Discovery of two clinical histamine H 3 receptor antagonists: Trans - N -ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl] cyclobutanecarboxamide (PF-03654746) and trans -3-fluoro-3-[3-fluoro-4- (pyrrolidin-1-ylmethyl)phenyl]- N -(2-methylpropyl)cyclobutanecarboxamide (PF-03654764)

Journal of Medicinal Chemistry

Volumn 54, Issue 21, 2011, Pages 7602-7620

  Wager, Travis T ^a   Pettersen, Betty A ^a   Schmidt, Anne W ^a   Spracklin, Douglas K ^a   Mente, Scot ^a   Butler, Todd W ^a   Howard, Harry ^a   Lettiere, Daniel J ^a   Rubitski, David M ^a   Wong, Diane F ^a   Nedza, Frank M ^a   Nelson, Frederick R ^a   Rollema, Hans ^a   Raggon, Jeffrey W ^a   Aubrecht, Jiri ^a   Freeman, Jody K ^a   Marcek, John M ^a   Cianfrogna, Julie ^a   Cook, Karen W ^a   James, Larry C ^a   Chatman, Linda A ^a   Iredale, Philip A ^a   Banker, Michael J ^a   Homiski, Michael L ^a   Munzner, Jennifer B ^a   Chandrasekaran, Rama Y ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 FLUORO 3 [3 FLUORO 4 (PYRROLIDIN 1 YLMETHYL)PHENYL] N (2 METHYLPROPYL)CYCLOBUTANECARBOXAMIDE; BETA LACTAMASE; CYCLIC AMP; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; N ETHYL 3 FLUORO 3 [3 FLUORO 4 (PYRROLIDINYLMETHYL)PHENYL]CYCLOBUTANECARBOXAMIDE; PF 03654746; PF 03654764; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DOG; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DESIGN; DRUG DISPOSITION; DRUG DOSE REDUCTION; DRUG HALF LIFE; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG SELECTIVITY; DRUG SYNTHESIS; DRUG TOLERABILITY; HUMAN; HUMAN CELL; NONHUMAN; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION; TRANS ISOMER;

ANIMALS; BLOOD PROTEINS; BLOOD-BRAIN BARRIER; CELL LINE; CYCLOBUTANES; DOGS; DRINKING BEHAVIOR; DRUG DESIGN; HIGH-THROUGHPUT SCREENING ASSAYS; HISTAMINE ANTAGONISTS; HUMANS; KIDNEY; LIPIDOSES; LUNG; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PHOSPHOLIPIDS; PROTEIN BINDING; PYRROLIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, HISTAMINE H3; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80455173697     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200939b     Document Type: Article

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