280781-39-7Relevant articles and documents
PEPTIDIC THROMBIN INHIBITOR COMPOUND
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Page 19, (2010/02/06)
The present invention relates to a novel thrombin inhibitor compound which has a good inhibitory effect against thrombosis and can be orally administered, a process for preparing the same, and to a composition for the therapeutic and/or prophylactic treatment of various diseases associated with thrombin inhibition mechanism, which comprises the same as an active ingredient.
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1
Lee, Koo,Jung, Won-Hyuk,Park, Cheol Won,Park, Hee Dong,Lee, Sun Hwa,Kwon, O Hwan
, p. 1017 - 1022 (2007/10/03)
A series of noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1 was investigated. While the amidrazone and the amine series displayed limited oral absorption, the amidine series demonstrated generally good oral absorption and strong antithrombotic activity; the single-digit picomolar Ki achieved from this series is among the best yet reported. The present work highlights the benzamidine compound 11f (LB30812) that exhibits excellent overall profiles of potency, oral absorption and antithrombotic efficacy.