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1. 发明申请

WO0146150A3 QUINOLONE COMPOUNDS FOR USE IN TREATING VIRAL INFECTIONS 审中-公开
标题翻译：喹诺酮化合物用于治疗病毒感染
公开(公告)号：WO0146150A3
公开(公告)日：2001-11-29
申请号：PCT/US0033930
申请日：2000-12-15
申请人： GLAXO GROUP LTD , ANDREWS CLARENCE WEBSTER III , FREEMAN GEORGE ANDREW , HOPKINS ANDREW LEE
发明人： ANDREWS CLARENCE WEBSTER III , FREEMAN GEORGE ANDREW , HOPKINS ANDREW LEE
IPC分类号： A61K9/08 , A61K9/10 , A61K9/20 , A61K9/48 , A61K31/4375 , A61K31/4704 , A61K31/4706 , A61K31/4709 , A61P31/12 , A61P31/18 , C07D215/22 , C07D215/227 , C07D215/36 , C07D215/42 , C07D215/48 , C07D405/12 , C07D471/04
CPC分类号： C07D215/227 , C07D215/22 , C07D215/36 , C07D215/42 , C07D215/48 , C07D405/12 , C07D471/04
摘要： The present invention relates to quinolone compounds, such as compounds of formula (Ia) wherein: R is hydrogen; R is oxygen or sulfur; R is trifluoromethyl; cyano; C1-8alkyl optionally substituted with C1-8alkyl or trifluoromethyl; or OR , wherein R is C1-8alkyl optionally substituted with C1-8alkyl; R is OR , wherein R is C2-8alkenyl optionally substituted with C1-8alkyl; C1-8alkyl optionally substituted with C1-8alkyl; C6-14arylalkyl; C3-6cycloalkyl; C3-6cycloalkylalkyl; heterocyclealkyl; heterocyclealkynyl; C3-6cycloalkylalkenyl; C6-14arylalkynyl; C3-6cycloalkylalkynyl; SR , wherein R is C3-6cycloalkyl; S(O)R , wherein R is C3-6cycloalkyl; or NR R wherein R and R , which may be the same or different, are hydrogen or C1-8alkyl, optionally substituted with C1-8alkyl; R is hydrogen; nitro; halogen; C1-8alkyl, optionally substituted with C1-8alkyl or trifluoromethyl; R is hydrogen; halogen; C1-8alkyl; cyano: trifluoromethyl; or OR wherein R is C1-8alkyl or trifluoromethyl; R is hydrogen; C1-8alkyl; halogen; C6-14aryl; C1-8alkylaryl; C2-8alkynyl; heteroaryl; or OR wherein R is C1-8alkyl; R is hydrogen; halogen; cyano; nitro; or OR , wherein R is hydrogen or C1-8alkyl optionally substituted with C1-8alkyl or trifluoromethyl; and their use in the treatment of viral infections.
摘要翻译：本发明涉及喹诺酮化合物，例如式（Ia）化合物，其中：R 1是氢; R 2是氧或硫; R 3是三氟甲基; 氰基; 任选被C 1-8烷基或三氟甲基取代的C 1-8烷基; 或OR 15，其中R 15是任选被C 1-8烷基取代的C 1-8烷基; R 4是OR 11，其中R 11是任选被C 1-8烷基取代的C 2-8烯基; 任选被C 1-8烷基取代的C 1-8烷基; C6-14arylalkyl; 3-6环; C3-6cycloalkylalkyl; 杂环烷基; heterocyclealkynyl; C3-6cycloalkylalkenyl; C6-14arylalkynyl; C3-6cycloalkylalkynyl; SR 12，其中R 12是C 3-6环烷基; S（O）R 12，其中R 12是C 3-6环烷基; 或NR 13 R 14，其中R 13和R 14可以相同或不同，是任选被C 1-8烷基取代的氢或C 1-8烷基; R 5是氢; 硝基; 卤素; 任选被C 1-8烷基或三氟甲基取代的C 1-8烷基; R 6是氢; 卤素; C1-8烷基; 氰基：三氟甲基; 或OR 10，其中R 10为C 1-8烷基或三氟甲基; R 7是氢; C1-8烷基; 卤素; C 6-14芳基; C1-8alkylaryl; C 2-8炔基; 杂; 或OR 9，其中R 9为C 1-8烷基; R 8是氢; 卤素; 氰基; 硝基; 或OR 16，其中R 16是氢或任选被C 1-8烷基或三氟甲基取代的C 1-8烷基; 并用于治疗病毒感染。

