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1. 发明申请

WO2004040003A3 NUCLEOTIDE-BINDING PROTEIN-DIRECTED PROBES AND METHODS OF THEIR SYNTHESIS AND USE 审中-公开
标题翻译：核蛋白结合蛋白质指导的探针及其合成与使用方法
公开(公告)号：WO2004040003A3
公开(公告)日：2004-12-23
申请号：PCT/US0334550
申请日：2003-10-29
申请人： ACTIVX BIOSCIENCES INC , CAMPBELL DAVID ALAN , SZARDENINGS ANNA KATRIN , SHREDER KEVIN ROBERT , BETANCORT JUAN MANUEL , WINN DAVID
发明人： CAMPBELL DAVID ALAN , SZARDENINGS ANNA KATRIN , SHREDER KEVIN ROBERT , BETANCORT JUAN MANUEL , WINN DAVID
IPC分类号： C07D405/12 , C07D405/14 , C07D473/00 , C07D487/14 , C07H19/23 , G01N33/573 , A61K38/00
CPC分类号： C07H19/23 , C07D405/12 , C07D405/14 , C07D473/00 , C07D487/14 , G01N33/573
摘要： The present invention provides nucleotide binding protein-directed affinity probes ("NBAPS"), and methods of their preparation and use. The subject methods and compositions can provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of nucleotide binding proteins in a complex protein mixture, preferably kinases, and most preferably active forms of kinases, using NBAPs that bind to target nucleotide binding protein(s). The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.
摘要翻译：本发明提供了核苷酸结合蛋白质指导的亲和探针（“NBAPS”）及其制备和使用方法。本发明的方法和组合物可以使用结合靶核苷酸的NBAP来鉴定复合蛋白混合物中优选激酶，最优选活性形式的激酶中核苷酸结合蛋白的存在，量或活性的变化的简单性和准确性结合蛋白。本文描述的谱分析方法可以具有导致鉴定复合蛋白质混合物中的靶核苷酸结合蛋白的多个步骤。

2. 发明申请

WO2004090154A2 ACYL- PHOSPHATE AND PHOSPHONATE PROBES AND METHODS OF THEIR SYNTHESIS AND USE IN PROTEOMIC ANALYSIS 审中-公开
标题翻译： ACYL-磷酸盐和磷酸盐探针及其合成和使用在保护性分析中的应用
公开(公告)号：WO2004090154A2
公开(公告)日：2004-10-21
申请号：PCT/US2004010075
申请日：2004-04-01
申请人： ACTIVX BIOSCIENCES INC , CAMPBELL DAVID ALAN , LIYANAGE MAREK , SZARDENINGS ANNA KATRIN , WU MIN
发明人： CAMPBELL DAVID ALAN , LIYANAGE MAREK , SZARDENINGS ANNA KATRIN , WU MIN
IPC分类号： C07F9/6512 , C07H19/10 , C07H19/20 , C07H21/04 , C07K9/00 , C12Q20060101 , C12Q1/68 , C12Q
CPC分类号： C07H19/10 , C07H19/20 , C07H21/04 , C12Q1/485
摘要： The present invention provides tagged acyl phosphate probes ("TAPPs"), and methods of their preparation and use. The subject methods and compositions can provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of target proteins in a complex protein mixture, preferably nucleotide binding proteins using nucleotide binding protein-directed TAPPs. The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.
摘要翻译：本发明提供标记的酰基磷酸酯探针（“TAPPs”）及其制备和使用的方法。本发明的方法和组合物可以提供增强的简单性和准确性，以鉴别复合蛋白混合物中靶蛋白的存在，量或活性的变化，优选使用核苷酸结合蛋白质导向的TAPP的核苷酸结合蛋白。本文描述的谱分析方法可以具有导致鉴定复合蛋白质混合物中的靶核苷酸结合蛋白的多个步骤。

