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1. 发明授权

US07244721B2 Peptides as NS3-serine protease inhibitors of hepatitis C virus 有权
标题翻译：肽作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
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。

2. 发明授权

US07012066B2 Peptides as NS3-serine protease inhibitors of hepatitis C virus 有权
公开(公告)号：US07012066B2
公开(公告)日：2006-03-14
申请号：US09908955
申请日：2001-07-19
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
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
IPC分类号： 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.

3. 发明申请

US20110117057A1 NOVEL PEPTIDES AS NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：新型肽作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
公开(公告)号：US20110117057A1
公开(公告)日：2011-05-19
申请号：US12973020
申请日：2010-12-20
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 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
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 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
IPC分类号： A61K38/06 , C07D207/16 , C07D403/10 , C07K5/083 , C07D209/42 , C07K5/107 , C07D215/48 , A61K38/05 , A61K38/07 , A61K38/21 , A61P31/14
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。

4. 再颁专利

USRE43298E1 Peptides as NS3-serine protease inhibitors of hepatitis C virus 有权
标题翻译：肽作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
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。

5. 发明授权

US07169760B2 Peptides as NS3-serine protease inhibitors of hepatitis C virus 有权
标题翻译：肽作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
公开(公告)号：US07169760B2
公开(公告)日：2007-01-30
申请号：US09909012
申请日：2001-07-19
申请人： Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Stephane L. Bogen , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. Mc Cormick , Haiyan Wang , Russell E. Pike , Yi-Tsung Liu , Tin-Yau Chan , Zhaoning Zhu , Ashok Arasappan , Kevin X. Chen , Srinkanth 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 K. Saksena , Viyyoor Moopil Girijavallabhan , Stephane L. Bogen , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. Mc Cormick , Haiyan Wang , Russell E. Pike , Yi-Tsung Liu , Tin-Yau Chan , Zhaoning Zhu , Ashok Arasappan , Kevin X. Chen , Srinkanth 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： A61K38/05 , A61K31/44 , A61K31/16 , A61K31/227
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。

6. 发明授权

US07595299B2 Peptides as NS3-serine protease inhibitors of hepatitis C virus 有权
标题翻译：肽作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
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。

7. 发明授权

US4956479A 23-deoxy-27-chloro derivatives of LL-F28249 compounds 失效
标题翻译： LL-F28249化合物的23-脱氧-27-氯衍生物
公开(公告)号：US4956479A
公开(公告)日：1990-09-11
申请号：US22848
申请日：1987-03-06
申请人： Susan Y. Tamura , Goro Asato
发明人： Susan Y. Tamura , Goro Asato
IPC分类号： A01N43/90 , A61K31/365 , A61P33/00 , C07D493/22 , C07H19/01 , C12P17/18 , C12R1/465
CPC分类号： C07H19/01 , A01N43/90 , C12P17/181 , C12R1/465
摘要： The present invention relates to novel derivatives of LL-F28249 compounds. These LL-F28249 compounds preferably are derived via a controlled microbiological fermentation of Streptomyces cyaneogriseus subspecies noncyanogenus having deposit accession number NRRL 15773. The 23-deoxy-27-halo(chloro) derivatives have the 23-hydroxy group of the LL-F28249 compounds replaced by hydrogen and a halogen such as chlorine in the 27-position with the double bond shifted to the 26,26'-position. The novel derivatives of the present invention possess activity as anthelmintic, ectoparasitic, insecticidal, acaricidal and nematicidal agents and are useful in areas of human and animal health and in agricultural crops. Compositions containing the present compounds also are presented herein.

8. 发明授权

US4876272A Mono- and diepoxide derivatives of LL-F28249 compounds 失效
标题翻译： LL-F28249化合物的单和二环氧化物衍生物
公开(公告)号：US4876272A
公开(公告)日：1989-10-24
申请号：US22849
申请日：1987-03-06
申请人： Goro Asato , Susan Y. Tamura
发明人： Goro Asato , Susan Y. Tamura
IPC分类号： C07D493/22 , A01N43/90 , A61K31/365 , A61P33/00 , C07H19/01
CPC分类号： C07H19/01 , A01N43/90
摘要： The present invention relates to novel mono- C(26,27) and diepoxide C(14,15;26,27) derivatives of LL-F28249.alpha., .beta., .epsilon., .zeta., .theta. and .iota. compounds. The LL-F28249 compounds (collectively) are isolates from the fermentation broth of Streptomyces cyaneogriseus subspecies noncyanogenus having deposit accession number NRRL-15773. The compounds of this present invention are derived by regioselective epoxidation of 5,23-0,0-bis-silylated LL-F28249 compounds at low temperature, followed by desilylation. These novel compounds have anthelmintic, insecticidal, ectoparasiticidal, nematicidal and acaricidal activity and also are useful intermediates for the preparation of further biologically active compounds. Compositions containing these described derivatives as active ingredients thereof are described.

