Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate

Journal of Medicinal Chemistry

Volumn 55, Issue 17, 2012, Pages 7472-7479

  Press, Neil J ^a   Taylor, Roger J ^a   Fullerton, Joseph D ^d   Tranter, Pamela ^a   McCarthy, Clive ^d   Keller, Thomas H ^d   Arnold, Nicola ^d   Beer, David ^c   Brown, Lyndon ^d   Cheung, Robert ^d   Christie, Julie ^d   Denholm, Alastair ^d   Haberthuer, Sandra ^d   Hatto, Julia D I ^a   Keenan, Mark ^d   Mercer, Mark K ^d   Oakman, Helen ^a   Sahri, Helene ^d   Tuffnell, Andrew R ^d   Tweed, Morris ^d   Tyler, John W ^a   Wagner, Trixie ^b   Fozard, John R ^b   Trifilieff, Alexandre ^b   more..

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

^c NOVARTIS INSTITUTE FOR TROPICAL DISEASES   (Singapore)

^d NONE

Author keywords

[No Author keywords available]

Indexed keywords

1 [(8 ARYL) 1,7 NAPHTHYRIDIN 6 YL]PIPERIDINE 4 CARBOXYLIC ACID DERIVATIVE; 1 [8 (3 FLUOROPHENYL) 1,7 NAPHTHYRIDIN 6 YL]PIPERIDINE 4 CARBOXYLIC ACID; 4 [(8 ARYL) 1,7 NAPHTHYRIDIN 6 YL]CYCLOHEXANECARBOXYLIC ACID DERIVATIVE; 4 [8 (3 (TRIFLUOROMETHOXY)PHENYL) 1,7 NAPHTHYRIDIN 6 YL]CYCLOHEXANECARBOXYLIC ACID; 4 [8 (3 FLUOROPHENYL) 1,7 NAPHTHYRIDIN 6 YL]CYCLOHEXANECARBOXYLIC ACID; CARBOXYLIC ACID DERIVATIVE; PHOSPHODIESTERASE IV INHIBITOR; ROFLUMILAST; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; CHRONIC OBSTRUCTIVE LUNG DISEASE; CONTROLLED STUDY; DIAZOTIZATION; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG HALF LIFE; DRUG SOLUBILITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; SUZUKI REACTION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; CELLS, CULTURED; DISEASE MODELS, ANIMAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; MICE; MODELS, MOLECULAR; PHOSPHODIESTERASE 4 INHIBITORS; RATS; SOLUBILITY; VOMITING;

EID: 84866314709     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300459a     Document Type: Article

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