公开(公告)号：WO2021016594A1

公开(公告)日：2021-01-28

申请号：PCT/US2020/043609

申请日：2020-07-24

申请人： OREGON HEALTH & SCIENCE UNIVERSITY

发明人： COHEN, Michael ,  FORTE, Michael ,  SILEIKYTE, Justina ,  NILSEN, Aaron ,  DEVEREAUX, Jordan ,  BERNARDI, Paolo

IPC分类号： A01N25/00 ,  A01N43/653 ,  C07D249/08

摘要： The present invention provides compounds useful as mitochondrial permeability transition pore (mtPTP) inhibitors, the compounds being of Formula (I), or a pharmaceutically acceptable salt thereof wherein R 1 is selected from the group of H, halogen, and C 1 -C 3 alkyl; and R 2 is selected from the group of H, CF 3 , and halogen; with the proviso that at least one of R 1 and R 2 is halogen or CF 3 .

公开(公告)号：WO2017015360A1

公开(公告)日：2017-01-26

申请号：PCT/US2016/043121

申请日：2016-07-20

申请人： OREGON HEALTH & SCIENCE UNIVERSITY ,  THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS

发明人： RISCOE, Michael ,  NILSEN, Aaron ,  STICKLES, Allison ,  MILEY, Galen ,  WINTER, Rolf ,  POU, Sovitj ,  LI, Yuexin ,  KELLY, Jane Xu ,  FORQUER, Isaac ,  DOGGETT, J. Stone ,  BRUZUAL, Igor ,  FRUEH, Lisa ,  DODEAN, Rozalia ,  SMILKSTEIN, Martin ,  ALDAY, Holland ,  KOOP, Dennis ,  BLEYLE, Lisa

IPC分类号： C07D215/233 ,  C07D409/12 ,  C07D405/12 ,  A61K31/47 ,  A61K31/4725

CPC分类号： C07D215/22 ,  C07D405/12 ,  C07D409/12

摘要： Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.

摘要翻译： 公开了ELQ-300的衍生化合物，其在位置4包括酯。这些化合物相对于ELQ-300具有增强的性质。 还公开了包含该化合物的药物组合物和治疗和预防涉及将该药物组合物施用于受试者的疟疾感染的方法。

公开(公告)号：WO2013106847A1

公开(公告)日：2013-07-18

申请号：PCT/US2013/021472

申请日：2013-01-14

申请人： OREGON HEALTH & SCIENCE UNIVERSITY ,  THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS

发明人： RISCOE, Michael K. ,  WINTER, Rolf W. ,  POU, Sovitj ,  HINRICHS, David J. ,  KELLY, Jane Xu ,  LI, Yuexin ,  NILSEN, Aaron

IPC分类号： C07D215/40 ,  A61K31/47 ,  A61P33/06

CPC分类号： C07D215/46 ,  A61K31/47 ,  C07D401/12 ,  Y02A50/411

摘要： Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.

摘要翻译： 提供了可用于治疗感染性疾病的化合物，组合物和方法。 特别地，公开了3-芳基喹啉化合物，其合成，其药物组合物和治疗感染性疾病如疟疾的方法。

公开(公告)号：WO2022197979A1

公开(公告)日：2022-09-22

申请号：PCT/US2022/020830

申请日：2022-03-17

申请人： OREGON HEALTH & SCIENCE UNIVERSITY ,  THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS

发明人： RISCOE, Michael K. ,  NILSEN, Aaron ,  JIN, Haihong ,  POU, Sovitj ,  WINTER, Rolf W. ,  DODEAN, Rozalia Ana ,  LIEBMAN, Katherine M.

IPC分类号： A61K31/395 ,  A61K31/435 ,  A61K31/47 ,  A61P33/06 ,  C07D215/20 ,  C07D215/22

摘要： Described herein are new synthetic routes for production of Endochin-Like Quinolone (ELQ) compounds. Synthetic routes to 3-substituted 4(1H)-quinolones are presented that are amenable to industrial scale preparation. One herein presented approach is relatively short, does not require palladium, and involves no chromatographic separation. A second herein presented approach is similarly relatively short, does not require palladium, involves no chromatographic separation, and also avoids high vacuum distillation. Additionally, both approaches require no protecting group chemistry because the insoluble 4(1H)-quinolone is not formed until the final reaction step.

公开(公告)号：WO2010065905A2

公开(公告)日：2010-06-10

申请号：PCT/US2009/066841

申请日：2009-12-04

申请人： OREGON HEALTH & SCIENCE UNIVERSITY ,  THE GOVERNMENT OF THE UNITED STATES OF AMERICA d.b.a. THE DEPARTMENT OF VETERANS AFFAIRS ,  RISCOE, Michael, K. ,  KELLY, Jane, X. ,  WINTER, Rolf, W. ,  HINRICHS, David, J. ,  SMILKSTEIN, Martin, J. ,  NILSEN, Aaron

发明人： RISCOE, Michael, K. ,  KELLY, Jane, X. ,  WINTER, Rolf, W. ,  HINRICHS, David, J. ,  SMILKSTEIN, Martin, J. ,  NILSEN, Aaron

IPC分类号： C07D215/04 ,  C07D403/04 ,  C07D403/12 ,  A61P31/04

CPC分类号： C07D215/60 ,  C07D215/233 ,  C07D215/42 ,  C07D239/90 ,  C07D279/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D491/052

摘要： Compounds of formula (I), or formula (II) or a pharmaceutically acceptable salt of formula (I) or formula (II), wherein: R 1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R 2 is methyl or haloalkyl; R 4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R 3 is aliphatic, aryl, aralkyl, or alkylaryl; and R 5 , R 6 , R 7 and R 8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or -SO 2 R 10 , wherein R 10 is H, alkyl, amino or haloalkyl; provided that in formula (I), R 5 and R 7 are not both H or R 6 is not H or methoxy; and in formula (II) that if R 4 is carbonyldioxy then R 7 is not methoxy.

摘要翻译： 式（I）或式（II）的化合物或式（I）或式（II）的药学上可接受的盐，其中：R 1为H， 羟基，烷氧基，酰基，烷基，环烷基，芳基或杂芳基; R 2是甲基或卤代烷基; R 4是羟基，羰氧基或羰基二氧基; 和R 3是脂族，芳基，芳烷基或烷芳基; 和R 5，R 6，R 7和R 8各自独立地为H，卤素，烷氧基，烷基 ，卤代烷基，芳基，硝基，氰基，氨基，酰氨基，酰基，羧基，取代的羧基或-SO 2 R 10，其中R 10为 是H，烷基，氨基或卤代烷基; 条件是在式（I）中，R 5和R 7不都是H或R 6不是H或甲氧基; 并且在式（II）中，如果R 4是羰基二氧基，那么R 7不是甲氧基。

公开(公告)号：WO2021231335A1

公开(公告)日：2021-11-18

申请号：PCT/US2021/031651

申请日：2021-05-10

申请人： OREGON HEALTH & SCIENCE UNIVERSITY ,  THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS ,  POU, Sovitj ,  WINTER, Rolf, W. ,  RISCOE, Michael, J. ,  DOGGETT, J., Stone ,  NILSEN, Aaron

发明人： POU, Sovitj ,  WINTER, Rolf, W. ,  RISCOE, Michael, J. ,  DOGGETT, J., Stone ,  NILSEN, Aaron

IPC分类号： A61K38/12 ,  A61K38/17 ,  A61K9/00

摘要： The present invention provides synthetic methods and novel intermediates in the preparation of 3-aryl Endochin-like quinolone (ELQ) compounds.