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1. 发明申请

WO2008100867A2 NOVEL INHIBITORS HEPATITIS C VIRUS REPLICATION 审中-公开
标题翻译：新型抑制剂HEPATITIS C VIRUS REPLICATION
公开(公告)号：WO2008100867A2
公开(公告)日：2008-08-21
申请号：PCT/US2008053617
申请日：2008-02-11
申请人： INTERMUNE INC , BEIGELMAN LEONID , BUCKMAN BRAD , WANG GUANGYI , MATULIC-ADAMIC JASENKA , STOYCHEVA ANTITSA DIMITROVA , ANDREWS STEVEN W , MISIALEK SHAWN MAURICE , RAJAGOPALAN P T RAVI , FRYER ANDREW M , GUNAWARDANA INDRANI , HAAS JULIA , HUANG LILY , MADDURU MACHENDER R , ZHANG GAN , KOSSEN KARL , SEREBRYANY VLADIMIR
发明人： BEIGELMAN LEONID , BUCKMAN BRAD , WANG GUANGYI , MATULIC-ADAMIC JASENKA , STOYCHEVA ANTITSA DIMITROVA , ANDREWS STEVEN W , MISIALEK SHAWN MAURICE , RAJAGOPALAN P T RAVI , FRYER ANDREW M , GUNAWARDANA INDRANI , HAAS JULIA , HUANG LILY , MADDURU MACHENDER R , ZHANG GAN , KOSSEN KARL , SEREBRYANY VLADIMIR
IPC分类号： C07D209/18 , C07D209/30 , C07D209/32 , C07D307/79 , C07D333/60 , C07D401/10 , C07D403/06 , C07D403/10 , C07D403/12 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06
CPC分类号： C07F9/65583 , C07D209/18 , C07D209/30 , C07D209/32 , C07D307/79 , C07D333/60 , C07D401/10 , C07D403/06 , C07D403/10 , C07D403/12 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D417/06 , C07D487/04 , C07F9/5728 , C12Q1/707 , G01N2333/186 , G01N2333/914
摘要： The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
摘要翻译：实施方案提供了通式I的化合物，以及包含主题化合物的组合物，包括药物组合物。实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。

2. 发明申请

WO2007053685A2 METHODS OF TREATING ATRIAL FIBRILLATION WITH P38 INHIBITOR COMPOUNDS 审中-公开
标题翻译：用P38抑制剂化合物治疗ATRIAL FIBRILLATION的方法
公开(公告)号：WO2007053685A2
公开(公告)日：2007-05-10
申请号：PCT/US2006042653
申请日：2006-11-01
申请人： INTERMUNE INC , UNIV CALIFORNIA , OLGIN JEFF , EISENBERG SUSAN , BLATT LAWRENCE M , SEIWERT SCOTT , KOSSEN KARL
发明人： OLGIN JEFF , EISENBERG SUSAN , BLATT LAWRENCE M , SEIWERT SCOTT , KOSSEN KARL
IPC分类号： A61K31/4412
CPC分类号： A61K31/47
摘要： The invention disclosed herein relates generally to compounds and methods useful in treating or preventing atrial fibrillation (AF).
摘要翻译：本文公开的发明一般涉及可用于治疗或预防心房颤动（AF）的化合物和方法。

3. 发明申请

WO2010135470A1 PIFENIDONE DERIVATIVES FOR TREATING BRONCHIAL ASTHMA 审中-公开
标题翻译：用于治疗青春期哮喘的菲尼他酮衍生物
公开(公告)号：WO2010135470A1
公开(公告)日：2010-11-25
申请号：PCT/US2010/035476
申请日：2010-05-19
申请人： INTERMUNE, INC. , KOSSEN, Karl , GELFAND, Erwin, W.
发明人： KOSSEN, Karl , GELFAND, Erwin, W.
IPC分类号： A61K31/352 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/444 , A61K31/4704 , A61K31/513 , A61K31/522 , A61K31/573 , A61K45/06 , A61P11/06
CPC分类号： A61K31/4418 , A61K31/00 , A61K31/352 , A61K31/437 , A61K31/443 , A61K31/4433 , A61K31/444 , A61K31/4704 , A61K31/513 , A61K31/522 , A61K31/573 , A61K45/06 , A61K2300/00
摘要： The invention relates to methods of treating patients with bronchial asthma with a pirfenidone analog.
摘要翻译：本发明涉及用吡非尼酮类似物治疗支气管哮喘患者的方法。

