Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 22, 1998, Pages 3143-3148

  Fevig, John M ^a   Cacciola, Joseph ^a   Alexander, Richard S ^a   Knabb, Robert M ^a   Lam, Gilbert N ^a,b   Wong, Pancras C ^a   Wexler, Ruth R ^a  

^a DUPONT COMPANY   (United States)

^b Department of Pharmacokinetics and Drug Metabolism   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANILINE DERIVATIVE; ANTICOAGULANT AGENT; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICOAGULATION; ARTERIOVENOUS SHUNT; ARTICLE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG HYDROLYSIS; DRUG POTENCY; DRUG SYNTHESIS; NONHUMAN; RABBIT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ANIMALIA; ORYCTOLAGUS CUNICULUS;

EID: 0032541991     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00574-5     Document Type: Article

References (16)

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15. 14. In this model, rabbits were infused with 5-10 mg/kg/h of compound and blood samples were taken prior to, during and up to four hours after the infusion. Blood samples were immediately worked up by solid phase extraction and analyzed for test compound by an ex vivo anti-Xa assay or by LC/MS/MS.
16. 15. Preliminary studies on several analogs have demonstrated plasma metabolism of the side chain and in some cases (compounds 13 and 17) complete loss of the side chain. Christ, D. D.; Mutlib, A., unpublished results.