Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists

Journal of Medicinal Chemistry

Volumn 57, Issue 7, 2014, Pages 2989-3004

  Horne, Daniel B ^a   Tamayo, Nuria A ^a   Bartberger, Michael D ^a   Bo, Yunxin ^a   Clarine, Jeffrey ^a   Davis, Carl D ^a   Gore, Vijay K ^a   Kaller, Matthew R ^a   Lehto, Sonya G ^a   Ma, Vu V ^a   Nishimura, Nobuko ^a   Nguyen, Thomas T ^a   Tang, Phi ^a   Wang, Weiya ^a   Youngblood, Beth D ^a   Zhang, Maosheng ^a   Gavva, Narender R ^a   Monenschein, Holger ^a   Norman, Mark H ^a  

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (3 FLUORO 4 (TRIFLUOROMETHYL)PHENYL) 1,2,3,4 TETRAHYDROISOQUINOLINE; 1 (4 (TRIFLUOROMETHYL)PHENYL) 1,2,3,4 TETRAHYDROISOQUINOLINE; 1 (6 (TRIFLUOROMETHYL)PYRIDIN 3 YL) 1,2,3,4 TETRAHYDROISOQUINOLINE; 1 METHYL 1 (4 (TRIFLUOROMETHYL)PHENYL) 1,2,3,4 TETRAHYDROISOQUINOLINE; 5 (4 (TRIFLUOROMETHYL)PHENYL) 5,6,7,8 TETRAHYDRO 1,6 NAPHTHYRIDINE; 8 (3 FLUORO 4 (TRIFLUOROMETHYL)PHENYL) 5,6,7,8 TETRAHYDRO 1,7 NAPHTHYRIDINE; 8 (4 (TRIFLUOROMETHYL)PHENYL) 5,6,7,8 TETRAHYDRO 1,7 NAPHTHYRIDINE; TETRAHYDROISOQUINOLINE DERIVATIVE; TRANSIENT RECEPTOR POTENTIAL CHANNEL AFFECTING AGENT; TRANSIENT RECEPTOR POTENTIAL CHANNEL M8; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BLADDER DISEASE; CHO CELL; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG STRUCTURE; DRUG SYNTHESIS; LIVER MICROSOME; NONHUMAN; PAIN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; BEHAVIOR, ANIMAL; CIRCULAR DICHROISM; COLD TEMPERATURE; DOGS; HUMANS; MALE; MICROSOMES, LIVER; MOTOR ACTIVITY; PYRIMIDINONES; RATS; RATS, SPRAGUE-DAWLEY; SPECTROMETRY, MASS, MATRIX-ASSISTED LASER DESORPTION-IONIZATION; STEREOISOMERISM; TETRAHYDROISOQUINOLINES; TISSUE DISTRIBUTION; TRPM CATION CHANNELS;

EID: 84898401505     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm401955h     Document Type: Article

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