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公开(公告)号：WO0047551A3
公开(公告)日：2001-08-16
申请号：PCT/US0003288
申请日：2000-02-09
Applicant: VERTEX PHARMA , HALE MICHAEL R , BAKER CHRISTOPHER T , STAMMERS TIMOTHY A , SHERRILL RONALD G , SPALTENSTEIN ANDREW , FURFINE ERIC S , MALTAIS FRANCOIS , ANDREWS CLARENCE WEBSTER III , MILLER JOHN F , SAMANO VICENTE
Inventor： HALE MICHAEL R , BAKER CHRISTOPHER T , STAMMERS TIMOTHY A , SHERRILL RONALD G , SPALTENSTEIN ANDREW , FURFINE ERIC S , MALTAIS FRANCOIS , ANDREWS CLARENCE WEBSTER III , MILLER JOHN F , SAMANO VICENTE
IPC: C07D317/28 , A61K9/20 , A61K9/48 , A61K31/27 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/5377 , A61K31/662 , A61P31/14 , A61P31/18 , A61P43/00 , C07B53/00 , C07C271/20 , C07C271/22 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/20 , C07D317/62 , C07D319/06 , C07D409/12 , C07D493/04 , C07F9/6561 , A61K31/18 , A61K31/665 , C07D407/12
CPC classification number: C07D493/04 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07C2601/08 , C07C2601/14 , C07D307/20 , C07D317/14 , C07D319/06 , C07D319/18 , C07D407/12 , C07F9/6561
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.
Abstract translation: 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶的活性的方法和用于筛选抗HIV活性化合物的方法。
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公开(公告)号：WO9965870A3
公开(公告)日：2001-03-15
申请号：PCT/US9913744
申请日：1999-06-17
Applicant: VERTEX PHARMA , SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
Inventor： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
IPC: A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , C07F9/6561 , A61K31/27 , A61K31/34 , A61K31/395 , C07D215/48
CPC classification number: C07D213/30 , C07C311/48 , C07C311/49 , C07C2601/08 , C07C2601/14 , C07D215/48 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D309/22 , C07D319/06 , C07D401/12 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , C07F9/6561
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.
Abstract translation: 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶的活性的方法和用于筛选抗HIV活性化合物的方法。
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3.发明专利
公开(公告)号：HU9901024A2
公开(公告)日：1999-09-28
申请号：HU9901024
申请日：1997-01-22
Applicant: VERTEX PHARMA
Inventor： ANDREWS CLARENCE WEBSTER III , BAKER CHRISTOPHER TODD , BHISETTI GOVINDA RAO , DEININGER DAVID D , KAZMIERSKI WIESLAW M , SALITURO FRANCESCO GERALD , SPALTENSTEIN ANDREW , TUNG ROGER DENNIS
IPC: C07D233/32 , A61K31/00 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/407 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4192 , A61K31/425 , A61K31/427 , A61K31/433 , A61K31/435 , A61K31/4353 , A61K31/437 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5365 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61P31/00 , A61P31/18 , A61P43/00 , C07D207/26 , C07D207/27 , C07D207/36 , C07D209/54 , C07D233/36 , C07D241/06 , C07D241/36 , C07D265/28 , C07D265/32 , C07D265/34 , C07D275/02 , C07D285/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/10 , C07D491/107 , C07D498/04 , C07D513/04 , C07D207/267 , A61K31/395 , C07D241/08
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公开(公告)号：AT311391T
公开(公告)日：2005-12-15
申请号：AT00913402
申请日：2000-02-09
Applicant: VERTEX PHARMA
Inventor： HALE MICHAEL R , BAKER CHRISTOPHER T , STAMMERS TIMOTHY A , SHERRILL RONALD G , SPALTENSTEIN ANDREW , FURFINE ERIC S , MALTAIS FRANCOIS , ANDREWS CLARENCE WEBSTER III , MILLER JOHN F , SAMANO VICENTE
IPC: C07D317/28 , A61K9/20 , A61K9/48 , A61K31/27 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/5377 , A61K31/662 , A61P31/14 , A61P31/18 , A61P43/00 , C07B53/00 , C07C271/20 , C07C271/22 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/18 , C07D307/20 , C07D317/62 , C07D319/06 , C07D409/12 , C07D493/04 , C07F9/6561 , C07D407/12
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公开(公告)号：HK1037605A1
公开(公告)日：2002-02-15
申请号：HK01106764
申请日：2001-09-25
Applicant: VERTEX PHARMA
Inventor： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , LOWEN GREGORY THOMAS , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III
