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公开(公告)号：IS2155B
公开(公告)日：2006-11-15
申请号：IS4574
申请日：1997-10-02
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D
IPC: C07D307/14 , A61K31/00 , 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
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公开(公告)号：NO20062428A
公开(公告)日：2006-05-29
申请号：NO20062428
申请日：2006-05-29
Applicant: VERTEX PHARMA
Inventor： PERNI ROBERT , TUNG ROGER D , CHANDORKAR GURUDATT
IPC: A61K31/7056 , A61K38/21 , A61K45/00 , A61K45/06
CPC classification number: A61K45/06 , A61K31/496 , A61K31/7056 , A61K38/21 , A61K38/2292 , A61K2300/00
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公开(公告)号：BRPI0408026A
公开(公告)日：2006-02-07
申请号：BRPI0408026
申请日：2004-03-03
Applicant: VERTEX PHARMA
Inventor： GONZALES JESUS E III , WILSON DEAN MITCHELL , TERMIN ANDREAS PETER , GROOTENHUIS PETER DIEDERIK JAN , ZHANG YULIAN , PETZOLDT BENJAMIN JOHN , FANNING LEV TYLER DEWEY , NEUBERT TIMOTHY DONALD , TUNG ROGER D , MARTINBOROUGH ESTHER , ZIMMERMANN NICOLE
IPC: A61K31/517 , A61K31/5377 , A61K31/541 , C07D20060101 , C07D239/91 , C07D239/94 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/02 , C07D413/12 , C07D417/02 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：SK284785B6
公开(公告)日：2005-11-03
申请号：SK143197
申请日：1996-04-18
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
Abstract: Described is a pharmaceutical composition comprising sulfonamide of general formula (I), wherein R1 is oxyorganic residue, D a D' is optionally always substituted aryl, optionally substituted carbocycle or optionally substituted heterocycle, optionally substituted C1-C5-alkyl or optionally substituted C2-C4-alkenyl, E is optionally substituted C3-C7-carbocycle, optionally substituted C6-C10-aryl, optionally phenyl substituted with fused heterocycle, optionally substituted heterocycle, optionally substituted hydroxy group, optionally substituted amino group, optionally substituted C1-C6-alkyl, optionally substituted C2-C6-alkenyl, which are aspartyl protease inhibitors. This pharmaceutical composition is suitable for inhibiting HIV-1 or HIV-2 protease activity and consequently may be used as anti-viral agents against the HIV-1 and HIV-2 viruses.
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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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Patent Agency Ranking
公开(公告)号：CA2517844A1
公开(公告)日：2004-09-16
申请号：CA2517844
申请日：2004-03-03
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , ZIMMERMANN NICOLE , TERMIN ANDREAS PETER , NEUBERT TIMOTHY DONALD , FANNING LEV TYLER DEWEY , WILSON DEAN MITCHELL , PETZOLDT BENJAMIN JOHN , GONZALES JESUS E III , GROOTENHUIS PETER DIEDERIK JAN , ZHANG YULIAN , MARTINBOROUGH ESTHER
IPC: A61K31/517 , A61K31/5377 , A61K31/541 , C07D20060101 , C07D239/91 , C07D239/94 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/02 , C07D413/12 , C07D417/02 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
Abstract: The present invention relates to quinazoline compounds of formula (I) useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. or a pharmaceutically acceptable derivative thereof, wherein R1, X, R3, x, and ring A are as defined in the present application.
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公开(公告)号：EE04307B1
公开(公告)日：2004-06-15
申请号：EE9700266
申请日：1996-04-18
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 present invention relates to a class of THF-containing 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：ES2200243T3
公开(公告)日：2004-03-01
申请号：ES98113921
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
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 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 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：CY2317B1
公开(公告)日：2003-11-14
申请号：CY0300013
申请日：2003-02-11
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
Abstract: The present invention relates to a class of THF-containing 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：PT885887E
公开(公告)日：2003-10-31
申请号：PT98113921
申请日：1993-09-07
Applicant: VERTEX PHARMA
Inventor： MURCKO MARK A , TUNG ROGER D , 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
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 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 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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