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公开(公告)号：EP2872125A2
公开(公告)日：2015-05-20
申请号：EP13817396.8
申请日：2013-07-10
IPC分类号： A61K31/136
CPC分类号： C07C223/06 , A61K31/136 , A61K31/15 , A61K31/164 , A61K31/165 , A61K31/216 , A61K31/395 , A61K31/4166 , A61K31/445 , A61K31/655 , A61K31/69 , A61K45/06 , C07C251/48 , C07C251/86 , C07D211/62 , C07D233/80 , A61K2300/00
摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, tautomers, stereoisomers, solvates, hydrates, polymorphs, and compositions thereof. Also provided are methods and kits involving the inventive compounds for treating proliferative diseases (e.g., cancers (e.g., breast cancer, prostate cancer, lung cancer, and ovarian cancer), benign neoplasms, angiogenesis, inflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound of the invention may enhance the anti-tumor immune response by inhibiting or eliminating the immune suppression mediated by immune suppressor myeloid cells (MDSCs), inducing apoptosis, and/or inhibit or down-regulate proteins (e.g., epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), estrogen receptor (ER), X-linked inhibitor of apoptosis protein (XIAP), and heat shock protein 90 (Hsp90)) in the subject.
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2.发明授权METHODS AND AGENTS FOR IMPROVING TARGETING OF CD138 EXPRESSING TUMOR CELLS 有权方式和途径改进ABZIELUNG ON CD138表达的肿瘤细胞
公开(公告)号：EP2240516B1
公开(公告)日：2015-07-08
申请号：EP08865592.3
申请日：2008-12-23
发明人： DAELKEN, Benjamin , UHEREK, Christoph , ANDERSON, Kenneth , HIDESHIMA, Teru , BRUECHER, Christoph , OSTERROTH, Frank , AIGNER, Silke , GERMER, Matthias
IPC分类号： C07K16/28 , C07K16/30 , A61P35/00 , A61K47/48 , A61K39/395
CPC分类号： A61K47/48561 , A61K47/6803 , A61K47/6809 , A61K47/6849 , A61K47/6851 , A61K47/6867 , A61K2039/505 , C07K16/2896 , C07K2317/34 , C07K2317/73 , C07K2317/92
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公开(公告)号：EP1861126A2
公开(公告)日：2007-12-05
申请号：EP06748614.2
申请日：2006-03-22
发明人： ANDERSON, Kenneth, C. , BRADNER, James, Elliott , GREENBERG, Edward, Franklin , HIDESHIMA, Teru , KWIATKOWSKI, Nicholas, Paul , MAZITSCHEK, Ralph , SCHREIBER, Stuart, L. , SHAW, Jared
IPC分类号： A61K51/00 , A61K39/395 , A61K33/36
CPC分类号： A61K38/05 , A61K31/35 , A61K31/357 , A61K31/422 , A61K31/4965 , A61K31/69 , A61K38/50 , A61K45/06 , A61K49/0008 , G01N33/5011 , A61K2300/00
摘要： The invention relates to methods of treating protein degradation disorders, such cellular proliferative disorders (e.g., cancer) and protein deposition disorders (e.g., neurodegenerative disorders). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating multiple myeloma. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
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4.发明公开METHODS AND COMPOSITIONS FOR TREATING CANCER USING PROTEASOME INHIBITORS 有权组合物用于使用所述蛋白酶体抑制剂PS-341治疗癌症
公开(公告)号：EP1565193A2
公开(公告)日：2005-08-24
申请号：EP03768749.8
申请日：2003-11-06
IPC分类号： A61K31/69
CPC分类号： A61K31/69 , A61K31/195 , A61K31/198 , A61K31/573 , A61K31/704 , A61K38/05 , A61K45/06 , A61K2300/00
摘要： The present invention relates to therapeutic compositions for treating cancer or preventing the growth of cancer cells, e.g., tumor growth, in a subject. The present invention also relates to methods for treating cancer, e.g., inhibiting tumor growth, in a subject who has become resistant to treatment, by administering to a subject an effective amount of a proteasome inhibitor and an effective amount of a therapeutic agent, e.g., a chemotherapeutic agent. The present invention further relates to methods for purging bone marrow, i.e., removing cancer cells from bone marrow, by exposing the bone marrow cells to a proteasome inhibitor and a therapeutic agent, e.g., a chemotherapeutic agent.
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5.发明授权
公开(公告)号：EP1565193B1
公开(公告)日：2013-04-24
申请号：EP03768749.8
申请日：2003-11-06
IPC分类号： A61K31/198 , A61K31/573 , A61K31/69 , A61K31/704 , A61K38/05 , A61K45/06 , A61P35/00
CPC分类号： A61K31/69 , A61K31/195 , A61K31/198 , A61K31/573 , A61K31/704 , A61K38/05 , A61K45/06 , A61K2300/00
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6.发明公开
公开(公告)号：EP4037694A1
公开(公告)日：2022-08-10
申请号：EP20870943.6
申请日：2020-10-01
IPC分类号： A61K31/7105 , A61K47/18 , A61K47/32
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公开(公告)号：EP3354265A1
公开(公告)日：2018-08-01
申请号：EP18157889.9
申请日：2006-03-22
发明人： ANDERSON, Kenneth, C , BRADNER, James, Elliott , GREENBERG, Edward, Franklin , HIDESHIMA, Teru , KWIATKOWSKI, Nicholas, Paul , MAZITSCHEK, Ralph , SCHREIBER, Stuart, L. , SHAW, Jared , HAGGARTY, Stephen, J
IPC分类号： A61K31/357 , A61K31/42 , A61K31/335 , A61K31/4965 , A61K45/06 , A61K31/35 , A61K31/39 , A61K31/69 , A61K38/55 , A61K49/00 , G01N33/50 , A61K31/422 , A61K38/50 , A61K38/05
CPC分类号： A61K38/05 , A61K31/35 , A61K31/357 , A61K31/422 , A61K31/4965 , A61K31/69 , A61K38/50 , A61K45/06 , A61K49/0008 , G01N33/5011 , A61K2300/00
摘要： The invention relates to methods of treating protein degradation disorders, such as cellular proliferative disorders (e.g., cancer). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating solid tumors. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
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9.发明公开METHODS AND AGENTS FOR IMPROVING TARGETING OF CD138 EXPRESSING TUMOR CELLS 有权方式和途径改进ABZIELUNG ON CD138表达的肿瘤细胞
公开(公告)号：EP2240516A1
公开(公告)日：2010-10-20
申请号：EP08865592.3
申请日：2008-12-23
发明人： DAELKEN, Benjamin , UHEREK, Christoph , ANDERSON, Kenneth , HIDESHIMA, Teru , BRUECHER, Christoph
IPC分类号： C07K16/28 , C07K16/30 , A61P35/00 , A61K47/48 , A61K39/395
CPC分类号： A61K47/48561 , A61K47/6803 , A61K47/6809 , A61K47/6849 , A61K47/6851 , A61K47/6867 , A61K2039/505 , C07K16/2896 , C07K2317/34 , C07K2317/73 , C07K2317/92
摘要： Disclosed are immunoconjugates having specificity for CD138 that diminish adhesion of CD138 expressing tumor cells to stroma cells and methods of using the same. This deminished adhesion renders the tumor cells not only susceptible to the immunconjugate, but also to other agents, in particular cytotoxic agents.
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