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...
Gespeichert in:
Hauptverfasser: | , , , , , |
---|---|
Format: | Patent |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext bestellen |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
container_end_page | |
---|---|
container_issue | |
container_start_page | |
container_title | |
container_volume | |
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. |
format | Patent |
fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_US7622490B2</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>US7622490B2</sourcerecordid><originalsourceid>FETCH-epo_espacenet_US7622490B23</originalsourceid><addsrcrecordid>eNrjZHB1KspPTCkuSE0uKS3KVTDSTczNzMvXTUrNq8qvSKzKz0lVKC7NScvPA4qnpCp4eIYpFBTll6QmFqcqZOZlZCZlluQXFfMwsKYl5hSn8kJpbgYFN9cQZw_d1IL8-NTigsTk1LzUkvjQYHMzIyMTSwMnI2MilAAAwlgzYg</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors</title><source>esp@cenet</source><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</creator><creatorcontrib>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</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. 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.</description><language>eng</language><subject>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</subject><creationdate>2009</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20091124&DB=EPODOC&CC=US&NR=7622490B2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76318</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20091124&DB=EPODOC&CC=US&NR=7622490B2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>VENDEVILLE SANDRINE MARIE HELENE</creatorcontrib><creatorcontrib>DE KOCK HERMAN AUGUSTINUS</creatorcontrib><creatorcontrib>SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN</creatorcontrib><creatorcontrib>DE BETHUNE MARIE-PIERRE T. M. M. G</creatorcontrib><creatorcontrib>VERSCHUEREN WIM GASTON</creatorcontrib><creatorcontrib>TAHRI ABDELLAH</creatorcontrib><title>Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors</title><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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2009</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZHB1KspPTCkuSE0uKS3KVTDSTczNzMvXTUrNq8qvSKzKz0lVKC7NScvPA4qnpCp4eIYpFBTll6QmFqcqZOZlZCZlluQXFfMwsKYl5hSn8kJpbgYFN9cQZw_d1IL8-NTigsTk1LzUkvjQYHMzIyMTSwMnI2MilAAAwlgzYg</recordid><startdate>20091124</startdate><enddate>20091124</enddate><creator>VENDEVILLE SANDRINE MARIE HELENE</creator><creator>DE KOCK HERMAN AUGUSTINUS</creator><creator>SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN</creator><creator>DE BETHUNE MARIE-PIERRE T. M. M. G</creator><creator>VERSCHUEREN WIM GASTON</creator><creator>TAHRI ABDELLAH</creator><scope>EVB</scope></search><sort><creationdate>20091124</creationdate><title>Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors</title><author>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</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US7622490B23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2009</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>VENDEVILLE SANDRINE MARIE HELENE</creatorcontrib><creatorcontrib>DE KOCK HERMAN AUGUSTINUS</creatorcontrib><creatorcontrib>SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN</creatorcontrib><creatorcontrib>DE BETHUNE MARIE-PIERRE T. M. M. G</creatorcontrib><creatorcontrib>VERSCHUEREN WIM GASTON</creatorcontrib><creatorcontrib>TAHRI ABDELLAH</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>VENDEVILLE SANDRINE MARIE HELENE</au><au>DE KOCK HERMAN AUGUSTINUS</au><au>SURLERAUX DOMINIQUE LOUIS NESTOR GHISLAIN</au><au>DE BETHUNE MARIE-PIERRE T. M. M. 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> |
fulltext | fulltext_linktorsrc |
identifier | |
ispartof | |
issn | |
language | eng |
recordid | cdi_epo_espacenet_US7622490B2 |
source | esp@cenet |
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 |
url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-10T17%3A52%3A36IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-epo_EVB&rft_val_fmt=info:ofi/fmt:kev:mtx:patent&rft.genre=patent&rft.au=VENDEVILLE%20SANDRINE%20MARIE%20HELENE&rft.date=2009-11-24&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3EUS7622490B2%3C/epo_EVB%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true |