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公开(公告)号：US20220370647A1
公开(公告)日：2022-11-24
申请号：US17211481
申请日：2021-03-24
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K51/04
摘要： The tumor stroma, which accounts for a large part of the tumor mass, represents an attractive target for the delivery of diagnostic and therapeutic compounds. Here, the focus is notably on a subpopulation of stromal cells, known as cancer-associated fibroblasts, which are present in more than 90% of epithelial carcinomas, including pancreatic, colon, and breast cancer. Cancer-associated fibroblasts feature high expression of FAP, which is not detectable in adult normal tissue but is associated with a poor prognosis in cancer patients. The present invention provides small-molecule radiopharmaceutical and imaging agents based on a FAP-specific inhibitor.
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公开(公告)号：US20220211883A1
公开(公告)日：2022-07-07
申请号：US17554823
申请日：2021-12-17
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K51/04
摘要： The present disclosure relates to fibroblast-activation protein (FAP)-activated theranostic prodrugs, pharmaceutical compositions comprising them, and methods of treating a disorder characterized by FAP upregulation, such as cancer.
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3.发明申请公开(公告)号：US20200054655A1
公开(公告)日：2020-02-20
申请号：US16603502
申请日：2018-04-06
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/69 , A61K31/415 , A61K31/635 , A61P35/00
摘要： Disclosed are combination therapies including administration of Caspase-1 dependent anticancer agents and PGE2 antagonists, and the use of such therapies in the treatment of cell proliferative diseases.
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公开(公告)号：US10117887B2
公开(公告)日：2018-11-06
申请号：US15655317
申请日：2017-07-20
IPC分类号： A61K47/64 , A61K31/704 , A61K47/54 , A61K47/62
摘要： Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
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公开(公告)号：US11957657B2
公开(公告)日：2024-04-16
申请号：US17368161
申请日：2021-07-06
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/402 , A61K31/4025 , A61K31/4035 , A61K31/4439 , A61K31/69 , A61K35/13 , A61K39/39 , A61K45/06 , A61P35/00 , A61P37/04 , A61K39/00
CPC分类号： A61K31/402 , A61K31/4025 , A61K31/4035 , A61K31/4439 , A61K31/69 , A61K35/13 , A61K39/39 , A61K45/06 , A61P35/00 , A61P37/04 , A61K2039/505 , A61K31/69 , A61K2300/00
摘要： Disclosed are combination therapies including administration of I-DASH inhibitors and PGE2 antagonists, and the use of such therapies in the treatment of cell proliferative diseases.
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公开(公告)号：US20230390241A1
公开(公告)日：2023-12-07
申请号：US18111143
申请日：2023-02-17
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/402 , A61K31/69 , A61K45/06 , A61K39/39 , A61P37/04 , A61P35/00 , A61K31/4025 , A61K31/4035 , A61K31/4439 , A61K35/13
CPC分类号： A61K31/402 , A61K31/69 , A61K45/06 , A61K39/39 , A61P37/04 , A61P35/00 , A61K31/4025 , A61K31/4035 , A61K31/4439 , A61K35/13 , A61K2039/505
摘要： Disclosed are potent immuno-DASH inhibitors, and their use in the treatment of cell proliferative diseases.
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公开(公告)号：US11583516B2
公开(公告)日：2023-02-21
申请号：US16331181
申请日：2017-09-07
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/402 , A61K31/69 , A61K45/06 , A61K39/39 , A61P37/04 , A61P35/00 , A61K31/4025 , A61K31/4035 , A61K31/4439 , A61K35/13 , A61K39/00
摘要： Disclosed are potent immuno-DASH inhibitors and their use in the treatment of cell proliferative diseases.
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公开(公告)号：US11559537B2
公开(公告)日：2023-01-24
申请号：US16603502
申请日：2018-04-06
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/415 , A61K31/69 , A61P35/00 , A61K31/635 , A61K45/06
摘要： Disclosed are combination therapies including administration of Caspase-1 dependent anticancer agents and PGE2 antagonists, and the use of such therapies in the treatment of cell proliferative diseases.
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公开(公告)号：US20190209525A1
公开(公告)日：2019-07-11
申请号：US16331181
申请日：2017-09-07
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/402 , A61K31/4035 , A61K31/4439 , A61K31/4025 , A61P35/00 , A61P37/04 , A61K35/13
CPC分类号： A61K31/402 , A61K31/4025 , A61K31/4035 , A61K31/4439 , A61K31/69 , A61K35/13 , A61K39/39 , A61K45/06 , A61K2039/505 , A61P35/00 , A61P37/04 , A61K2300/00
摘要： Disclosed are potent immuno-DASH inhibitors, and their use in the treatment of cell proliferative diseases.
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公开(公告)号：US20170319609A1
公开(公告)日：2017-11-09
申请号：US15655317
申请日：2017-07-20
IPC分类号： A61K31/704 , A61K47/64
CPC分类号： A61K31/704 , A61K47/545 , A61K47/62 , A61K47/64
摘要： Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
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