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公开(公告)号：EP4132918A1
公开(公告)日：2023-02-15
申请号：EP21717085.1
申请日：2021-04-08
IPC分类号： C07D401/04 , C07D403/04 , A61P33/06 , A61K31/4725 , A61K31/506
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公开(公告)号：EP3022200B1
公开(公告)日：2017-03-01
申请号：EP14759317.2
申请日：2014-07-17
发明人： BURROWS, Jeremy , WYVRATT, Matthew , VAIDYA, Akhil , KORTAGERE, Sandhya , FAN, Erkang , CHATTERJEE, Arnab Kumar , NAGLE, Advait Suresh , KATO, Tomoyo
IPC分类号： C07D403/12 , C07D231/40 , A61K31/415 , A61K31/4184 , A61P33/06
CPC分类号： C07D231/40 , A61K31/415 , A61K31/4184 , A61K45/06 , C07D403/12
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公开(公告)号：EP3118198A1
公开(公告)日：2017-01-18
申请号：EP15176514.6
申请日：2015-07-13
发明人： WATERSON, David , WITTY, Michael John , CHIBALE, Kelly , STREET, Leslie , GONZALEZ CABRERA, Diego , PAQUET, Tanya
IPC分类号： C07D401/04 , A61K31/4965 , A61K31/497 , C07D241/20 , A61P33/06
CPC分类号： C07D241/20 , A61K31/4965 , A61K31/497 , A61K45/06 , A61P33/06 , C07D401/04 , Y02A50/411 , A61K2300/00
摘要： The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
摘要翻译： 本发明涉及氨基吡嗪衍生物在制备用于预防或治疗疟疾的药物中的用途。 具体地，本发明涉及可用于制备用于抑制疟疾寄生虫增殖的药物制剂的氨基吡嗪衍生物。
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公开(公告)号：EP2203457B1
公开(公告)日：2014-03-05
申请号：EP08845311.3
申请日：2008-10-29
发明人： VENNERSTROM, Jonathan, L. , DONG, Yuxiang , CHARMAN, Susan, A. , WITTLIN, Sergio , CHOLLET, Jacques , CREEK, Darren, J. , WANG, Xiaofang , SRIRAGHAVAN, Kamaraj , ZHOU, Lin , MATILE, Hugues , CHARMAN, William, N.
IPC分类号： C07D493/10 , A61K31/343 , A61K31/4525 , A61K31/496 , A61P33/06 , A61K31/553 , A61K31/5377 , A61K31/541
CPC分类号： C07D493/10 , C07D323/02 , C07D405/12 , C07D413/12
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公开(公告)号：EP2203457A2
公开(公告)日：2010-07-07
申请号：EP08845311.3
申请日：2008-10-29
发明人： VENNERSTROM, Jonathan, L. , DONG, Yuxiang , CHARMAN, Susan, A. , WITTLIN, Sergio , CHOLLET, Jacques , CREEK, Darren, J. , WANG, Xiaofang , SRIRAGHAVAN, Kamaraj , ZHOU, Lin , MATILE, Hugues , CHARMAN, William, N.
IPC分类号： C07D493/10 , A61K31/343 , A61K31/4525 , A61K31/496 , A61P33/06 , A61K31/553 , A61K31/5377 , A61K31/541
CPC分类号： C07D493/10 , C07D323/02 , C07D405/12 , C07D413/12
摘要： A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.