4. 发明申请

WO2009149188A1 COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS 审中-公开
标题翻译：用于治疗炎症和纤维性疾病的化合物和方法
公开(公告)号：WO2009149188A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/046136
申请日：2009-06-03
申请人： INTERMUNE, INC. , KOSSEN, Karl , SEIWERT, Scott, D. , SEREBRYANY, Vladimir , RUHRMUND, Donald , BEIGELMAN, Leonid , RAVEGLIA, Luca, Francesco Mario , VALLESE, Stefania , BIANCHI, Ivana , HU, Tao
发明人： KOSSEN, Karl , SEIWERT, Scott, D. , SEREBRYANY, Vladimir , RUHRMUND, Donald , BEIGELMAN, Leonid , RAVEGLIA, Luca, Francesco Mario , VALLESE, Stefania , BIANCHI, Ivana , HU, Tao
IPC分类号： A61K31/44 , C07D213/22
CPC分类号： C07D213/63 , C07D213/22 , C07D213/64 , C07D213/69 , C07D213/71 , C07D213/85 , C07D237/14 , C07D239/36 , C07D239/54 , C07D241/18 , C07D251/10 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
摘要翻译：公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出低的抑制p38MAPK的能力; 并且其中所述接触以对所述化合物抑制p38MAPK的抑制浓度低的SAPK调节浓度进行。还公开了吡非尼酮的衍生物和类似物，其可用于调节应激活化蛋白激酶（SAPK）系统。

5. 发明申请

WO2007062167A2 METHOD OF MODULATING STRESS-ACTIVATED PROTEIN KINASE SYSTEM 审中-公开
标题翻译：调节应激激活的蛋白激酶系统的方法
公开(公告)号：WO2007062167A2
公开(公告)日：2007-05-31
申请号：PCT/US2006/045287
申请日：2006-11-22
申请人： INTERMUNE, INC. , SEIWERT, Scott D. , KOSSEN, Karl , SEREBRYANY, Vladimir
发明人： SEIWERT, Scott D. , KOSSEN, Karl , SEREBRYANY, Vladimir
CPC分类号： C07D495/04
摘要： It has now been discovered that a high therapeutic effect in treating various disorders associated with enhanced activity of kinase p38 may be achieved by using a potent p38? kinase inhibitor compound which also has inhibitory activity against p38?. Furthermore, reducing the activities of both kinase p38? and kinase p38? without reducing the activity of a kinase p38? to such an extent that undesired side effects are observed upon administration to a subject having a disorder associated with enhanced activity of kinase p38 has been discovered to be achievable by modifying inhibitors of p38? such that the modification engenders inhibitory activity against p38?. Described are compounds with activity against p38? and p38?. Disclosed are methods of using described compounds and compositions to modulate a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits inhibition of the p38? and p38? MAPKs. Also disclosed are methods for identifying compounds which inhibit p38? and p38? MAPKs and which can modulate a stress activated protein kinase (SAPK) system.
摘要翻译：现在已经发现，通过使用有效的p38β4可以实现治疗与增强的激酶p38活性相关的各种病症的高治疗效果。激酶抑制剂化合物也具有抑制p38β的活性。此外，降低激酶p38的活性？和激酶p38？而不降低激酶p38的活性？在给予患有与激酶p38活性增强有关的病症的受试者时观察到不希望的副作用的程度已经被发现可以通过修饰p38β3抑制剂实现，使得修饰产生针对p38β的抑制活性。描述的是具有抗p38活性的化合物和p38 ?. 公开了使用所述化合物和组合物用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中所述活性化合物表现出对p38β 和p38？的MAPK。还公开了鉴定抑制p38？和p38？ MAPKs并且可以调节应激活化蛋白激酶（SAPK）系统。

