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1. 发明申请

WO2011146401A1 NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION 审中-公开
标题翻译： HEPATITIS C VIRUS REPLICATION的新型抑制剂
公开(公告)号：WO2011146401A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/036671
申请日：2011-05-16
申请人： INTERMUNE, INC. , BUCKMAN, Brad , NICHOLAS, John, B. , SEREBRYANY, Vladimir , SEIWERT, Scott, D.
发明人： BUCKMAN, Brad , NICHOLAS, John, B. , SEREBRYANY, Vladimir , SEIWERT, Scott, D.
IPC分类号： C07D403/04 , A61K31/506 , C07D403/14 , A61K31/4025 , A61K31/517 , C07D405/14 , A61K31/4178 , A61K31/519 , C07D407/14 , A61K31/4184 , A61K31/55 , C07D409/14 , A61K31/423 , A61K31/558 , C07D413/14 , A61K31/428 , A61K31/5585 , C07D417/14 , A61K31/4365 , A61P31/14 , C07D471/04 , A61K31/437 , C07D207/16 , C07D487/04 , A61K31/439 , C07D401/12 , C07D495/04 , A61K31/4985 , C07D403/12 , C07D513/04 , C07D401/14
CPC分类号： C07D403/04 , A61K31/4025 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4365 , A61K31/437 , A61K31/439 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/558 , A61K31/5585 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The embodiments provide compounds of the general Formulae (VI), (VII), (VIII), (IX), (X), (XI), (XII), (XIII), (XIV), and (XV) 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 and methods of treating liver fibrosis, 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（VI），（VII），（VIII），（IX），（X），（XI），（XII），（XIII），（XIV）和（XV）作为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和治疗肝纤维化的方法，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

WO2011038283A1 NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION 审中-公开
标题翻译： HEPATITIS C VIRUS REPLICATION的新型大环内酰胺酶抑制剂
公开(公告)号：WO2011038283A1
公开(公告)日：2011-03-31
申请号：PCT/US2010/050284
申请日：2010-09-24
申请人： HOFFMANN-LA ROCHE INC. , F. HOFFMANN-LA ROCHE LTD , SEIWERT, Scott, D. , NICHOLAS, John, B. , BUCKMAN, Brad , SEREBRYANY, Vladimir
发明人： SEIWERT, Scott, D. , NICHOLAS, John, B. , BUCKMAN, Brad , SEREBRYANY, Vladimir
IPC分类号： C07D487/04 , A61K38/05 , A61P31/14 , A61K31/4035 , A61P1/16 , C07K5/072
CPC分类号： A61K31/4035 , A61K38/212 , A61K38/217 , C07D487/04 , C07K5/0804
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 and methods of treating liver fibrosis, 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和治疗肝纤维化的方法，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。

