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1. 发明公开

EP2585072A1 NIACIN MIMETICS, AND METHODS OF USE THEREOF 审中-公开
标题翻译： NIACIN MIMETICS，及其使用方法
公开(公告)号：EP2585072A1
公开(公告)日：2013-05-01
申请号：EP11799009.3
申请日：2011-06-24
申请人： Trustees of Tufts College , Arisaph Pharmaceuticals, Inc.
发明人： BACHOVCHIN, William, W. , LAI, Hung-sen , O'CONNELL, Daniel , WU, Wengen , KIRITSY, Christopher, P.
IPC分类号： A61K31/535
CPC分类号： A61K31/5377 , A61K31/366 , A61K31/40 , A61K31/535 , A61K45/06 , C07D213/80
摘要： Disclosed are 6-(morpholinoalkyl)-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6-（吗啉代烷基） - 取代的吡啶及其药学上可接受的盐和前药。

2. 发明公开

EP2584899A1 NIACIN MIMETICS, AND METHODS OF USE THEREOF 有权
标题翻译： NIACINMIMESIS及其使用方法
公开(公告)号：EP2584899A1
公开(公告)日：2013-05-01
申请号：EP11799002.8
申请日：2011-06-24
申请人： Trustees of Tufts College , Arisaph Pharmaceuticals, Inc.
发明人： BACHOVCHIN, William, W. , LAI, Hung-Sen , O'CONNELL, Daniel , WU, Wengen , KIRITSY, Christopher, P.
IPC分类号： A01N43/40 , A61K31/44
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.

3. 发明公开

EP2054386A2 NON-FLUSHING NIACIN ANALOGUES, AND METHODS OF USE THEREOF 有权
标题翻译：非冲洗尼克酸类似物及其使用方法
公开(公告)号：EP2054386A2
公开(公告)日：2009-05-06
申请号：EP07799967.0
申请日：2007-08-01
申请人： TRUSTEES OF TUFTS COLLEGE
发明人： BACHOVCHIN, William, W. , LAI, Hung-sen
IPC分类号： C07D213/02 , A61K31/44
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 pharmaceutially 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的吡啶及其药学上可接受的盐。本发明的另一方面涉及药物组合物，其包含本发明化合物或其药学上可接受的盐; 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，所述疾病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，pellagra，Hartnup's 综合征，类癌综合征，动脉闭塞性疾病，肥胖症，甲状腺功能减退症，血管收缩，骨关节炎，类风湿性关节炎，糖尿病，阿尔茨海默氏病，脂肪代谢障碍或血脂异常，升高血清高密度脂蛋白（HDL）水平和降低血清低密度脂蛋白）水平。

4. 发明公开

EP1469873A2 PEPTIDOMIMETIC INHIBITORS OF POST-PROLINE CLEAVING ENZYMES 审中-公开
标题翻译：拟肽抑制剂技术脯氨酸裂解酶
公开(公告)号：EP1469873A2
公开(公告)日：2004-10-27
申请号：EP02792306.9
申请日：2002-11-26
申请人： Trustees of Tufts College
发明人： BACHOVCHIN, William, W.
IPC分类号： A61K38/05 , A61K38/04 , A61K31/69 , A61K31/675 , A61K31/401 , C07K5/04 , C07K5/06 , C07F9/572 , C07F5/04 , C07D207/12
CPC分类号： A61K31/69 , A61K9/0019 , A61K9/0053 , A61K9/28 , A61K38/28 , A61K45/06 , C07D207/16 , C07F5/025
摘要： The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.; The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.

5. 发明公开

EP4262878A1 FAP-ACTIVATED RADIOTHERANOSTICS, AND USES RELATED THERETO 审中-实审
公开(公告)号：EP4262878A1
公开(公告)日：2023-10-25
申请号：EP21844512.0
申请日：2021-12-17
申请人： TRUSTEES OF TUFTS COLLEGE
发明人： BACHOVCHIN, William, W. , LAI, Hung-sen , WU, Wengen
IPC分类号： A61K47/42 , A61P35/00

6. 发明授权

EP2584899B1 NIACIN MIMETICS, AND USE THEREOF 有权
标题翻译： NIACIN MIMETICS，及其用途
公开(公告)号：EP2584899B1
公开(公告)日：2018-01-10
申请号：EP11799002.8
申请日：2011-06-24
申请人： Trustees of Tufts College , Arisaph Pharmaceuticals, Inc.
发明人： BACHOVCHIN, William, W. , LAI, Hung-Sen , O'CONNELL, Daniel , WU, Wengen , KIRITSY, Christopher, P.
IPC分类号： A61K31/44 , A61K31/192 , A61K31/22 , A61K31/366 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/455 , A61K31/47 , A61K31/505 , A61K31/5377 , A61K31/616 , A61K31/167 , A61K45/06 , C07D213/80 , A01N43/40 , A61P3/06
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.

