Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists

Journal of Medicinal Chemistry

Volumn 51, Issue 9, 2008, Pages 2744-2757

  Tamayo, Nuria ^a   Liao, Hongyu ^a   Stec, Markian M ^a   Wang, Xianghong ^a   Chakrabarti, Partha ^a   Retz, Dan ^a   Doherty, Elizabeth M ^a   Surapaneni, Sekhar ^a   Tamir, Rami ^a   Bannon, Anthony W ^a   Gavva, Narender R ^a   Norman, Mark H ^a  

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [2 [6 (2 ACETAMIDOBENZO[D]THIAZOL 4 YLOXY)PYRIMIDIN 4 YL] 5 (TRIFLUOROMETHYL)PHENYL] 3 TERT BUTYLUREA; 1 [2 [6 (3 AMINO 2 OXO 1,2 DIHYDROQUINOXALIN 5 YLOXY)PYRIMIDIN 4 YL] 5 (TRIFLUOROMETHYL)PHENYL] 3 TERT BUTYLUREA; 3 [6 (3 AMINO 2 OXO 1,2 DIHYDROQUINOXALIN 5 YLOXY) 2 (1 METHOXYPROPAN 2 YLAMINO)PYRIMIDIN 4 YL] 6 (TRIFLUOROMETHYL)PYRIDIN 2 AMINIUM TRIFLUOROACETATE; 3 AMINO 5 [2 (1 METHOXYPROPAN 2 YLAMINO) 6 [4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [2 (2 METHOXYETHYLAMINO) 6 [4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [2 [(1 NEOPENTYLPIPERIDIN 2 YL)METHYLAMINOAMINO] 6 [4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE TRIFLUOROACETATE; 3 AMINO 5 [2 [1 (PYRIDIN 2 YL)ETHYLAMINO] 6 [4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [2 AMINO 6 [2 AMINO 4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 (2 METHOXYETHYLAMINO) 6 (TRIFLUOROMETHYL)PYRIDIN 3 YL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 (2 MORPHOLINOETHYLAMINO) 6 (TRIFLUOROMETHYL)PYRIDIN 3 YL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 (TETRAHYDROFURAN 3 YLAMINO) 6 (TRIFLUOROMETHYL)PYRIDIN 3 YL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 [(1 ISOBUTYLPIPERIDIN 2 YL)METHYLAMINO] 6 (TRIFLUOROMETHYL)PYRIDIN 3 YL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 AMINO 4 (TRIFLUOROMETHYL)PHENYL] 2 (1 METHOXYPROPAN 2 YLAMINO)PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 AMINO 4 (TRIFLUOROMETHYL)PHENYL] 2 (2 METHOXYETHYLAMINO)PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 AMINO 4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 3 AMINO 5 [6 [2 AMINO 6 (TRIFLUOROMETHYL)PYRIDIN 3 YL]PYRIMIDIN 4 YLOXY]QUINOXALIN 2(1H) ONE; 4 (3 AMINO 2 OXO 1,2 DIHYDROQUINOXALIN 5 YLOXY) 6 [4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 2 AMINIUM TRIFLUOROACETATE; 4 (3 AMINO 2 OXO 1,2 DIHYDROQUINOXALIN 5 YLOXY) N (3 HYDROXYBUTYL) 6 [4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 2 AMINIMIUM TRIFLUOROACETATE; AMG 517; N [2 [6 (3 AMINO 2 OXO 1,2 DIHYDROQUINOXALIN 5 YLOXY)PYRIMIDIN 4 YL] 5 (TRIFLUOROMETHYL)PHENYL]ISONICOTINAMIDE; N [2 [6 (3 AMINO 2 OXO 1,2 DIHYDROQUINOXALIN 5 YLOXY)PYRIMIDIN 4 YL] 5 (TRIFLUOROMETHYL)PHENYL]PICOLINAMIDE; N [4 [2 AMINO 6 [4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]BENZO[D]THIAZOL 2 YL]ACETAMIDE; N [4 [6 [2 AMINO 4 (TRIFLUOROMETHYL)PHENYL]PYRIMIDIN 4 YLOXY]BENZO[D]THIAZOL 2 YL]ACETAMIDE; RECEPTOR BLOCKING AGENT; VANILLOID RECEPTOR 1;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; CORE TEMPERATURE; DRUG ACTIVITY; DRUG DESIGN; DRUG EFFECT; DRUG POTENCY; DRUG SYNTHESIS; HYPERALGESIA; HYPERTHERMIA; IN VIVO STUDY; MALE; NONHUMAN; RAT; RECEPTOR BLOCKING; SINGLE DRUG DOSE;

ANALGESICS; ANIMALS; BENZOTHIAZOLES; BLOOD-BRAIN BARRIER; BODY TEMPERATURE; CAPSAICIN; FEVER; MALE; PAIN MEASUREMENT; QUINOXALINES; RATS; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TELEMETRY; TRPV CATION CHANNELS;

EID: 42949108141     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm7014638     Document Type: Article

References (31)

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26. Unpublished results.
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