Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 22, 1998, Pages 3193-3198

  St Denis, Yves ^a,c   Augelli Szafran, Corinne E ^b   Bachand, Benoit ^a   Berryman, Kent A ^b   DiMaio, John ^a   Doherty, Annette M ^b   Edmunds, Jeremy J ^b   Leblond, Lorraine ^a   Lévesque, Sophie ^a   Narasimhan, Lakshmi S ^b   Penvose Yi, Jan R ^b   Rubin, J Ronald ^b   Tarazi, Micheline ^a   Winocour, Peter D ^a   Siddiqui, M Arshad ^a  

^a Shire Canada   (Canada)

^b PFIZER INC   (United States)

^c GSK   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

BICYCLO COMPOUND; LACTAM DERIVATIVE; THROMBIN INHIBITOR;

ANIMAL MODEL; ANTICOAGULATION; ARTERY THROMBOSIS; ARTICLE; BINDING AFFINITY; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG MECHANISM; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HYDROPHOBICITY; INTRAVENOUS DRUG ADMINISTRATION; MASS SPECTROMETRY; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; THROMBIN TIME;

ANIMALIA;

EID: 0032541995     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00550-2     Document Type: Article

References (12)

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8. 8. The reaction performed with commercially available Grignard reagent failed to give good results.
9. 9. Berryman, K.A.; Doherty, A.M.; Edmunds, J.J.; Plummer, J.S. WO9748687, 1997. See also: Bachand, B.; DiMaio, J.; Siddiqui, M.A. Bioorg. Med. Chem. Lett. 1998; manuscript submitted.
10. 9. Berryman, K.A.; Doherty, A.M.; Edmunds, J.J.; Plummer, J.S. WO9748687, 1997. See also: Bachand, B.; DiMaio, J.; Siddiqui, M.A. Bioorg. Med. Chem. Lett. 1998; manuscript submitted.
11. 10. Finkle, C.D.; St-Pierre, A.; Leblond, L.; Deschênes, I.; DiMaio, J.; Winocour, P.D. Thrombosis and Haemostasis, 1998, 79, 431.
12. 50 (S isomer) = 4 nM.