专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20220370647A1 FAP-TARGETED RADIOPHARMACEUTICALS AND IMAGING AGENTS, AND USES RELATED THERETO 有权
公开(公告)号：US20220370647A1
公开(公告)日：2022-11-24
申请号：US17211481
申请日：2021-03-24
申请人： Trustees of Tufts College
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.

2. 发明申请

US20220211883A1 FAP-ACTIVATED RADIOTHERANOSTICS AND USES RELATED THERETO 有权
公开(公告)号：US20220211883A1
公开(公告)日：2022-07-07
申请号：US17554823
申请日：2021-12-17
申请人： Trustees of Tufts College
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.

3. 发明申请

US20200054655A1 COMBINATION THERAPIES USING CASPASE-1 DEPENDENT ANTICANCER AGENTS AND PGE2 ANTAGONISTS 审中-公开
公开(公告)号：US20200054655A1
公开(公告)日：2020-02-20
申请号：US16603502
申请日：2018-04-06
申请人： Trustees of Tufts College
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.

4. 发明授权

US10117887B2 FAP-activated therapeutic agents, and uses related thereto 有权
公开(公告)号：US10117887B2
公开(公告)日：2018-11-06
申请号：US15655317
申请日：2017-07-20
申请人： Trustees of Tufts College
发明人： William W. Bachovchin , Hung-sen Lai , David G. Sanford , Sarah E. Poplawski , Wengen Wu
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.

5. 发明授权

US09956297B2 FAP-activated proteasome inhibitors for treating solid tumors 有权
公开(公告)号：US09956297B2
公开(公告)日：2018-05-01
申请号：US15167109
申请日：2016-05-27
申请人： Trustees of Tufts College
发明人： William W. Bachovchin , Hung-sen Lai , Sarah E. Poplawski
IPC分类号： A61K31/69 , A61K47/48 , A61K45/06 , G01N33/574 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/107 , C07K5/065 , C07K5/062 , A61K38/07 , A61K47/54 , A61K38/00
CPC分类号： A61K47/64 , A61K31/69 , A61K38/00 , A61K38/07 , A61K45/06 , A61K47/54 , C07K5/06026 , C07K5/06034 , C07K5/06078 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0821 , C07K5/1016 , G01N33/574 , A61K2300/00
摘要： Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

6. 发明申请

US20170246255A1 Stable Analogs of Peptide and Polypeptide Therapeutics 审中-公开
公开(公告)号：US20170246255A1
公开(公告)日：2017-08-31
申请号：US14808121
申请日：2015-07-24
申请人： Trustees of Tufts College
发明人： William W. Bachovchin , Hung-sen Lai , David G. Sanford
IPC分类号： A61K38/26 , A61K38/18 , A61K38/22
CPC分类号： C07K14/575 , A23K20/168 , A23K20/184 , A61K38/00 , A61K38/1709 , A61K38/177 , A61K38/22 , A61K38/26 , A61K39/00 , C07K7/08 , C07K14/005 , C07K14/47 , C07K14/57545 , C07K14/57563 , C07K14/60 , C07K14/605 , C07K14/765
摘要： The present invention relates to compositions of peptide and polypeptide analogs that are resistant to proteolysis, pharmaceutical uses thereof, and methods of preparation thereof.

7. 发明授权

US08889720B2 Non-flushing niacin analogues, and methods of use thereof 有权
标题翻译：非潮红烟酸类似物及其使用方法
公开(公告)号：US08889720B2
公开(公告)日：2014-11-18
申请号：US13715242
申请日：2012-12-14
申请人： Trustees of Tufts College
发明人： William W. Bachovchin , Hung-sen Lai
IPC分类号： C07D213/02 , C07D401/06 , A61K31/44 , A61K31/4439 , C07D213/80 , A61K45/06 , C07D213/55
CPC分类号： A61K31/4439 , A61K45/06 , C07D213/55 , C07D213/80 , C07D401/06
摘要： One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.
摘要翻译：本发明的一个方面涉及对一系列哺乳动物疾病具有活性的取代吡啶及其药学上可接受的盐。本发明的另一方面涉及包含本发明化合物或其药学上可接受的盐的药物组合物; 和药学上可接受的赋形剂。本发明还涉及治疗一系列哺乳动物疾病或病症的方法，包括但不限于高脂血症，高胆固醇血症，动脉粥样硬化，冠状动脉疾病，充血性心力衰竭，心血管疾病，高血压，冠心病，心绞痛，皮癣，Hartnup's 综合征，类癌综合征，动脉闭塞性疾病，肥胖，甲状腺功能减退，血管收缩，骨关节炎，类风湿性关节炎，糖尿病，阿尔茨海默病，脂肪营养不良或血脂异常，提高血清高密度脂蛋白（HDL）水平，降低血清低密度脂蛋白）级别。

8. 发明公开

US20240277659A1 COMBINATION THERAPIES USING IMMUNO-DASH INHIBITORS AND PGE2 ANTAGONISTS 审中-公开
公开(公告)号：US20240277659A1
公开(公告)日：2024-08-22
申请号：US18405593
申请日：2024-01-05
申请人： Trustees of Tufts College
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 , A61K39/00 , A61K39/39 , A61K45/06 , A61P35/00 , A61P37/04
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
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.

9. 发明申请

US20200323994A1 FAP-ACTIVATED PROTEASOME INHIBITORS FOR TREATING SOLID TUMORS 审中-公开
公开(公告)号：US20200323994A1
公开(公告)日：2020-10-15
申请号：US16688574
申请日：2019-11-19
申请人： Trustees of Tufts College
发明人： William W. Bachovchin , Hung-sen Lai , Sarah E. Poplawski
IPC分类号： A61K47/64 , A61K47/54 , A61K31/69 , A61K45/06 , G01N33/574 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/107 , C07K5/065 , C07K5/062 , A61K38/07
摘要： Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

10. 发明申请

US20160151343A1 NON-FLUSHING NIACIN ANALOGUES, AND METHODS OF USE THEREOF 有权
标题翻译：非冲洗型NIACIN类似物及其使用方法
公开(公告)号：US20160151343A1
公开(公告)日：2016-06-02
申请号：US14932506
申请日：2015-11-04
申请人： Trustees of Tufts College
发明人： William W. Bachovchin , Hung-sen Lai
IPC分类号： A61K31/4439 , A61K45/06
CPC分类号： A61K31/4439 , A61K45/06 , C07D213/55 , C07D213/80 , C07D401/06
摘要： One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.
摘要翻译：本发明的一个方面涉及对一系列哺乳动物疾病具有活性的取代吡啶及其药学上可接受的盐。本发明的另一方面涉及包含本发明化合物或其药学上可接受的盐的药物组合物; 和药学上可接受的赋形剂。本发明还涉及治疗一系列哺乳动物疾病或病症的方法，包括但不限于高脂血症，高胆固醇血症，动脉粥样硬化，冠状动脉疾病，充血性心力衰竭，心血管疾病，高血压，冠心病，心绞痛，皮癣，Hartnup's 综合征，类癌综合征，动脉闭塞性疾病，肥胖症，甲状腺机能亢进，血管收缩，骨关节炎，类风湿性关节炎，糖尿病，阿尔茨海默病，脂肪营养不良或血脂异常，提高血清高密度脂蛋白（HDL）水平，降低血清低密度脂蛋白）级别。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式