IPC: A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , C07F9/6561 , C07C
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：CA2335477A1
公开(公告)日：1999-12-23
申请号：CA2335477
申请日：1999-06-17
Applicant: VERTEX PHARMA
Inventor： FURFINE ERIC STEVEN , SPALTENSTEIN ANDREW , LOWEN GREGORY THOMAS , ANDREWS CLARENCE WEBSTER III , SHERRILL RONALD GEORGE , HALE MICHAEL R
IPC: A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , C07F9/6561
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 f or 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：CZ9802344A3
公开(公告)日：1998-10-14
申请号：CZ234498
申请日：1997-01-22
Applicant: VERTEX PHARMA
Inventor： TUNG ROGER DENNIS , SALITURO FRANCESCO GERALD , DEININGER DAVID D , BHISETTI GOVINDA RAO , BAKER CHRISTOPHER TODD , SPALTENSTEIN ANDREW , KAZMIERSKI WIESLAW M , ANDREWS CLARENCE WEBSTER III
IPC: C07D233/32 , A61K31/00 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/407 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4192 , A61K31/425 , A61K31/427 , A61K31/433 , A61K31/435 , A61K31/4353 , A61K31/437 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5365 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61P31/00 , A61P31/18 , A61P43/00 , C07D207/26 , C07D207/27 , C07D207/36 , C07D209/54 , C07D233/36 , C07D241/06 , C07D241/36 , C07D265/28 , C07D265/32 , C07D265/34 , C07D275/02 , C07D285/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/10 , C07D491/107 , C07D498/04 , C07D513/04
CPC classification number: C07D207/27 , C07D233/36 , C07D265/32 , C07D265/34 , C07D285/10 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D491/10
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公开(公告)号：CA2243121A1
公开(公告)日：1997-07-31
申请号：CA2243121
申请日：1997-01-22
Applicant: VERTEX PHARMA
Inventor： ANDREWS CLARENCE WEBSTER III , DEININGER DAVID D , TUNG ROGER DENNIS , SALITURO FRANCESCO GERALD , KAZMIERSKI WIESLAW M , SPALTENSTEIN ANDREW , BAKER CHRISTOPHER TODD , BHISETTI GOVINDA RAO
IPC: C07D233/32 , A61K31/00 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/407 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4192 , A61K31/425 , A61K31/427 , A61K31/433 , A61K31/435 , A61K31/4353 , A61K31/437 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5365 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61P31/00 , A61P31/18 , A61P43/00 , C07D207/26 , C07D207/27 , C07D207/36 , C07D209/54 , C07D233/36 , C07D241/06 , C07D241/36 , C07D265/28 , C07D265/32 , C07D265/34 , C07D275/02 , C07D285/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/10 , C07D491/107 , C07D498/04 , C07D513/04 , A61K31/395 , C07D241/08 , C07D265/36 , C07D413/04 , C07D493/04 , C07D495/04
Abstract: This invention relates to a novel class of compounds of formula (I) that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of 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 aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention. A compound according to formula (I) wherein each Z is (a) or (b) or (c) wherein any Z may be optionally fused with R6; each X and X' is independently selected from the group consisting of C-C(O)-, C(O)C(O)-, -S(O)- and -S(O)2; each Y and Y' is independently selected from the group consisting of -(C(R2)2)p-, -NR2-, -(C(CR2)2)p-M-, C=C(R2)2, and -N(R2)-CH2-.
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公开(公告)号：AU767728B2
公开(公告)日：2003-11-20
申请号：AU4576099
申请日：1999-06-17
Applicant: VERTEX PHARMA
Inventor： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
IPC: A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , C07F9/6561
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：AU4576099A
公开(公告)日：2000-01-05
申请号：AU4576099
申请日：1999-06-17
Applicant: VERTEX PHARMA
Inventor： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
IPC: A61P31/18 , C07C303/00 , C07C311/48 , C07C311/49 , C07D213/30 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D241/42 , C07D243/04 , C07D265/02 , C07D277/30 , C07D307/20 , C07D309/06 , C07D309/12 , C07D319/06 , C07D405/12 , C07D407/12 , C07D413/06 , C07D417/12 , C07D493/04 , C07F9/6561
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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