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21. 发明授权

US08178520B2 Macrocyclic compounds as antiviral agents 有权
标题翻译：大环化合物作为抗病毒剂
公开(公告)号：US08178520B2
公开(公告)日：2012-05-15
申请号：US12300887
申请日：2007-05-11
申请人： Maria Emilia Di Francesco , Emanuela Nizi , Paola Pace , Vincenzo Summa
发明人： Maria Emilia Di Francesco , Emanuela Nizi , Paola Pace , Vincenzo Summa
IPC分类号： A61K31/33 , A61K31/44 , A61K31/519 , A61K38/06 , C07K5/00 , C07D295/00 , C07D267/22 , C07D245/00
CPC分类号： C07K5/0806 , A61K38/00 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要： The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R1, Ra, Rb, R3, R4, M, Z, ring A and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
摘要翻译：本发明涉及式（I）的大环化合物：其中W，n，R 1，R a，R b，R 3，R 4，M，Z，环A和环B在本文中定义，及其药学上可接受的盐，它们及其用于治疗或预防丙型肝炎病毒感染的用途。

22. 发明申请

US20090258891A1 Macrocyclic Compounds As Antiviral Agents 有权
标题翻译：大环化合物作为抗病毒剂
公开(公告)号：US20090258891A1
公开(公告)日：2009-10-15
申请号：US12300887
申请日：2007-05-11
申请人： Maria Emilia Di Francesco , Emanuela Nizi , Paola Pace , Vincenzo Summa
发明人： Maria Emilia Di Francesco , Emanuela Nizi , Paola Pace , Vincenzo Summa
IPC分类号： A61K31/4748 , A61K31/4245 , C07D498/22
CPC分类号： C07K5/0806 , A61K38/00 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要： The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R1, Ra, Rb, R3, R4, M, Z, ring A and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
摘要翻译：本发明涉及式（I）的大环化合物：其中W，n，R 1，R a，R b，R 3，R 4，M，Z，环A和环B在本文中定义，及其药学上可接受的盐，它们及其用于治疗或预防丙型肝炎病毒感染的用途。

23. 发明申请

US20110257162A1 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：US20110257162A1
公开(公告)日：2011-10-20
申请号：US13172393
申请日：2011-06-29
申请人： Vincenzo Summa , Paola Pace , Philip Jones , Alessia Petrocchi , Maria del Rosario Rico Ferreira , Giuseppe Cecere
发明人： Vincenzo Summa , Paola Pace , Philip Jones , Alessia Petrocchi , Maria del Rosario Rico Ferreira , Giuseppe Cecere
IPC分类号： A61K31/551 , A61P31/18 , C07D513/04 , A61K31/542 , C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , C07D487/14 , C07D513/04 , C07D513/14
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein m, n, X, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中m，n，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10如本文所定义。该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防，治疗或延迟。这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

24. 发明授权

US07091209B2 Dihydroxypyridmidine carboxylic acids as viral polymerase inhibitors 失效
标题翻译：二羟基吡啶并咪唑羧酸作为病毒聚合酶抑制剂
公开(公告)号：US07091209B2
公开(公告)日：2006-08-15
申请号：US10333431
申请日：2001-07-11
申请人： Cristina Gardelli , Claudio Giuliano , Steven Harper , Uwe Koch , Frank Narjes , Jesus Maria Ontoria Ontoria , Marco Poma , Simona Ponzi , Ian Stansfield , Vincenzo Summa
发明人： Cristina Gardelli , Claudio Giuliano , Steven Harper , Uwe Koch , Frank Narjes , Jesus Maria Ontoria Ontoria , Marco Poma , Simona Ponzi , Ian Stansfield , Vincenzo Summa
IPC分类号： C07D239/557 , C07D409/04 , C07D409/12 , C07D417/14 , C07D401/12
CPC分类号： C07D239/557 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclicgroup; as well as compounds of formula (I) which are derivatized at one or more of the 4-hydroxy, 5-hydroxy or 6-carboxy groups; and tautomers thereof, and pharmaceutically acceptable salts or esters thereof; and inhibitors of viral polymerases, especially the hepatitis C virus (HCV) polymerase enzyme
摘要翻译：一类式（I）的2-芳基-4,5-二羟基-6-羧基嘧啶：其中Ar是任选取代的芳基或杂环基; 以及在一个或多个4-羟基，5-羟基或6-羧基衍生化的式（I）化合物; 及其互变异构体及其药学上可接受的盐或酯; 和病毒聚合酶抑制剂，特别是丙型肝炎病毒（HCV）聚合酶

25. 发明申请

US20130178413A1 HCV NS3 PROTEASE INHIBITORS 审中-公开
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：US20130178413A1
公开(公告)日：2013-07-11
申请号：US13825245
申请日：2011-09-16
申请人： John A. McCauley , Nigel J. Liverton , Michael T. Rudd , Kevin F. Gilbert , Marco Ferrara , Vincenzo Summa , Benedetta Crescenzi
发明人： John A. McCauley , Nigel J. Liverton , Michael T. Rudd , Kevin F. Gilbert , Marco Ferrara , Vincenzo Summa , Benedetta Crescenzi
IPC分类号： A61K38/07 , C07K5/103 , A61K45/06 , C07K5/107
CPC分类号： A61K38/07 , A61K45/06 , C07D498/18 , C07K5/101 , C07K5/1016
摘要： The present invention relates to macrocyclic compounds of formula I that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
摘要翻译：本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式I的大环化合物。