3. 发明申请

WO2005110455A3 COMBINATION THERAPY FOR TREATING HEPATITIS VIRUS INFECTION 审中-公开
标题翻译：用于治疗乙型肝炎病毒感染的组合治疗
公开(公告)号：WO2005110455A3
公开(公告)日：2007-12-21
申请号：PCT/US2005016353
申请日：2005-05-09
申请人： INTERMUNE INC , OZES OSMAN N , SEIWERT SCOTT D , BLATT LAWRENCE M
发明人： OZES OSMAN N , SEIWERT SCOTT D , BLATT LAWRENCE M
IPC分类号： A01N43/04 , A61K31/70 , A61K31/7056 , A61K38/05 , A61K38/19 , C07H19/00 , C07H21/00
CPC分类号： A61K38/212 , A61K31/7056 , A61K2300/00
摘要： The present invention provides methods of treating a viral infection, e.g., a hepatitis C virus (HCV) infection; methods of reducing the incidence of complications associated with HCV infection and cirrhosis of the liver; and methods of reducing viral load, or reducing the time to viral clearance, or reducing morbidity or mortality in the clinical outcomes, in patients suffering from a viral infection, e.g., an HCV infection. The methods generally involve administering to the individual i) a stress-activated protein kinase inhibitor; and ii) a Type I interferon receptor agonist. The present invention provides a method of treating alcoholic liver disease, the method involving administering to an individual in need thereof an effective amount of a stress-activated protein kinase (SAPK) inhibitor, alone or in combination therapy. The present invention further provides methods for treating non-alcoholic steatohepatitis, the method generally involving administering to an individual in need thereof an effective amount of a SAPK inhibitor, alone or in combination therapy.
摘要翻译：本发明提供了治疗病毒感染例如丙型肝炎病毒（HCV）感染的方法; 降低HCV感染和肝硬化相关并发症发生率的方法; 以及在患有病毒感染（例如HCV感染）的患者中减少病毒载量或减少病毒清除时间或降低临床结果的发病率或死亡率的方法。所述方法通常涉及对个体施用i）应激活化蛋白激酶抑制剂; 和ii）I型干扰素受体激动剂。本发明提供一种治疗酒精性肝病的方法，所述方法包括单独给药或联合治疗给有需要的个体有效量的应激活化蛋白激酶（SAPK）抑制剂。本发明还提供了治疗非酒精性脂肪性肝炎的方法，所述方法通常涉及单独或联合治疗单独施用有效量的SAPK抑制剂的需要的个体。

4. 发明申请

WO2007044893A2 COMPOUNDS AND METHODS FOR INHIBITING HEPATITIS C VIRAL REPLICATION 审中-公开
标题翻译：用于抑制乙型肝炎病毒复制的化合物和方法
公开(公告)号：WO2007044893A2
公开(公告)日：2007-04-19
申请号：PCT/US2006/040049
申请日：2006-10-10
申请人： INTERMUNE, INC. , ARRAY BIOPHARMA, INC. , BEIGELMAN, Leonid , SEIWERT, Scott D. , BLATT, Lawrence M. , ANDREWS, Steven , HAAS, Julia
发明人： BEIGELMAN, Leonid , SEIWERT, Scott D. , BLATT, Lawrence M. , ANDREWS, Steven , HAAS, Julia
CPC分类号： C07D487/04 , C07D471/04
摘要： Macrocyclic compounds having the structures described herein are useful for inhibiting replication of the hepatitis C virus (HCV). In preferred embodiments, the compounds are active against both the NS3 protease and the NS3 helicase of HCV.
摘要翻译：具有本文所述结构的大环化合物可用于抑制丙型肝炎病毒（HCV）的复制。在优选的实施方案中，所述化合物对NS3蛋白酶和HCV的NS3解旋酶均有活性。

5. 发明申请

WO2013025733A1 LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：赖氨酸磷酸受体拮抗剂
公开(公告)号：WO2013025733A1
公开(公告)日：2013-02-21
申请号：PCT/US2012/050824
申请日：2012-08-14
申请人： INTERMUNE, INC. , BUCKMAN, Brad, O. , NICHOLAS, John, B. , EMAYAN, Kumaraswamy , SEIWERT, Scott, D.
发明人： BUCKMAN, Brad, O. , NICHOLAS, John, B. , EMAYAN, Kumaraswamy , SEIWERT, Scott, D.
IPC分类号： C07D413/04 , C07D413/10 , C07D261/14 , C07D231/40 , C07D249/06 , C07D401/04 , C07D401/10 , C07D405/12 , C07D263/48 , C07D333/20 , A61K31/4155 , A61K31/42 , A61K31/4427 , A61K31/4192 , A61K31/381 , A61K31/415 , A61K31/421 , A61P19/04 , A61P1/16 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , A61K31/425 , A61K31/426 , C07D275/03 , C07D257/06 , C07D277/46 , C07D307/66 , C07D207/34 , C07D471/04 , C07D491/04 , C07D495/04
CPC分类号： C07D495/04 , A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/4427 , C07D207/34 , C07D213/75 , C07D231/40 , C07D249/06 , C07D257/06 , C07D261/14 , C07D263/48 , C07D275/03 , C07D277/46 , C07D307/66 , C07D333/20 , C07D401/04 , C07D401/10 , C07D405/12 , C07D413/04 , C07D413/10 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07H15/26
摘要： Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
摘要翻译：提供了化合物，制备这种化合物的方法，药物组合物和包含这些化合物的药物，以及使用这些化合物治疗，预防或诊断与一种或多种溶血磷脂酸受体相关的疾病，病症或病症的方法。

