发明名称 SULFATE SALT OF AN HIV PROTEASE INHIBITOR HAVING AN IMPROVED ORAL ABSORPTION AND BIOAVAILABILITY
摘要 This invention relates to a sulfate salt of an HIV protease inhibitor, Compound (A), which is useful in the treatment of AIDS, ARC or HIV infection in adults and children. More specifically, the invention provides a sulfate salt of the HIV protease inhibitor, Compound (A) having substantially improved solibility in dilute HC1 (gastric acid) solution which results in much greater oral absorption and bioavailability in animal models. Processes for making the sulfate salt of the particular HIV protease inhibitor compounds are also disclosed.
申请公布号 WO9854178(A1) 申请公布日期 1998.12.03
申请号 WO1998US10633 申请日期 1998.05.26
申请人 MERCK & CO., INC.;ASKIN, DAVID;HOERRNER, R., SCOTT;PURICK, ROBERT, M.;REIDER, PAUL;VARSOLONA, RICHARD, J.;VOLANTE, RALPH, P. 发明人 ASKIN, DAVID;HOERRNER, R., SCOTT;PURICK, ROBERT, M.;REIDER, PAUL;VARSOLONA, RICHARD, J.;VOLANTE, RALPH, P.
分类号 A61K31/496;A61P31/18;A61P43/00;C07D405/06;(IPC1-7):C07D405/06;A61K31/495;A61K31/34 主分类号 A61K31/496
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