1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d] azepines as TRPV1 antagonists with improved properties

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 23, 2010, Pages 7142-7146

  Lebsack, Alec D ^a   Rech, Jason C ^a   Branstetter, Bryan J ^a   Hawryluk, Natalie A ^a   Merit, Jeffrey E ^a   Allison, Brett ^a   Rynberg, Raymond ^a   Buma, Johnathan ^a   Rizzolio, Michele ^a   Swanson, Nadia ^a   Ao, Hong ^a   Maher, Michael P ^a   Herrmann, Michelle ^a   Freedman, Jamie ^a   Scott, Brian P ^a   Luo, Lin ^a   Bhattacharya, Anindya ^a   Wang, Qi ^a   Chaplan, Sandra R ^a   Wickenden, Alan D ^a   Breitenbucher, J Guy ^a   more..

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Antagonists; Azepine; TRPV1

Indexed keywords

6,7,8,9 TETRAHYDRO 5H PYRIMIDO[4,5 D]AZEPINE DERIVATIVE; AZEPINE DERIVATIVE; ETHYLENEDIAMINE DERIVATIVE; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1 ANTAGONIST;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HYPERALGESIA; NONHUMAN; RAT; REACTION ANALYSIS; SPRAGUE DAWLEY RAT; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ANIMALS; AZEPINES; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; HYDROGEN-ION CONCENTRATION; HYPERALGESIA; RATS; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; TRPV CATION CHANNELS;

RATTUS;

EID: 78149284731     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.09.006     Document Type: Article

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