7. 发明公开

EP3154594A1 FAP-ACTIVATED THERAPEUTIC AGENTS, AND USES RELATED THERETO 有权转让
标题翻译： FAP-AKTIVIERTE THERAPEUTISCHE MITTEL UND DAMIT VERBUNDENE VERWENDUNGEN
公开(公告)号：EP3154594A1
公开(公告)日：2017-04-19
申请号：EP15807049.0
申请日：2015-06-15
申请人： Trustees of Tufts College
发明人： BACHOVCHIN, William, W. , LAI, Hung-sen , SANFORD, David, G. , POPLAWSKI, Sarah, E. , WU, Wengen
IPC分类号： A61K47/50
CPC分类号： A61K31/337 , A61K31/4155 , A61K31/4375 , A61K31/4545 , A61K31/517 , A61K31/519 , A61K31/69 , A61K31/704 , 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.
摘要翻译：公开了治疗或显像剂的前药，其前药由成纤维细胞激活蛋白（FAP）选择性切割以释放药剂。在通过FAP底物FAP切割时，前药将其以活性形式或易于代谢为其活性形式的形式释放。还公开了包含前药的药物组合物，以及使用前药治疗以FAP上调为特征的病症的方法。

8. 发明授权

EP2054386B1 NON-FLUSHING NIACIN ANALOGUES, AND METHODS OF USE THEREOF 有权
标题翻译：非冲洗尼克酸类似物及其使用方法
公开(公告)号：EP2054386B1
公开(公告)日：2014-10-08
申请号：EP07799967.0
申请日：2007-08-01
申请人： TRUSTEES OF TUFTS COLLEGE
发明人： BACHOVCHIN, William, W. , LAI, Hung-sen
IPC分类号： C07D213/02 , A61K31/44 , C07D213/80 , A61P3/06
CPC分类号： A61K31/4439 , A61K45/06 , C07D213/55 , C07D213/80 , C07D401/06

9. 发明公开

EP2782994A1 SMALL MOLECULE ENHANCER FOR DENDRITIC CELL CANCER VACCINES 有权
标题翻译：小分子放大器癌症疫苗与树突细胞
公开(公告)号：EP2782994A1
公开(公告)日：2014-10-01
申请号：EP12850873.6
申请日：2012-11-15
申请人： Trustees of Tufts College
发明人： BACHOVCHIN, William, W.
IPC分类号： C12N5/07
CPC分类号： A61K31/69 , A61K35/17 , A61K38/05 , A61K38/20 , A61K38/21 , A61K39/0005 , A61K39/0011 , A61K45/06 , A61K2039/5154 , A61K2039/5158 , A61N5/10 , C07F5/025 , A61K2300/00
摘要： Disclosed is a method of treating cancer, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound that inhibits a plurality of mammalian DASH serine proteases. Also disclosed is a method of (a) increasing antitumor immunity, (b) stimulating or enhancing an immune response, (c) treating a condition characterized by abnormal cell proliferation, (d) increasing cytokine and/or chemokine production, or (e) stimulating or enhancing production of T-cells, in a mammal, comprising administering to a mammal in need thereof an effective amount of a compound that inhibits a plurality of mammalian DASH serine proteases. For example, the compound that inhibits a plurality of mammalian DASH serine proteases may be t -butylGly-boroPro.

10. 发明公开

EP2400976A1 SOFT PROTEASE INHIBITORS, AND PRO-SOFT FORMS THEREOF 有权
标题翻译： GENTLE蛋白酶抑制剂和PRO-软形式
公开(公告)号：EP2400976A1
公开(公告)日：2012-01-04
申请号：EP10746977.7
申请日：2010-03-01
申请人： Trustees Of Tufts College
发明人： BACHOVCHIN, William, W. , LAI, Hung-Sen , WU, Wengen
IPC分类号： A61K38/00
CPC分类号： C07F5/025
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. Another aspect of the invention provides for the use of the disclosed compounds for treating Type II diabetes, insulin resistance, glucose intolerance, hyperglycemia, hypoglycemia, hyperinsulinemia, obesity, hyperlipidemia, or hyperlipoproteinemia.

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