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公开(公告)号：DK0933372T3
公开(公告)日：2008-04-28
申请号：DK98104292
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： SPALTENSTEIN ANDREW , TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW
IPC: C07D307/20 , A61K31/16 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/665 , A61K31/70 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/18 , C07H15/26
Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
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公开(公告)号：DE69838903D1
公开(公告)日：2008-02-07
申请号：DE69838903
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW , SPALTENSTEIN ANDREW
IPC: C07D307/20 , A61K31/16 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/665 , A61K31/70 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/18 , C07H15/26
Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
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公开(公告)号：LU91426I9
公开(公告)日：2018-12-28
申请号：LU91426
申请日：2008-04-02
Applicant: VERTEX PHARMA
Inventor： TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW , SPALTENSTEIN ANDREW
IPC: 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 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D307/20 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/26
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公开(公告)号：ES2299193T3
公开(公告)日：2008-05-16
申请号：ES98104292
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW
IPC: C07D307/20 , A61K31/16 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/665 , A61K31/70 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/18 , C07H15/26
Abstract: LA PRESENTE INVENCION SE REFIERE A PROFARMACOS DE UN TIPO DE SULFONAMIDAS QUE SON INHIBIDORES DE ASPARTIL PROTEASA. EN UNA REALIZACION DE LA INVENCION, SE DESCRIBE UNA NUEVA CLASE DE PROFARMACOS DE INHIBIDORES DE ASPARTIL PROTEASA DE VIH, CARACTERIZADOS POR UNA SOLUBILIDAD EN AGUA ADECUADA, UNA ELEVADA BIODISPONIBILIDAD Y UNA FACIL PRODUCCION IN VIVO DEL INGREDIENTE ACTIVO. LA INVENCION SE REFIERE TAMBIEN A COMPOSICIONES FARMACEUTICAS QUE COMPRENDEN DICHOS PROFARMACOS. LOS PROFARMACOS Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN SON ESPECIALMENTE ADECUADOS PARA REDUCIR EL VOLUMEN DE PILDORAS Y PARA INCREMENTAR LA CONFORMIDAD DEL PACIENTE. LA INVENCION SE REFIERE ASIMISMO A PROCEDIMIENTOS DE TRATAMIENTO DE MAMIFEROS CON DICHOS PROFARMACOS Y COMPOSICIONES FARMACEUTICAS.
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Patent Agency Ranking
公开(公告)号：AT382042T
公开(公告)日：2008-01-15
申请号：AT98104292
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW , SPALTENSTEIN ANDREW
IPC: C07D307/20 , A61K31/16 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/665 , A61K31/70 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/26
Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
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公开(公告)号：IS2817B
公开(公告)日：2012-11-15
申请号：IS5546
申请日：2000-06-22
Applicant: VERTEX PHARMA
Inventor： TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW , SPALTENSTEIN ANDREW
IPC: C07D307/20 , A61K31/16 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/665 , A61K31/70 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/18 , C07H15/26
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公开(公告)号：SI0933372T1
公开(公告)日：2008-06-30
申请号：SI9830903
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW , SPALTENSTEIN ANDREW
IPC: C07D307/00 , A61K31/00 , 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 , C07C311/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D307/20 , C07D405/00 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/00 , C07F9/655 , C07F9/6584 , C07H15/00 , C07H15/04 , C07H15/26
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公开(公告)号：DE69838903T2
公开(公告)日：2008-09-18
申请号：DE69838903
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： TUNG ROBERT D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW , SPALTENSTEIN ANDREW
IPC: C07D307/20 , A61K31/16 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/665 , A61K31/70 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/18 , C07H15/26
Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
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9.发明专利
公开(公告)号：PT933372E
公开(公告)日：2008-03-31
申请号：PT98104292
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： KAZMIERSKI WIESLAW MIECZYSLAW , HALE MICHAEL R , SPALTENSTEIN ANDREW , KALDOR ISTVAN , TUNG ROBERT D , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN
IPC: C07D307/20 , A61K31/16 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/665 , A61K31/70 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/18 , C07H15/26
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