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1. 发明申请

WO2003049760A1 COMPOSITIONS AND METHOD 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物和方法
公开(公告)号：WO2003049760A1
公开(公告)日：2003-06-19
申请号：PCT/US2002/039101
申请日：2002-12-05
申请人： INTERMUNE, INC. , RADHAKRISHNAN, Ramachandran , VISOR, Gary , VAN VLASSELAER, Peter , LOVE, Richard, B.
发明人： RADHAKRISHNAN, Ramachandran , VISOR, Gary , VAN VLASSELAER, Peter , LOVE, Richard, B.
IPC分类号： A61K38/21
CPC分类号： A61K38/212 , A61K38/217 , A61K47/60 , A61K2300/00
摘要： The present invention provides compositions and methods of treating hepatitis virus infection, particularly hepatitis C virus infection. The invention provides methods of treating a hepatitis virus infection, involving administering a first form and a second form of IFN-α to provide a multiphasic pharmacokinetic profile. The multiphasic antiviral agent serum concentration profile that is achieved effects an initial rapid drop in viral titer, followed by a further decrease in viral titer over time, to achieve a sustained viral response. The invention further provides compositions that are effective in achieving a multiphasic IFN-α profile. Compositions of the invention comprise at least a first form of interferon-α (IFN-α) that has a first pharmacokinetic profile and a second form of IFN-α that has a second pharmacokinetic profile, where the second form of IFN-α has a longer mean residence time than that of the first form of IFN-α. The invention further provides compositions comprising C-terminally modified IFN-α.
摘要翻译：本发明提供治疗肝炎病毒感染，特别是丙型肝炎病毒感染的组合物和方法。本发明提供治疗肝炎病毒感染的方法，包括施用第一种形式和第二种形式的IFN-α以提供多相药代动力学特征。实现的多相抗病毒剂血清浓度分布影响病毒滴度的初始快速下降，随后随着时间的推移进一步降低病毒滴度，以实现持续的病毒反应。本发明还提供了有效实现多相IFN-α谱的组合物。本发明的组合物包含具有第一药代动力学特征的第一形式的干扰素-α（IFN-α）和具有第二药代动力学特征的第二形式的IFN-α，其中第二形式的IFN-α具有比第一种形式的IFN-α的平均停留时间更长。本发明还提供包含C-末端修饰的IFN-α的组合物。

2. 发明申请

WO2010114928A3 PROPANE- I-SULFONIC ACID {3- [5- (4 -CHLORO-PHENYL) -1H-PYRROLO [2, 3-B] PYRIDINE-3-CARBONYL] -2, 4-DIFLUORO-PHENY L } -AMIDE COMPOSITIONS AND USES THEREOF 审中-公开
公开(公告)号：WO2010114928A3
公开(公告)日：2010-10-07
申请号：PCT/US2010/029489
申请日：2010-03-31
申请人： F.HOFFMANN-LA ROCHE AG , PLEXXIKON, INC. , DESAI, Dipen , DIODONE, Ralph , GO, Zenaida , IBRAHIM, Prabha, N. , IYER, Raman, Mahadevan , MAIR, Hans-Juergen , SANDHU, Harpreet, K. , SHAH, Navnit, Hargovindas , VISOR, Gary, Conard , WYTTENBACH, Nicole , LAUPER, Stephan , PUDEWELL, Johannes , WIERSCHEM, Frank
发明人： DESAI, Dipen , DIODONE, Ralph , GO, Zenaida , IBRAHIM, Prabha, N. , IYER, Raman, Mahadevan , MAIR, Hans-Juergen , SANDHU, Harpreet, K. , SHAH, Navnit, Hargovindas , VISOR, Gary, Conard , WYTTENBACH, Nicole , LAUPER, Stephan , PUDEWELL, Johannes , WIERSCHEM, Frank
IPC分类号： C07D471/04 , A61P35/00 , A61K31/437
摘要： Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1 -sulfonic acid {3-[5-(4-chloro-pheny!)-lH-pyrrolo[2,3-b]pyridine-3-carbonyl]- 2,4-difluoro-phenyl} -amide. (Formula I).

