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1.
公开(公告)号:US5403937A
公开(公告)日:1995-04-04
申请号:US55268
申请日:1993-04-30
申请人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Russell E. Pike , Haiyan Wang , Raymond G. Lovey , Yi-Tsung Liu , Ashit K. Ganguly , William B. Morgan , Aleksey Zaks
发明人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Russell E. Pike , Haiyan Wang , Raymond G. Lovey , Yi-Tsung Liu , Ashit K. Ganguly , William B. Morgan , Aleksey Zaks
IPC分类号: C07C69/63 , C07C69/65 , C07D263/26 , C07D307/12 , C07D405/06 , C07D413/06 , C07D417/06 , C07D521/00 , C12P7/04 , C12P7/62 , C12P41/00 , C07D249/08
CPC分类号: C07D249/08 , C07C69/63 , C07C69/65 , C07D231/12 , C07D233/56 , C07D263/26 , C07D307/12 , C07D405/06 , C07D413/06 , C07D417/06 , C12P41/004 , C12P7/62 , Y02P20/55
摘要: Disclosed is a process for preparing chiral compounds of the formula (I) ##STR1## wherein: X.sup.1 and X.sup.2 are independently F or Cl; and E is --SO.sub.2 R.sup.2, wherein R.sup.2 is C.sub.1 -C.sub.6 alkyl, --C.sub.6 H.sub.4 CH.sub.3 or --CF.sub.3 ; its enantiomer and racemates thereof, useful in the synthesis of tetrahydrofuran azole antifungals. Novel compounds of the formula ##STR2## wherein: X.sup.1 and X.sup.2 are independently F or Cl; B represents --C(O)Q* or --CH.sub.2 OR"; Q* represents a chiral auxiliary group; R" represents a hydroxy protecting group selected from --CH.sub.2 C.sub.6 H.sub.5, or --C(O)R.sup.1, wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl; and A represents Cl, Br, I or triazolyl; are also disclosed.
摘要翻译: 公开了制备式(I)的手性化合物(I)的方法,其中:X 1和X 2独立地是F或Cl; 并且E是-SO 2 R 2,其中R 2是C 1 -C 6烷基,-C 6 H 4 CH 3或-CF 3; 其对映体和外消旋体,可用于四氢呋喃唑类抗真菌剂的合成。 新颖的式(III)化合物或其成分:其中:X 1和X 2独立地为F或Cl; B表示-C(O)Q *或-CH 2 OR“; Q *表示手性辅助基团; R“表示选自-CH 2 C 6 H 5或-C(O)R 1的羟基保护基,其中R 1是C 1 -C 6烷基; A表示Cl,Br,I或三唑基; 也被披露。
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公开(公告)号:US5710154A
公开(公告)日:1998-01-20
申请号:US459225
申请日:1995-06-02
申请人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
发明人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
IPC分类号: C07D405/14 , A61K31/41 , A61K31/495 , A61K31/675 , A61P31/00 , A61P31/10 , C07D521/00 , C07F9/6558 , C07D413/14 , C07F9/6518
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586
摘要: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two groups convertible in vivo into hydroxy moieties, (e.g., a polyether ester, amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要翻译: 由式I表示的化合物其中X独立地为F或两者为Cl或一个X独立地为F,另一个独立地为Cl; R1是被体内转化成羟基的一个或两个基团(例如,其聚醚酯,氨基酸酯或磷酸酯)或其药学上可接受的盐和药学上可接受的盐取代的直链或支链(C3至C8)烷基 公开了可用于治疗和/或预防真菌感染的组合物。
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公开(公告)号:US5714490A
公开(公告)日:1998-02-03
申请号:US458543
申请日:1995-06-02
申请人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
发明人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
IPC分类号: C07D405/14 , A61K31/41 , A61K31/495 , A61K31/675 , A61P31/00 , A61P31/10 , C07D521/00 , C07F9/6558
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586
摘要: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two amino acid ester groups (e.g., an amino acid ester group convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要翻译: 由式I表示的化合物其中X独立地为F或两者为Cl或一个X独立地为F,另一个独立地为Cl; R1是被一个或两个氨基酸酯基(例如,在体内可转化为羟基的氨基酸酯基)或其药学上可接受的盐取代的直链或支链(C3至C8)烷基和其药物组合物 有用于治疗和/或预防真菌感染。
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公开(公告)号:US5703236A
公开(公告)日:1997-12-30
申请号:US458551
申请日:1995-06-02
申请人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
发明人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
IPC分类号: C07D405/14 , A61K31/41 , A61K31/495 , A61K31/675 , A61P31/00 , A61P31/10 , C07D521/00 , C07F9/6558
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586
摘要: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether ester (e.g., a polyetherester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要翻译: 由式I表示的化合物其中X独立地为F或两者为Cl或一个X独立地为F,另一个独立地为Cl; R1是被一个或两个羟基部分取代的直链或支链(C3至C8)烷基,其醚酯(例如,聚醚酯或磷酸酯)或其药学上可接受的盐和用于治疗和/ 或预防真菌感染。
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公开(公告)号:US5703079A
公开(公告)日:1997-12-30
申请号:US460400
申请日:1995-06-02
申请人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
发明人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
IPC分类号: C07D405/14 , A61K31/41 , A61K31/495 , A61K31/675 , A61P31/00 , A61P31/10 , C07D521/00 , C07F9/6558
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586
摘要: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two polyetyher ester groups (e.g., a polyether ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要翻译: 由式I表示的化合物其中X独立地为F或两者为Cl或一个X独立地为F,另一个独立地为Cl; R1是被一个或两个聚烯酯基团取代的直链或支链(C3至C8)烷基(例如,可在体内转化为羟基的聚醚酯)或其药学上可接受的盐和其用于治疗的药物组合物 和/或预防真菌感染。
