Discovery of (S)-N-{2-[1-(3-ethoxy-4-methoxy-phenyl)-2- methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1 H-isoindol-4-yl}acetamide (Apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-a inhibitor

Journal of Medicinal Chemistry

Volumn 52, Issue 6, 2009, Pages 1522-1524

  Man, Hon Wah ^a   Schafer, Peter ^a   Wong, Lu Min ^a   Patterson, Rebecca T ^a   Corral, Laura G ^a   Raymon, Heather ^a   Blease, Kate ^a   Leisten, Jim ^a   Shirley, Michael A ^a   Tang, Yang ^a   Babusis, Darius M ^a   Chen, Roger ^a   Stirling, Dave ^a   Muller, George W ^a  

^a CELGENE CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

APREMILAST; LIPOPOLYSACCHARIDE; PHOSPHODIESTERASE IV INHIBITOR; PHTHALIMIDE; ROFLUMILAST; ROLIPRAM; TUMOR NECROSIS FACTOR ALPHA; TUMOR NECROSIS FACTOR ALPHA INHIBITOR; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CHRONIC OBSTRUCTIVE LUNG DISEASE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; IC 50; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; CYCLIC NUCLEOTIDE PHOSPHODIESTERASES, TYPE 4; DRUG DISCOVERY; HUMANS; PHOSPHODIESTERASE INHIBITORS; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THALIDOMIDE; TUMOR NECROSIS FACTOR-ALPHA;

EID: 64349119966     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900210d     Document Type: Article

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