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1. 发明申请

WO9800173A3 TARGETED DRUG DELIVERY USING SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：使用磺酰胺衍生物的目标药物递送
公开(公告)号：WO9800173A3
公开(公告)日：1998-05-07
申请号：PCT/US9710817
申请日：1997-07-01
申请人： UPJOHN CO , ZHAO ZHIYANG , TOMASSELLI ALFREDO G , KOEPLINGER KENNETH A , PETERSON TILLIE , SUARATO ANTONINO
发明人： ZHAO ZHIYANG , TOMASSELLI ALFREDO G , KOEPLINGER KENNETH A , PETERSON TILLIE , SUARATO ANTONINO
IPC分类号： C07D475/08 , A61K31/44 , A61K31/4433 , A61K31/519 , A61K31/7032 , A61K31/704 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K47/48 , A61P21/02 , A61P23/00 , A61P25/24 , A61P31/12 , A61P35/00 , A61P43/00 , C07D213/85 , C07D405/12 , C07D487/04 , C07D487/14 , C07H15/252 , C07H19/06 , C07H19/073 , C07H19/173 , C07H19/23 , C07H23/00
CPC分类号： A61K47/54
摘要： The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free -NH- which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN- or p-NO2-pyridinylsulfonyl groups, or p-NO2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The precursor is a synthetic intermediate carrying a free -NH- which has been derivatized by the attachment of an electrophile via a sulfonamide bond.

2. 发明申请

WO2002002601A3 MUTANT PRESENILIN 1 AND PRESENILIN 2 POLYPEPTIDES 审中-公开
公开(公告)号：WO2002002601A3
公开(公告)日：2002-01-10
申请号：PCT/US2001/016508
申请日：2001-06-29
申请人： PHARMACIA & UPJOHN COMPANY , CARTER, Donald, B. , TOMASSELLI, Alfredo, G.
发明人： CARTER, Donald, B. , TOMASSELLI, Alfredo, G.
IPC分类号： C12N15/12
摘要： The present invention provides mutant presenilin 1 and presenilin 2 polypeptides and polynucleotides encoding the polypeptides and methods for their production by recombinant and PCR techniques are disclosed. Methods for utilizing the mutant polypeptides in screens for inhibitors of activity are also disclosed.

3. 发明申请

WO0202601A2 MUTANT PRESENILIN 1 AND PRESENILIN 2 POLYPEPTIDES 审中-公开
标题翻译： MUTANT PRESENILIN 1和PRESENILIN 2 POLYPEPTIDS
公开(公告)号：WO0202601A2
公开(公告)日：2002-01-10
申请号：PCT/US0116508
申请日：2001-06-29
申请人： UPJOHN CO , CARTER DONALD B , TOMASSELLI ALFREDO G
发明人： CARTER DONALD B , TOMASSELLI ALFREDO G
IPC分类号： C07K14/47 , C07K14/00
CPC分类号： C07K14/4711 , A01K2217/05
摘要： The present invention provides mutant presenilin 1 and presenilin 2 polypeptides and polynucleotides encoding the polypeptides and methods for their production by recombinant and PCR techniques are disclosed. Methods for utilizing the mutant polypeptides in screens for inhibitors of activity are also disclosed.
摘要翻译：本发明提供了突变型早老素1和早老素2多肽和编码多肽的多核苷酸及其通过重组和PCR技术生产的方法。还公开了筛选中用于活性抑制剂的突变体多肽的方法。

4. 发明申请

WO0077184A9 CASPASE-8 CRYSTALS, MODELS AND METHODS 审中-公开
标题翻译： CASPASE-8水晶，模型和方法
公开(公告)号：WO0077184A9
公开(公告)日：2001-03-08
申请号：PCT/US0015882
申请日：2000-06-09
申请人： UPJOHN CO , WATT WILLIAM , WATENPAUGH KEITH D , KOEPLINGER KENNETH A , MILDNER ANA M , HEINRIKSON ROBERT L , TOMASSELLI ALFREDO G
发明人： WATT WILLIAM , WATENPAUGH KEITH D , KOEPLINGER KENNETH A , MILDNER ANA M , HEINRIKSON ROBERT L , TOMASSELLI ALFREDO G
IPC分类号： C12N15/09 , A61K38/00 , A61K38/46 , A61K45/00 , A61P9/00 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P35/00 , A61P43/00 , C07K5/103 , C12N9/64 , A61K38/07 , C12Q1/37
CPC分类号： C12N9/6475 , A61K38/00 , C07K5/101 , C07K2299/00
摘要： A caspase-8/inhibitor complex has been crytallized, and the three dimensional x-ray crystal structure of a recombinant human caspase-8 has been solved at atomic resolution (1.2 ANGSTROM ), and substrate binding pocket has been identified. The x-ray crystal structure is useful for solving the structure of other molecules or molecular complexes, and designing modulators of caspase-8 activity.
摘要翻译：已经将半胱天冬酶-8抑制剂复合物凝聚，重组人半胱天冬酶-8的三维X射线晶体结构已经以原子分辨率（1.2安格姆）解决，已经鉴定出底物结合口袋。 x射线晶体结构可用于解决其他分子或分子复合物的结构，并设计半胱天冬酶-8活性的调节剂。