3. 发明申请

WO2008070358A2 HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR 审中-公开
标题翻译： HEPATITIS C丝氨酸蛋白酶抑制剂及其用途
公开(公告)号：WO2008070358A2
公开(公告)日：2008-06-12
申请号：PCT/US2007083034
申请日：2007-10-30
申请人： PHENOMIX CORP , CAMPBELL DAVID ALAN , HEPPERLE MICHAEL E , WINN DAVID T , BETANCORT JUAN MANUEL
发明人： CAMPBELL DAVID ALAN , HEPPERLE MICHAEL E , WINN DAVID T , BETANCORT JUAN MANUEL
CPC分类号： C07K5/0812 , C07D209/44 , C07D403/12 , C07D487/04 , C07K5/06191
摘要： The present invention provides novel compounds that mimic peptides with a C-terminal penultimate proline, such compounds being useful as protease inhibitors, particularly as inhibitors of serine proteases, and more particularly as inhibitors of the NS3 serine protease from hepatitis C virus. The compounds find utility as antiviral agents directed at hepatitis C. The invention further provides methods of employing such inhibitors, alone or in combination with other therapeutic agents, to treat hepatitis C infection in a subject in need of such treatment.
摘要翻译：本发明提供了模拟具有C-末端倒数第二脯氨酸的肽的新化合物，所述化合物可用作蛋白酶抑制剂，特别是作为丝氨酸蛋白酶的抑制剂，更具体地，作为来自丙型肝炎病毒的NS3丝氨酸蛋白酶的抑制剂。该化合物可用作针对丙型肝炎的抗病毒剂。本发明还提供了使用这种抑制剂单独或与其它治疗剂组合的方法来治疗需要这种治疗的受试者中的丙型肝炎感染。

4. 发明申请

WO2007089618A3 HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR 审中-公开
标题翻译： HEPATITIS C丝氨酸蛋白酶抑制剂及其用途
公开(公告)号：WO2007089618A3
公开(公告)日：2008-01-03
申请号：PCT/US2007002225
申请日：2007-01-25
申请人： PHENOMIX CORP , CAMPBELL DAVID ALAN , HEPPERLE MICHAEL E , WINN DAVID T , BETANCORT JUAN MANUEL
发明人： CAMPBELL DAVID ALAN , HEPPERLE MICHAEL E , WINN DAVID T , BETANCORT JUAN MANUEL
IPC分类号： A61K38/00 , C07K2/00 , C07K4/00
CPC分类号： C07F5/025 , A61K38/212 , A61K2300/00
摘要： The invention provides compounds that inhibit a viral protease enzyme of the hepatitis C virus (HCV). The compounds are adapted for treatment of a HCV infection in a patient with the disease. The compounds include analogs of tripeptides and tetrapeptides that resemble the viral protease substrate. The invention also provides pharmaceutical compositions and combinations, methods of preparation of the compounds, and methods of treatment of patients afflicted with HCV using the compounds.
摘要翻译：本发明提供抑制丙型肝炎病毒（HCV）病毒蛋白酶的化合物。该化合物适于治疗患有该疾病的患者中的HCV感染。这些化合物包括类似于病毒蛋白酶底物的三肽和四肽的类似物。本发明还提供药物组合物和组合，化合物的制备方法，以及使用该化合物治疗患有HCV的患者的方法。

