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Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.

Merck Research Laboratories
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.

Merck Research Laboratories
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.

Merck Research Laboratories
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.

Merck Research Laboratories
Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).

Merck Research Laboratories
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.

Merck Research Laboratories
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.

Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.

Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.

Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.

Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.

Merck Research Laboratories
Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.

TBA
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.

Merck Research Laboratories
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.

Merck Research Laboratories
2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Merck Research Laboratories
Proline bis-amides as potent dual orexin receptor antagonists.

Merck Research Laboratories
A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.

Merck Research Laboratories
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Merck Research Laboratories
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.

Merck Research Laboratories
Indazole derivatives as novel bradykinin B1 receptor antagonists.

Merck Research Laboratories
Pyridyl amides as potent inhibitors of T-type calcium channels.

Merck Research Laboratories
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.

Merck Research Laboratories
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

Merck Research Laboratories
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.

Merck Research Laboratories
Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.

Merck
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.

Merck Research Laboratories
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.

Merck Research Laboratories
Design, synthesis, and optimization of novel PD-L1 inhibitors and the identification of a highly potent and orally bioavailable PD-L1 inhibitor.

Chulalongkorn University
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.

Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.

Merck Research Laboratories
Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.

Merck
Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.

Merck
Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.

Merck Research Laboratories
5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.

Merck Research Laboratories
Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.

TBA
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.

Merck Research Laboratories
Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.

Merck
2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.

Merck Research Laboratories
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.

Merck Research Laboratories
2,3-diaminopyridine bradykinin B1 receptor antagonists.

Merck Research Laboratories
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.

Merck Research Laboratories
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.

Merck Research Laboratories
Compounds and methods for the treatment of cancer

University of Illinois
CGRP receptor antagonists

Heptares Therapeutics
1,2,5,6-tetra-O-benzyl-D-mannitol derivatives as novel HIV protease inhibitors.

Pharmacor