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1. 发明授权

US09873661B2 Small molecule malarial Aldolase-TRAP enhancers and glideosome inhibitors 有权
公开(公告)号：US09873661B2
公开(公告)日：2018-01-23
申请号：US14353438
申请日：2012-10-25
申请人： NEW YORK UNIVERSITY , THE JOHNS HOPKINS UNIVERSITY
发明人： Timothy J. Cardozo , Jürgen Bosch , Sondra Maureen Nemetski
IPC分类号： A61K31/535 , C07C249/16 , C12Q1/527 , C07D239/54 , C07D277/34 , C07C235/78 , C07C243/18 , C07D207/337 , C07D215/14 , C07D239/46 , C07D239/47 , C07D271/12 , C07D333/24 , C07D487/04 , G06F19/12 , G06F19/16
CPC分类号： C07C249/16 , C07C235/78 , C07C243/18 , C07D207/337 , C07D215/14 , C07D239/46 , C07D239/47 , C07D239/54 , C07D271/12 , C07D277/34 , C07D333/24 , C07D487/04 , C12Q1/527 , G01N2333/44 , G01N2333/445 , G01N2500/04 , G06F19/12 , G06F19/16
摘要： In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase. The method includes providing a first model comprising Aldolase or residues of the amino acid sequence corresponding to SEQ ID NO: 1 said residues being at amino acid positions selected from the group consisting of 10-13, 26, 27, 29, 30, 31, 32, 33, 37, 39, 40, 41, 43, 44, 47, 48, 51, 52, 60, 63, 66, 79, 84, 85, 92, 93, 103, 106-109, 112-117, 138, 142, 146, 148, 151, 153, 179, 182, 183, 185, 186, 194, 196, 197, 198, 199, 208, 226-228, 231-269, 270, 272, 277-283, 285-289, 294, 295, 297-299, 301-304, 306-310, 312, 313, 316, 317, 319, 321, 323, 326, 330, 344, 345, and 347, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for modifying the activity of Aldolase. The present invention also discloses compounds and compositions which modify the activity of Aldolase, or a complex between Aldolase and TRAP. Methods of treating or preventing malaria, or an infection by apicomplexan organisms are also disclosed.

2. 发明申请

US20140275088A1 SMALL MOLECULE MALARIAL ALDOLASE-TRAP ENHANCERS AND GLIDEOSOME INHIBITORS 有权
标题翻译：小分子MALALAL ALDOLASE-TRAP增强剂和GLIDEOSOME抑制剂
公开(公告)号：US20140275088A1
公开(公告)日：2014-09-18
申请号：US14353438
申请日：2012-10-25
申请人： NEW YORK UNIVERSITY , JOHNS HOPKINS UNIVERSITY
发明人： Timothy J. Cardozo , Jürgen Bosch , Sondra Maureen Nemetski
IPC分类号： C07C249/16 , C07D215/14 , C07D333/24 , C07D207/337 , C07C235/78 , G06F19/12 , C07D239/47 , C07D487/04 , C07D239/46 , G06F19/16 , C12Q1/527 , C07C243/18 , C07D271/12
CPC分类号： C07C249/16 , C07C235/78 , C07C243/18 , C07D207/337 , C07D215/14 , C07D239/46 , C07D239/47 , C07D239/54 , C07D271/12 , C07D277/34 , C07D333/24 , C07D487/04 , C12Q1/527 , G01N2333/44 , G01N2333/445 , G01N2500/04 , G06F19/12 , G06F19/16
摘要： In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase. The method includes providing a first model comprising Aldolase or residues of the amino acid sequence corresponding to SEQ ID NO: 1 said residues being at amino acid positions selected from the group consisting of 10-13, 26, 27, 29, 30, 31, 32, 33, 37, 39, 40, 41, 43, 44, 47, 48, 51, 52, 60, 63, 66, 79, 84, 85, 92, 93, 103, 106-109, 112-117, 138, 142, 146, 148, 151, 153, 179, 182, 183, 185, 186, 194, 196, 197, 198, 199, 208, 226-228, 231-269, 270, 272, 277-283, 285-289, 294, 295, 297-299, 301-304, 306-310 312, 313, 316, 317, 319, 321, 323, 326, 330, 344, 345, and 347, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for modifying the activity of Aldolase. The present invention also discloses compounds and compositions which modify the activity of Aldolase, or a complex between Aldolase and TRAP. Methods of treating or preventing malaria, or an infection by apicomplexan organisms are also disclosed.
摘要翻译：一方面，本发明涉及鉴定可用于改变醛缩酶活性的化合物的方法。该方法包括提供包含Aldolase或对应于SEQ ID NO：1的氨基酸序列的残基的第一模型，所述残基位于选自下组的氨基酸位置：10-13,26,27,29,30,31， 32，33，37，39，40，41，43，44，47，48，51，52，60，63，66，79，84，85，92，93，103，106-109，112-117， 138,142,146,148,151,153,179,182,183,185,186,194,196,197,198,199,208,226-228,231-269,270,272,277-283， 285-289,294,295,297-299,301-304,306-310 312,313,316,317,319,321,232,326,330,344,345和347，提供一种或多种候选化合物评估候选化合物与第一模型之间的接触以确定一种或多种候选化合物中的哪一种具有结合和/或适合于第一模型的能力，以及鉴定化合物，其基于所述评估具有与第一模型结合和/或适合作为可能用于改变醛缩酶活性的化合物。本发明还公开了改变Aldolase活性的化合物和组合物，或Aldolase和TRAP之间的复合物。还公开了治疗或预防疟疾或由复合物有机体感染的方法。

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