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31. 发明申请

WO0249576A2 FAB I AND INHIBITION OF APICOMPLEXAN PARASITES 审中-公开
标题翻译： FAB I和APICOMPLEXAN PARASITES的抑制作用
公开(公告)号：WO0249576A2
公开(公告)日：2002-06-27
申请号：PCT/US0149738
申请日：2001-12-20
申请人： MCLEOD RIMA , MUENCH STEPHEN P , RAFFERTY JOHN B , KYLE DENNIS E , MUI ERNEST J , KIRISITS MICHAEL J , MACK DOUGLAS G , ROBERTS CRAIG W , SAMUEL BENJAMIN U , LYONS RUSSEL E , MILHOUS WILBUR K , RICE DAVID W , PRIGGE SEAN
发明人： MCLEOD RIMA , MUENCH STEPHEN P , RAFFERTY JOHN B , KYLE DENNIS E , MUI ERNEST J , KIRISITS MICHAEL J , MACK DOUGLAS G , ROBERTS CRAIG W , SAMUEL BENJAMIN U , LYONS RUSSEL E , MILHOUS WILBUR K , RICE DAVID W , PRIGGE SEAN
IPC分类号： A61K31/05 , A61K31/09 , A61K38/44 , A61P33/02 , A61P33/06 , C12N9/00 , C12N9/02 , C12N15/10 , C12Q1/68 , G01N33/50 , G01N33/53 , G01N33/569 , A61K
CPC分类号： A61K31/09 , A61K38/00 , C12N9/001 , C12Y103/01009
摘要： Discovery and characterization of an apicomplexan Fab I gene and encoded enzyme and discovery of the triclosan as a lead compound, provide means to rationally design novel inhibitory compositions useful for prevention and treatment of apicomplexan related diseases.
摘要翻译： apicomplexan Fab I基因和编码酶的发现和表征以及三氯生作为先导化合物的发现提供了合理设计用于预防和治疗apicomplexan相关疾病的新型抑制性组合物的手段。

32. 发明申请

WO0018769A3 INDOLO[2,1-b]QUINAZOLE-6,12-DIONE ANTIMALARIAL COMPOUNDS AND METHODS OF TREATING MALARIA THEREWITH 审中-公开
标题翻译：吲哚并[2,1-b]喹唑-6,12-二酮类抗疟化合物及其治疗疟疾的方法
公开(公告)号：WO0018769A3
公开(公告)日：2000-09-08
申请号：PCT/US9922569
申请日：1999-09-28
申请人： WRAIR WALTER REID ARMY INST OF , PITZER KEVIN K , SCOVILL JOHN P , KYLE DENNIS E , GERENA LUCIA
发明人： PITZER KEVIN K , SCOVILL JOHN P , KYLE DENNIS E , GERENA LUCIA
IPC分类号： C07D471/14 , C07D487/04 , C07D487/14 , C07D498/04 , C07D513/04 , C07D487/22 , A61K31/38
CPC分类号： C07D471/14 , C07D487/04 , C07D487/14 , C07D513/04 , Y10S514/895
摘要： New use for compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo[2,1-b]quinazoline-6,12-dione compounds of Formula (I), wherein A, B, C, D, E, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, with the proviso that not more than three of A, B, C, D, E, F, G and H are other than carbon; wherein R1 through R8 are independently selected from the group consisting of, but not limited to, the halogens (F, Cl, Br, and I), alkyl groups, trifluoromethyl groups, methoxyl groups, the carboxy methyl or carboxy ethyl group (COOCH3 or COOCH2CH3), nitro, aryl, heteroaryl, cyano, amino, dialkylaminoalkyl, 1-(4-alkylpiperazinyl), and the pharmaceutically acceptable salts thereof; and wherein X is independently selected from the group consisting of any atom especially oxygen, or any side chain necessary to make the indolo[2,1-b]quinazoline-6,12-dione compound a "prodrug" as the term is understood by one of ordinary skill in the art of medicinal chemistry. In other words, a side chain having a structure where a carbon-nitrogen double bond bears substituents that make the prodrug more water soluble and bioavailable.
摘要翻译：提供了通过施用式（I）的吲哚并[2,1-b]喹唑啉-6,12-二酮化合物在体外和体内治疗疟疾寄生虫的化合物，组合物和方法的新用途，其中A，B，C， D，E，F，G和H独立地选自碳和氮，或者A和B或C和D可以合在一起形成氮或硫，附带条件是A，B，C， D，E，F，G和H不是碳; 其中R 1至R 8独立地选自但不限于卤素（F，Cl，Br和I），烷基，三氟甲基，甲氧基，羧甲基或羧乙基（COOCH 3或硝基，芳基，杂芳基，氰基，氨基，二烷基氨基烷基，1-（4-烷基哌嗪基）及其药学上可接受的盐; 并且其中X独立地选自由任何原子特别是氧原子或任何制备吲哚并[2,1-b]喹唑啉-6,12-二酮化合物所必需的侧链，该术语可理解为“前药” 药物化学领域的普通技术人员之一。换句话说，具有碳 - 氮双键带有取代基的结构的侧链使得前药更易溶于水且具有生物利用度。

