Antiviral ethers of aspartate protease substrate isosteres

US5935976A · kind A · utility

Assignee

• Novartis AG · CH

Inventors

• Guido Bold · Gipf-Oberfrick, CH
• Hans-Georg Capraro · Rheinfelden, CH
• Alexander Fassler · Macclesfield, GB
• Marc Lang · Mulhouse, FR
• Shripad S. Bhagwat · San Diego, US
• Satish Chandra Khanna · Bottmingen, CH
• Janis Karlis Lazdins · Basel, CH
• Jurgen Mestan · Denzlingen, DE

Key dates

• Filing date: Aug 21, 1998
• Grant date: Aug 10, 1999
• Expiry date: Aug 21, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2602/10
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.1 is an acyl radical lower-alkoxy-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amino, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl; PA1 or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals); PA1 R.sub.2 and R.sub.3 are in each case cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl which are unsubstituted or substituted by…