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公开(公告)号：WO0047551A3
公开(公告)日：2001-08-16
申请号：PCT/US0003288
申请日：2000-02-09
Applicant: VERTEX PHARMA , HALE MICHAEL R , BAKER CHRISTOPHER T , STAMMERS TIMOTHY A , SHERRILL RONALD G , SPALTENSTEIN ANDREW , FURFINE ERIC S , MALTAIS FRANCOIS , ANDREWS CLARENCE WEBSTER III , MILLER JOHN F , SAMANO VICENTE
Inventor： HALE MICHAEL R , BAKER CHRISTOPHER T , STAMMERS TIMOTHY A , SHERRILL RONALD G , SPALTENSTEIN ANDREW , FURFINE ERIC S , MALTAIS FRANCOIS , ANDREWS CLARENCE WEBSTER III , MILLER JOHN F , SAMANO VICENTE
IPC: C07D317/28 , A61K9/20 , A61K9/48 , A61K31/27 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/5377 , A61K31/662 , A61P31/14 , A61P31/18 , A61P43/00 , C07B53/00 , C07C271/20 , C07C271/22 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/20 , C07D317/62 , C07D319/06 , C07D409/12 , C07D493/04 , C07F9/6561 , A61K31/18 , A61K31/665 , C07D407/12
CPC classification number: C07D493/04 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07C2601/08 , C07C2601/14 , C07D307/20 , C07D317/14 , C07D319/06 , C07D319/18 , C07D407/12 , C07F9/6561
Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
Abstract translation: 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶的活性的方法和用于筛选抗HIV活性化合物的方法。
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公开(公告)号：WO9933792A3
公开(公告)日：1999-09-16
申请号：PCT/US9827403
申请日：1998-12-23
Applicant: VERTEX PHARMA , HALE MICHAEL R , TUNG ROGER D , BAKER CHRISTOPHER T , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW
Inventor： HALE MICHAEL R , TUNG ROGER D , BAKER CHRISTOPHER T , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW
IPC: C07C311/18 , C07D307/20 , C07D405/12 , C07F9/655 , C07F9/6584 , A61K31/34 , A61K31/66 , A61K31/70 , C07F9/09 , C07F9/141 , C07H15/04
CPC classification number: C07D405/12 , C07C311/18 , C07D307/20 , C07F9/65515 , C07F9/65844
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 whith these prodrugs and pharmaceutical compositons.
Abstract translation: 本发明涉及一类为天冬氨酰蛋白酶抑制剂的磺酰胺的前药。 在一个实施方案中，本发明涉及一类新型HIV天冬氨酰蛋白酶抑制剂的前体药物，其特征在于有利的水溶性，高的口服生物利用度和活体成分的容易的体内生成。 本发明还涉及包含这些前药的药物组合物。 本发明的前体药物和药物组合物特别适合于减轻药丸负担并增加患者依从性。 本发明还涉及用这些前体药物和药物组合物治疗哺乳动物的方法。
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公开(公告)号：WO9933793A3
公开(公告)日：1999-09-10
申请号：PCT/US9827424
申请日：1998-12-23
Applicant: VERTEX PHARMA , HALE MICHAEL R , TUNG ROGER D , BAKER CHRISTOPHER T , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW
Inventor： HALE MICHAEL R , TUNG ROGER D , BAKER CHRISTOPHER T , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW
IPC: A61K31/34 , A61K31/341 , A61K31/4172 , A61K31/44 , A61K31/496 , A61K31/66 , A61K31/665 , A61K31/7024 , A61P31/18 , A61P37/04 , A61P43/00 , C07C311/18 , C07D307/20 , C07D317/34 , C07D405/12 , C07F9/655 , C07F9/6584 , C07D319/06 , A61K31/335 , A61K31/70 , C07D309/12 , C07D317/24 , C07D493/04 , C07F9/09
CPC classification number: C07D405/12 , A61K31/34 , A61K31/4172 , A61K31/44 , A61K31/496 , A61K31/66 , A61K31/7024 , C07C311/18 , C07D307/20 , C07D317/34 , C07F9/65515 , C07F9/65844
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.
