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公开(公告)号：WO9965870A3
公开(公告)日：2001-03-15
申请号：PCT/US9913744
申请日：1999-06-17
Applicant: VERTEX PHARMA , SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
Inventor： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
IPC: A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , C07F9/6561 , A61K31/27 , A61K31/34 , A61K31/395 , C07D215/48
CPC classification number: C07D213/30 , C07C311/48 , C07C311/49 , C07C2601/08 , C07C2601/14 , C07D215/48 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D309/22 , C07D319/06 , C07D401/12 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , 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：ES2375823T3
公开(公告)日：2012-03-06
申请号：ES06009072
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN , BRIEGER MICHAEL STEPHEN
IPC: C07C311/16 , C07D317/62 , A61K20060101 , A61K31/34 , A61K31/343 , A61K31/352 , A61K31/36 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07C20060101 , C07C311/18 , C07C311/29 , C07D20060101 , C07D317/46 , C07D407/12 , C07D493/04
Abstract: Un compuesto seleccionado de los números de compuestos: 5a, 5b, 5c, 5d, 5e, 5f, 5g, 10-21, 58, 67, 68 y 328, en donde dicho compuesto tiene la estructura:**Fórmula**
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公开(公告)号：CA2335477C
公开(公告)日：2010-11-30
申请号：CA2335477
申请日：1999-06-17
Applicant: VERTEX PHARMA
Inventor： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
IPC: C07D493/04 , A61K31/34 , A61K31/351 , A61K31/36 , A61K31/4184 , A61K31/426 , A61K31/4709 , A61K31/498 , A61K31/535 , A61K31/5355 , A61K31/536 , A61K31/5395 , A61K31/551 , A61K31/635 , A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D413/12 , C07D417/12 , 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.
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Patent Agency Ranking
公开(公告)号：SK287123B6
公开(公告)日：2009-12-07
申请号：SK9662000
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 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
Abstract: Prodrugs of a class of sulfonamides defined by the general formula (I) which are aspartyl protease inhibitors, especially HIV aspartyl protease inhibitors, that are characterized by favorable aqueous solubility in water, high oral bioavailability and facile in vivo generation of the active ingredient. Pharmaceutical compositions containing these drugs and prodrugs are particularly well suited for decreasing the pill burden and increasing patient compliance.
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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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8.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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公开(公告)号：NO323951B1
公开(公告)日：2007-07-23
申请号：NO20016034
申请日：2001-12-10
Applicant: VERTEX PHARMA
Inventor： SPALTENSTEIN ANDREW , TUNG ROGER D , HALE MICHAEL ROBIN , FURFINE ERIC STEVEN , KALDOR ISTVAN , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , SAMANO VICENTE , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN , JARVIS ASHLEY NICHOLAS
IPC: C07D317/62 , A61K20060101 , A61K31/34 , A61K31/343 , A61K31/352 , A61K31/36 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07C20060101 , C07C311/18 , C07D20060101 , C07D317/46 , C07D407/12 , C07D493/04
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.
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公开(公告)号：AP1717A
公开(公告)日：2007-01-30
申请号：AP2000002023
申请日：1999-06-17
Applicant: VERTEX PHARMA
Inventor： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS III CLARENCE WEBSTER , LOWEN GREGORY THOMAS
IPC: A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , 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.
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