公开(公告)号：WO2010065905A3

公开(公告)日：2010-10-14

申请号：PCT/US2009066841

申请日：2009-12-04

申请人： UNIV OREGON HEALTH & SCIENCE ,  US GOV DBA 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 ,  A61P31/04 ,  C07D403/04 ,  C07D403/12

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: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl or haloalkyl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R3 is aliphatic, aryl, aralkyl, or alkylaryl; and R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or -SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; provided that in formula (I), R5 and R7 are not both H or R6 is not H or methoxy; and in formula (II) that if R4 is carbonyldioxy then R7 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：R1是H，羟基，烷氧基，酰基，烷基，环烷基，芳基或杂芳基; R2是甲基或卤代烷基; R4是羟基，羰基氧基或羰基二氧基; 并且R 3是脂族，芳基，芳烷基或烷基芳基; 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，酰胺基，酰基，羧基，取代的羧基或-SO 2 R 10，其中R 10为H，烷基，氨基 或卤代烷基; 条件是在式（I）中，R5和R7不同时为H或R6不为H或甲氧基; 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：WO2012167237A3

公开(公告)日：2013-04-11

申请号：PCT/US2012040712

申请日：2012-06-04

申请人： RISCOE MICHAEL K ,  KELLY JANE X ,  WINTER ROLF W ,  HINRICHS DAVID J ,  SMILKSTEIN MARTIN J ,  NILSEN AARON ,  MEDICINES MALARIA VENTURE MMV ,  UNIV SOUTH FLORIDA ,  BURROWS JEREMY ,  KYLE DENNIS ,  MANETSCH ROMAN ,  CROSS RICHARD M ,  MONASTYRSKYI ANDRII ,  FLANIGAN DAVID L ,  UNIV OREGON HEALTH & SCIENCE ,  US GOV DBA VETERANS AFFAIRS

发明人： RISCOE MICHAEL K ,  KELLY JANE X ,  WINTER ROLF W ,  HINRICHS DAVID J ,  SMILKSTEIN MARTIN J ,  NILSEN AARON ,  BURROWS JEREMY ,  KYLE DENNIS ,  MANETSCH ROMAN ,  CROSS RICHARD M ,  MONASTYRSKYI ANDRII ,  FLANIGAN DAVID L

IPC分类号： C07D215/233 ,  A61K31/47 ,  A61P31/04 ,  A61P31/12

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

摘要： Compound of formula I: or formula II, or a pharmaceutically acceptable salt of formula I or formula II, wherein: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl, haloalkyl, or heteroaryl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or -SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; and R3 is

摘要翻译： 式I化合物或式II化合物或式I或式II的药学上可接受的盐，其中：R 1是H，羟基，烷氧基，酰基，烷基，环烷基，芳基或杂芳基; R2是甲基，卤代烷基或杂芳基; R4是羟基，羰基氧基或羰基二氧基; R5，R6，R7和R8分别为H，卤素，烷氧基，烷基，卤代烷基，芳基，硝基，氰基，氨基，酰胺基，酰基，羧基，取代的羧基或-SO2R10，其中R10为H，烷基，氨基或 卤代; 和R3是

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：WO1992018118A1

公开(公告)日：1992-10-29

申请号：PCT/US1992003094

申请日：1992-04-15

申请人： STATE OF OREGON, acting by and through THE OREGON ,  RISCOE, Michael, K. ,  TOWER, Paula, A. ,  FITCHEN, John, H. ,  FERRO, Adolph, J.

发明人： STATE OF OREGON, acting by and through THE OREGON

IPC分类号： A61K31/195

CPC分类号： A61K31/34 ,  A61K31/41 ,  A61K33/00 ,  Y02A50/411 ,  A61K31/22 ,  A61K31/195 ,  A61K2300/00

摘要： Pharmaceutical compositions are described comprising methylthioribose (MTR) kinase inhibitors (e.g. trifluoromethylthioribose) and inhibitors of de novo methionine synthesis (e.g. 1,2,4-triazole, azaserine or propargylglycine).

摘要翻译： 描述了包含甲基二糖（MTR）激酶抑制剂（例如三氟甲基硫代糖）和从头甲硫氨酸合成的抑制剂（例如1,2,4-三唑，重氮丝氨酸或炔丙基甘氨酸）的药物组合物。

公开(公告)号：WO2012167237A2

公开(公告)日：2012-12-06

申请号：PCT/US2012/040712

申请日：2012-06-04

申请人： RISCOE, MICHAEL, K. ,  KELLY, Jane, X. ,  WINTER, Rolf, W. ,  HINRICHS, David, J. ,  SMILKSTEIN, Martin, J. ,  NILSEN, Aaron ,  MEDICINES FOR MALARIA VENTURE ,  UNIVERSITY OF SOUTH FLORIDA ,  BURROWS, Jeremy ,  KYLE, Dennis ,  MANETSCH, Roman ,  CROSS, Richard, M. ,  MONASTYRSKYI, Andrii ,  FLANIGAN, David, L.