6. 发明申请

WO2008100867A3 NOVEL INHIBITORS HEPATITIS C VIRUS REPLICATION 审中-公开
公开(公告)号：WO2008100867A3
公开(公告)日：2008-08-21
申请号：PCT/US2008/053617
申请日：2008-02-11
申请人： INTERMUNE, INC. , BEIGELMAN, Leonid , BUCKMAN, Brad , WANG, Guangyi , MATULIC-ADAMIC, Jasenka , STOYCHEVA, Antitsa Dimitrova , ANDREWS, Steven, W. , MISIALEK, Shawn, Maurice , RAJAGOPALAN, P.T., Ravi , FRYER, Andrew, M. , GUNAWARDANA, Indrani , HAAS, Julia , HUANG, Lily , MADDURU, Machender, R. , ZHANG, Gan , KOSSEN, Karl , SEREBRYANY, Vladimir
发明人： BEIGELMAN, Leonid , BUCKMAN, Brad , WANG, Guangyi , MATULIC-ADAMIC, Jasenka , STOYCHEVA, Antitsa Dimitrova , ANDREWS, Steven, W. , MISIALEK, Shawn, Maurice , RAJAGOPALAN, P.T., Ravi , FRYER, Andrew, M. , GUNAWARDANA, Indrani , HAAS, Julia , HUANG, Lily , MADDURU, Machender, R. , ZHANG, Gan , KOSSEN, Karl , SEREBRYANY, Vladimir
IPC分类号： C07D209/18 , C07D209/30 , C07D209/32 , C07D307/79 , C07D333/60 , C07D401/10 , C07D403/06 , C07D403/10 , C07D403/12 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06
摘要： The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. Formula (I)

7. 发明申请

WO2007062167A9 METHOD OF MODULATING STRESS-ACTIVATED PROTEIN KINASE SYSTEM 审中-公开
标题翻译：调节应激激活蛋白激酶系统的方法
公开(公告)号：WO2007062167A9
公开(公告)日：2007-07-26
申请号：PCT/US2006045287
申请日：2006-11-22
申请人： INTERMUNE INC , SEIWERT SCOTT D , KOSSEN KARL , SEREBRYANY VLADIMIR
发明人： SEIWERT SCOTT D , KOSSEN KARL , SEREBRYANY VLADIMIR
IPC分类号： C07D495/04 , A61K31/4365 , A61P29/00
CPC分类号： C07D495/04
摘要： It has now been discovered that a high therapeutic effect in treating various disorders associated with enhanced activity of kinase p38 may be achieved by using a potent p38? kinase inhibitor compound which also has inhibitory activity against p38?. Furthermore, reducing the activities of both kinase p38? and kinase p38? without reducing the activity of a kinase p38? to such an extent that undesired side effects are observed upon administration to a subject having a disorder associated with enhanced activity of kinase p38 has been discovered to be achievable by modifying inhibitors of p38? such that the modification engenders inhibitory activity against p38?. Described are compounds with activity against p38? and p38?. Disclosed are methods of using described compounds and compositions to modulate a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits inhibition of the p38? and p38? MAPKs. Also disclosed are methods for identifying compounds which inhibit p38? and p38? MAPKs and which can modulate a stress activated protein kinase (SAPK) system.
摘要翻译：现在已经发现，通过使用有效的p38α可以实现治疗与激酶p38活性增强相关的各种疾病的高治疗效果。激酶抑制剂化合物，其也对p38α具有抑制活性。此外，减少激酶p38的活性？和激酶p38？而不降低激酶p38的活性？已经被发现通过修饰p38的抑制剂可以实现在对具有与激酶p38的活性增强相关的病症的受试者施用时观察到不期望的副作用的程度。使得该修饰产生对p38β的抑制活性。描述的是具有抗p38活性的化合物？和p38？公开了使用所述化合物和组合物以活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出对p38β的抑制作用。和p38？的MAPK。还公开了用于鉴定抑制p38的化合物的方法和p38？ MAPKs，可调节应激活化蛋白激酶（SAPK）系统。