6. 发明申请

WO2011075607A1 NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION 审中-公开
标题翻译： HEPATITIS C VIRUS REPLICATION的新型抑制剂
公开(公告)号：WO2011075607A1
公开(公告)日：2011-06-23
申请号：PCT/US2010/060893
申请日：2010-12-16
申请人： INTERMUNE, INC. , BUCKMAN, Brad , NICHOLAS, John, B. , SEREBRYANY, Vladimir , SEIWERT, Scott, D.
发明人： BUCKMAN, Brad , NICHOLAS, John, B. , SEREBRYANY, Vladimir , SEIWERT, Scott, D.
IPC分类号： C07D207/16 , A61K31/4178 , A61K31/422 , A61K31/4025 , A61K31/4184 , A61K31/423 , A61K31/424 , A61K31/427 , A61K31/428 , A61K31/429 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/549 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61P1/16 , A61P31/14 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/14 , C07D498/04 , C07D513/04
CPC分类号： C07D207/16 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/14 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04
摘要： The embodiments provide compounds of the general Formulae I, II, III, IV, or V 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 and methods of treating liver fibrosis, 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，II，III，IV或V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和治疗肝纤维化的方法，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。

7. 发明申请

WO2004105684A3 COMBINATION THERAPY FOR PROLIFERATIVE DISORDERS 审中-公开
标题翻译：加重疾病的组合治疗
公开(公告)号：WO2004105684A3
公开(公告)日：2008-12-11
申请号：PCT/US2004015346
申请日：2004-05-13
申请人： INTERMUNE INC , BLATT LAWRENCE M , SEIWERT SCOTT D , OZES OSMAN N
发明人： BLATT LAWRENCE M , SEIWERT SCOTT D , OZES OSMAN N
IPC分类号： A61K38/00 , A61K20060101 , A61K31/00 , C07K14/00
CPC分类号： A61K38/212 , A61K31/573 , A61K38/217 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods of treating proliferative disorders, including angiogenesis-mediated disorders, cancer, and fibrotic disorders. In some embodiments, the methods involve administering a Type II interferon receptor agonist and a Type I interferon receptor agonist. In other embodiments, the methods involve administering a Type II interferon receptor agonist, a stress-activated protein kinase (SAPK) inhibitor, and a third therapeutic agent. In other embodiments, the methods involve administering a Type II interferon receptor agonist and a vascular endothelial growth factor (VEGF) antagonist. In other embodiments, the methods involve administering a VEGF antagonist and a SAPK inhibitor. The present invention further provides methods of treating fibrotic disorders. In some embodiments, the methods involve administering a Type I interferon receptor agonist, a Type II interferon receptor agonist; and a tumor necrosis factor (TNF) antagonist. In other embodiments, the methods involve administering a Type II interferon receptor agonist and a TNF antagonist. In other embodiments, the methods involve administering pirfenidone or a pirfenidone analog and a TNF antagonist. In other embodiments, the methods involve administering a Type II interferon receptor agonist and a transformining growth factor-beta (TGF-ß) antagonist. In other embodiments, the methods involve administering a SAPK inhibitor alone or in combination with a Type II interferon receptor agonist. In other embodiments, the methods involve administering N-acetyl cysteine (NAC) and a SAPK inhibitor. In other embodiments, the methods involve administering NAC and a Type II interferon receptor agonist.
摘要翻译：本发明提供了治疗增殖性疾病，包括血管发生介导的病症，癌症和纤维化病症的方法。在一些实施方案中，所述方法包括施用II型干扰素受体激动剂和I型干扰素受体激动剂。在其它实施方案中，所述方法包括施用II型干扰素受体激动剂，应激激活蛋白激酶（SAPK）抑制剂和第三治疗剂。在其它实施方案中，所述方法包括施用II型干扰素受体激动剂和血管内皮生长因子（VEGF）拮抗剂。在其它实施方案中，所述方法包括施用VEGF拮抗剂和SAPK抑制剂。本发明还提供治疗纤维化疾病的方法。在一些实施方案中，所述方法包括施用I型干扰素受体激动剂，II型干扰素受体激动剂; 和肿瘤坏死因子（TNF）拮抗剂。在其它实施方案中，所述方法包括施用II型干扰素受体激动剂和TNF拮抗剂。在其它实施方案中，所述方法包括施用吡非尼酮或吡非尼酮类似物和TNF拮抗剂。在其它实施方案中，所述方法包括施用II型干扰素受体激动剂和变应性生长因子-β（TGF-β）拮抗剂。在其它实施方案中，所述方法包括单独或与II型干扰素受体激动剂组合施用SAPK抑制剂。在其它实施方案中，所述方法包括给予N-乙酰半胱氨酸（NAC）和SAPK抑制剂。在其它实施方案中，所述方法包括施用NAC和II型干扰素受体激动剂。