9. 发明授权

US4886830A Mono- and diepoxide derivatives of 23-deoxyl-LL-F28249 compounds 失效
标题翻译： 23-脱氧-LL-F28249化合物的单和二环氧化物衍生物
公开(公告)号：US4886830A
公开(公告)日：1989-12-12
申请号：US22847
申请日：1987-03-06
申请人： Goro Asato , Susan Y. Tamura
发明人： Goro Asato , Susan Y. Tamura
IPC分类号： A01N43/90 , A61K31/365 , A61P33/00 , C07D493/22 , C07H19/01 , C12P17/18 , C12R1/465
CPC分类号： C07H19/01 , A01N43/90 , C12P17/181 , C12R1/465
摘要： The present invention relates to novel derivatives of LL-F28249 compounds wherein the 23-hydroxyl group is replaced with hydrogen and the double bond at the C(26,27)-position is epoxidized concomitant with or without epoxidation of the double bond at the C(14,15)-position. The LL-F28249 compounds (collectively) are isolates from the fermentation broth of Streptomyces cyaneogriseus subspecies noncyanogenus having deposit accession number NRRL 15773. The compounds of the present invention are derived by regioselective epoxidation of 5,23-O,O-bissilylated LL-F28249 compounds at low temperature, desilylation, re-silylation of the 5-hydroxyl group, thiocarbonylation of the 23-hydroxyl group, disilyation followed by tributyltin hydride reduction. The novel deoxy compounds of the present invention have anthelmintic, insecticidal, ectoparasiticidal, nematicidal and acaricidal activity. Compositions containing these described derivatives as active ingredients thereof are described herein.

10. 发明授权

US4886829A 23-Oxo (keto) and 23-imino derivatives of mono- and diepoxy LL-F28249 compounds 失效
标题翻译：单 - 和二环氧基LL-F28249化合物的23-氧代（酮）和23-亚氨基衍生物
公开(公告)号：US4886829A
公开(公告)日：1989-12-12
申请号：US22850
申请日：1987-03-06
申请人： Goro Asato , Susan Y. Tamura
发明人： Goro Asato , Susan Y. Tamura
IPC分类号： C07D493/22 , A01N43/90 , A01N47/24 , A01N47/34 , A01N47/44 , A61K31/365 , A61P33/00 , A61P33/10 , C07H19/01
CPC分类号： C07D493/22 , A01N43/90 , A01N47/24 , A01N47/34
摘要： The present invention relates to novel 23-oxo (keto) and 23-imino derivatives of certain C(26,27)-epoxy- and C(14,15;26,27)-diepoxy-LL-F28249 compounds. The LL-F28249 compounds (collectively) are isolates from the fermentation broth of Streptomyces cyaneogriseus subspecies noncyanogenus having deposit accession no. NRRL-15773. The derivatives are obtained by oxidation of the 23-hydroxy group of 5-O-silylated-C(26,27)-epoxy and C(14,15;26,27)diepoxy-LL-F28249 compounds, followed by desilylation and derivatization with amino compounds. The novel compounds have anthelmintic, ectoparasiticidal, nematicidal, insecticidal and acaricidal activity and are, therefore, useful in the treatment of infections in warm-blooded animals and infestations in agricultural crops. Compositions containing the present compounds as active ingredients thereof also are presented.
摘要翻译：本发明涉及某些C（26,27） - 环氧 - 和C（14,15; 26,27） - 二环氧-LL-F28249化合物的新型23-氧代（酮）和23-亚氨基衍生物。 LL-F28249化合物（共同）是具有存放登记号的非花青素Streptomyces cyaneogriseus亚种的发酵液的分离物。 NRRL-15773。衍生物通过氧化5-O-甲硅烷基化C（26,27） - 环氧基和C（14,15; 26,27）二环氧-LL-F28249化合物的23-羟基获得，然后脱甲硅烷基化和衍生化与氨基化合物。这种新型化合物具有驱虫，外寄生性杀线虫，杀线虫，杀虫和杀螨活性，因此可用于治疗温血动物感染和农作物侵染。还提供了含有本发明化合物作为其活性成分的组合物。

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