8. 发明申请

WO2005028650A2 RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS C VIRUS (HCV) EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) 审中-公开
标题翻译： RNA干扰介导的抑制HEPATITIS C病毒（HCV）表达使用短暂的干扰核酸（siNA）
公开(公告)号：WO2005028650A2
公开(公告)日：2005-03-31
申请号：PCT/US2004031012
申请日：2004-09-15
申请人： SIRNA THERAPEUTICS INC , JADHAV VASANT , KOSSEN KARL , ZINNEN SHAWN , VAISH NARENDRA , MCSWIGGEN JAMES
发明人： JADHAV VASANT , KOSSEN KARL , ZINNEN SHAWN , VAISH NARENDRA , MCSWIGGEN JAMES
IPC分类号： A61K38/00 , C12N15/11 , C12N15/113 , C12N15/87
CPC分类号： C12N15/113 , A61K38/00 , C12N15/111 , C12N15/1131 , C12N15/1137 , C12N15/1138 , C12N15/87 , C12N2310/111 , C12N2310/12 , C12N2310/121 , C12N2310/14 , C12N2310/315 , C12N2310/316 , C12N2310/317 , C12N2310/318 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12N2310/333 , C12N2310/346 , C12N2310/53 , C12N2330/30 , C12Y103/01022 , C12N2310/3521 , C12N2310/3533
摘要： This invention relates to compounds, compositions, and methods useful for modulating HCVgene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of HCV gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of HCV genes.
摘要翻译：本发明涉及可用于使用短干扰核酸（siNA）分子调节HCV基因表达的化合物，组合物和方法。本发明还涉及可用于通过使用小核酸分子调节参与通过RNA干扰（RNAi）的HCV基因表达和/或活性的途径的其它基因的表达和活性的化合物，组合物和方法。特别地，本发明的特征在于小核酸分子，例如短干扰核酸（siNA），短干扰RNA（siRNA），双链RNA（dsRNA），微RNA（miRNA）和短发夹RNA（shRNA））分子和用于调节HCV基因表达的方法。

9. 发明申请

WO2005028649A1 RNA INTERFERENCE MEDIATED INHIBITION OF VASCULAR ENDOTHELIAL GROWTH FACTOR AND VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) 审中-公开
标题翻译： RNA干扰介导的血管内皮生长因子和血管内皮生长因子受体基因表达的抑制使用短暂的核酸（siNA）
公开(公告)号：WO2005028649A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/030488
申请日：2004-09-16
申请人： SIRNA THERAPEUTICS, INC. , JADHAV, Vasant , KOSSEN, Karl , ZINNEN, Shawn , VAISH, Narendra , MCSWIGGEN, James
发明人： JADHAV, Vasant , KOSSEN, Karl , ZINNEN, Shawn , VAISH, Narendra , MCSWIGGEN, James
IPC分类号： C12N15/11
CPC分类号： C12N15/111 , C12N15/1136 , C12N15/1138 , C12N2310/14 , C12N2310/315 , C12N2310/317 , C12N2310/51 , C12N2310/321 , C12N2310/3521 , C12N2310/322 , C12N2310/3533
摘要： This invention relates to compounds, compositions, and methods useful for modulating VEGF and/or VEGFR gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of VEGF and/or VEGFR gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of VEGF and/or VEGFR genes.
摘要翻译：本发明涉及使用短干扰核酸（siNA）分子调节VEGF和/或VEGFR基因表达的化合物，组合物和方法。本发明还涉及可用于通过使用小核酸分子调节参与VEGF和/或VEGFR基因表达和/或活性的其它基因的表达和活性的化合物，组合物和方法，所述基因表达和/或活性通过RNA干扰（RNAi）。特别地，本发明的特征在于小核酸分子，例如短干扰核酸（siNA），短干扰RNA（siRNA），双链RNA（dsRNA），微RNA（miRNA）和短发夹RNA（shRNA））分子和用于调节VEGF和/或VEGFR基因表达的方法。

10. 发明申请

WO2010132864A1 METHODS OF TREATING HIV PATIENTS WITH ANTI-FIBROTICS 审中-公开
标题翻译：用抗纤维蛋白治疗艾滋病患者的方法
公开(公告)号：WO2010132864A1
公开(公告)日：2010-11-18
申请号：PCT/US2010/035042
申请日：2010-05-15
申请人： INTERMUNE, INC. , UNIVERSITY OF MINNESOTA , KOSSEN, Karl , SCHACKER, Timothy
发明人： KOSSEN, Karl , SCHACKER, Timothy
IPC分类号： A61K31/4412 , A61K31/513 , A61P31/18 , A61P43/00
CPC分类号： A61K31/4412 , A61K31/513 , A61K2300/00
摘要： The invention relates to methods of treating patients infected with human immunodeficiency virus (HIV) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.
摘要翻译：本发明涉及用具有抗纤维化作用的治疗剂治疗感染人类免疫缺陷病毒（HIV）的患者的方法，例如吡非尼酮及其类似物。

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