5. 发明申请

WO2008070733A2 MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR 审中-公开
标题翻译：大环内酯类抗生素C丝氨酸蛋白酶抑制剂及其用途
公开(公告)号：WO2008070733A2
公开(公告)日：2008-06-12
申请号：PCT/US2007086530
申请日：2007-12-05
申请人： PHENOMIX CORP , CAMPBELL DAVID ALAN , HEPPERLE MICHAEL E , WINN DAVID T , BETANCORT JUAN MANUEL
发明人： CAMPBELL DAVID ALAN , HEPPERLE MICHAEL E , WINN DAVID T , BETANCORT JUAN MANUEL
IPC分类号： C07F5/02 , A61K31/69 , A61P31/14 , C07F5/04
CPC分类号： C07F5/025
摘要： Macrocyclic inhibitors of Hepatitis C protease are provided, the inhibitors including a boronic acid or ester group, a macrocyclic ring of about 13 to 25 atoms including at least two amide linkages, a proline-analogous group, and a connecting segment joining moieties on either side of the proline-analogous group. Methods of making the HCV protease-inhibitory compounds, methods of using the compounds, formulations of the compounds, and pharmaceutical combinations including the compounds, are provided.
摘要翻译：提供丙型肝炎蛋白酶的大环抑制剂，所述抑制剂包括硼酸或酯基，约13至25个原子的大环，包括至少两个酰胺键，脯氨酸类似基团和连接部分连接任一侧的部分的脯氨酸类似组。提供制备HCV蛋白酶抑制化合物的方法，使用化合物的方法，化合物的制剂以及包括该化合物的药物组合。

6. 发明申请

WO2007016476A3 HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR 审中-公开
标题翻译： HEPATITIS C丝氨酸蛋白酶抑制剂及其用途
公开(公告)号：WO2007016476A3
公开(公告)日：2008-01-17
申请号：PCT/US2006029708
申请日：2006-07-28
申请人： PHENOMIX CORP , CAMPBELL DAVID ALAN , WINN DAVID T , BETANCORT JUAN MANUEL , HEPPERLE MICHAEL E
发明人： CAMPBELL DAVID ALAN , WINN DAVID T , BETANCORT JUAN MANUEL , HEPPERLE MICHAEL E
IPC分类号： C07F5/02 , A61K31/4025 , A61K31/69 , A61P31/14 , C07D207/12 , C07D207/14 , C07D207/16 , C07D215/233 , C07D215/38
CPC分类号： A61K38/05 , C07K5/06191
摘要： The present invention provides novel compounds which mimic peptides with a C-terminal penultimate proline, such compounds being useful as protease inhibitors, particularly as inhibitors of serine proteases, and more particularly as inhibitors of the NS3 serine protease from hepatitis C. The compounds find utility as antiviral agents directed at hepatitis C. The invention further provides methods of employing such inhibitors, alone or in combination with other therapeutic agents, to treat hepatitis C infection in a subject in need of such treatment.
摘要翻译：本发明提供了模拟具有C-末端倒数第二脯氨酸的肽的新型化合物，这些化合物可用作蛋白酶抑制剂，特别是作为丝氨酸蛋白酶的抑制剂，更特别地，作为来自丙型肝炎的NS3丝氨酸蛋白酶的抑制剂。作为针对丙型肝炎的抗病毒剂。本发明还提供了使用这种抑制剂单独或与其它治疗剂组合的方法来治疗需要这种治疗的受试者中的丙型肝炎感染。

7. 发明申请

WO2004033397A2 ACTIVITY-BASED PROBES, AND METHODS OF THEIR PREPARATION AND USE 审中-公开
标题翻译：基于活性的探针及其制备和使用方法
公开(公告)号：WO2004033397A2
公开(公告)日：2004-04-22
申请号：PCT/US0332152
申请日：2003-10-08
申请人： ACTIVX BIOSCIENCES INC , WINN DAVID , CAMPBELL DAVID ALAN
发明人： WINN DAVID , CAMPBELL DAVID ALAN
IPC分类号： C07C20060101 , C07C1/00 , C07C237/10 , C07C257/10 , C07C323/24 , C07D207/16 , C07D209/44 , C07D311/86 , C07D495/04 , C07F5/02 , C12Q1/37 , C07C
CPC分类号： C07D311/90 , C07D311/82 , C12Q1/37
摘要： The present invention provides compositions and methods for assessing profiles of catalytically active enzymes in compositions containing a plurality of proteins. In preferred embodiments, the enzyme is a hydrolase, most preferably a cysteine protease. The methods described herein use activity based probes ("ABPs") that have an affinity moiety for directing the binding of the ABP to one or more catalytically active target enzymes, a reactive group for forming a covalent bond at an active site of the target enzyme(s), and a TAG (e.g., a detectable label, preferably a fluorophore). One or more ABPs may be combined with a protein-containing sample under conditions for binding and reaction of the ABP(s) with target enzyme(s) that are present in the sample. The resulting products may then be used to assess the active enzyme profile of the sample, and can be correlated to the presence, amount, or activity of one or more target enzyme(s) present in the original complex protein mixture.
摘要翻译：本发明提供了用于在含有多种蛋白质的组合物中评估催化活性酶的谱的组合物和方法。在优选的实施方案中，酶是水解酶，最优选半胱氨酸蛋白酶。本文描述的方法使用具有亲和部分的活性基探针（“ABP”），该亲和部分用于引导ABP与一种或多种催化活性靶酶的结合，用于在靶酶的活性位点形成共价键的反应性基团（例如，可检测标记，优选荧光团）。可以在ABP与样品中存在的目标酶的结合和反应的条件下，将一种或多种ABP与含蛋白质的样品组合。然后可以将所得产物用于评估样品的活性酶谱，并且可与存在于原始复合蛋白混合物中的一种或多种目标酶的存在，量或活性相关。

