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1. 发明申请

WO2004017923A2 COMPOSITIONS AND METHODS OF THERAPY FOR CANCERS CHARACTERIZED BY EXPRESSION OF THE TUMOR-ASSOCIATED ANTIGEN MN/CA IX 审中-公开
标题翻译：肿瘤相关抗原MN / CA IX的表达特征的组合物和治疗方法
公开(公告)号：WO2004017923A2
公开(公告)日：2004-03-04
申请号：PCT/US2003/026612
申请日：2003-08-25
申请人： CHIRON CORPORATION , WONG, Justin , WINTER, Jill , LALEHZADEH, Guita , WARNE, Robert
发明人： WONG, Justin , WINTER, Jill , LALEHZADEH, Guita , WARNE, Robert
IPC分类号： A61K
CPC分类号： C07K16/30 , C07K16/40
摘要： Compositions and methods useful in inhibiting proliferation of CA IX + preneoplastic or neoplastic cells in a mammal are provided. The compositions are antagonist anti-CA IX antibodies and other inhibitory agents that target carbonic anhydrase activity of CA IX on these cells. The antagonist anti-CA IX antibodies or antigen-binding fragments thereof are specifically reactive with an inhibitory epitope of CA IX or biologically active variant thereof. Formation of an antibody-antigen complex between the antagonist anti-CA IX antibodies or antigen-binding fragments thereof and the respective inhibitory epitopes results in inhibition of carbonic anhydrase activity of CA IX or biologically active variant thereof. Other small molecule agents that inhibit carbonic anhydrase activity of CA IX or biologically active variant thereof and screening assays for identifying such agents are also provided. The antagonist anti-CA IX antibodies, antigen-binding fragments thereof, and other CA IX inhibitory agents identified herein are useful in the treatment of cancers characterized by the expression of the CA IX tumor-associated antigen.
摘要翻译：提供了可用于抑制哺乳动物中CA IX +肿瘤前和肿瘤细胞增殖的组合物和方法。该组合物是拮抗性抗CA IX抗体和其它抑制剂，其靶向这些细胞上CA IX的碳酸酐酶活性。拮抗性抗CA IX抗体或其抗原结合片段与CA IX或其生物活性变体的抑制性表位特异性反应。拮抗性抗CA IX抗体或其抗原结合片段之间的抗体 - 抗原复合物的形成和各自的抑制性表位导致CA IX或其生物活性变体的碳酸酐酶活性的抑制。还提供了抑制CA IX或其生物活性变体的碳酸酐酶活性的其它小分子试剂和用于鉴定这些试剂的筛选试验。本文鉴定的拮抗性抗CAⅨ抗体，其抗原结合片段和其它CAⅨ抑制剂可用于治疗特征在于表达CAⅨ肿瘤相关抗原的癌症。

2. 发明申请

WO2007117607A9 QUINAZOLINES FOR PDK1 INHIBITION 审中-公开
标题翻译：用于PDK1抑制剂的喹唑啉
公开(公告)号：WO2007117607A9
公开(公告)日：2008-03-06
申请号：PCT/US2007008592
申请日：2007-04-05
申请人： NOVARTIS VACCINES & DIAGNOSTIC , RAMURTHY SAVITHRI , LIN XIADONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAJONG M , JAIN RAMA , MURRAY JEREMY M , BASMAN STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN , WANG WEIBO , JANSEN JOHANNA M , WAGMAN ALLAN S , PFISTER KEITH B , NG SIMON C
发明人： RAMURTHY SAVITHRI , LIN XIADONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAJONG M , JAIN RAMA , MURRAY JEREMY M , BASMAN STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN , WANG WEIBO , JANSEN JOHANNA M , WAGMAN ALLAN S , PFISTER KEITH B , NG SIMON C
IPC分类号： C07D239/94 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12
CPC分类号： C07D239/94 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D451/06 , C07D453/02
摘要： The invention provides quinazoline compounds that are inhibitors of PDKl. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
摘要翻译：本发明提供作为PDK1抑制剂的喹唑啉化合物。还提供了包含该化合物的药物组合物，以及用化合物或组合物治疗增殖性疾病如癌症的方法。