2. 发明申请

WO2009020457A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2009020457A2
公开(公告)日：2009-02-12
申请号：PCT/US2007/071056
申请日：2007-06-13
申请人： SMITHKLINE BEECHAM CORPORATION , ANDREWS, Clarence, Webster, III , CAO, Ping , FREEMAN, George, Andrew , QU, Junya
发明人： ANDREWS, Clarence, Webster, III , CAO, Ping , FREEMAN, George, Andrew , QU, Junya
IPC分类号： A61K31/513
CPC分类号： C07D417/04 , C07D239/22 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to dihydropyrimidine derivatives that are non- nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Such dihydropyrimidine derivatives are useful in the treatment of human immunodeficiency virus infection.
摘要翻译：本发明涉及非核苷逆转录酶抑制剂的二氢嘧啶衍生物及其制备和使用方法。这种二氢嘧啶衍生物可用于治疗人类免疫缺陷病毒感染。

3. 发明申请

WO0047551A3 INHIBITORS OF ASPARTYL PROTEASE 审中-公开
标题翻译： ASPARTYL PROTEASE的抑制剂
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
申请人： 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
发明人： 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分类号： 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分类号： 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
摘要： 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.
摘要翻译：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。

4. 发明申请

WO9965870A3 SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE 审中-公开
标题翻译： ASPARTYL PROTEASE的磺酰胺抑制剂
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
申请人： VERTEX PHARMA , SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
发明人： SHERRILL RONALD GEORGE , HALE MICHAEL R , SPALTENSTEIN ANDREW , FURFINE ERIC STEVEN , ANDREWS CLARENCE WEBSTER III , LOWEN GREGORY THOMAS
IPC分类号： 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分类号： 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
摘要： 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.
摘要翻译：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。

5. 发明申请

WO1997027180A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO1997027180A1
公开(公告)日：1997-07-31
申请号：PCT/US1997001610
申请日：1997-01-22
申请人： VERTEX PHARMACEUTICALS INCORPORATED , TUNG, Roger, Dennis , SALITURO, Francesco, Gerald , DEININGER, David, D. , BHISETTI, Govinda, Rao , BAKER, Christopher, Todd , SPALTENSTEIN, Andrew , KAZMIERSKI, Wieslaw, M. , ANDREWS, Clarence, Webster, III
发明人： VERTEX PHARMACEUTICALS INCORPORATED
IPC分类号： C07D233/36
CPC分类号： 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
摘要： 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 R ; 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(R )2)p-, -NR -, -(C(CR )2)p-M-, C=C(R )2, and -N(R )-CH2-.
摘要翻译：本发明涉及新型的式（I）化合物，其为天冬氨酰蛋白酶抑制剂。在一个实施方案中，本发明涉及以特异性结构和物理化学特征为特征的新型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的化合物和组合物来抑制天冬氨酰蛋白酶活性的方法和治疗病毒感染的方法。根据式（I）的化合物，其中每个Z是（a）或（b）或（c），其中任何Z可以任选地与R 6稠合; 每个X和X'独立地选自C-C（O） - ， - C（O）C（O） - ， - S（O） - 和-S（O）每个Y和Y'独立地选自 - （C（R 2）2）p - ， - NR 2 - ， - （C（CR 2）2）p M-，C = C（R 2）2和-N（R 2）-CH 2 - 。

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