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1. 发明申请

US20050267018A1 Macrocyclic compounds as inhibitors of viral replication 有权
标题翻译：大环化合物作为病毒复制的抑制剂
公开(公告)号：US20050267018A1
公开(公告)日：2005-12-01
申请号：US11093884
申请日：2005-03-29
申请人： Lawrence Blatt , Steven Andrews , Kevin Condroski , George Doherty , Yutong Jiang , John Josey , April Kennedy , Machender Madduru , Peter Stengel , Steven Wenglowsky , Benjamin Woodard , Laura Woodard
发明人： Lawrence Blatt , Steven Andrews , Kevin Condroski , George Doherty , Yutong Jiang , John Josey , April Kennedy , Machender Madduru , Peter Stengel , Steven Wenglowsky , Benjamin Woodard , Laura Woodard
IPC分类号： A61K31/4709 , A61K38/12
CPC分类号： C07K5/0804
摘要： The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including 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-XIX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，包括治疗黄病毒感染的方法，包括丙型肝炎病毒感染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

US20070054842A1 Novel macrocyclic inhibitors of hepatitis C virus replication 有权
标题翻译：丙型肝炎病毒复制的新型大环抑制剂
公开(公告)号：US20070054842A1
公开(公告)日：2007-03-08
申请号：US11491126
申请日：2006-07-21
申请人： Lawrence Blatt , Scott Seiwert , Steven Andrews , Pierre Martin , Andreas Schumacher , Bradley Barnett , C. Eary , Robert Kaus , Timothy Kercher , Weidong Liu , Michael Lyon , Paul Nichols , Bin Wang , Tarek Sammakia , April Kennedy , Yutong Jiang
发明人： Lawrence Blatt , Scott Seiwert , Steven Andrews , Pierre Martin , Andreas Schumacher , Bradley Barnett , C. Eary , Robert Kaus , Timothy Kercher , Weidong Liu , Michael Lyon , Paul Nichols , Bin Wang , Tarek Sammakia , April Kennedy , Yutong Jiang
IPC分类号： A61K38/12
CPC分类号： C07K5/0806 , A61K38/00 , A61K38/1793 , A61K38/212 , A61K38/217 , A61K38/2292 , A61K38/55 , C07D471/04 , C07D487/04 , C07K5/0804 , A61K2300/00
摘要： The embodiments provide compounds of the general Formulae I through general Formula VIII, 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：实施方案提供通式I至通式VIII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

US20080019942A1 NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION 失效
标题翻译： HEPATITIS C VIRUS REPLICATION的新型抑制剂
公开(公告)号：US20080019942A1
公开(公告)日：2008-01-24
申请号：US11773912
申请日：2007-07-05
申请人： Scott Seiwert , Leonid Beigelman , Lawrence Blatt , Timothy Kercher , April Kennedy , Steven Andrews
发明人： Scott Seiwert , Leonid Beigelman , Lawrence Blatt , Timothy Kercher , April Kennedy , Steven Andrews
IPC分类号： A61K38/21 , A61K31/4035 , A61K31/416 , A61K31/437 , C07D209/44 , C07D471/04 , C07D231/54 , A61P31/12 , A61K31/505 , A61K31/52
CPC分类号： C07D403/14 , C07D231/56 , C07D471/04
摘要： The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula III, 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。实施方案提供了通式II的化合物，以及包含主题化合物的组合物，包括药物组合物。实施方案提供了通式III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。

4. 发明申请

US20090093533A1 COMPOUNDS AND METHODS FOR INHIBITING HEPATITIS C VIRAL REPLICATION 失效
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：US20090093533A1
公开(公告)日：2009-04-09
申请号：US12089895
申请日：2006-10-10
申请人： Leonid Beigelman , Scott D. Seiwert , Lawrence Blatt , Steven Andrews , Julia Haas
发明人： Leonid Beigelman , Scott D. Seiwert , Lawrence Blatt , Steven Andrews , Julia Haas
IPC分类号： A61K31/407 , C07D245/00 , A61P31/12
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. 发明授权