3. 发明申请

WO2007117607A3 QUINAZOLINES FOR PDK1 INHIBITION 审中-公开
公开(公告)号：WO2007117607A3
公开(公告)日：2007-10-18
申请号：PCT/US2007/008592
申请日：2007-04-05
申请人： NOVARTIS VACCINES & DIAGNOSTICS, INC. , RAMURTHY, Savithri , LIN, Xiadong , SUBRAMANIAN, Sharada , RICO, Alice, C. , WANG, Xiajong, M. , JAIN, Rama , MURRAY, Jeremy, M. , BASMAN, Steven, E. , WARNE, Robert, L. , SHU, Wei , ZHOU, Yasheen , DOVE, Jeffrey , AIKAWA, Mina , AMIRI, Payman , WANG, Weibo , JANSEN, Johanna, M. , WAGMAN, Allan, S. , PFISTER, Keith, B. , NG, Simon, C.
发明人： RAMURTHY, Savithri , LIN, Xiadong , SUBRAMANIAN, Sharada , RICO, Alice, C. , WANG, Xiajong, M. , JAIN, Rama , MURRAY, Jeremy, M. , BASMAN, Steven, E. , WARNE, Robert, L. , SHU, Wei , ZHOU, Yasheen , DOVE, Jeffrey , AIKAWA, Mina , AMIRI, Payman , WANG, Weibo , JANSEN, Johanna, M. , WAGMAN, Allan, S. , PFISTER, Keith, B. , NG, Simon, C.
IPC分类号： C07D239/94 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12
摘要： The invention provides quinazoline compounds that are inhibitors of PDKl. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.

4. 发明申请

WO2008079988A3 QUINAZOLINES FOR PDK1 INHIBITION 审中-公开
标题翻译：用于PDK1抑制剂的喹唑啉
公开(公告)号：WO2008079988A3
公开(公告)日：2008-10-16
申请号：PCT/US2007088392
申请日：2007-12-20
申请人： NOVARTIS VACCINES & DIAGNOSTIC , RAMURTHY SAVITHRI , LIN XIAODONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAOJING M , JAIN RAMA , MURRAY JEREMY M , BASHAM STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN
发明人： RAMURTHY SAVITHRI , LIN XIAODONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAOJING M , JAIN RAMA , MURRAY JEREMY M , BASHAM STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN
IPC分类号： C07D239/84 , A61K31/517 , A61P35/00 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D411/04 , C07D413/14 , C07D417/04
CPC分类号： C07D239/84 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D411/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
摘要翻译：本发明提供了作为PDK1抑制剂的新型化合物。还提供了包含该化合物的药物组合物，以及用化合物或组合物治疗增殖性疾病如癌症的方法。

5. 发明申请

WO2008079988A9 QUINAZOLINES FOR PDK1 INHIBITION 审中-公开
公开(公告)号：WO2008079988A9
公开(公告)日：2008-07-03
申请号：PCT/US2007/088392
申请日：2007-12-20
申请人： NOVARTIS AG , RAMURTHY, Savithri , LIN, Xiaodong , SUBRAMANIAN, Sharada , RICO, Alice, C. , WANG, Xiaojing, M. , JAIN, Rama , MURRAY, Jeremy, M. , BASHAM, Steven, E. , WARNE, Robert, L. , SHU, Wei , ZHOU, Yasheen , DOVE, Jeffrey , AIKAWA, Mina , AMIRI, Payman
发明人： RAMURTHY, Savithri , LIN, Xiaodong , SUBRAMANIAN, Sharada , RICO, Alice, C. , WANG, Xiaojing, M. , JAIN, Rama , MURRAY, Jeremy, M. , BASHAM, Steven, E. , WARNE, Robert, L. , SHU, Wei , ZHOU, Yasheen , DOVE, Jeffrey , AIKAWA, Mina , AMIRI, Payman
IPC分类号： C07D239/84 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D411/04 , C07D413/14 , C07D417/04 , A61K31/517 , A61P35/00
摘要： The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.

6. 发明申请

WO2008079988A2 QUINAZOLINES FOR PDK1 INHIBITION 审中-公开
标题翻译：喹唑啉对PDK1的抑制作用
公开(公告)号：WO2008079988A2
公开(公告)日：2008-07-03
申请号：PCT/US2007088392
申请日：2007-12-20
申请人： NOVARTIS VACCINES & DIAGNOSTIC , RAMURTHY SAVITHRI , LIN XIAODONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAOJING M , JAIN RAMA , MURRAY JEREMY M , BASHAM STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN
发明人： RAMURTHY SAVITHRI , LIN XIAODONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAOJING M , JAIN RAMA , MURRAY JEREMY M , BASHAM STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN
CPC分类号： C07D239/84 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D411/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
摘要翻译：本发明提供了作为PDK1抑制剂的新化合物。还提供了包含所述化合物的药物组合物，以及用所述化合物或组合物治疗增殖性疾病如癌症的方法。

