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41. 发明授权

US07365092B2 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白酶
公开(公告)号：US07365092B2
公开(公告)日：2008-04-29
申请号：US10821663
申请日：2004-04-09
申请人： Kevin M. Cottrell , John Maxwell , Robert B. Perni , Janos Pitlik
发明人： Kevin M. Cottrell , John Maxwell , Robert B. Perni , Janos Pitlik
IPC分类号： A61K31/4025 , C07D207/30
CPC分类号： C07K5/0804 , A61K31/40 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，并且作为抗病毒剂是有用的。本发明还涉及包含用于离体使用或用于给予HCV感染患者的所述化合物的药学上可接受的组合物以及制备该化合物的方法。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗患者HCV感染的方法。

42. 发明授权

US07273885B2 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白酶
公开(公告)号：US07273885B2
公开(公告)日：2007-09-25
申请号：US10412600
申请日：2003-04-11
申请人： Janos Pitlik , Kevin M. Cottrell , Luc J. Farmer , Robert B. Perni , Lawrence F. Courtney , John H. van Drie , Mark A. Murcko
发明人： Janos Pitlik , Kevin M. Cottrell , Luc J. Farmer , Robert B. Perni , Lawrence F. Courtney , John H. van Drie , Mark A. Murcko
IPC分类号： A61K31/403 , A61K31/435 , C07D209/02 , C07D221/00
CPC分类号： C07D209/42 , C07D209/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D471/04 , C07K5/06008 , C07K5/0812 , C07K5/1024 , C07K5/1027
摘要： The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的化合物。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。本发明还涉及包含这些化合物的组合物，用于离体使用或给予患有HCV感染的患者。本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。本发明还涉及制备这些化合物的方法。

43. 发明授权

US07208600B2 Inhibitors of serine proteases, particularly HCV NS3-NS4A proteases 失效
标题翻译：丝氨酸蛋白酶抑制剂，特别是HCV NS3-NS4A蛋白酶
公开(公告)号：US07208600B2
公开(公告)日：2007-04-24
申请号：US10964214
申请日：2004-10-12
申请人： Kevin M. Cottrell , Robert B. Perni , Janos Pitlik
发明人： Kevin M. Cottrell , Robert B. Perni , Janos Pitlik
IPC分类号： C07D241/10 , A61K31/495
CPC分类号： C07K7/06 , A61K38/08
摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
摘要翻译：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐或混合物。因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。本发明还涉及包含用于离体使用或用于给予HCV感染患者的这些化合物的组合物和制备该化合物的方法。本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。本发明还涉及制备这些化合物的方法。

44. 发明授权

US09326986B2 Quinazolinone, quinolone and related analogs as sirtuin modulators 有权
标题翻译：喹唑啉酮，喹诺酮和相关类似物作为沉默调节剂
公开(公告)号：US09326986B2
公开(公告)日：2016-05-03
申请号：US13121411
申请日：2009-09-29
申请人： Chi B. Vu , Christopher Oalmann , Robert B. Perni , Brian White
发明人： Chi B. Vu , Christopher Oalmann , Robert B. Perni , Brian White
IPC分类号： A61K31/5377 , A61K31/353 , A61K31/4025 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/4433 , A61K31/4439 , A61K31/497 , A61K31/506 , C07D405/12 , C07D417/12 , C07D417/14 , C07D405/14 , A61K45/06 , C07D311/30
CPC分类号： A61K31/5377 , A61K31/353 , A61K31/4025 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/4433 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K45/06 , C07D311/30 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14 , A61K2300/00
摘要： Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病，心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。还提供了包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

45. 发明授权

US08846947B2 Benzimidazoles and related analogs as sirtuin modulators 有权
标题翻译：苯并咪唑和相关类似物作为沉默调节剂
公开(公告)号：US08846947B2
公开(公告)日：2014-09-30
申请号：US12999795
申请日：2009-07-02
申请人： Chi B. Vu , Jeremy S. Disch , Pui Yee Ng , Charles A. Blum , Robert B. Perni
发明人： Chi B. Vu , Jeremy S. Disch , Pui Yee Ng , Charles A. Blum , Robert B. Perni
IPC分类号： A61K31/4184 , A61K31/5377 , A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4545 , C07D235/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/5355 , C07D471/08 , C07D405/12 , A61K31/437 , C07D405/14 , A61K31/495 , A61K31/427 , A61K31/4427 , A61K45/06 , A61K31/422 , A61K31/46 , C07D513/04 , C07D471/04
CPC分类号： C07D513/04 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/439 , A61K31/4427 , A61K31/4439 , A61K31/46 , A61K31/495 , A61K31/497 , A61K31/5355 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02 , C07D471/04 , C07D471/08 , C07D498/04 , A61K2300/00
摘要： Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了式（II）的沉默调节蛋白的调节性化合物。沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病，心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。还提供了包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

