PRODRUG OF ASPARTYL PROTEASE INHIBITOR - VERTEX PHARMACEUTICALS INCORPORATED

Title:

PRODRUG OF ASPARTYL PROTEASE INHIBITOR

Document Type and Number:

Japanese Patent JP3736964

Kind Code:

B2

Abstract:

PROBLEM TO BE SOLVED: To obtain a new compound having excellent characteristics of high water solubility, high oral bioavailability, etc., useful as a prodrug of an aspartyl protease inhibitor, especially for a HIV aspartyl protease inhibitor, suitable for reducing an unpleasant load and raising the administration ratio of patient.
SOLUTION: This compound is shown by formula I {A is H, R1-1-6C alkyl or the like; R1 is C(O), S(O)2 or the like; B is N(R2)-C(R3)2-C(O); R2 is H or a 1-4C alkyl; R3 is H, a 1-6C alkyl or the like; (x) is 0 or 1; G is H, R7 or the like; R7 is a group of formula II or formula III [M is H, K or the like; Z is O, CH3 or the like; Y is P or S; X is O or S; R7 is a C(R2)2, O or the like]; D and D' are each a 1-6C alkyl, a 2-4C alkenyl or the like; E is a 3-7C cycloalkyl, O-R3 or the like} such as a compound of formula IV. The compound is obtained, for example, by starting from a 4-nitrophenyl derivative of formula V.

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Inventors:

Roger Dee. Tan
Michael Earl Hale
Christopher T. Baker
Eric Stephen Farfine
Istvan Cordor
Weeslow Meeslow Kazumireski
Andrew Spartenstein

Application Number:

JP5870598A

Publication Date:

January 18, 2006

Filing Date:

March 10, 1998

Export Citation:

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Assignee:

VERTEX PHARMACEUTICALS INCORPORATED

International Classes:

C07C311/15; A61K31/18; A61K31/215; A61K31/265; A61K31/27; A61K31/34; A61K31/341; A61K31/4025; A61K31/496; A61K31/66; A61K31/661; A61K31/664; A61K31/7048; A61K45/00; A61P31/12; A61P31/18; A61P43/00; C07C311/18; C07C311/37; C07D277/30; C07D307/20; C07D405/12; C07D407/12; C07D417/12; C07F9/655; C07F9/6584; C07H15/04; C07H15/26; (IPC1-7): C07C311/15; A61K31/215; A61K31/27; A61K31/34; A61K31/66; C07C311/37; C07D307/20; C07D405/12; C07D407/12; C07D417/12; C07H15/04

Domestic Patent References:

JP8501299A

Attorney, Agent or Firm:

Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita

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