-
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。
-
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。
-
公开(公告)号：WO2005042020A3
公开(公告)日：2005-06-23
申请号：PCT/US2004035549
申请日：2004-10-27
Applicant: VERTEX PHARMA , TUNG ROGER D , CHANDORKAR GURUDATT , PERNI ROBERT B
Inventor： TUNG ROGER D , CHANDORKAR GURUDATT , PERNI ROBERT B
IPC: A61K31/7056 , A61K38/21 , A61K45/00 , A61K45/06
CPC classification number: A61K45/06 , A61K31/496 , A61K31/7056 , A61K38/21 , A61K38/2292 , A61K2300/00
Abstract: The present invention relates to co-administering a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The combination acts by interfering with the life cycle of the hepatitis C virus and is therefore useful as an antiviral therapy. As such, the combination may be used for treating or preventing Hepatitis C infections in patients. The invention also relates to compositions comprising the combination of inhibitors. The invention also relates to kits and pharmaceutical packs comprising a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The invention also relates to processes for preparing these compositions, combinations, kits, and packs.
Abstract translation: 本发明涉及共同给予丙型肝炎病毒NS3 / 4A蛋白酶抑制剂和细胞色素P450单加氧酶抑制剂。 该组合通过干扰丙型肝炎病毒的生命周期起作用，因此可用作抗病毒疗法。 如此，该组合可用于治疗或预防患者的丙型肝炎感染。 本发明还涉及包含抑制剂组合的组合物。 本发明还涉及包含丙型肝炎病毒NS3 / 4A蛋白酶抑制剂和细胞色素P450单加氧酶抑制剂的试剂盒和药物包装。 本发明还涉及制备这些组合物，组合物，试剂盒和包装的方法。
-
公开(公告)号：WO2004108133A3
公开(公告)日：2005-03-31
申请号：PCT/US2004017779
申请日：2004-06-04
Applicant: VERTEX PHARMA , MAKINGS LEWIS R , GROOTENHUIS PETER , HURLEY DENNIS JAMES , TUNG ROGER D , TERMIN ANDREAS P
Inventor： MAKINGS LEWIS R , GROOTENHUIS PETER , HURLEY DENNIS JAMES , TUNG ROGER D , TERMIN ANDREAS P
IPC: A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/497 , A61K31/501 , A61K31/506 , A61P1/00 , A61P11/00 , A61P11/06 , A61P13/10 , A61P17/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P43/00 , C07D231/56 , C07D235/06 , C07D235/26 , C07D241/44 , C07D263/58 , C07D277/68 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/02 , C07D498/02
CPC classification number: A61K31/497 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/501 , A61K31/506 , C07D231/56 , C07D235/06 , C07D235/26 , C07D241/44 , C07D263/58 , C07D277/68 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: The present invention relates to compounds useful as modulators of the vanilloid receptor, and also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Abstract translation: 本发明涉及可用作香草素受体调节剂的化合物，并且还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。
-
公开(公告)号：HU228198B1
公开(公告)日：2013-01-28
申请号：HU9500685
申请日：1993-09-07
Applicant: VERTEX PHARMA
Inventor： BHISETTI GOVINDA RAO , MURCKO MARK A , TUNG ROGER D
IPC: C07D215/48 , 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 , 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.
-
Patent Agency Ranking
公开(公告)号：AU2004217891B2
公开(公告)日：2011-06-23
申请号：AU2004217891
申请日：2004-03-03
Applicant: VERTEX PHARMA
Inventor： DEWEY FANNING LEV TYLER , TUNG ROGER D , YULIAN ZHANG , GONZALES JESUS E III , PETER TERMIN ANDREAS , DONALD NEUBERT TIMOTHY , ESTHER MARTINBOROUGH , JOHN PETZOLDT BENJAMIN , JAN GROOTENHUIS PETER DIEDERIK , MITCHELL WILSON DEAN , NICOLE ZIMMERMANN
IPC: C07D239/94 , A61K31/517 , A61K31/5377 , A61K31/541 , C07D20060101 , C07D239/91 , 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 R, X, R, x, and ring A are as defined in the present application.
-
公开(公告)号：CZ301653B6
公开(公告)日：2010-05-12
申请号：CZ20002363
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 MIECZYSLAV , SPALTENSTEIN ANDREW
IPC: C07C311/15 , A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/425 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/18 , C07C311/37 , C07D277/30 , C07D277/36 , C07D307/20 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/26
Abstract: Sulfonamidové deriváty obecného vzorce I nebo XXIII, jejichž symboly mají specifický význam, a farmaceutické prostredky s jejich obsahem. Tyto deriváty jsou proléciva ze trídy sulfonamidu, která jsou inhibitory aspartylproteázy, napr. HIV aspartylproteázy, a vyznacují se výhodnou rozpustností ve vode, vysokou biologickou využitelností pri perorálním podávání a snadnou in vivo generací aktivní složky. Proléciva a farmaceutické prostredky podle vynálezu jsou zvlášte vhodné pro snížení zatížení pilulkami a zlepšení spolupráce pacienta.
-
公开(公告)号：DE602004024873D1
公开(公告)日：2010-02-11
申请号：DE602004024873
申请日：2004-03-03
Applicant: VERTEX PHARMA
Inventor： GONZALES JESUS E , WILSON DEAN MITCHELL , TERMIN ANDREAS PETER , GROOTENHUIS PETER DIEDERIK , ZHANG YULIAN , PETZOLDT BENJAMIN JOHN , FANNING LEV TYLER , NEUBERT TIMOTHY DONALD , TUNG ROGER D , MARTINBOROUGH ESTHER , ZIMMERMANN NICOLE
IPC: C07D239/94 , A61K31/517 , A61K31/5377 , A61K31/541 , C07D20060101 , C07D239/91 , 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.
-
公开(公告)号：CA2217737C
公开(公告)日：2009-04-07
申请号：CA2217737
申请日：1996-04-18
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER D
IPC: C07D307/14 , C07D307/18 , A61K31/33 , 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 , C07D405/14 , C07D407/00 , C07D407/12 , C07D409/00 , C07D409/12 , C07D409/14 , C07D411/00 , C07D413/00 , C07D413/12 , C07D413/14 , C07D417/00 , C07D417/12 , C07D493/04 , C07D521/00 , C07K5/078
Abstract: The present invention relates to a class of THF-containing sulfonamides whic h 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 activit y 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.
-
公开(公告)号：DE60230044D1
公开(公告)日：2009-01-08
申请号：DE60230044
申请日：2002-06-11
Applicant: VERTEX PHARMA
Inventor： COCHRAN JOHN E , TUNG ROGER D
IPC: A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/551 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/00 , A61P7/02 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D217/12 , C07D217/18 , C07D217/22 , C07D217/24 , C07D401/04
Abstract: The present invention relates to inhibitors (Ia-Ib) of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders. All substituents are as in claim 1.
-
-
-
-
-
-
-
-
-
Search Results
300
records
(took 0.028 seconds)
