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公开(公告)号：SI1194404T1
公开(公告)日：2006-10-31
申请号：SI200030872
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN
IPC: C07C311/00 , C07D317/62 , A61K20060101 , A61K31/00 , A61K31/34 , A61K31/343 , A61K31/352 , A61K31/36 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C20060101 , C07C311/18 , C07D20060101 , C07D317/00 , C07D317/46 , C07D407/12 , C07D493/00 , C07D493/04
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公开(公告)号：HK1046899A1
公开(公告)日：2003-01-30
申请号：HK02106939
申请日：2002-09-23
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE EREIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN
IPC: C07C20060101 , C07D317/62 , A61K20060101 , A61K31/34 , A61K31/343 , A61K31/352 , A61K31/36 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , 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：NO20016034A
公开(公告)日：2002-01-18
申请号：NO20016034
申请日：2001-12-10
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER D , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN
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 , C07C311/16
CPC classification number: C07D493/04 , A61K31/352 , A61K31/36 , A61K45/06 , C07C311/18 , C07C311/29 , C07C311/39 , C07C2601/08 , C07D317/46 , A61K2300/00
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公开(公告)号：PE02302001A1
公开(公告)日：2001-03-15
申请号：PE0005732000
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： SPALTENSTEIN ANDREW , KALDOR ISTVAN , SAMANO VICENTE , TUNG ROGER , WILKES ROBIN DAVID , JARVIS ASHLEY NICHOLAS , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN , FURFINE ERIC STEVEN , SCHAIRER WAYNE CARL , PRICE STEPHEN , HALE MICHAEL ROBIN
IPC: C07D317/62 , A61K20060101 , A61K31/34 , A61K31/343 , A61K31/352 , A61K31/36 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07C20060101 , C07C311/16 , C07C311/18 , C07C311/29 , C07D20060101 , C07D317/46 , C07D407/12 , C07D493/04
CPC classification number: C07D493/04 , A61K31/352 , A61K31/36 , A61K45/06 , C07C311/18 , C07C311/29 , C07C311/39 , C07C2601/08 , C07D317/46 , A61K2300/00
Abstract: SE REFIERE A UN COMPUESTO SULFONAMIDA DE FORMULA I, DONDE: A ES H, Ht, R1-Ht, R1-ALQUILO C1-C6; R1 ES -C(O)-, S(O)2, -C(O)-C(O)-, -O-C(O)-, O-S(O)2, ENTRE OTROS; Ht ES CICLOALQUILO C3-C7, CICLOALQUENILO C5-C7, ARILO C6-C14, HETEROCICLO C5-C7 QUE CONTIENE N, N(R2), O, S, S(O)n, DICHO ARILO O HETEROCICLO ESTA FUSIONADO A Q; R2 ES H, ALQUILO C1-C4 OPCIONALMENTE SUSTITUIDO CON UN ANILLO CARBOXICLICO DE 3 A 7 MIEMBROS, HETEROCICLO DE 5-7 MIEMBROS OPCIONALMENTE SUSTITUIDO CON 1-4 -X`-Y', O-ARILALQUILO, ENTRE OTROS; X' ES O, S, NH, NHCO, NHCOO, ENTRE OTROS; Y' ES ALQUILO C1-C15, ALQUENILO C2-C15; G ES H, R7, ALQUILO C1-C4; CUANDO G ES ALQUILO C1-C4, G Y R7 ESTAN UNIDOS Y FORMAN UN ANILLO HETEROCICLO; D ES ALQUILO C1-C6 SUSTITUIDO CON Q OPCIONALMENTE SUSTITUIDO CON CICLOALQUILO C3-C6, ENTRE OTROS; E ES Ht, O-Ht, ALQUILO C1-C6, ENTRE OTROS; R7 ES GRUPO a, b; M ES Na, Mg, ENTRE OTROS; M' ES H, ALQUILO C1-C12, ALQUENILO C2-C12, ENTRE OTROS; x ES 0-1; y ES P, S; X ES O, S; Z ES O, S, N(R2)2. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS (1O,2ß,3O)-9-[2,3-BIS(HIDROXIMETIL)CICLOBUTIL]GUANINA, NUCLEOSIDOS ACICLICOS, ACICLOVIR, LAMIVUDINA, RIBAVIRINA, INTERFERON, ENTRE OTROS. EL COMPUESTO I INHIBE A LA ASPARTIL PROTEASA HIVY PUEDE SER UTIL PARA EL TRATAMIENTO DEL SIDA, LINFADENOPATIA PROGRESIVA GENERALIZADA, SARCOMA DE KAPOSI
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公开(公告)号：AU5600600A
公开(公告)日：2001-01-02
申请号：AU5600600
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN
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 , C07C311/16 , C07C311/29
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：CY1112632T1
公开(公告)日：2016-02-10
申请号：CY121100182
申请日：2012-02-22
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , 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: Ηπαρούσαεφεύρεσηαφοράνέακατηγορίασουλφοναμιδίωνπουείναιαναστολείςασπαρτύλπρωτεάσης. Σεμίαπραγματοποίηση, αυτήη εφεύρεσηαφοράσενέακατηγορίααναστολέωνΑσπαρτύλπρωτεάσης HIV πουχαρακτηρίζονταιαπόειδικήσύνταξηκαιφυσικοχημικάχαρακτηριστικά. Αυτήη εφεύρεσηεπίσηςαφοράσεφαρμακευτικέςσυνθέσειςπουπεριλαμβάνουναυτέςτιςενώσεις. ΟιενώσειςκαιοιφαρμακευτικέςσυνθέσειςαυτήςτηςεφεύρεσηςείναιιδιαιτέρωςκατάλληλεςγιααναστολήδραστικότηταςπρωτεάσηςΗΙV-1 καιΗΙV-2 καιεπομένωςμπορείναχρησιμοποιηθούνωςαντι-ιικοίπαράγοντεςέναντιτωνΗΙV-1 καιΗIV-2 ιών. Αυτήη εφεύρεσηεπίσηςαφοράσεμεθόδουςγιααναστολήτηςδραστικότηταςασπαρτύλπρωτεάσηςΗIV χρησιμοποιώνταςτιςενώσειςαυτήςτηςεφεύρεσηςκαιμεθόδουςγιαδιαλογήενώσεωνγιααντι-ΗIV δραστικότητα.
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公开(公告)号：PL210227B1
公开(公告)日：2011-12-30
申请号：PL35283000
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , 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
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公开(公告)号：AT325091T
公开(公告)日：2006-06-15
申请号：AT00941279
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN
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 , C07C311/16 , C07C311/29
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：DE60027722D1
公开(公告)日：2006-06-08
申请号：DE60027722
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： HALE ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER FRANKLIN , BRIEGER 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: 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：CZ20014431A3
公开(公告)日：2002-06-12
申请号：CZ20014431
申请日：2000-06-08
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL ROBIN , TUNG ROGER , PRICE STEPHEN , WILKES ROBIN DAVID , SCHAIRER WAYNE CARL , JARVIS ASHLEY NICHOLAS , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , SAMANO VICENTE , KALDOR ISTVAN , MILLER JOHN FRANKLIN , BRIEGER MICHAEL STEPHEN
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 , C07C311/16 , C07C311/29
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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