3. 发明申请

WO2004076474A2 POLYETHYLENE GLYCOL MODIFIED INTERFERON COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：聚乙烯甘油改性干扰素组合物及其使用方法
公开(公告)号：WO2004076474A2
公开(公告)日：2004-09-10
申请号：PCT/US2004/005649
申请日：2004-02-24
申请人： INTERMUNE INC. , VAN VLASSELAER, Peter , ROBERTS, Michael J. , VISOR, Gary , CHARLES, Stephen A.
发明人： VAN VLASSELAER, Peter , ROBERTS, Michael J. , VISOR, Gary , CHARLES, Stephen A.
IPC分类号： C07K
CPC分类号： C07K14/56 , A61K38/00 , A61K47/60
摘要： Interferon alpha (IFN-α) linked to a linear polyethylene glycol (PEG) molecule having a nominal molecular weight of about 30 kD, and compositions comprising the same, are provided. The invention further provides methods of treating a viral infection with the subject PEG-modified IFN-α.
摘要翻译：提供了与标称分子量为约30kD的线性聚乙二醇（PEG）分子连接的干扰素α（IFN-α）和包含其的组合物。本发明还提供用受试者PEG修饰的IFN-α治疗病毒感染的方法。

4. 发明申请

WO2012161776A1 SOLID FORMS OF A PHARMACEUTICALLY ACTIVE SUBSTANCE 审中-公开
标题翻译：药物活性物质的固体形式
公开(公告)号：WO2012161776A1
公开(公告)日：2012-11-29
申请号：PCT/US2012/025965
申请日：2012-02-21
申请人： PLEXXIKON INC. , F.HOFFMANN-LA ROCHE AG , DIODONE, Ralph , FAHNRICH, Karsten , IBRAHIM, Prabha, N. , KUANG, Shan-ming , VISOR, Gary, Conard , ZHAO, Baoshu , SCHWITTER, Urs
发明人： DIODONE, Ralph , FAHNRICH, Karsten , IBRAHIM, Prabha, N. , KUANG, Shan-ming , VISOR, Gary, Conard , ZHAO, Baoshu , SCHWITTER, Urs
IPC分类号： A61P35/00
CPC分类号： C07D471/04 , A61K31/437
摘要： The present invention provides solid forms of the compound of formula 1 and pharmaceutical uses thereof. (I)
摘要翻译：本发明提供式1化合物的固体形式及其药物用途。（一世）

5. 发明申请

WO2010114928A2 COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：组合物及其用途
公开(公告)号：WO2010114928A2
公开(公告)日：2010-10-07
申请号：PCT/US2010029489
申请日：2010-03-31
申请人： HOFFMANN LA ROCHE , PLEXXIKON INC , DESAI DIPEN , DIODONE RALPH , GO ZENAIDA , IBRAHIM PRABHA N , IYER RAMAN MAHADEVAN , MAIR HANS-JUERGEN , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS , VISOR GARY CONARD , WYTTENBACH NICOLE , LAUPER STEPHAN , PUDEWELL JOHANNES , WIERSCHEM FRANK
发明人： DESAI DIPEN , DIODONE RALPH , GO ZENAIDA , IBRAHIM PRABHA N , IYER RAMAN MAHADEVAN , MAIR HANS-JUERGEN , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS , VISOR GARY CONARD , WYTTENBACH NICOLE , LAUPER STEPHAN , PUDEWELL JOHANNES , WIERSCHEM FRANK
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , A61K9/0014 , A61K9/0019 , A61K9/10 , A61K9/1635 , A61K9/1652 , A61K31/437 , C07B2200/13
摘要： Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide.
摘要翻译：提供的是固体分散体，固体分子复合物，盐和结晶多晶型物，其涉及丙烷-1-磺酸{3- [5-（4-氯 - 苯基）-1H-吡咯并[2,3-b]吡啶-3-羰基] -2,4-二氟 - 苯基} - 酰胺。