46. 发明授权

US08486989B2 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease 失效
公开(公告)号：US08486989B2
公开(公告)日：2013-07-16
申请号：US11805085
申请日：2007-05-22
申请人： Luc J. Farmer , Robert B. Perni , Janos Pitlik , John H. van Drie, Jr.
发明人： Luc J. Farmer , Robert B. Perni , Janos Pitlik , John H. van Drie, Jr.
IPC分类号： A61K31/40 , A61K51/00 , A01N43/38 , C07D209/56 , C07D487/00 , C07D491/00
CPC分类号： C07D491/147 , A61K31/407 , A61K38/00 , A61K45/06 , C07D403/12 , C07K5/06191 , C07K5/0827 , C07K5/101 , C07K5/1027 , C07K7/02 , C07K7/06
摘要： The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

47. 发明申请

US20120270318A1 ION CHANNEL MODULATORS AND METHODS OF USE 有权
标题翻译：离子通道调制器和使用方法
公开(公告)号：US20120270318A1
公开(公告)日：2012-10-25
申请号：US13538667
申请日：2012-06-29
申请人： ESTHER MARTINBOROUGH , Nicole Zimmermann , Robert B. Perni , Michael Arnost , Upul K. Bandarage , Francois Maltais , Guy Bemis
发明人： ESTHER MARTINBOROUGH , Nicole Zimmermann , Robert B. Perni , Michael Arnost , Upul K. Bandarage , Francois Maltais , Guy Bemis
IPC分类号： C12N5/071
CPC分类号： C07D409/14 , A61K31/506 , C07D239/28 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06
摘要： In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels.
摘要翻译：通常，本发明涉及可用作离子通道调节剂的化合物。现已发现，本发明的化合物及其药学上可接受的组合物可用作电压门控钠通道和/或钙通道的抑制剂。

48. 发明授权

US08268862B2 Sirtuin modulating compounds 失效
标题翻译：沉默调节蛋白调节化合物
公开(公告)号：US08268862B2
公开(公告)日：2012-09-18
申请号：US13012775
申请日：2011-01-24
申请人： Jean Bemis , Jeremy S. Disch , Pui Yee Ng , Christopher Oalmann , Robert B. Perni , Chi B. Vu
发明人： Jean Bemis , Jeremy S. Disch , Pui Yee Ng , Christopher Oalmann , Robert B. Perni , Chi B. Vu
IPC分类号： A61K31/44 , A61K31/425 , A61K31/385 , A61K31/38
CPC分类号： C07D513/04
摘要： Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病，心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。还提供了包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

49. 发明授权

US08236815B2 Ion channel modulators and methods of uses 有权
标题翻译：离子通道调节剂和使用方法
公开(公告)号：US08236815B2
公开(公告)日：2012-08-07
申请号：US12724077
申请日：2010-03-15
申请人： Esther Martinborough , Nicole Zimmermann , Robert B. Perni , Michael Arnost , Upul Bandarage , Francois Maltais , Guy Bemis
发明人： Esther Martinborough , Nicole Zimmermann , Robert B. Perni , Michael Arnost , Upul Bandarage , Francois Maltais , Guy Bemis
IPC分类号： A01N43/54 , A61K31/505 , C07D239/02
CPC分类号： C07D409/14 , A61K31/506 , C07D239/28 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06
摘要： The invention relates to ion channel modulators of formula Ia, pharmaceutical compositions thereof, and to methods of treating diseases using such compounds where activation or hyperactivity of calcium and/or sodium ion channels is implicated in the disease state.
摘要翻译：本发明涉及式Ia的离子通道调节剂，其药物组合物，以及使用这样的化合物治疗疾病的方法，其中钙和/或钠离子通道的活化或多动症涉及疾病状态。

50. 发明申请

US20110263564A1 PYRIDINE, BICYCLIC PYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS 审中-公开
标题翻译：吡啶，双环吡啶和相关模拟物作为SIRTUIN调节剂
公开(公告)号：US20110263564A1
公开(公告)日：2011-10-27
申请号：US13125788
申请日：2009-10-29
申请人： Radha Narayan , Jeremy S. Disch , Robert B. Perni , Chi B. Vu
发明人： Radha Narayan , Jeremy S. Disch , Robert B. Perni , Chi B. Vu
IPC分类号： A61K31/497 , A61K31/5377 , A61K31/506 , A61K31/47 , A61K31/444 , A61K31/4439 , A61K31/443 , A61K31/4418 , C07D413/14 , C07D491/052 , C07D413/06 , C07D401/12 , C07D215/48 , C07D417/12 , C07D401/06 , C07D405/12 , C07D213/56 , A61P5/50 , A61P3/00 , A61P3/10 , A61K31/4709
CPC分类号： C07D213/40 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D491/04
摘要： Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
摘要翻译：本文提供了新的沉默调节蛋白的调节化合物及其使用方法。沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病，心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。还提供了包含与另一种治疗剂组合的沉默调节蛋白的调节化合物的组合物。

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