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公开(公告)号:US5693626A
公开(公告)日:1997-12-02
申请号:US459145
申请日:1995-06-02
申请人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
发明人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
IPC分类号: C07D405/14 , A61K31/41 , A61K31/495 , A61K31/675 , A61P31/00 , A61P31/10 , C07D521/00 , C07F9/6558 , C07D413/14 , C07F9/6518
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586
摘要: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two phosphate ester groups (e.g., a phosphate ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要翻译: 由式I表示的化合物其中X独立地为F或两者为Cl或一个X独立地为F,另一个独立地为Cl; R1是被一个或两个磷酸酯基团取代的直链或支链(C3至C8)烷基(例如,可在体内转化为羟基的磷酸酯)或其药学上可接受的盐和用于治疗的药物组合物 和/或预防真菌感染。
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公开(公告)号:US5661151A
公开(公告)日:1997-08-26
申请号:US460752
申请日:1995-06-02
申请人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
发明人: Anil K. Saksena , Viyyoor M. Girijavallabhan , Raymond G. Lovey , Russell E. Pike , Haiyan Wang , Yi-Tsung Liu , Ashit K. Ganguly , Frank Bennett
IPC分类号: C07D405/14 , A61K31/41 , A61K31/495 , A61K31/675 , A61P31/00 , A61P31/10 , C07D521/00 , C07F9/6558 , C07D413/14 , C07F9/6518
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586
摘要: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether or ester thereof (e.g., a polyether ester amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要翻译: 由式I表示的化合物其中X独立地为F或两者为Cl或一个X独立地为F,另一个独立地为Cl; R1是被一个或两个羟基部分取代的直链或支链(C3至C8)烷基,其醚或酯(例如,聚醚酯氨基酸酯或磷酸酯)或其药学上可接受的盐和药物组合物 其用于治疗和/或预防真菌感染。
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8.
公开(公告)号:US07595299B2
公开(公告)日:2009-09-29
申请号:US11089192
申请日:2005-03-24
申请人: Anil Saksena , Viyyoor M. Girijavallabhan , Stephane L. Bogen , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. McCormick , Haiyan Wang , Russell E. Pike , Yi-Tsung Liu , Tin-Yau Chan , Zhaoning Zhu , Ashok Arasappan , Kevin X. Chen , Srikanth Venkatraman , Tejal Parekh , Patrick A. Pinto , Bama Santhanam , F. George Njoroge , Ashit K. Ganguly , Henry A. Vaccaro , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura
发明人: Anil Saksena , Viyyoor M. Girijavallabhan , Stephane L. Bogen , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. McCormick , Haiyan Wang , Russell E. Pike , Yi-Tsung Liu , Tin-Yau Chan , Zhaoning Zhu , Ashok Arasappan , Kevin X. Chen , Srikanth Venkatraman , Tejal Parekh , Patrick A. Pinto , Bama Santhanam , F. George Njoroge , Ashit K. Ganguly , Henry A. Vaccaro , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura
IPC分类号: A61K38/00
CPC分类号: C07K7/06 , A61K31/16 , A61K31/195 , A61K31/27 , A61K31/357 , A61K31/385 , A61K31/403 , A61K31/4164 , A61K31/445 , A61K38/05 , C07C205/51 , C07K5/101 , C07K7/02 , A61K2300/00
摘要: The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译: 本发明公开了具有HCV蛋白酶抑制活性的新型肽化合物及其制备方法。 在另一个实施方案中,本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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9.
公开(公告)号:US07244721B2
公开(公告)日:2007-07-17
申请号:US10052386
申请日:2002-01-18
申请人: Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. Mc Cormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry A. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang , Jesse K. Wong , Latha G. Nair
发明人: Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. Mc Cormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry A. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang , Jesse K. Wong , Latha G. Nair
IPC分类号: A61K31/497 , A61K31/407 , A61K31/454 , A61K31/4025
CPC分类号: C07K5/0804 , A61K38/00 , C07K5/0202 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译: 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中,本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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10.
公开(公告)号:USRE43298E1
公开(公告)日:2012-04-03
申请号:US13068159
申请日:2011-04-22
申请人: Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. McCormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry M. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang
发明人: Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. McCormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry M. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang
IPC分类号: A61K38/00 , A01N37/18 , A61P1/16 , A61P31/12 , A61K39/12 , G01N33/53 , A61K38/07 , A61K38/06 , C07K5/08 , C07K5/10
CPC分类号: C07K5/0202 , A61K38/00 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译: 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中,本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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