US08119592B2 Compounds and methods for inhibiting hepatitis C viral replication 失效
标题翻译：用于抑制丙型肝炎病毒复制的化合物和方法
公开(公告)号：US08119592B2
公开(公告)日：2012-02-21
申请号：US12089895
申请日：2006-10-10
申请人： Leonid Beigelman , Scott D. Seiwert , Lawrence Blatt , Steven Andrews , Julia Haas
发明人： Leonid Beigelman , Scott D. Seiwert , Lawrence Blatt , Steven Andrews , Julia Haas
IPC分类号： A61K38/12
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。

6. 发明申请

US20070026394A1 Modulation of gene expression associated with inflammation proliferation and neurite outgrowth using nucleic acid based technologies 审中-公开
标题翻译：使用基于核酸的技术调控与炎症增殖和神经突生长相关的基因表达
公开(公告)号：US20070026394A1
公开(公告)日：2007-02-01
申请号：US10471271
申请日：2002-04-03
申请人： Lawrence Blatt , Bharat Chowrira , Peter Haeberli , James McSwiggen , Kathy Fosnaugh
发明人： Lawrence Blatt , Bharat Chowrira , Peter Haeberli , James McSwiggen , Kathy Fosnaugh
IPC分类号： C12Q1/68 , C07H21/02 , A61K48/00
CPC分类号： C12N15/1137 , A61K38/00 , C12N15/113 , C12N15/1138 , C12N2310/12 , C12N2310/121 , C12N2310/13 , C12N2310/14 , C12N2310/18 , C12N2310/315 , C12N2310/317 , C12N2310/321 , C12N2310/332 , C12N2310/346 , C12N2310/3521
摘要： The present invention relates to nucleic acid molecules, including antisense, enzymatic nucleic acid molecules, and RNA interference molecules, such as hammerhead ribozymes, DNAzymes, allozymes, siRNA, decoys and antisense, which modulate the expression of prostaglandin D2 (PTGDS), prostaglandin D2 receptor (PTGDR), adenosine receptor, NOGO and NOGO receptor, and IKK genes, such as IKK-gamma, IKK-alpha, or IKK-beta, and PKR genes.
摘要翻译：本发明涉及核酸分子，包括反义，酶核酸分子和RNA干扰分子，例如调节前列腺素D2（PTGDS），前列腺素D2（PTGDS）的表达的锤头核酶，DNA酶，同工酶，siRNA，诱饵和反义受体（PTGDR），腺苷受体，NOGO和NOGO受体以及IKK基因，例如IKK-γ，IKK-α或IKK-β和PKR基因。

7. 发明申请

US20060270612A1 Method of modulating stress-activated protein kinase system 有权
标题翻译：调节应激激活蛋白激酶系统的方法
公开(公告)号：US20060270612A1
公开(公告)日：2006-11-30
申请号：US11431132
申请日：2006-05-09
申请人： Lawrence Blatt , Scott Seiwert , Leonid Beigelman , Ramachandran Radhakrishnan
发明人： Lawrence Blatt , Scott Seiwert , Leonid Beigelman , Ramachandran Radhakrishnan
IPC分类号： A61K31/7052 , A61K31/4704 , A61K31/4412
CPC分类号： A61K31/4412 , A61K31/44 , A61K31/444 , A61K31/45 , A61K31/4704 , A61K31/7052 , A61K47/56 , A61K47/58 , C07D213/16 , C07D213/26 , C07D213/63 , C07D213/64 , C07D213/69 , C07D215/227 , C07H15/26 , C07K1/1077 , C08F289/00 , Y02A50/401 , Y02A50/409 , Y02A50/411 , Y02A50/475
摘要： Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one 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 at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
摘要翻译：公开了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至少一种p38MAPK的能力; 并且其中所述接触以对所述化合物抑制至少一种p38MAPK的低百分比抑制浓度的SAPK-调节浓度进行。还公开了吡非尼酮的衍生物。这些衍生物可以调节应激活化蛋白激酶（SAPK）系统。

8. 发明申请

US20060204473A1 Synthetic hyperglycosylated, and hyperglycosylated protease-resistant polypeptide variants, oral formulations and methods of using the same 有权
公开(公告)号：US20060204473A1
公开(公告)日：2006-09-14
申请号：US11351163
申请日：2006-02-08
申请人： Lawrence Blatt , Scott Seiwert , Jin Hong
发明人： Lawrence Blatt , Scott Seiwert , Jin Hong
IPC分类号： A61K38/21 , C07K14/56 , C07K14/565 , C07K14/57
CPC分类号： C07K14/555 , A61K38/00 , C07K14/56 , C07K14/565 , C07K14/57 , Y02A50/385 , Y02A50/387 , Y02A50/393
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.