Abstract translation: 本发明涉及作为天冬氨酰蛋白酶抑制剂的一类磺酰胺的前药。 在一个实施方案中，本发明涉及HIV天冬氨酰蛋白酶抑制剂的新一类前药，其特征在于有利的水溶性，高口服生物利用度和活性成分的体内易生成。 本发明还涉及包含这些前药的药物组合物。 本发明的前药和药物组合物特别适用于降低药丸负担并增加患者依从性。 本发明还涉及用这些前药和药物组合物治疗哺乳动物的方法。
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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：CZ301653B6
公开(公告)日：2010-05-12
申请号：CZ20002363
申请日：1998-03-09
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , HALE MICHAEL R , BAKER CHRISTOPHER T , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAV , SPALTENSTEIN ANDREW
IPC: C07C311/15 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/425 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/18 , C07C311/37 , C07D277/30 , C07D277/36 , C07D307/20 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/26
Abstract: Sulfonamidové deriváty obecného vzorce I nebo XXIII, jejichž symboly mají specifický význam, a farmaceutické prostredky s jejich obsahem. Tyto deriváty jsou proléciva ze trídy sulfonamidu, která jsou inhibitory aspartylproteázy, napr. HIV aspartylproteázy, a vyznacují se výhodnou rozpustností ve vode, vysokou biologickou využitelností pri perorálním podávání a snadnou in vivo generací aktivní složky. Proléciva a farmaceutické prostredky podle vynálezu jsou zvlášte vhodné pro snížení zatížení pilulkami a zlepšení spolupráce pacienta.
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Patent Agency Ranking
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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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：SI1159278T1
公开(公告)日：2006-06-30
申请号：SI200030800
申请日：2000-02-09
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL R , BAKER CHRISTOPHER T , STAMMERS TIMOTHY A , SHERRILL RONALD G , SPALTENSTEIN ANDREW , FURFINE ERIC S , MALTAIS FRANCOIS , ANDREWS CLARENCE WEBSTER III , MILLER JOHN F , SAMANO VICENTE
IPC: C07D317/28 , C07D493/00 , A61K9/20 , A61K9/48 , A61K31/00 , A61K31/27 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/5377 , A61K31/662 , A61P31/14 , A61P31/18 , A61P43/00 , C07B53/00 , C07C271/20 , C07C271/22 , C07C311/00 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/00 , C07D307/20 , C07D317/00 , C07D317/62 , C07D319/00 , C07D319/06 , C07D407/00 , C07D409/12 , C07D493/04 , C07F9/00 , C07F9/6561
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公开(公告)号：DK1159278T3
公开(公告)日：2006-04-10
申请号：DK00913402
申请日：2000-02-09
Applicant: VERTEX PHARMA
Inventor： MALTAIS FRANCIOS , HALE MICHAEL R , BAKER CHRISTOPHER T , STAMMERS TIMOTHY A , SHERRILL RONALD G , SPALTENSTEIN ANDREW , FURFINE ERIC S , ANDREWS CLARENCE WEBSTER III , MILLER JOHN F , SAMANO VICENTE
IPC: C07D317/28 , C07D493/04 , A61K9/20 , A61K9/48 , A61K31/18 , A61K31/27 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/5377 , A61K31/662 , A61K31/665 , A61P31/14 , A61P31/18 , A61P43/00 , C07B53/00 , C07C271/20 , C07C271/22 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/20 , C07D317/62 , C07D319/06 , C07D407/12 , C07D409/12 , C07F9/6561
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公开(公告)号：CA2231700C
公开(公告)日：2005-08-09
申请号：CA2231700
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： BAKER CHRISTOPHER T , SPALTENSTEIN ANDREW , HALE MICHAEL R , TUNG ROGER D , KALDOR ISTVAN , KAZMIERSKI WIESLAW MIECZYSLAW , FURFINE ERIC STEVEN
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 , C07D241/04 , C07D243/04 , C07D401/06 , C07D401/12 , C07D207/14 , C07D403/14 , C07C311/19 , C07D217/26 , A61K31/665
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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