Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD

Journal of Medicinal Chemistry

Volumn 57, Issue 11, 2014, Pages 4661-4676

  De Savi, Chris ^a   Cox, Rhona J ^a,b   Warner, Daniel J ^a   Cook, Anthony R ^a   Dickinson, Mark R ^a   McDonough, Amy ^a   Morrill, Louis C ^a   Parker, Beth ^a   Andrews, Glen ^a   Young, Simon S ^a   Gilmour, Peter S ^a   Riley, Rob ^a   Dearman, Matthew S ^a,b  

^a ASTRAZENECA   (United Kingdom)

^b ASTRAZENECA R AND D   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4' [(3,5 DIMETHYLPIPERAZIN 1 YL)METHYL] 2' (MORPHOLINOMETHYL)BIPHENYL 3 YLOXY] 5 FLUORO N [4 (2 HYDROXY 5 METHYLBENZAMIDO)CYCLOHEXYL]NICOTINAMIDE; CILOMILAST; GSK 256066; N [4 (1,5 DIMETHYL 1H PYRAZOLE 3 CARBOXAMIDO)CYCLOHEXYL] 2 [4' [3 (3,5 DMETHYLPIPERAZIN 1 YL)PROPYL]BIPHENYL 3 YLOXY] 5 FLUORONICOTINAMIDE; N [4 (1,5 DIMETHYL 1H PYRAZOLE 3 CARBOXAMIDO)CYCLOHEXYL] 5 FLUORO 2 [4' HYDROXY 2' (MORPHOLINOMETHYL)BIPHENYL 3 YLOXY]NICOTINAMIDE; N [4 (1,5 DIMETHYL 1H PYRAZOLE 3 CARBOXAMIDO)CYCLOHEXYL] 5 FLUORO 2 [4' [2 [4 (PYRROLIDIN 1 YL)PIPERIDIN 1 YL]ETHYL]BIPHENYL 3 YLOXY]NICOTINAMIDE; N [4 [2 [4' [(3,5 DIMETHYLPIPERAZIN 1 YL)METHYL] 2' (MORPHOLINOMETHYL)BIPHENYL 3 YLOXY] 5 FLUORONICOTINAMIDO]CYCLOHEXYL] 4 METHYLTHIAZOLE 2 CARBOXAMIDE; PHOSPHODIESTERASE IV INHIBITOR; ROFLUMILAST; ROLIPRAM; UK 500 001; UNCLASSIFIED DRUG;

ALLERGIC RHINITIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; ASTHMA; CHRONIC OBSTRUCTIVE LUNG DISEASE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG STRUCTURE; ENZYME INHIBITION; HUMAN; IC 50; NAUSEA; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; VOMITING;

ADMINISTRATION, INHALATION; ANIMALS; ANTI-INFLAMMATORY AGENTS; BENZAMIDES; DOGS; FERRETS; HUMANS; LIPOPOLYSACCHARIDES; LUNG; NEUTROPHILS; NIACINAMIDE; PHOSPHODIESTERASE 4 INHIBITORS; PULMONARY DISEASE, CHRONIC OBSTRUCTIVE; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; VOMITING;

EID: 84902438482     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5001216     Document Type: Article

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