5. 发明申请

WO0206306A3 SUBSTRATES AND ASSAYS FOR -SECRETASE ACTIVITY 审中-公开
标题翻译：基质活性的基质和测定
公开(公告)号：WO0206306A3
公开(公告)日：2002-07-25
申请号：PCT/US0123035
申请日：2001-07-19
申请人： UPJOHN CO , YAN RIQIAN , TOMASSELLI ALFREDO G , GURNEY MARK E , EMMONS THOMAS L , BIENKOWSKI MICHAEL JEROME , HEINRIKSON ROBERT L
发明人： YAN RIQIAN , TOMASSELLI ALFREDO G , GURNEY MARK E , EMMONS THOMAS L , BIENKOWSKI MICHAEL JEROME , HEINRIKSON ROBERT L
IPC分类号： G01N33/50 , A61K45/00 , A61P25/28 , A61P43/00 , C07K2/00 , C07K5/00 , C07K5/103 , C07K7/06 , C07K7/08 , C07K14/47 , C07K19/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12Q1/02 , C12Q1/37 , G01N33/15 , C12N15/62 , A61K38/04 , C12Q1/68 , G01N33/68
CPC分类号： C07K14/4711 , C07K5/1013 , C07K7/06 , C07K7/08 , C07K14/4702 , C12Q1/37 , G01N2333/96425 , G01N2500/02
摘要： The present invention is directed to novel substrates for Hu-Asp. More particularly, the invention provides peptide substrates and fusion polypeptide substrates comprising a -secretase cleavage site. Methods and compositions for making and using the peptides are disclosed.
摘要翻译：本发明涉及用于Hu-Asp的新型底物。更具体地，本发明提供了包含分泌酶切割位点的肽底物和融合多肽底物。公开了制备和使用肽的方法和组合物。

6. 发明申请

WO1998000173A2 TARGETED DRUG DELIVERY USING SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：使用磺酰胺衍生物的目标药物递送
公开(公告)号：WO1998000173A2
公开(公告)日：1998-01-08
申请号：PCT/US1997010817
申请日：1997-07-01
申请人： PHARMACIA & UPJOHN COMPANY , ZHAO, Zhiyang , TOMASSELLI, Alfredo, G. , KOEPLINGER, Kenneth, A. , PETERSON, Tillie , SUARATO, Antonino
发明人： PHARMACIA & UPJOHN COMPANY
IPC分类号： A61K47/48
CPC分类号： A61K47/54
摘要： The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free -NH- which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN- or p-NO2-pyridinylsulfonyl groups, or p-NO2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The precursor is a synthetic intermediate carrying a free -NH- which has been derivatized by the attachment of an electrophile via a sulfonamide bond.
摘要翻译：本发明涉及谷胱甘肽S-转移酶（GST）/还原型谷胱甘肽（GSH），其作为通过磺酰胺键与特定亲电部分缀合的药物的体内释放的手段。所述药物可以是携带游离-NH-的抗癌剂（或具有其它治疗性质的物质），其通过附着含有部分的亲电子试剂例如p-CN-或p- NO2-吡啶基磺酰基衍生化，或 p-NO 2 - 或2,4-二硝基苯磺酰基或其合适的衍生物，以制备前体药物。任选地，磺酰胺部分可以与其连接有靶向分子。本发明还提供谷胱甘肽S-转移酶（GST）/还原型谷胱甘肽（GSH），作为释放通过磺酰胺键与特定亲电部分缀合的被保护的氨基衍生物的手段。前体是携带游离-NH-的合成中间体，其已经通过连接亲电子试剂通过磺酰胺键衍生化。

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