26. 发明申请

US20050130997A1 Pyrimidinone viral polymerase inhibitors 审中-公开
标题翻译：嘧啶酮病毒聚合酶抑制剂
公开(公告)号：US20050130997A1
公开(公告)日：2005-06-16
申请号：US10500971
申请日：2003-01-15
申请人： Salvatore Avolio , Stefania Colarusso , Immacolata Conte , Steven Harper , Uwe Koch , Savina Malancona , Vincenzo Summa , Frank Narjes , Alessia Petrocchi
发明人： Salvatore Avolio , Stefania Colarusso , Immacolata Conte , Steven Harper , Uwe Koch , Savina Malancona , Vincenzo Summa , Frank Narjes , Alessia Petrocchi
IPC分类号： A61K31/513 , A61K31/695 , A61P31/12 , A61P31/14 , A61P43/00 , C07D239/54 , C07D239/557 , C07D405/04 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14 , C07D49/02
CPC分类号： C07D239/557 , C07D409/04 , C07D417/04
摘要： A class of pyrimidinone derivatives of formula (I): wherein Z, R1, R2 and R3 are as defined herein; and pharmaceutically acceptable salts thereof; are inhibitors of viral polymerases, especially (the hepatitis C virus (HCV) polymerase enzyme.
摘要翻译：一类式（I）的嘧啶酮衍生物：其中Z，R 1，R 2和R 3如本文所定义; 及其药学上可接受的盐; 是病毒聚合酶的抑制剂，特别是（丙型肝炎病毒（HCV）聚合酶）。

27. 发明申请

US20100099695A1 HCV NS3 Protease Inhibitors 审中-公开
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：US20100099695A1
公开(公告)日：2010-04-22
申请号：US12447342
申请日：2007-10-23
申请人： Nigel J. Liverton , Vincenzo Summa , Maria Emilia Di Francesco , Marco Ferrara , Kevin F. Gilbert , Steven Harper , John A. McCauley , Charles A. McIntyre , Alessia Petrocchi , Marco Pompei , Joseph J. Romano , Michael T. Rudd , John W. Butcher , M. Katharine Holloway
发明人： Nigel J. Liverton , Vincenzo Summa , Maria Emilia Di Francesco , Marco Ferrara , Kevin F. Gilbert , Steven Harper , John A. McCauley , Charles A. McIntyre , Alessia Petrocchi , Marco Pompei , Joseph J. Romano , Michael T. Rudd , John W. Butcher , M. Katharine Holloway
IPC分类号： A61K31/439 , C07D513/18 , C07D513/08 , A61K31/407 , A61K31/4748 , A61P31/12
CPC分类号： C07D498/22 , A61K31/407 , A61K31/4192 , A61K31/437 , A61K31/439 , A61K38/00 , A61K45/06 , C07D498/08 , C07D498/18 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
摘要翻译：本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。

28. 发明申请

US20070161639A1 Hiv integrase inhibitors 审中-公开
标题翻译： Hiv整合酶抑制剂
公开(公告)号：US20070161639A1
公开(公告)日：2007-07-12
申请号：US10587601
申请日：2005-03-01
申请人： Philip Jones , Vincenzo Summa , Monica Donghi , Cristina Gardelli
发明人： Philip Jones , Vincenzo Summa , Monica Donghi , Cristina Gardelli
IPC分类号： A61K31/525 , A61K31/498 , C07D487/02
CPC分类号： C07D471/04 , C07D487/04 , C07D487/16
摘要： Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula (I); wherein G, Q, bond a, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：吡啶并吡嗪和嘧啶并吡嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。在一个实施方案中，二羟基吡啶甲酰胺具有式（I）; 其中G，Q，键a，R 5，R 6和R 7均在本文中定义。这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

29. 发明授权

US07981879B2 HIV integrase inhibitors 有权
标题翻译： HIV整合酶抑制剂
公开(公告)号：US07981879B2
公开(公告)日：2011-07-19
申请号：US11887305
申请日：2006-03-22
申请人： Vincenzo Summa , Paola Pace
发明人： Vincenzo Summa , Paola Pace
IPC分类号： A61P31/00 , A61K31/553 , C07D498/04
CPC分类号： C07D487/04 , C07D487/14 , C07D513/04 , C07D513/14
摘要： Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HTV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HTV infection and ADDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物是FHV整合酶的抑制剂和FHV复制抑制剂（I），其中m，n，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7; R8，R9和R10在本文中定义。该化合物可用于预防或治疗HTV感染以及预防，治疗或延迟AIDS发病。该化合物用于抗HTV感染和ADDS作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

30. 发明申请

US20140328799A1 COMPOSITIONS USEFUL FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：用于治疗病毒性疾病的组合物
公开(公告)号：US20140328799A1
公开(公告)日：2014-11-06
申请号：US14355363
申请日：2012-10-26
申请人： Steven S. Carroll , John A. McCauley , David B. Olsen , Vincenzo Summa , Michael Rowley , Mark W. Stahlhut , Daria Hazuda
发明人： Steven S. Carroll , John A. McCauley , David B. Olsen , Vincenzo Summa , Michael Rowley , Mark W. Stahlhut , Daria Hazuda
IPC分类号： A61K38/06 , A61K31/553 , A61K31/519 , A61K31/4178 , A61K31/7064
CPC分类号： A61K38/06 , A61K31/403 , A61K31/407 , A61K31/4178 , A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/553 , A61K31/7064 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395 , A61K2300/00
摘要： The present invention is directed to compositions comprising inhibitors of hepatitis C virus (HCV) protease and one or more additional therapeutically effective agents. Uses of such compositions as HCV inhibitors and methods of treating infection by HCV by administration of such compositions are also disclosed.
摘要翻译：本发明涉及包含丙型肝炎病毒（HCV）蛋白酶抑制剂和一种或多种另外的治疗有效试剂的组合物。还公开了使用这些组合物作为HCV抑制剂和通过施用这种组合物治疗HCV感染的方法。

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