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公开(公告)号：EA003509B1
公开(公告)日：2003-06-26
申请号：EA200000703
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 WIECZYSLAW , 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 , C07C311/16 , A61K31/63 , A61K31/635 , A61K31/665
Abstract: Настоящееизобретениеотноситсяк пролекарствамклассасульфонамидов, которыепредставляютсобойингибиторыаспартилпротеаз. Водномизвоплощенийданноеизобретениеотноситсяк новомуклассупролекарств, являющихсяингибиторамиаспартилпротеазВИЧ, характеризующихсяхорошейводорастворимостью, высокойбиологическойдоступностьюприпероральномприменениии легкимвоспроизведением in vivo активногокомпонента. Данноеизобретениетакжеотноситсяк фармацевтическимкомпозициям, содержащимданныепролекарства. Пролекарствои фармацевтическиепрепаратыподанномуизобретениюявляютсянаиболееподходящимидляснижениялекарственнойнагрузкии большегоудобствапациентов. Данноеизобретениетакжеотноситсяк способамлечениямлекопитающихданнымипролекарствамии фармацевтическимикомпозициями .
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公开(公告)号：PT969828E
公开(公告)日：2003-01-31
申请号：PT98910204
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , LI BIQIN , SU MICHAEL SHIN-SAN
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公开(公告)号：CA2143208C
公开(公告)日：2003-01-07
申请号：CA2143208
申请日：1993-09-07
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , MURCKO MARK A , BHISETTI GOVINDA RAO
IPC: G01N33/53 , A61K31/16 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/255 , A61K31/27 , A61K31/325 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/35 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/63 , A61K38/00 , A61K38/55 , A61P31/12 , A61P31/18 , C07C307/02 , C07C307/06 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/39 , C07C311/41 , C07C311/46 , C07D207/12 , C07D207/26 , C07D207/27 , C07D207/28 , C07D209/08 , C07D209/10 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D239/54 , C07D263/24 , C07D271/08 , C07D277/20 , C07D277/36 , C07D295/12 , C07D305/12 , C07D307/12 , C07D307/14 , C07D307/20 , C07D307/52 , C07D307/64 , C07D307/79 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/14 , C07G99/00 , C07K5/078 , G01N33/569 , C07D271/12 , C07D407/12 , A61K31/33
Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors, of formula (I). 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 com- pounds and pharmaceutical compositions of this invention are particularly we ll suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as antiviral 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：BG63677B1
公开(公告)日：2002-09-30
申请号：BG10204897
申请日：1997-11-17
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D
IPC: C07D307/14 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/42 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/535 , A61K38/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07D207/26 , C07D209/08 , C07D213/30 , C07D215/48 , C07D231/14 , C07D239/22 , C07D263/24 , C07D271/08 , C07D277/36 , C07D307/12 , C07D307/20 , C07D307/52 , C07D307/64 , C07D307/79 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D521/00 , C07K5/078 , A61K31/16 , C07D307/66
Abstract: The invention relates to tetrahydrofuran-containing sulphonamides having the general from shown in the description which are inhibitors of aspatylprotease, and to pharmaceutical compositions containing these compounds. In particular they are very suitable for the inhibition of HIV-1 and HIV-2 protease activity and can be used as antiviral medicaments against HIV-1 and HIV-2 viruses. The invention also relates to methods for the inhibition of the activity of HIV aspartylprotease. 44 claims
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公开(公告)号：AT223214T
公开(公告)日：2002-09-15
申请号：AT98910204
申请日：1998-03-10
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , LI BIQIN , SU MICHAEL SHIN-SAN
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Patent Agency Ranking
公开(公告)号：HK1042892A1
公开(公告)日：2002-08-30
申请号：HK02102257
申请日：1998-09-22
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , BHISETTI GOVINDA RAO
IPC: C07D20060101 , A61K20060101 , A61P20060101
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公开(公告)号：AT212344T
公开(公告)日：2002-02-15
申请号：AT96913811
申请日：1996-04-18
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , BHISETTI GOVINDA RAO
IPC: A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61P31/12 , A61P43/00 , C07D307/20 , C07D309/12 , C07D317/24 , C07D319/06 , C07D493/04
Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. 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.
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公开(公告)号：NO20016034L
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
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：EA001915B1
公开(公告)日：2001-10-22
申请号：EA199900388
申请日：1997-10-17
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , HARBESON SCOTT L , DEININGER DAVID D , BHISETTI GOVANDA RAO , FARMER LUC J
IPC: A61K38/00 , A61K38/08 , C07K5/02 , C07K5/10 , C07K5/117 , C07K7/02 , C07K7/06 , A61K38/55 , A61K38/04 , A61P1/16
Abstract: Настоящееизобретениеотноситсяк соединениям, способами фармацевтическимкомпозициямдляингибированияпротеаз, втомчислесерин-протеаз, вчастности NS3 протеазвирусагепатитаС (HCV). Соединения, композициии способыс ихиспользованиеммогутбытьпримененыотдельноилив сочетаниидляингибированиявирусов, вчастностивирусагепатитаС (HCV).
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公开(公告)号：PL342113A1
公开(公告)日：2001-05-21
申请号：PL34211398
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: 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
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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