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公开(公告)号：US11707539B2
公开(公告)日：2023-07-25
申请号：US17211481
申请日：2021-03-24
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
CPC分类号： A61K51/0482 , A61K49/0002 , A61K49/006 , A61K49/0032 , A61K49/0052 , A61K51/0497
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：US11096924B2
公开(公告)日：2021-08-24
申请号：US16331346
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 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：US20200022956A1
公开(公告)日：2020-01-23
申请号：US16331346
申请日：2017-09-07
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/4035 , A61K35/13 , A61P35/00 , A61K31/4025 , A61K31/4439 , A61K31/69
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：US10245248B2
公开(公告)日：2019-04-02
申请号：US15318627
申请日：2015-06-15
IPC分类号： A61K31/704 , A61K31/337 , A61K31/4155 , A61K31/4375 , A61K31/4545 , A61K31/517 , A61K31/519 , A61K31/69 , A61K31/7068 , A61K47/54 , A61K47/64
摘要： Disclosed are prodrugs of therapeutic or imaging agents, which prodrugs are selectively cleaved by fibroblast activating protein (FAP) to release the agents. Upon cleavage by FAP of the FAP substrate, the prodrug releases the agent in its active form or in a form that is readily metabolized to its active form. Pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation are also disclosed.
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公开(公告)号：US20160250237A1
公开(公告)日：2016-09-01
申请号：US14932560
申请日：2015-11-04
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
CPC分类号： A61K31/69 , A61K38/05 , A61K38/28 , A61K45/06 , C07D207/10 , C07D207/16 , C07D241/24 , C07D403/12 , C07F5/025 , C12N9/99
摘要： The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
摘要翻译： 本发明提供了抑制蛋白酶的化合物和方法。 本发明的一个方面具有与活化蛋白酶反应以释放靠近靶蛋白酶的活性抑制剂部分的促软抑制剂。 在某些情况下，化合物抑制蛋白酶体和/或后脯氨酸切割酶（PPCE），例如二肽基肽酶IV。 本发明的化合物提供了更好的治疗指标，部分原因是毒性降低和/或改善了靶向蛋白酶的特异性。
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公开(公告)号：US20230330275A1
公开(公告)日：2023-10-19
申请号：US17990347
申请日：2022-11-18
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
CPC分类号： A61K51/0482 , A61K49/006 , A61K49/0002 , A61K49/0032 , A61K49/0052 , A61K51/0497
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：US09737556B2
公开(公告)日：2017-08-22
申请号：US15318607
申请日：2015-06-15
IPC分类号： A61K31/704 , A61K47/48
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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公开(公告)号：US20170128476A1
公开(公告)日：2017-05-11
申请号：US15318607
申请日：2015-06-15
IPC分类号： A61K31/704
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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公开(公告)号：US08933056B2
公开(公告)日：2015-01-13
申请号：US14041201
申请日：2013-09-30
发明人： William W. Bachovchin , Hung-sen Lai , Wengen Wu
IPC分类号： A61K31/69 , C07F5/02 , C07D207/10 , C07D207/16 , C07D241/24 , C07D403/12 , A61K38/28 , A61K45/06 , C12N9/99
CPC分类号： A61K31/69 , A61K38/05 , A61K38/28 , A61K45/06 , C07D207/10 , C07D207/16 , C07D241/24 , C07D403/12 , C07F5/025 , C12N9/99
摘要： The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
摘要翻译： 本发明提供了抑制蛋白酶的化合物和方法。 本发明的一个方面具有与活化蛋白酶反应以释放靠近靶蛋白酶的活性抑制剂部分的促软抑制剂。 在某些情况下，化合物抑制蛋白酶体和/或后脯氨酸切割酶（PPCE），例如二肽基肽酶IV。 本发明的化合物提供了更好的治疗指标，部分原因是毒性降低和/或改善了靶向蛋白酶的特异性。
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