Inhalation by design: Novel tertiary amine muscarinic M 3 receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease

Journal of Medicinal Chemistry

Volumn 54, Issue 19, 2011, Pages 6888-6904

  Glossop, Paul A ^a   Watson, Christine A L ^a   Price, David A ^a,c   Bunnage, Mark E ^a   Middleton, Donald S ^a   Wood, Anthony ^a,c   James, Kim ^a,c   Roberts, Dannielle ^a   Strang, Ross S ^a   Yeadon, Michael ^b   Perros Huguet, Christelle ^a,b   Clarke, Nicholas P ^b,c   Trevethick, Michael A ^b   MacHin, Ian ^b   Stuart, Emilio F ^b   Evans, Steven M ^b   Harrison, Anthony C ^a   Fairman, David A ^a,d   Agoram, Balaji ^a,e   Burrows, Jane L ^a   Feeder, Neil ^a   Fulton, Craig K ^a   Dillon, Barry R ^a   Entwistle, David A ^a   Spence, Fiona J ^c   more..

^a Sandwich Laboratories   (United Kingdom)

^b Allergy and Respiratory Research Unit   (United Kingdom)

^c PFIZER INC   (United States)

^d Peakdale Chemistry Services   (United Kingdom)

^e MEDIMMUNE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 (3 HYDROXYAZETIDIN 1 YL) 5 METHYL 2,2 DIPHENYLHEXANE NITRILE; 5 [3 (3 HYDROXYPHENOXY)AZETIDIN 1 YL] 5 METHYL 2,2 DIPHENYLHEXANAMIDE; 5 [3 (3 METHOXYPHENOXY)AZETIDIN 1 YL] 5 METHYL 2,2 DIPHENYLHEXANENITRILE; ACLIDINIUM BROMIDE; AZETIDINE; DAROTROPIUM BROMIDE; GLYCOPYRRONIUM BROMIDE; IPRATROPIUM BROMIDE; METHANESULFONIC ACID 1 (4 CYANO 1,1 DIMETHYL 4,4 DIPHENYLBUTYL) AZETIDIN 3 YL ESTER; MUSCARINIC M3 RECEPTOR ANTAGONIST; PF 3635659; TIOTROPIUM BROMIDE; TROSPIUM CHLORIDE; UNCLASSIFIED DRUG;

AMINATION; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; BINDING KINETICS; BRONCHOSPASM; CHRONIC OBSTRUCTIVE LUNG DISEASE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG GLUCURONIDATION; DRUG HALF LIFE; DRUG HYDROLYSIS; DRUG MECHANISM; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; FORCED EXPIRATORY VOLUME; GUINEA PIG; HYDROGENATION; LUNG RESISTANCE; MALE; NONHUMAN; OXIDATIVE STRESS; SINGLE DRUG DOSE; SMOOTH MUSCLE RELAXATION; TRACHEA;

ADMINISTRATION, INHALATION; ANIMALS; AZETIDINES; BRONCHODILATOR AGENTS; CELL LINE; CELL MEMBRANE PERMEABILITY; CHO CELLS; CRICETINAE; CRICETULUS; DIPHENYLACETIC ACIDS; DOGS; FEMALE; GUINEA PIGS; HEPATOCYTES; HUMANS; KINETICS; MALE; MICROSOMES, LIVER; MUSCLE RELAXATION; MUSCLE, SMOOTH; PULMONARY DISEASE, CHRONIC OBSTRUCTIVE; RADIOLIGAND ASSAY; RATS; RECEPTOR, MUSCARINIC M3; RECOMBINANT PROTEINS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRACHEA;

EID: 80053911301     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200884j     Document Type: Article

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