Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 23, 2010, Pages 7137-7141

  Hawryluk, Natalie A ^a   Merit, Jeffrey E ^a   Lebsack, Alec D ^a   Branstetter, Bryan J ^a   Hack, Michael D ^a   Swanson, Nadia ^a   Ao, Hong ^a   Maher, Michael P ^a   Bhattacharya, Anindya ^a   Wang, Qi ^a   Freedman, Jamie M ^a   Scott, Brian P ^a   Wickenden, Alan D ^a   Chaplan, Sandra R ^a   Breitenbucher, J Guy ^a  

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

Author keywords

Tetrahydro pyrimdoazepine; TRPV1; Vanilloid

Indexed keywords

3 TRIFLUOROMETHYLPYRIDINE; 4 [3 (TRIFLUOROMETHYL) 2 PYRIDINYL] N [5 (TRIFLUOROMETHYL) 2 PYRIDINYL] 1 PIPERAZINECARBOXAMIDE; 6,7,8,9 TETRAHYDRO 5H PYRIMIDO[4,5 D]AZEPINE DERIVATIVE; ANALGESIC AGENT; AZEPINE DERIVATIVE; CAPSAICIN; CARRAGEENAN; PIPERAZINE DERIVATIVE; PYRIDINE DERIVATIVE; UNCLASSIFIED DRUG; UREA DERIVATIVE; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 1 ANTAGONIST;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HYPERALGESIA; IC 50; MAXIMUM PLASMA CONCENTRATION; MOLECULAR MODEL; NONHUMAN; RAT; RECEPTOR BLOCKING; STRUCTURE ACTIVITY RELATION;

ANIMALS; AZEPINES; DRUG DISCOVERY; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TRPV CATION CHANNELS;

EID: 78149284010     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.09.023     Document Type: Article

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