8. 发明专利

IL175550A HETEROCYCLIC BORONIC ACID COMPOUNDS, MIXTURES THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 未知
公开(公告)号：IL175550A
公开(公告)日：2011-11-30
申请号：IL17555006
申请日：2006-05-10
申请人： PHENOMIX CORP , CAMPBELL DAVID ALAN , WINN DAVID T , BETANCORT JUAN M
发明人： CAMPBELL DAVID ALAN , WINN DAVID T , BETANCORT JUAN M
IPC分类号： C07F5/02
摘要： Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula (VI): including all cyclic isomers thereof, stereoisomers thereof, solvates thereof, hydrates thereof, and pharmaceutically acceptable salts thereof, and any prodrug thereof, their method of preparing and use, and a pharmaceutical composition of compound (VI).

9. 发明专利

CA2521130C ACYL-PHOSPHATE AND PHOSPHONATE PROBES AND METHODS OF THEIR SYNTHESIS AND USE IN PROTEOMIC ANALYSIS 未知
公开(公告)号：CA2521130C
公开(公告)日：2013-05-14
申请号：CA2521130
申请日：2004-04-01
申请人： ACTIVX BIOSCIENCES INC
发明人： CAMPBELL DAVID ALAN , LIYANAGE MAREK , SZARDENINGS ANNA KATRIN , WU MIN
IPC分类号： C12Q1/68 , C07F9/6512 , C07H19/10 , C07H19/20 , C07H21/04 , C07K9/00 , C12Q20060101
摘要： The present invention provides tagged acyl phosphate probes ("TAPPs"), and methods of their preparation and use. The subject methods and compositions can provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of target proteins in a complex protein mixture, preferably nucleotide binding proteins using nucleotide binding protein-directed TAPPs. The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.

10. 发明专利

CA2521130A1 ACYL- PHOSPHATE AND PHOSPHONATE PROBES AND METHODS OF THEIR SYNTHESIS AND USE IN PROTEOMIC ANALYSIS 未知
公开(公告)号：CA2521130A1
公开(公告)日：2004-10-21
申请号：CA2521130
申请日：2004-04-01
申请人： ACTIVX BIOSCIENCES INC
发明人： CAMPBELL DAVID ALAN , WU MIN , SZARDENINGS ANNA KATRIN , LIYANAGE MAREK
IPC分类号： C07F9/6512 , C07H19/10 , C07H19/20 , C07H21/04 , C07K9/00 , C12Q20060101 , C12Q1/68
摘要： The present invention provides tagged acyl phosphate probes ("TAPPs"), and methods of their preparation and use. The subject methods and compositions c an provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of target proteins in a complex protein mixtur e, preferably nucleotide binding proteins using nucleotide binding protein- directed TAPPs. The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.

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