8. 发明申请

WO2005123113A2 INTERFERON COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：干扰素组合物及其使用方法
公开(公告)号：WO2005123113A2
公开(公告)日：2005-12-29
申请号：PCT/US2005/021050
申请日：2005-06-14
申请人： INTERMUNE, INC. , SEIWERT, Scott D. , BLATT, Lawrence M. , TAN, Hua , DERRICK, Jena Rey , HONG, Jin , RADHAKRISHNAN, Ramachandran
发明人： SEIWERT, Scott D. , BLATT, Lawrence M. , TAN, Hua , DERRICK, Jena Rey , HONG, Jin , RADHAKRISHNAN, Ramachandran
IPC分类号： A61K38/21
CPC分类号： A61K38/212 , A61K38/21 , A61K38/217 , A61K2300/00
摘要： The present invention provides compositions, including pharmaceutical compositions, comprising IFN-α and IFN-γ. The present invention further provides methods of treating various disorders, the methods comprising administering an effective amount of a subject composition.
摘要翻译：本发明提供包含IFN-α和IFN-γ的组合物，包括药物组合物。本发明还提供了治疗各种疾病的方法，所述方法包括施用有效量的受试者组合物。

9. 发明申请

WO2007044893A3 COMPOUNDS AND METHODS FOR INHIBITING HEPATITIS C VIRAL REPLICATION 审中-公开
标题翻译：用于抑制乙型肝炎病毒复制的化合物和方法
公开(公告)号：WO2007044893A3
公开(公告)日：2008-10-02
申请号：PCT/US2006040049
申请日：2006-10-10
申请人： INTERMUNE INC , ARRAY BIOPHARMA INC , BEIGELMAN LEONID , SEIWERT SCOTT D , BLATT LAWRENCE M , ANDREWS STEVEN , HAAS JULIA
发明人： BEIGELMAN LEONID , SEIWERT SCOTT D , BLATT LAWRENCE M , ANDREWS STEVEN , HAAS JULIA
IPC分类号： C07D471/04 , A61K31/407 , A61P31/14 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Macrocyclic compounds having the structures described herein arc useful for inhibiting replication of the hepatitis C virus (HCV). In preferred embodiments, the compounds are active against both the NS3 protease and the NS3 helicase of HCV. Formulae (I), (II), (III), (IV) and (V).
摘要翻译：具有本文所述结构的大环化合物可用于抑制丙型肝炎病毒（HCV）的复制。在优选的实施方案中，所述化合物对NS3蛋白酶和HCV的NS3解旋酶均有活性。式（I），（II），（III），（IV）和（V）。