9. 发明申请

US20100240604A1 PROTECTED NUCLEOTIDE ANALOGS 审中-公开
标题翻译：保护核苷类似物
公开(公告)号：US20100240604A1
公开(公告)日：2010-09-23
申请号：US12728068
申请日：2010-03-19
申请人： Leonid Beigelman , Lawrence Blatt , Harri Lonnberg
发明人： Leonid Beigelman , Lawrence Blatt , Harri Lonnberg
IPC分类号： A61K31/7072 , C07H19/056 , A61K31/7056 , C07H19/10 , A61K31/7068 , A61P35/00 , A61P31/12 , A61P35/02 , A61P31/18 , A61P33/00 , A61P31/20 , A61P31/14 , A61P31/22
CPC分类号： C07H19/073 , C07F9/6512 , C07F9/65616 , C07H19/056 , C07H19/10 , C07H19/14 , C07H19/173 , C07H19/20
摘要： Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.
摘要翻译：本文公开了具有被保护的磷酸盐的核苷酸类似物，与被保护的磷酸盐合成核苷酸类似物的方法以及用被保护的磷酸盐的核苷酸类似物治疗疾病和/或病症如病毒感染，癌症和/或寄生虫病的方法。

10. 发明申请

US20070117841A1 Use of pirfenidone in therapeutic regimens 失效
标题翻译：吡非尼酮在治疗方案中的应用
公开(公告)号：US20070117841A1
公开(公告)日：2007-05-24
申请号：US10574631
申请日：2004-10-21
申请人： Osman Ozes , Lawrence Blatt , Scott Seiwert
发明人： Osman Ozes , Lawrence Blatt , Scott Seiwert
IPC分类号： A61K31/47
CPC分类号： A61K31/47 , A61K31/4412 , A61K38/212 , A61K38/217 , A61K45/06 , G01N33/5091 , Y02A50/411 , A61K2300/00
摘要： The present invention provides methods for treating a disorder, and methods for inhibiting a stress-activated protein kinase (SAPK) in a cell in an individual, the methods generally involving administering to an individual in need thereof an effective amount of pirfenidone or a pirfenidone analog; comparing a post-treatment SAPK activity level in a biological sample from the individual with a pre-treatment SAPK activity level; and adjusting the dose of the pirfenidone or pirfenidone analog based on the results of the comparison step. The present invention provides methods for treating a disorder, and methods for inhibiting a SAPK in a cell in an individual, the methods generally involving administering to an individual in need thereof an effective amount of pirfenidone or a pirfenidone analog; comparing a second post-treatment SAPK activity level in a biological sample from the individual with a first post-treatment SAPK activity level; and adjusting the dose of the pirfenidone or pirfenidone analog based on the results of the comparison step.
摘要翻译：本发明提供了治疗病症的方法以及在个体细胞中抑制应激活化蛋白激酶（SAPK）的方法，所述方法通常涉及向有需要的个体施用有效量的吡非尼酮或吡非尼酮类似物 ; 将来自个体的生物样品中的后处理SAPK活性水平与预处理SAPK活性水平进行比较; 并根据比较步骤的结果调整吡非尼酮或吡非尼酮类似物的剂量。本发明提供了治疗病症的方法以及在个体细胞中抑制SAPK的方法，所述方法通常涉及向有需要的个体施用有效量的吡非尼酮或吡非尼酮类似物; 将来自个体的生物样品中的第二后处理SAPK活性水平与第一后处理SAPK活性水平进行比较; 并根据比较步骤的结果调整吡非尼酮或吡非尼酮类似物的剂量。

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