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公开(公告)号：AU3309395A
公开(公告)日：1996-01-11
申请号：AU3309395
申请日：1995-10-06
Applicant: VERTEX PHARMA
Inventor： ARMISTEAD DAVID M , BOGER JOSHUA S , MEYERS HAROLD V , SAUNDERS JEFFREY O , TUNG ROGER D
IPC: A61K31/34 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61P25/02 , A61P37/06 , C07C233/56 , C07C235/12 , C07C235/34 , C07D207/08 , C07D207/16 , C07D211/60 , C07D307/54 , C07D317/60 , C07D333/24 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D409/06 , A61K31/335
Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
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公开(公告)号：CZ58795A3
公开(公告)日：1995-12-13
申请号：CZ58795
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：AP390A
公开(公告)日：1995-08-02
申请号：AP9300572
申请日：1993-09-08
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 , C07D239/72
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 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 aspartly protease using the compounds of this invention and methods for screening compounds for ant-hiv activity
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公开(公告)号：HU9500685D0
公开(公告)日：1995-04-28
申请号：HU9500685
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：CA2217745C
公开(公告)日：2011-07-05
申请号：CA2217745
申请日：1996-04-18
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , BHISETTI GOVINDA RAO
IPC: C07D493/04 , A61K31/33 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61P31/12 , A61P43/00 , C07D307/20 , C07D309/12 , C07D317/24 , C07D319/06 , C07D405/12 , C07D405/14 , C07D407/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00
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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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：PL1677827T3
公开(公告)日：2009-06-30
申请号：PL04810032
申请日：2004-10-27
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , CHANDORKAR GURUDATT , PERNI ROBERT B
IPC: A61K45/00 , A61K31/7056 , A61K38/21 , A61K45/06
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公开(公告)号：ES2319775T3
公开(公告)日：2009-05-12
申请号：ES04810032
申请日：2004-10-27
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , CHANDORKAR GURUDATT , PERNI ROBERT B
IPC: A61K45/00 , A61K31/7056 , A61K38/21 , A61K45/06
Abstract: Una composición farmacéutica que comprende: (a) el inhibidor de la proteasa NS3 4A del virus de la hepatitis un estereoisómero del mismo o una sal del mismo farmacéuticamente aceptable; (b) ritonavir o una sal del mismo farmacéuticamente aceptable; y (c) un vehículo farmacéuticamente aceptable.
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公开(公告)号：NZ542664A
公开(公告)日：2009-03-31
申请号：NZ54266404
申请日：2004-03-03
Applicant: VERTEX PHARMA
Inventor： GONZALES JESUS E , 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 disclosure relates to quinazoline compounds of formula (IA-ii) useful as inhibitors of voltage-gated sodium channels and calcium channels, wherein the variables are as defined in the specification. Also described are pharmaceutically acceptable compositions comprising the compounds of formula (I) and their use for the manufacture of a medicament for treating or lessening the severity of a disease, disorder, or condition selected from acute, chronic, neuropathic, or inflammatory pain, arthritis, migraine, cluster headaches, trigeminal neuralgia, herpetic neuralgia, general neuralgias, epilepsy or an epilepsy condition, a neurodegenerative disorder, a psychiatric disorders such as anxiety and depression, myotonia, arrhythmia, a movement disorder, a neuroendocrine disorder, ataxia, multiple sclerosis, irritable bowel syndrome, or incontinence.
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公开(公告)号：SK286105B6
公开(公告)日：2008-03-05
申请号：SK51099
申请日：1997-10-17
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D , HARBESON SCOTT L , DEININGER DAVID D , MURCKO MARK A , BHISETTI GOVINDA RAO , FARMER LUC J
IPC: C07K5/00 , A61K38/00 , A61K38/08 , C07K5/02 , C07K5/10 , C07K5/117 , C07K7/00 , C07K7/02 , C07K7/06
Abstract: The present invention relates to compounds of general formula (II), and pharmaceutical compositions containing them, for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds and the compositions can be used particularly for treating a hepatitis C viral infection and other viral infection with serine protease dependent proliferation.
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