Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 7, 2014, Pages 1784-1789

  Kuduk, Scott D ^a   Skudlarek, Jason W ^a   Di Marco, Christina N ^a   Bruno, Joseph G ^a   Pausch, Mark A ^a   O'Brien, Julie A ^a   Cabalu, Tamara D ^a   Stevens, Joanne ^a   Brunner, Joseph ^a   Tannenbaum, Pamela L ^a   Gotter, Anthony L ^a   Winrow, Christopher J ^a   Renger, John J ^a   Coleman, Paul J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Antagonist; Insomnia; Orexin

Indexed keywords

ACETYLENE DERIVATIVE; ALKYNE DERIVATIVE; FILOREXANT; OREXIN RECEPTOR; ACETYLENE; CARBON; G PROTEIN COUPLED RECEPTOR; OREXIN 1 RECEPTOR; OREXIN 2 RECEPTOR; SUVOREXANT; (5-((5-FLUOROPYRIDIN-2-YLOXY)METHYL)-2-METHYLPIPERIDIN-1-YL)(5-METHYL-2-(PYRIMIDIN-2-YL)PHENYL)METHANONE; CD200R1 PROTEIN, MOUSE; HCRTR1 PROTEIN, MOUSE; PIPERIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; CHEMICAL MODIFICATION; CONTROLLED STUDY; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; ELECTROENCEPHALOGRAM; ELECTROENCEPHALOGRAPHY; ELECTROMYOGRAM; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; MOUSE; NONHUMAN; SLEEP; STRUCTURE ACTIVITY RELATION; WILD TYPE; ALKYNYLATION; ANIMAL MODEL; HUMAN; HUMAN CELL; LINKAGE ANALYSIS; PHARMACODYNAMICS; REACTION ANALYSIS; SLEEP STAGE; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DEFICIENCY; DOSE RESPONSE; KNOCKOUT MOUSE; METABOLISM; SYNTHESIS;

ACETYLENE; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; MICE; MICE, KNOCKOUT; MOLECULAR STRUCTURE; OREXIN RECEPTORS; PIPERIDINES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84897392830     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.02.026     Document Type: Article

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