PRODRUG OF ASPARTYL PROTEASE INHIBITOR

Japanese Patent JP2009102400

A

To provide a prodrug of a class of sulfonamides which is an aspartyl protease inhibitor.

This invention relates to a new class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable water solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to a pharmaceutical composition comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to a method of treating mammals with these prodrugs and pharmaceutical compositions.

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ROGER D TAN
MICHAEL R HALE
CHRISTOPHER T BAKER
ERIC STEVEN FARFAIN
ISTVAN COLDOLL
WISLOW MIIJIISUROU KAZMIERSKI
ANDREW SPALTENSTEIN

JP2009016033A

May 14, 2009

January 27, 2009

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VERTEX PHARMACEUT INC

A61K31/265; A61K31/18; A61K31/215; A61K31/27; A61K31/34; A61K31/341; A61K31/4025; A61K31/4178; A61K31/443; A61K31/496; A61K31/66; A61K31/661; A61K31/664; A61K31/675; A61K31/685; A61K31/7048; A61K45/00; A61P31/12; A61P31/18; A61P43/00; C07C311/15; C07C311/18; C07C311/37; C07D277/30; C07D307/20; C07D405/12; C07D407/12; C07D417/12; C07F9/655; C07F9/6584; C07H15/04; C07H15/26

Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita

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