-
31.发明申请Broad Spectrum Inhibitors of the Post Proline Cleaving Enzymes for Treatment of Hepatitis C Virus Infections 审中-公开用于治疗丙型肝炎病毒感染的后脯氨酸切割酶的广谱抑制剂公开(公告)号：US20150202218A1
公开(公告)日：2015-07-23
申请号：US14416220
申请日：2013-08-01
CPC分类号： A61K31/69 , A61K31/16 , A61K31/40 , A61K31/4985 , A61K31/7056 , A61K38/21 , A61K45/06 , A61K2300/00
摘要： Disclosed are methods of treating, inhibiting, or preventing a viral infection in a mammal in need thereof by administering a therapeutically or prophylactically effective amount of an inhibitor of FAP, an inhibitor of DPPIV, an inhibitor of DPP8, or an inhibitor of DPP9. The inhibitor may act as both an inhibitor of DPPIV and an inhibitor of DPP8/9. The viral infection includes, but is not limited to, hepatitis B virus, hepatitis C virus, human immunodeficiency virus, Polio virus, Coxsackie A virus, Coxsackie B virus, Rhino virus, respiratory syncytial virus, dengue virus, equine infectious anemia virus, Echo virus, small pox virus, Ebola virus, and West Nile virus.
摘要翻译： 公开了通过施用治疗或预防有效量的FAP抑制剂，DPPIV抑制剂，DPP8抑制剂或DPP9抑制剂来治疗，抑制或预防有需要的哺乳动物的病毒感染的方法。 抑制剂可以作为DPPIV的抑制剂和DPP8 / 9的抑制剂。 病毒感染包括但不限于乙型肝炎病毒，丙型肝炎病毒，人类免疫缺陷病毒，脊髓灰质炎病毒，柯萨奇A病毒，柯萨奇B病毒，犀牛病毒，呼吸道合胞病毒，登革热病毒，马传染性贫血病毒，回声 病毒，小痘病毒，埃博拉病毒和西尼罗病毒。
-
公开(公告)号：US20150157684A1
公开(公告)日：2015-06-11
申请号：US14572015
申请日：2014-12-16
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.
-
公开(公告)号：US20150094303A1
公开(公告)日：2015-04-02
申请号：US14566343
申请日：2014-12-10
发明人： William W. Bachovchin , Hung-sen Lai , Daniel P. O'Connell , Wengen Wu , Christopher P. Kiritsy
IPC分类号： C07D213/80 , A61K45/06 , A61K31/5377
CPC分类号： C07D213/80 , A61K31/167 , A61K31/192 , A61K31/22 , A61K31/366 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/44 , A61K31/455 , A61K31/47 , A61K31/505 , A61K31/5377 , A61K31/616 , A61K45/06 , A61K2300/00
摘要： Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.
摘要翻译： 公开了对一系列哺乳动物治疗适应症具有活性的杂环基烷基取代和杂芳烷基取代的吡啶及其药学上可接受的盐和前药。
-
公开(公告)号：US20140128344A1
公开(公告)日：2014-05-08
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： C07F5/02
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。
-
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.
-
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.
-
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.
-
公开(公告)号：US09629921B2
公开(公告)日：2017-04-25
申请号：US13784087
申请日：2013-03-04
IPC分类号： A61K47/48 , C07F5/02 , C07K5/065 , C07K5/06 , C07K5/09 , C07K5/08 , C07K5/103 , C07K5/107 , C07K5/10 , C07K7/06 , A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , A61K47/64 , C07F5/025 , C07K5/06052 , C07K5/06078 , C07K5/06191 , C07K5/0817 , C07K5/0827 , C07K5/1008 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1027
摘要： The present invention relates to prodrugs of protease inhibitors, such as inhibitors of the proteosome, DPP IV, FAPα and the like. These“pro-inhibitors” are activated, i.e., cleaved, by an “activated protease” to release an active inhibitor moiety in proximity to a “target protease”. The identity of activating protease and target protease can be the same (such as pro-inhibitors being referred to as “Target-Activated Smart Protease Inhibitors” or “TASPI”) or different (e.g., “Target-Directed Smart Protease Inhibitors” or “TDSPI”). After activation of the pro-inhibitor, the active inhibitor moiety can self-inactivate by, e.g., intramolecular-cyclization or cis-trans isomerization.
-
39.发明授权公开(公告)号：US09044424B2
公开(公告)日：2015-06-02
申请号：US13951060
申请日：2013-07-25
IPC分类号： A61K38/02 , A61K38/05 , A61K38/55 , A61K31/00 , A61K31/155 , A61K31/401 , A61K31/4025 , A61K31/675 , A61K31/69 , A61K31/702 , A61K45/06
CPC分类号： A61K38/05 , A61K31/00 , A61K31/155 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/675 , A61K31/69 , A61K31/702 , A61K38/005 , A61K38/28 , A61K38/55 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods for modification and regulation of glucose metabolism by administering to an animal a therapeutically effective amount of an inhibitor of dipeptidylpeptidase IV (DPIV) or a pharmaceutically acceptable salt thereof, where the inhibitor has a Ki for inhibition of DPIV of 10 nM or less; and the inhibitor is administered in an amount sufficient to increase the plasma half-life of glucagon-like peptide 1 (GLP-1) but not sufficient to suppress the immune system of the animal.
摘要翻译： 本发明提供了通过向动物施用治疗有效量的二肽基肽酶IV（DPIV）或其药学上可接受的盐的抑制剂或其药学上可接受的盐来修饰和调节葡萄糖代谢的方法，其中抑制剂具有抑制DPIV的Ki为10nM 或更少; 并且以足以增加胰高血糖素样肽1（GLP-1）的血浆半衰期的量施用抑制剂，但不足以抑制动物的免疫系统。
-
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。
-
-
-
-
-
-
-
-
-
搜索结果
56 条记录 (耗时 0.039 秒)