6. 发明申请

WO2004076474A3 POLYETHYLENE GLYCOL MODIFIED INTERFERON COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：聚乙烯甘油改性干扰素组合物及其使用方法
公开(公告)号：WO2004076474A3
公开(公告)日：2005-01-06
申请号：PCT/US2004005649
申请日：2004-02-24
申请人： INTERMUNE INC , VAN VLASSELAER PETER , ROBERTS MICHAEL J , VISOR GARY , CHARLES STEPHEN A
发明人： VAN VLASSELAER PETER , ROBERTS MICHAEL J , VISOR GARY , CHARLES STEPHEN A
IPC分类号： A61K38/00 , A61K47/48 , C07K20060101 , C07K1/107 , C07K1/113 , C07K14/56
CPC分类号： C07K14/56 , A61K38/00 , A61K47/60
摘要： Interferon alpha (IFN-alpha) linked to a linear polyethylene glycol (PEG) molecule having a nominal molecular weight of about 30 kD, and compositions comprising the same, are provided. The invention further provides methods of treating a viral infection with the subject PEG-modified IFN-alpha.
摘要翻译：提供了与标称分子量为约30kD的线性聚乙二醇（PEG）分子连接的干扰素α（IFN-α）和包含其的组合物。本发明还提供用受试者PEG修饰的IFN-α治疗病毒感染的方法。

7. 发明申请

WO2003030923A1 METHOD OF TREATING HEPATITIS VIRUS INFECTION WITH A MULTIPHASIC INTERFERON DELIVERY PROFILE 审中-公开
标题翻译：用多功能干扰素递送谱描述乙型肝炎病毒感染的方法
公开(公告)号：WO2003030923A1
公开(公告)日：2003-04-17
申请号：PCT/US2002/030837
申请日：2002-09-26
申请人： INTERMUNE, INC. , VISOR, Gary , VAN VLASSELAER Peter
发明人： VISOR, Gary , VAN VLASSELAER Peter
IPC分类号： A61K38/00
CPC分类号： A61K38/212 , A61K38/217
摘要： The present invention provides methods of treating hepatitis virus infection. The methods generally involve administering a composition comprising an antiviral agent in a dosing regimen that achieves a multiphasic serum concentration profile of the antiviral agent. The dosing regiment includes dosing events that are less frequent than with currently available hepatitis therapies. The multiphasic antiviral agent serum concentration profile that is achieved using the methods of the invention effects an initial rapid drop in viral titer, followed by a further decrease in viral titer over time, to achieve a sustained viral response.
摘要翻译：本发明提供治疗肝炎病毒感染的方法。所述方法通常包括在实现抗病毒剂的多相血清浓度分布的给药方案中施用包含抗病毒剂的组合物。给药组包括比目前可用的肝炎疗法更少的给药事件。使用本发明的方法实现的多相抗病毒剂血清浓度分布影响病毒滴度的初始快速下降，随后随着时间的推移进一步降低病毒滴度，以达到持续的病毒反应。

8. 发明申请

WO2010129570A1 SOLID FORMS OF SULFONAMIDES AND AMINO ACIDS 审中-公开
标题翻译：磺酰胺和氨基酸的固体形式
公开(公告)号：WO2010129570A1
公开(公告)日：2010-11-11
申请号：PCT/US2010/033576
申请日：2010-05-04
申请人： PLEXXIKON, INC. , VISOR, Gary Conard , IBRAHIM, Prabha N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , WU, Guoxian
发明人： VISOR, Gary Conard , IBRAHIM, Prabha N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , WU, Guoxian
IPC分类号： C07D213/56 , C07D471/04 , A61K9/16 , A61K47/48 , A61K9/00 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer.
摘要翻译：描述了对蛋白激酶（包括Raf蛋白激酶）有活性的式（I）的苯基磺酰胺化合物的固体形式，以及使用这些固体形式治疗与蛋白激酶活性相关的疾病和病症的方法，例如， Raf蛋白激酶，包括疼痛，多囊肾病，黑素瘤和结肠直肠癌。

9. 发明申请

WO2009117482A8 MTOR INHIBITOR SALT FORMS 审中-公开
公开(公告)号：WO2009117482A8
公开(公告)日：2009-09-24
申请号：PCT/US2009/037505
申请日：2009-03-18
申请人： OSI PHARMACEUTICALS, INC , CASTELHANO, Arlindo, L. , MULVIHILL, Kristen, Michelle , VISOR, Gary, C. , RECHKA, Josef, A.
发明人： CASTELHANO, Arlindo, L. , MULVIHILL, Kristen, Michelle , VISOR, Gary, C. , RECHKA, Josef, A.
IPC分类号： C07D487/04 , A61K45/06
摘要： Salt forms of mTOR inhibitors of the Formula (I) and methods of preparation, formulation, and use in treating disease.

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