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1. 发明申请

WO2006130628A3 COMBINATION OF HCV PROTEASE INHIBITORS WITH A SURFACTANT 审中-公开
标题翻译： HCV蛋白酶抑制剂与表面活性剂的组合
公开(公告)号：WO2006130628A3
公开(公告)日：2007-09-13
申请号：PCT/US2006021003
申请日：2006-05-31
申请人： SCHERING CORP , MALCOLM BRUCE A , BRADLEY PRUDENCE K , PAVLOVSKY ANASTASIA , CHO WING-KEE PHILIP , QIU ZHIHUI
发明人： MALCOLM BRUCE A , BRADLEY PRUDENCE K , PAVLOVSKY ANASTASIA , CHO WING-KEE PHILIP , QIU ZHIHUI
IPC分类号： A61K31/454 , A61K38/05 , A61K38/06 , A61P31/14
CPC分类号： A61K38/12 , A61K31/454 , A61K31/4709 , A61K38/05 , A61K38/06 , A61K38/08 , A61K47/10 , A61K2300/00
摘要： Pharmaceutical formulations containing at least one compound of Formulae I-XXVI herein and at least one surfactant. Pharmaceutically acceptable carriers and excipients may also be included in the formulations. The formulations of the present invention are suited for use in single unit dosages.
摘要翻译：含有至少一种本文的式I-XXVI化合物和至少一种表面活性剂的药物制剂。药学上可接受的载体和赋形剂也可以包括在制剂中。本发明的制剂适用于单一单位剂量。

2. 发明申请

WO2006130607A2 CONTROLLED-RELEASE FORMULATION 审中-公开
标题翻译：控制释放配方
公开(公告)号：WO2006130607A2
公开(公告)日：2006-12-07
申请号：PCT/US2006020969
申请日：2006-05-31
申请人： SCHERING CORP , MALCOLM BRUCE A , BRADLEY PRUDENCE K , CHO WING-KEE PHILIP , QIU ZHIHUI
发明人： MALCOLM BRUCE A , BRADLEY PRUDENCE K , CHO WING-KEE PHILIP , QIU ZHIHUI
CPC分类号： A61K38/04
摘要： Controlled release dosage formulations including at least one compound of Formulae (I) to (XXVI) herein and a controlled-release carrier and methods of treatment using the same as provided.
摘要翻译：控制释放剂量制剂，包括至少一种本文的式（I）至（XXVI）的化合物和控制释放载体以及使用其提供的治疗方法。

3. 发明申请

WO2006130552A3 METHODS OF TREATING HEPATITIS C VIRUS 审中-公开
标题翻译：治疗乙型肝炎病毒的方法
公开(公告)号：WO2006130552A3
公开(公告)日：2007-09-07
申请号：PCT/US2006020732
申请日：2006-05-31
申请人： SCHERING CORP , GUPTA SAMIR K , MALCOLM BRUCE A
发明人： GUPTA SAMIR K , MALCOLM BRUCE A
IPC分类号： A61K38/04 , A61P17/16
CPC分类号： A61K38/04 , A61K31/4709 , A61K38/05
摘要： Methods for preventing, ameliorating or treating one or more symptoms of Hepatitis C virus (HCV), modulating HCV protease activity and/or inhibiting cathepsin activity in a subject, wherein the methods comprise administering to a subject in need of such treatment a dosage formulation containing at least one compound of Formulae (I) - XXVI herein, wherein the dosage formulation is capable of maintaining an average Cmin plasma concentration of the compound at or above 10ng/ml.
摘要翻译：用于预防，改善或治疗丙型肝炎病毒（HCV）的一种或多种症状，调节HCV蛋白酶活性和/或抑制受试者中组织蛋白酶活性的方法，其中所述方法包括向需要这种治疗的受试者施用含有至少一种本文的式（I）-ⅩⅩⅥ化合物，其中剂量制剂能够维持化合物的平均Cmin血浆浓度在10ng / ml以上。