7. 发明申请

WO2007117607A2 QUINAZOLINES FOR PDK1 INHIBITION 审中-公开
标题翻译：用于PDK1抑制剂的喹唑啉
公开(公告)号：WO2007117607A2
公开(公告)日：2007-10-18
申请号：PCT/US2007008592
申请日：2007-04-05
申请人： NOVARTIS VACCINES & DIAGNOSTIC , RAMURTHY SAVITHRI , LIN XIADONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAJONG M , JAIN RAMA , MURRAY JEREMY M , BASHMAN STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN , WANG WEIBO , JENSEN JOHANNA M , WAGMAN ALLAN S , PFISTER KEITH B , NG SIMON C
发明人： RAMURTHY SAVITHRI , LIN XIADONG , SUBRAMANIAN SHARADA , RICO ALICE C , WANG XIAJONG M , JAIN RAMA , MURRAY JEREMY M , BASHMAN STEVEN E , WARNE ROBERT L , SHU WEI , ZHOU YASHEEN , DOVE JEFFREY , AIKAWA MINA , AMIRI PAYMAN , WANG WEIBO , JENSEN JOHANNA M , WAGMAN ALLAN S , PFISTER KEITH B , NG SIMON C
IPC分类号： C07D239/94 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04
CPC分类号： C07D239/94 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D451/06 , C07D453/02
摘要： The invention provides novel quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
摘要翻译：本发明提供了作为PDK1抑制剂的新型喹唑啉化合物。还提供了包含该化合物的药物组合物，以及用化合物或组合物治疗增殖性疾病如癌症的方法。

8. 发明申请

WO2004017923A3 COMPOSITIONS AND METHODS OF THERAPY FOR CANCERS CHARACTERIZED BY EXPRESSION OF THE TUMOR-ASSOCIATED ANTIGEN MN/CA IX 审中-公开
标题翻译：肿瘤相关抗原MN / CA IX的表达特征的组合物和治疗方法
公开(公告)号：WO2004017923A3
公开(公告)日：2005-07-14
申请号：PCT/US0326612
申请日：2003-08-25
申请人： CHIRON CORP , WONG JUSTIN , WINTER JILL , LALEHZADEH GUITA , WARNE ROBERT
发明人： WONG JUSTIN , WINTER JILL , LALEHZADEH GUITA , WARNE ROBERT
IPC分类号： C12N15/09 , A61K20060101 , A61K38/00 , A61K39/395 , A61K45/00 , A61P35/00 , A61P43/00 , C07K16/00 , C07K16/30 , C07K16/40 , C12N9/88 , C12N9/99 , C12P21/08 , C12Q1/02 , C12Q1/527 , G01N33/573
CPC分类号： C07K16/30 , C07K16/40
摘要： Compositions and methods useful in inhibiting proliferation of CA IX + preneoplastic or neoplastic cells in a mammal are provided. The compositions are antagonist anti-CA IX antibodies and other inhibitory agents that target carbonic anhydrase activity of CA IX on these cells. The antagonist anti-CA IX antibodies or antigen-binding fragments thereof are specifically reactive with an inhibitory epitope of CA IX or biologically active variant thereof. Formation of an antibody-antigen complex between the antagonist anti-CA IX antibodies or antigen-binding fragments thereof and the respective inhibitory epitopes results in inhibition of carbonic anhydrase activity of CA IX or biologically active variant thereof. Other small molecule agents that inhibit carbonic anhydrase activity of CA IX or biologically active variant thereof and screening assays for identifying such agents are also provided. The antagonist anti-CA IX antibodies, antigen-binding fragments thereof, and other CA IX inhibitory agents identified herein are useful in the treatment of cancers characterized by the expression of the CA IX tumor-associated antigen.
摘要翻译：提供了可用于抑制哺乳动物中CA IX +肿瘤前和肿瘤细胞增殖的组合物和方法。该组合物是拮抗性抗CA IX抗体和其它抑制剂，其靶向这些细胞上CA IX的碳酸酐酶活性。拮抗性抗CA IX抗体或其抗原结合片段与CA IX或其生物活性变体的抑制性表位特异性反应。拮抗性抗CA IX抗体或其抗原结合片段之间的抗体 - 抗原复合物的形成和各自的抑制性表位导致CA IX或其生物活性变体的碳酸酐酶活性的抑制。还提供了抑制CA IX或其生物活性变体的碳酸酐酶活性的其它小分子试剂和用于鉴定这些试剂的筛选试验。本文鉴定的拮抗性抗CAⅨ抗体，其抗原结合片段和其它CAⅨ抑制剂可用于治疗特征在于表达CAⅨ肿瘤相关抗原的癌症。

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