ANTIVIRAL ETHERS OF ASPARTATE PROTEASE SUBSTRATE ISOSTERES

Japanese Patent JP3192070

B2

PROBLEM TO BE SOLVED: To obtain antiviral ethers of aspartate protease substrate isosteres expressed in a specific formula, excellent in pharmacological properties such as pharmacodynamics, biocompatibility, tolerance, etc., having antiretroviral activity against HIV and is useful in the therapy, etc., of AIDS.
SOLUTION: The compounds expressed by formula I [R1 is (substituted) lower alkoxycarbonyl or the like; R2 and R3 are each in the following combination: R2 is phenyl, R3 is cyanophenyl; R2 is phenyl, R3 is difluorophenyl or the like; R4 is isopropyl or the like; R5 is methyl or the like; and n=1], for example, 5(S)-(Boc-amino)-4(S)-hydroxy-6-phenyl-2(R)-[(2,3,4-trimethoxyphenyl)methyl]- hexanoyl-(L)-Val-N-(2-methoxyethyl)amide or the like. The subject compounds are preferably obtained by carrying out the condensation of acid of R1-OH or reactive derivatives of the acid with the amino compounds of formula II or reactive derivatives, protecting free functional groups, or removing the protective functional groups, etc.

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Guido Bolt
Hans-Georg Capraro
Alexander fassler
Marc Lang
Shri Pad Sabray Bagwat
Satish shandra kanna
Janis Carlis Ratsden
Jurgen Mestan

JP29502495A

July 23, 2001

October 19, 1995

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Novartis Actien Gezel Shaft

A61K31/075; A61K31/16; A61K31/165; A61K31/275; A61K31/325; A61K31/35; A61K31/351; A61K31/352; A61K31/395; A61K31/425; A61K31/426; A61K31/44; A61K31/4406; A61K31/4418; A61K31/4427; A61K31/445; A61K31/47; A61K31/495; A61K31/535; A61K31/5375; A61K31/695; A61K38/05; A61P31/12; A61P31/18; C07C237/22; C07C255/60; C07C271/22; C07C311/19; C07C311/42; C07C317/50; C07D207/12; C07D207/16; C07D295/12; C07D207/26; C07D207/28; C07D209/18; C07D209/42; C07D211/40; C07D211/46; C07D211/48; C07D211/60; C07D211/62; C07D213/30; C07D213/65; C07D213/81; C07D213/82; C07D277/06; C07D277/20; C07D277/40; C07D277/56; C07D295/155; C07D295/215; C07D307/20; C07D307/33; C07D309/04; C07D309/12; C07D311/24; C07D317/60; C07D401/04; C07K5/00; (IPC1-7): C07C271/22; A61K31/16; A61K31/165; A61K31/275; A61K31/35; A61K31/395; A61K31/425; A61K31/44; A61K31/445; A61K31/47; A61K31/495; A61K31/535; A61K31/695; A61P31/12; C07C311/19; C07C311/42; C07C317/50; C07D207/12; C07D207/16; C07D209/18; C07D211/40; C07D211/60; C07D213/81; C07D213/82; C07D277/06; C07D277/56; C07D295/12; C07D307/20; C07D307/33; C07D309/12; C07D311/24; C07D401/04

JP2209854A
JP7316191A

Takashi Ta (3 outside)

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