4. 发明申请

WO2006130553A3 HCV PROTEASE INHIBITORS 审中-公开
标题翻译： HCV蛋白酶抑制剂
公开(公告)号：WO2006130553A3
公开(公告)日：2007-07-19
申请号：PCT/US2006020733
申请日：2006-05-31
申请人： SCHERING CORP , ALBRECHT JANICE K , LAUGHLIN MARK A , MALCOLM BRUCE A
发明人： ALBRECHT JANICE K , LAUGHLIN MARK A , MALCOLM BRUCE A
IPC分类号： A61K31/40 , A61P31/12 , C07K5/08
CPC分类号： A61K31/40 , A61K38/08 , C07K5/0802 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/1005 , C07K5/101 , C07K5/1016 , C07K7/06
摘要： A method of treating, preventing or ameliorating one or more symptoms associated with hepatitis C virus (HCV) in a patient in whom either the HCV is of Genotype 1 and/or the patient was previously treated with interferon and the previous interferon therapy was ineffective to treat the one or more symptoms associated with HCV, comprising administering to such a patient an effective amount of at least one compound of formulae I-XXVI of which the structural formula (I) is exemplary or a pharmaceutically acceptable salt, solvate or ester thereof. Optional combined administration of said at least one compound with an interferon or pegylated interferon and/or ribaviron is also contemplated.
摘要翻译：在丙型肝炎病毒（HCV）与丙型肝炎病毒（HCV）为基因型1和/或患者之前的治疗，预防或改善一种或多种与干扰素治疗有关的症状的方法，先前的干扰素治疗无效治疗与HCV相关的一种或多种症状，其包括向所述患者施用有效量的至少一种结构式（I）为其的式I-XXVI化合物或其药学上可接受的盐，溶剂合物或酯。还考虑了所述至少一种化合物与干扰素或聚乙二醇化干扰素和/或ribaviron的任选组合给药。

5. 发明申请

WO2006017505A3 PHARMACEUTICAL FORMULATIONS COMPRISING PLECONARIL FOR THE TREATMENT OF AIRWAY DISEASES 审中-公开
标题翻译：包含用于治疗气道疾病的药物的药物制剂
公开(公告)号：WO2006017505A3
公开(公告)日：2006-12-14
申请号：PCT/US2005027428
申请日：2005-08-03
申请人： SCHERING CORP , LITHGOW THEODORE L , MEDEIROS PAUL T , ELLWAY KEITH ANTHONY , HIGGINS THOMAS J , LORBER RICHARD R , MALCOLM BRUCE A , RADWANSKI ELAINE , STAUDINGER HERIBERT W
发明人： LITHGOW THEODORE L , MEDEIROS PAUL T , ELLWAY KEITH ANTHONY , HIGGINS THOMAS J , LORBER RICHARD R , MALCOLM BRUCE A , RADWANSKI ELAINE , STAUDINGER HERIBERT W
IPC分类号： A61K31/4245 , A61K45/06 , A61P11/00 , A61P31/16
CPC分类号： A61K45/06 , A61K31/4245 , A61K31/573 , A61K2300/00
摘要： Disclosed are medicaments containing, separately or together, (A) Pleconaril or a pharmaceutically acceptable salt thereof and (B) a pharmaceutically active agent for simultaneous, sequential or separate administration in the treatment of a viral infection and/or other disease states and the symptoms associated therewith.
摘要翻译：披露了（A）Pleconaril或其药学上可接受的盐和（B）用于在治疗病毒感染和/或其他疾病状态下同时，连续或分开给药的药物活性剂的药物，以及症状相关联。