10. 发明申请

WO2007092537A3 SYNTHETIC HYPERGLYCOSYLATED, AND HYPERGLYCOSYLATED PROTEASE-RESISTANT POLYPEPTIDE VARIANTS, ORAL FORMULATIONS AND METHODS OF USING THE SAME 审中-公开
标题翻译：合成高效液相色谱法和超高效抗菌多肽变体，口服制剂及其使用方法
公开(公告)号：WO2007092537A3
公开(公告)日：2008-01-24
申请号：PCT/US2007003333
申请日：2007-02-07
申请人： ALIOS BIOPHARMA INC , BLATT LAWRENCE M , SEIWERT SCOTT D , HONG JIN
发明人： BLATT LAWRENCE M , SEIWERT SCOTT D , HONG JIN
IPC分类号： C07K14/555 , A61K38/21 , C07K14/56 , C07K14/565 , C07K14/57
CPC分类号： C07K14/555 , A61K38/00 , C07K14/56 , C07K14/565 , C07K14/57
摘要： The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites. The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites, as well as erythropoietin and darbepoetin alfa, each of which are linked to a penetrating peptide that facilitates translocation of a substance across a biological barrier as well as pharmaceutical compositions, including oral formulations, of the same. The present invention further provides oral formulations of hyperglycosylated or protease-resistant, hyperglycosylated polypeptide variants, which polypeptide variants lack at least one protease cleavage site found in a parent polypeptide, and thus exhibit increased protease resistance compared to the parent polypeptide, which polypeptide variants further include (1) a carbohydrate moiety covalently linked to at least one non-native glycosylation site not found in the parent protein therapeutic or (2) a carbohydrate moiety covalently linked to at least one native glycosylation site found but not glycosylated in the parent protein therapeutic. The present invention further provides compositions, including oral pharmaceutical compositions, comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides containers, devices, and kits comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides therapeutic methods involving administering an effective amount of an oral pharmaceutical composition comprising a synthetic Type I interferon receptor polypeptide agonist, a hyperglycosylated polypeptide variant, or a hyperglycosylated, protease-resistant polypeptide variant to an individual in need thereof.
摘要翻译：本发明提供含有一个或多个天然或非天然糖基化位点的含有共有或混合型I型干扰素受体多肽激动剂的合成的I型干扰素受体多肽激动剂。本发明提供合成的I型干扰素受体多肽激动剂，其包含含有一个或多个天然或非天然糖基化位点的共有或混合型I型干扰素受体多肽激动剂，以及红细胞生成素和达比泊汀α，其各自与渗透性促进物质穿过生物屏障移位的肽以及包含口服制剂的药物组合物。本发明进一步提供高糖基化或蛋白酶抗性，高糖基化多肽变体的口服制剂，该多肽变体在母体多肽中缺少至少一个蛋白酶切割位点，因此与亲本多肽相比表现出增加的蛋白酶抗性，该多肽变体进一步包括（1）与亲本蛋白质治疗剂中未发现的至少一个非天然糖基化位点共价连接的碳水化合物部分，或（2）与母体蛋白质治疗中发现但未糖基化的至少一个天然糖基化位点共价连接的碳水化合物部分。本发明还提供包含口服药物组合物的组合物，其包含合成的I型干扰素受体多肽激动剂，高糖基化多肽变体或高糖基化的，蛋白酶抗性多肽变体。本发明还提供了包含合成的I型干扰素受体多肽激动剂，高糖基化多肽变体或高糖基化的蛋白酶抗性多肽变体的容器，装置和试剂盒。本发明进一步提供治疗方法，其涉及向有需要的个体施用有效量的包含合成的I型干扰素受体多肽激动剂，高糖基化多肽变体或高糖基化的，蛋白酶抗性多肽变体的口服药物组合物。

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