99 articles for thisTarget
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Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
Merck Frosst Centre For Therapeutic Research
Design and synthesis of potent, isoxazole-containing renin inhibitors.
Merck Frosst Centre For Therapeutic Research
Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor.
Merck Frosst Centre For Therapeutic Research
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Merck Frosst Centre For Therapeutic Research
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.
Merck Frosst Centre For Therapeutic Research
Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.
Merck Frosst Centre For Therapeutic Research
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Comparison between two classes of selective EP(3) antagonists and their biological activities.
Merck Frosst Centre For Therapeutic Research
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Merck Frosst Centre For Therapeutic Research
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
Merck Frosst Centre For Therapeutic Research
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.
Merck Frosst Centre For Therapeutic Research
Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability.
Merck Frosst Centre For Therapeutic Research
Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (+-)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3- (dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic
Merck Frosst Centre For Therapeutic Research
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.
Merck Frosst Centre For Therapeutic Research
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Merck Frosst Centre For Therapeutic Research
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
Merck Frosst Centre For Therapeutic Research
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
Merck Frosst Centre For Therapeutic Research
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
Merck Frosst Centre For Therapeutic Research
Nicotinic acids: liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy.
Merck Frosst Centre For Therapeutic Research
Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series.
Merck Frosst Centre For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.
Merck Frosst Centre For Therapeutic Research
Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.
Merck Frosst Centre For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.
Merck Frosst Centre For Therapeutic Research
Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors.
Merck Frosst Centre For Therapeutic Research
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Merck Frosst Centre For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Merck Frosst Centre For Therapeutic Research
The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.
Merck Frosst Centre For Therapeutic Research
The discovery and synthesis of potent zwitterionic inhibitors of renin.
Merck Frosst Centre For Therapeutic Research
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor.
Merck Frosst Centre For Therapeutic Research
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Merck Frosst Centre For Therapeutic Research
The identification of substituted benzothiophene derivatives as PGE(2) subtype 4 receptor antagonists: From acid to non-acid.
Merck Frosst Centre For Therapeutic Research
Azaindoles as potent CRTH2 receptor antagonists.
Merck Frosst Centre For Therapeutic Research
Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: discovery of MK-5286.
Merck Frosst Centre For Therapeutic Research
Potent and highly selective DP1 antagonists with 2,3,4,9-tetrahydro-1H-carbazole as pharmacophore.
Merck Frosst Centre For Therapeutic Research
2-Aryl benzimidazoles: human SCD1-specific stearoyl coenzyme-A desaturase inhibitors.
Merck Frosst Centre For Therapeutic Research
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.
Merck Frosst Centre For Therapeutic Research
Addressing time-dependent CYP 3A4 inhibition observed in a novel series of substituted amino propanamide renin inhibitors, a case study.
Merck Frosst Centre For Therapeutic Research
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.
Merck Frosst Centre For Therapeutic Research
SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Merck Frosst Centre For Therapeutic Research
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Merck Frosst Centre For Therapeutic Research
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Merck Frosst Centre For Therapeutic Research
Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
Merck Frosst Centre For Therapeutic Research
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
Merck Frosst Centre For Therapeutic Research
Thiazole analog as stearoyl-CoA desaturase 1 inhibitor.
Merck Frosst Centre For Therapeutic Research
Discovery of potent and selective DP1 receptor antagonists in the azaindole series.
Merck Frosst Centre For Therapeutic Research
Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors.
Merck Frosst Centre For Therapeutic Research
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
Merck Frosst Centre For Therapeutic Research
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
Merck Frosst Centre For Therapeutic Research
Primary amides as selective inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.
Merck Frosst Centre For Therapeutic Research
Substituted coumarins as potent 5-lipoxygenase inhibitors.
Merck Frosst Centre For Therapeutic Research
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.
Merck Frosst Centre For Therapeutic Research
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Merck Frosst Centre For Therapeutic Research
2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Merck Frosst Centre For Therapeutic Research
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.
Merck Frosst Centre For Therapeutic Research
Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis.
Merck Frosst Centre For Therapeutic Research
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Merck Frosst Centre For Therapeutic Research
The development of potent non-peptidic PTP-1B inhibitors.
Merck Frosst Centre For Therapeutic Research
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
Merck Frosst Centre For Therapeutic Research
Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.
Merck Frosst Centre For Therapeutic Research
Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.
Merck Frosst Centre For Therapeutic Research
Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.
Merck Frosst Centre For Therapeutic Research
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
Merck Frosst Centre For Therapeutic Research
Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors.
Merck Frosst Centre For Therapeutic Research
Pyridazinones as selective cyclooxygenase-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile.
Merck Frosst Centre For Therapeutic Research
Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor.
Merck Frosst Centre For Therapeutic Research
In vitro metabolism considerations, including activity testing of metabolites, in the discovery and selection of the COX-2 inhibitor etoricoxib (MK-0663).
Merck Frosst Centre For Therapeutic Research
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.
Merck Frosst Centre For Therapeutic Research
Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).
Merck Frosst Centre For Therapeutic Research
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Merck Frosst Centre For Therapeutic Research
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.
Merck Frosst Centre For Therapeutic Research
SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor.
Merck Frosst Centre For Therapeutic Research
2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
Substituted furans as inhibitors of the PDE4 enzyme.
Merck Frosst Centre For Therapeutic Research
Substituted heterocyclic analogs as selective COX-2 inhibitors in the flosulide class.
Merck Frosst Centre For Therapeutic Research
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.
Merck Frosst Centre For Therapeutic Research
Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530.
Merck Frosst Centre For Therapeutic Research
Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives.
Merck Frosst Centre For Therapeutic Research
Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816.
Merck Frosst Centre For Therapeutic Research
Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5 -dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic acid.
Merck Frosst Centre For Therapeutic Research
Naphthalenic lignan lactones as selective, nonredox 5-lipoxygenase inhibitors. Synthesis and biological activity of (methoxyalkyl)thiazole and methoxytetrahydropyran hybrids.
Merck Frosst Centre For Therapeutic Research
Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.
Merck Frosst Centre For Therapeutic Research
Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl] [[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist.
Merck Frosst Centre For Therapeutic Research
Development of 2,3-dihydro-6-(3-phenoxypropyl)-2-(2-phenylethyl)-5-benzofuranol (L-670,630) as a potent and orally active inhibitor of 5-lipoxygenase.
Merck Frosst Centre For Therapeutic Research
Substituted indazole derivatives active as kinase inhibitiors
Nerviano Medical Sciences
Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).
Amgen
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
Universitat De Barcelona
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.
Astrazeneca