Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: A novel, potent and orally active direct inhibitor of factor Xa

Bioorganic and Medicinal Chemistry

Volumn 17, Issue 3, 2009, Pages 1193-1206

  Nagata, Tsutomu ^a   Yoshino, Toshiharu ^a   Haginoya, Noriyasu ^a   Yoshikawa, Kenji ^a   Nagamochi, Masatoshi ^a   Kobayashi, Syozo ^a   Komoriya, Satoshi ^a   Yokomizo, Aki ^a   Muto, Ryo ^a   Yamaguchi, Mitsuhiro ^a   Osanai, Ken ^a   Suzuki, Makoto ^a   Kanno, Hideyuki ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Anticoagulant; Factor Xa inhibitors; Lipophilicity; Non amidino compound; Oral bioavailability; Protein binding

Indexed keywords

1,2 DIAMINOCYCLOHEXANE; 2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; [2 [[(5 CHLOROINDOL 2 YL)CARBONYL]AMINO] 5 (DIMETHYLCARBAMOYL)CYCLOHEXYL] 5 METHYL 4,5,6,7 TETRAHYDROTHIAZOLO[5,4 C]PYRIDINE 2 CARBOXAMIDE; BLOOD CLOTTING FACTOR 10A INHIBITOR; PYRROLIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTICOAGULATION; AREA UNDER THE CURVE; ARTICLE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; LIPOPHILICITY; NONHUMAN; NORMAL HUMAN; REACTION ANALYSIS; STRUCTURE ANALYSIS;

ADMINISTRATION, ORAL; ANIMALS; ANTICOAGULANTS; BIOLOGICAL AVAILABILITY; CRYSTALLOGRAPHY, X-RAY; FACTOR XA; HAPLORHINI; HUMANS; INDOLES; NAPHTHALENES; PROPIONIC ACIDS; PROTEIN BINDING; THIAZOLES;

EID: 58949103808     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2008.12.037     Document Type: Article

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