发明人： RISCOE, MICHAEL, K. ,  KELLY, Jane, X. ,  WINTER, Rolf, W. ,  HINRICHS, David, J. ,  SMILKSTEIN, Martin, J. ,  NILSEN, Aaron ,  BURROWS, Jeremy ,  KYLE, Dennis ,  MANETSCH, Roman ,  CROSS, Richard, M. ,  MONASTYRSKYI, Andrii ,  FLANIGAN, David, L.

IPC分类号： C07D215/233 ,  A61K31/47 ,  A61P31/04 ,  A61P31/12

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

摘要： Compound 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, haloalkyl, or heteroaryl; R 4 is hydroxyl, carbonyloxy, or carbonyldioxy; 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; and R 3 is

摘要翻译： 式I化合物或式II化合物或式I或式II的药学上可接受的盐，其中：R 1是H，羟基，烷氧基，酰基，烷基，环烷基，芳基或杂芳基; R2是甲基，卤代烷基或杂芳基; R4是羟基，羰基氧基或羰基二氧基; R5，R6，R7和R8分别为H，卤素，烷氧基，烷基，卤代烷基，芳基，硝基，氰基，氨基，酰胺基，酰基，羧基，取代的羧基或-SO2R10，其中R10为H，烷基，氨基或 卤代; 和R3是

公开(公告)号：WO2010059633A3

公开(公告)日：2010-09-23

申请号：PCT/US2009064811

申请日：2009-11-17

申请人： UNIV OREGON HEALTH & SCIENCE ,  US GOV DBA VETERANS AFFAIRS ,  RISCOE MICHAEL K ,  WINTER ROLF W ,  HINRICHS DAVID J

发明人： RISCOE MICHAEL K ,  WINTER ROLF W ,  HINRICHS DAVID J

IPC分类号： C07D215/04 ,  A61K31/4706 ,  A61P33/14

CPC分类号： C07D215/46 ,  A61K31/4706

摘要： A compound, particularly an antimalarial compound, according to formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is an electron-withdrawing group; A is an optionally substituted alkanediyl or an optionally substituted cycloalkanediyl that includes 2 to 5 carbon atoms; and R1 and R2 are each individually H, tert-butyl, isopropyl, or optionally substituted cycloalkyl.

摘要翻译： 根据式（I）的化合物，特别是抗疟药化合物或其药学上可接受的盐，其中：X是吸电子基团; A是任选取代的烷二基或任选取代的包含2至5个碳原子的环烷二基; 且R 1和R 2各自独立地为H，叔丁基，异丙基或任选取代的环烷基。

公开(公告)号：WO2010059633A2

公开(公告)日：2010-05-27

申请号：PCT/US2009/064811

申请日：2009-11-17

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. ,  WINTER, Rolf, W. ,  HINRICHS, David, J.

发明人： RISCOE, Michael, K. ,  WINTER, Rolf, W. ,  HINRICHS, David, J.

IPC分类号： C07D215/04 ,  A61K31/4706 ,  A61P33/14

CPC分类号： C07D215/46 ,  A61K31/4706 ,  Y02A50/411

摘要： A compound, particularly an antimalarial compound, according to formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is an electron-withdrawing group; A is an optionally substituted alkanediyl or an optionally substituted cycloalkanediyl that includes 2 to 5 carbon atoms; and R 1 and R 2 are each individually H, tert-butyl, isopropyl, or optionally substituted cycloalkyl.

摘要翻译： 根据式（I）的化合物，特别是抗疟疾化合物或其药学上可接受的盐，其中：X是吸电子基团; A是包含2至5个碳原子的任选取代的链烷二基或任选取代的环链烷二基; 并且R 1和R 2各自独立地为H，叔丁基，异丙基或任选取代的环烷基。

公开(公告)号：WO2008064011A1

公开(公告)日：2008-05-29

申请号：PCT/US2007/084560

申请日：2007-11-13

申请人： THE GOVERNMENT OF THE U.S. OF AMERICA AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS ,  OREGON HEALTH & SCIENCE UNIVERSITY ,  RISCOE, Michael, K. ,  WINTER, Rolf ,  KELLY, Jane, X. ,  HINRICHS, David, J. ,  SMILKSTEIN, Martin, J.

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

IPC分类号： C07D219/06 ,  C07D401/06 ,  A61K31/473 ,  A61P33/06

CPC分类号： C07D219/14 ,  A61K31/4706 ,  A61K31/473 ,  C07D219/06 ,  C07D401/06 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414 ,  Y02A50/423 ,  Y02A50/491

摘要： A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.

摘要翻译： 已经发现一类具有化学敏感性和抗寄生虫活性的吖啶酮化合物。 本文描述了用于治疗寄生虫感染如疟疾和弓形虫病的药物组合物和方法，并使抗药性细胞（例如多药耐药性细胞）对其它治疗剂敏感。 药物组合物和方法也可用于治疗和/或预防精神病如精神分裂症。