Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors

The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2; R1 may also be a radical...

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Hauptverfasser: VENDEVILLE SANDRINE MARIE HELENE, DE KOCK HERMAN AUGUSTINUS, SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN, DE BETHUNE MARIE-PIERRE T. M. M. G, VERSCHUEREN WIM GASTON, TAHRI ABDELLAH
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creator VENDEVILLE SANDRINE MARIE HELENE
DE KOCK HERMAN AUGUSTINUS
SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN
DE BETHUNE MARIE-PIERRE T. M. M. G
VERSCHUEREN WIM GASTON
TAHRI ABDELLAH
description The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(-O)-, -O-C(-O)-, -NR8-C(-O)-, -C1-6alkanediyl-C(-O)-, -NR8-C1-6alkanediyl-C(-O)-, -S(-O)2-, -O-S(-O)2-, -NR9-S(-O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(-O), carboxyl, aminoC(-O), mono- or di(C1-4alkyl)aminoC(-O), C3-7 cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
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G ; VERSCHUEREN WIM GASTON ; TAHRI ABDELLAH</creatorcontrib><description>The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(-O)-, -O-C(-O)-, -NR8-C(-O)-, -C1-6alkanediyl-C(-O)-, -NR8-C1-6alkanediyl-C(-O)-, -S(-O)2-, -O-S(-O)2-, -NR9-S(-O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(-O), carboxyl, aminoC(-O), mono- or di(C1-4alkyl)aminoC(-O), C3-7 cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. 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G</au><au>VERSCHUEREN WIM GASTON</au><au>TAHRI ABDELLAH</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors</title><date>2009-11-24</date><risdate>2009</risdate><abstract>The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(-O)-, -O-C(-O)-, -NR8-C(-O)-, -C1-6alkanediyl-C(-O)-, -NR8-C1-6alkanediyl-C(-O)-, -S(-O)2-, -O-S(-O)2-, -NR9-S(-O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(-O), carboxyl, aminoC(-O), mono- or di(C1-4alkyl)aminoC(-O), C3-7 cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors
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