6. 发明申请

WO2007092645A3 NOVEL HCV INHIBITOR COMBINATIONS AND METHODS 审中-公开
标题翻译：新的HCV抑制剂组合和方法
公开(公告)号：WO2007092645A3
公开(公告)日：2007-10-04
申请号：PCT/US2007003807
申请日：2007-02-09
申请人： SCHERING CORP , VIROPHARMA INC , WYETH CORP , EMINI EMILIO ANTHONY , FLINT MICHAEL JAMES , HOWE ANITA YEE MEI , MALCOLM BRUCE A , MULLEN STANLEY L , RALSTON ROBERT ORVILLE , TONG XIAO
发明人： EMINI EMILIO ANTHONY , FLINT MICHAEL JAMES , HOWE ANITA YEE MEI , MALCOLM BRUCE A , MULLEN STANLEY L , RALSTON ROBERT ORVILLE , TONG XIAO
IPC分类号： A61K38/06 , A61K31/343 , A61P31/14
CPC分类号： A61K31/343 , A61K31/407 , A61K31/7056 , A61K38/06 , A61K38/21 , A61K2300/00
摘要： Novel hepatitis C virus ("HCV") inhibitor combinations comprising an HCV protease inhibitor and HCV polymerase inhibitor, and optionally one or more biologically active agents, as well as uses of these combinations as HCV inhibitors and for treating hepatitis C and related disorders are disclosed.
摘要翻译：公开了包含HCV蛋白酶抑制剂和HCV聚合酶抑制剂和任选的一种或多种生物活性剂的新型丙型肝炎病毒（“HCV”）抑制剂组合以及这些组合作为HCV抑制剂和用于治疗丙型肝炎和相关病症的用途。

7. 发明申请

WO2006130626A3 METHOD FOR MODULATING ACTIVITY OF HCV PROTEASE THROUGH USE OF A NOVEL HCV PROTEASE INHIBITOR TO REDUCE DURATION OF TREATMENT PERIOD 审中-公开
标题翻译：通过使用新型HCV蛋白酶抑制剂来调节HCV蛋白酶的活性以减少治疗时间的方法
公开(公告)号：WO2006130626A3
公开(公告)日：2007-09-20
申请号：PCT/US2006021001
申请日：2006-05-31
申请人： SCHERING CORP , MALCOLM BRUCE A
发明人： MALCOLM BRUCE A
IPC分类号： A61K38/04 , A61K38/21 , A61P31/12
CPC分类号： A61K38/04 , A61K31/4709 , A61K38/05 , A61K38/06 , A61K38/08 , A61K38/12 , A61K38/212
摘要： Methods are provided for using at least one novel hepatitis C ("HCV") protease inhibitor in combination with at least one antiviral and/or immunomodulatory agent, which is different from the at least one HCV protease inhibitor, for treating a wide variety of diseases or disorders associated with hepatitis C virus by modulating the activity of HCV protease (for example HCV NS3/NS4a serine protease) and reducing HCV viral load in a subject in a reduced treatment period. With the present invention, a hepatitis C viral load is reduced in a subject to a concentration of less than 6 x10 -5 HCV virions per milliliter of plasma in a time period of less than or equal to about 24 weeks. With the present invention, a hepatitis C viral production is suppressed with an effectiveness in a range of 0.7 to 0.997.
摘要翻译：提供了使用至少一种新型丙型肝炎（“HCV”）蛋白酶抑制剂与至少一种与至少一种HCV蛋白酶抑制剂不同的抗病毒和/或免疫调节剂组合用于治疗各种疾病的方法或通过调节HCV蛋白酶（例如HCV NS3 / NS4a丝氨酸蛋白酶）的活性并在减少的治疗期内降低受试者中HCV病毒载量而与丙型肝炎病毒相关的疾病。利用本发明，在小于或等于约24小时的时间内，受试者中丙型肝炎病毒载量降低到每毫升血浆中小于6×10 -5个HCV病毒粒子的浓度周。通过本发明，可以抑制丙型肝炎病毒的产生，效果在0.7〜0.997的范围内。

8. 发明申请

WO2006113942A3 METHOD OF INHIBITING CATHEPSIN ACTIVITY 审中-公开
标题翻译：抑制CATHEPSIN活性的方法
公开(公告)号：WO2006113942A3
公开(公告)日：2008-01-03
申请号：PCT/US2006015578
申请日：2006-04-20
申请人： SCHERING CORP , MALCOLM BRUCE A
发明人： MALCOLM BRUCE A
IPC分类号： C07K5/08 , A61P9/00 , A61P19/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号： A61K38/08 , C07K5/1005 , C07K5/101 , C07K5/1016 , C07K5/1027
摘要： The present invention provides methods of inhibiting cathepsin activity in a subject in need thereof comprising administering to said subject an effective amount of at least one compound of various formulae (e.g., formula I-XXVI) disclosed herein. The present invention also provides methods of treatment of various diseases utilizing the foregoing compounds.
摘要翻译：本发明提供了在有需要的受试者中抑制组织蛋白酶活性的方法，包括向所述受试者施用有效量的至少一种本文公开的各种式（如式I-XXVI）的化合物。本发明还提供了利用上述化合物治疗各种疾病的方法。

