliflora as inhibitors of HCV NS3 protease.
Schering-Plough Research Institute
A new sterol sulfate, Sch 572423, from a marine sponge, Topsentia sp.
Schering-Plough Research Institute
Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist.
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.
Schering-Plough Research Institute
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
Schering-Plough Research Institute
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.
Schering-Plough Research Institute
Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5.
Schering-Plough Research Institute
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.
Schering-Plough Research Institute
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors.
Schering-Plough Research Institute
Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase.
Schering-Plough Research Institute
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.
Schering-Plough Research Institute
Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.
Schering-Plough Research Institute
Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists.
Schering-Plough Research Institute
Azapeptides as inhibitors of the hepatitis C virus NS3 serine protease.
Schering-Plough Research Institute
Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family.
Schering-Plough Research Institute
Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.
Schering-Plough Research Institute
Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.
Schering-Plough Research Institute
Potent, low molecular weight thrombin receptor antagonists.
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.
Schering-Plough Research Institute
Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
Schering-Plough Research Institute
Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.
Schering-Plough Research Institute
Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.
Schering-Plough Research Institute
Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.
Schering-Plough Research Institute
Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.
Schering-Plough Research Institute
Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.
Schering-Plough Research Institute
The design and synthesis of novel NK1/NK2 dual antagonists.
Schering-Plough Research Institute
Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.
Schering-Plough Research Institute
Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.
Schering-Plough Research Institute
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.
Schering-Plough Research Institute
Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.
Schering-Plough Research Institute
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Schering-Plough Research Institute
Analogs of 4-(3-bromo-8-methyl-10-methoxy-6,11-dihydro-5H-benzo[5,6]-cyclo hepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N-oxide as inhibitors of farnesyl protein transferase.
Schering-Plough Research Institute
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.
Schering-Plough Research Institute
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.
Schering-Plough Research Institute
Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors.
Schering-Plough Research Institute
Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.
Schering-Plough Research Institute
Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.
Schering-Plough Research Institute
4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor.
Schering-Plough Research Institute
Novel H3 receptor antagonists. Sulfonamide homologs of histamine.
Schering-Plough Research Institute
A depsipeptide fungal metabolite inhibitor of cholesteryl ester transfer protein.
Schering-Plough Research Institute
Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.
Schering-Plough Research Institute
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand.
Schering-Plough Research Institute
Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.
Schering-Plough Research Institute
Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine.
Schering-Plough Research Institute
Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors.
Schering-Plough Research Institute
Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compounds.
Schering-Plough Research Institute
Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods.
Schering-Plough Research Institute
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.
Schering-Plough Research Institute
Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies.
Schering-Plough Research Institute
Synthesis and phosphodiesterase activity of carboxylic acid mimetics of cyclic guanosine 3',5'-monophosphate.
Schering-Plough Research Institute
Mercaptoacyl amino acid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives.
Schering-Plough Research Institute
2-Azetidinones as inhibitors of cholesterol absorption.
Schering-Plough Research Institute
Substituted (1,2-diarylethyl)amide acyl-CoA:cholesterol acyltransferase inhibitors: effect of polar groups on in vitro and in vivo activity.
Schering-Plough Research Institute
A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist.
Schering-Plough Research Institute
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.
Schering-Plough Research Institute
Tetrahydroquinoline sulfonamides as gamma-secretase inhibitors.
Schering-Plough Research Institute
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Schering-Plough Research Institute
A new antitumor compound from the plant Oryctanthus sp. as a VEGF receptor binding inhibitor.
Schering-Plough Research Institute
Carboxyalkyl dipeptides with atrial natriuretic factor potentiating and antihypertensive activity.
Schering-Plough Research Institute
Small peptide inhibitors of smooth muscle myosin light chain kinase.
Schering-Plough Research Institute
Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
Forma Therapeutics
Fused heterocyclic or carbocyclic compounds carrying a substituted cycloaliphatic radical and use thereof for treating vasopressin-related diseases
Abbvie Deutschland
N-aralkylcarbonyl-piperazine and -homopiperazine compounds and personal care compositions comprising the same
Conopco
Quinolone derivatives as fibroblast growth factor receptor inhibitors
Principia Biopharma
Substituted indazole derivatives active as kinase inhibitiors
Nerviano Medical Sciences
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis
Imidazolin-5-one derivative useful as FASN inhibitors for the treatment of cancer
Janssen Pharmaceutica
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.
Vanderbilt University
Rigid duplex alpha-cyclodextrin reversibly connected with disulfide bonds. Synthesis and inclusion complexes.
Institute of Organic Chemistry and Biochemistry As Cr
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
Pfizer
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Takeda Pharmaceutical
Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.
Novartis
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.
University of Bologna
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.
Shanghai Institute of Materia Medica
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.
Eli Lilly
Nonpeptidic potent HIV-1 protease inhibitors: (4-hydroxy-6-phenyl-2-oxo-2H- pyran-3-yl)thiomethanes that span P1-P2' subsites in a unique mode of active site binding.
Parke-Davis Pharmaceutical Research
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant.
Sapienza University of Rome
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.
Sapienza University of Rome
5H-pyrrolo[1,2-b] [1,2,5]benzothiadiazepines (PBTDs): a novel class of non-nucleoside reverse transcriptase inhibitors.
Sapienza University of Rome