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公开(公告)号：EP2194985B1
公开(公告)日：2019-02-20
申请号：EP08837766.8
申请日：2008-10-08
发明人： YUTHAVONG, Yongyuth , VILAVAIN, Tirayut , KAMCHONWONGPAISAN, Sumalee , TARCHOMPOO, Bongkoch , THONGPANCHANG, Chawanee , CHITNUMSUB, Penchit , YUVANIYAMA, Jirundon , MATTHEWS, David , CHARMAN, Susan , CHARMAN, William , VIVAS, Livia , KATIYAR, Sanjay, Babu
IPC分类号： C07D239/48 , C07D401/04 , C07D401/12 , A61K31/495 , A61K31/496
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公开(公告)号：EP3137455B1
公开(公告)日：2018-08-15
申请号：EP15713170.7
申请日：2015-03-26
发明人： HAMEED PEER MOHAMED, Shahul , PATIL, Vikas , MURUGAN, Kannan , VITHALRAO BELLALE, Eknath , RAICHURKAR, Anandkumar , LANDGE, Sudhir , PUTTUR, Jayashree , ROY CHOUDHURY, Nilanjana , SHANBHAG, Gajanan , KOUSHIK, Krishna , IYER, Pravin , KIRTHIKA SAMBANDAMURTHY, Vasan , SOLAPURE, Suresh , NARAYANAN, Shridhar
IPC分类号： C07D401/14 , C07D403/14 , A61K31/506 , A61P33/06
CPC分类号： C07D401/14 , A61K31/506 , A61K45/06 , C07D403/14 , Y02A50/411
摘要： The present invention relates to triaminopyrimidines and to pharmaceutically acceptable salts thereof, to their use in the treatment and/or prevention of malaria caused by plasmodium species, and to their methods of preparation.
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公开(公告)号：EP2526090A2
公开(公告)日：2012-11-28
申请号：EP11704673.0
申请日：2011-01-17
IPC分类号： C07D213/73 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/06 , A61K31/44 , A61K31/4427 , A61P33/06
CPC分类号： C07D213/73 , C07D213/74 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/04 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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公开(公告)号：EP2370411A2
公开(公告)日：2011-10-05
申请号：EP09831228.3
申请日：2009-12-04
申请人： Oregon Health and Science University , THE GOVERNMENT OF THE UNITED STATES OF AMERICA D.B.A THE DEPARTMENT OF VETERANS AFFAIRS , University Of South Florida , Medicines for Malaria Venture
发明人： RISCOE, Michael,K. , KELLY, Jane, X. , WINTER, Rolf, W. , HINRICHS, David, J. , SMILKSTEIN, Martin, J. , NILSEN, Aaron , MONASTYRSKYI, Andrii , CROSS, Richard M. , BURROWS, Jeremy , KYLE, Dennis , MANETSCH, Roman , FLANIGAN, David L.
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： A method for inhibiting a parasitic or infectious disease in a subject, wherein the parasitic or infectious disease is selected from one caused by Eimeria sp., Babesia sp., Theileria sp. or Neospora caninum, the method comprising administering to the subject a therapeutically effective amount of a 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; 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 H or R6 is not H or methoxy; and in formula II that if R4 is carbonyldioxy then R7 is not methoxy.
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公开(公告)号：EP1414813A1
公开(公告)日：2004-05-06
申请号：EP02763208.2
申请日：2002-06-21
发明人： VENNERSTROM, J.,University of Nebraska Med. Ctr. , CHOLLET, Jacques,Pharma Research Department , DONG, Y.,University of Nebraska Medical Center , MATILE, Hugues,Pharma Research Department , PADMANILAYAM, M.,University of Nebraska Med. Ctr. , TANG, Y.,University of Nebraska Medical Center , CHARMAN, William N.,Victorian College of Pharmacy
IPC分类号： C07D323/02 , C07D493/10 , C07D405/14 , C07D405/08 , C07D419/08 , C07D521/00 , A61P33/06
CPC分类号： C07D405/12 , A61K31/335 , A61K31/357 , C07D323/02 , C07D405/14 , C07D491/10 , C07D493/10 , C07D495/10 , Y02A50/411 , Y02A50/423 , A61K2300/00
摘要： A means and method for treating malaria using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl or spiropiperidyl ring on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably functionalized or substituted at the 4-position or a spiropiperidyl ring that is functionalized or substituted at the nitrogen atom. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
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