Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)- pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} as a clinical candidate

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 17, 2010, Pages 5313-5319

  Anselm, Lilli ^a   Banner, David W ^a   Benz, Jörg ^a   Groebke Zbinden, Katrin ^a   Himber, Jacques ^a   Hilpert, Hans ^a   Huber, Walter ^a   Kuhn, Bernd ^a   Mary, Jean Luc ^a   Otteneder, Michael B ^a   Panday, Narendra ^a,b   Ricklin, Fabienne ^a   Stahl, Martin ^a   Thomi, Stefan ^a   Haap, Wolfgang ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b EUROPEAN PATENT OFFICE   (Germany)

Author keywords

Anticoagulation; Factor Xa inhibitors; Structure based design; X ray analysis

Indexed keywords

1 (2,2 DIFLUOROETHYL)PYRROLIDINE 3,4 DICARBOXYLIC ACID 3 [(5 CHLORO PYRIDIN 2 YL)AMIDE] 4 [[2 FLUORO 4 (2 OXO 2H PYRIDIN 1 YL)PHENYL]AMIDE]; BLOOD CLOTTING FACTOR 10A INHIBITOR; PYRIDINE DERIVATIVE; R 1663; SERINE PROTEINASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTICOAGULATION; ANTITHROMBOTIC ACTIVITY; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG PROTEIN BINDING; DRUG SYNTHESIS; EXPERIMENTAL MONKEY; NONHUMAN; PROCESS OPTIMIZATION; RAT; SAPONIFICATION; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

FACTOR XA; PYRROLIDINES;

RATTUS;

EID: 77955663098     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.06.126     Document Type: Article

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