9. 发明申请

WO2007092616A3 COMBINATIONS COMPRISING HCV PROTEASE INHIBITOR(S) AND HCV POLYMERASE INHIBITOR(S), AND METHODS OF TREATMENT RELATED THERETO 审中-公开
标题翻译：包含HCV蛋白酶抑制剂（S）和HCV聚合酶抑制剂（S）的组合以及与其相关的治疗方法
公开(公告)号：WO2007092616A3
公开(公告)日：2007-10-04
申请号：PCT/US2007003556
申请日：2007-02-09
申请人： SCHERING CORP , TONG XIAO , MALCOLM BRUCE A , HUANG HSUEH-CHENG
发明人： TONG XIAO , MALCOLM BRUCE A , HUANG HSUEH-CHENG
IPC分类号： A61K38/06 , A61K38/07 , A61K38/08 , A61K45/06 , A61P31/14
CPC分类号： A61K38/07 , A61K38/06 , A61K38/08 , A61K45/06 , A61K2300/00
摘要： Disclosed are medicaments, pharmaceutical compositions, pharmaceutical kits, and methods based on combinations of at least one HCV protease inhibitor and at least one HCV polymerase inhibitor but not HCV-796; for concurrent or consecutive administration in treating or ameliorating one or more symptoms of HCV, or disorders associated with HCV in a subject in need thereof.
摘要翻译：公开了基于至少一种HCV蛋白酶抑制剂和至少一种HCV聚合酶抑制剂但不是HCV-796的组合的药物，药物组合物，药物试剂盒和方法; 用于在有需要的受试者中同时或连续施用以治疗或改善HCV的一种或多种症状或与HCV有关的病症。

10. 发明申请

WO2006130688A3 COMPOUNDS FOR INHIBITING CATHEPSIN ACTIVITY 审中-公开
标题翻译：抑制CATHEPSIN活性的化合物
公开(公告)号：WO2006130688A3
公开(公告)日：2007-08-09
申请号：PCT/US2006021117
申请日：2006-05-31
申请人： SCHERING CORP , MALCOLM BRUCE A
发明人： MALCOLM BRUCE A
IPC分类号： C07K5/08 , A61P9/00 , A61P19/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号： C07K5/0808 , A61K31/40 , A61K31/4709 , A61K38/04 , A61K38/05 , C07K5/0202 , C07K5/0217 , C07K5/0804 , C07K5/0806 , C07K7/02
摘要： A method of treating, preventing or ameliorating one or more symptoms of hepatitis C, or inhibiting cathepsin activity, in a subject is provided, in which at least one compound (e.g., a HCV protease inhibitor) is administered in one or more discrete dosages over a twenty-four hour time interval in an asymmetric pattern as to dosage amount and/or timing of dosage, wherein the at least one compound is selected from the group consisting of compounds of Formulae I-XXVI, described herein. Methods of modulating the activity of hepatitis C virus protease in a subject are also provided. Asymmetric dosing as to amount of dose and/or timing of dose permits adjustment of dosing to accommodate variations in drug metabolism and/or viral activity caused by viral cell division or a patient's circadian rhythms, thus delivering the maximum amount of dose at the time or times it is most effective.
摘要翻译：提供了治疗，预防或改善患者中一种或多种丙型肝炎症状或抑制组织蛋白酶活性的方法，其中至少一种化合物（例如，HCV蛋白酶抑制剂）以一种或多种离散剂量施用以剂量和/或剂量时间为非对称模式的二十四小时时间间隔，其中所述至少一种化合物选自本文所述的式I-XXVI化合物。还提供了调节受试者中丙型肝炎病毒蛋白酶活性的方法。对剂量和/或剂量时间的不对称剂量允许调整剂量以适应由病毒细胞分裂或患者的昼夜节律引起的药物代谢和/或病毒活性的变化，从而在该时间内递送最大量的剂量次最有效。

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