33. 发明申请

WO2009055650A2 POLYACRYLATE NANOPARTICLE DRUG DELIVERY 审中-公开
标题翻译：聚丙烯酸纳米脂药物递送
公开(公告)号：WO2009055650A2
公开(公告)日：2009-04-30
申请号：PCT/US2008/081080
申请日：2008-10-24
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , CORMIER, Ryan , KYLE, Dennis E.
发明人： TUROS, Edward , CORMIER, Ryan , KYLE, Dennis E.
IPC分类号： A61K9/18
CPC分类号： A61K9/5138 , A61K9/5192 , Y02A50/411
摘要： Drug delivery of resistance reversal agents by polyacrylate nanoparticles for treatment of drug (e.g. chloroquine) resistant malaria. Also provided are drug delivery by polyacrylate nanoparticles of ciprofloxacin for treatment of anthrax.
摘要翻译：用于治疗药物（例如氯喹）抗性疟疾的聚丙烯酸酯纳米颗粒的药物递送抗逆转剂。还提供了用于治疗炭疽的环丙沙星的聚丙烯酸酯纳米颗粒的药物递送。

34. 发明申请

WO2004016220A3 APICOMPLEXAN PATHWAYS, INHIBITIORS, AND DRUG DELIVERY 审中-公开
标题翻译： APICOMPLEXAN PATHWAYS，INHIBITIORS和DRUG DELIVERY
公开(公告)号：WO2004016220A3
公开(公告)日：2005-02-24
申请号：PCT/US0325571
申请日：2003-08-14
申请人： MCLEOD RIMA L , MUI ERNEST J , SAMUEL BENJAMIN U , MACK DOUGLAS G , KIRISITS MICHAEL J , WENDER PAUL , ROTHBARD JONATHAN , HEARN BRIAN , ROBERTS CRAIG W , RICE DAVID W , MUENCH STEPHEN P , PRIGGE SEAN , CAMPBELL SAMANTHA A , COGGINS JOHN R , ROBERTS FIONA , HENRIQUEZ FIONA L , MILHOUS WILBUR K , KYLE DENNIS E
发明人： MCLEOD RIMA L , MUI ERNEST J , SAMUEL BENJAMIN U , MACK DOUGLAS G , KIRISITS MICHAEL J , WENDER PAUL , ROTHBARD JONATHAN , HEARN BRIAN , ROBERTS CRAIG W , RICE DAVID W , MUENCH STEPHEN P , PRIGGE SEAN , CAMPBELL SAMANTHA A , COGGINS JOHN R , ROBERTS FIONA , HENRIQUEZ FIONA L , MILHOUS WILBUR K , KYLE DENNIS E
IPC分类号： C12N1/21 , C12N9/02 , C12N9/88 , C12N15/12 , C12N15/31 , C12Q1/18 , A61K39/012 , C07H21/04 , C12N5/10 , C12N15/63 , C12P21/06
CPC分类号： C12N9/001 , C12N9/88 , C12Q1/18
摘要： An apicomplexan Fab I gene and the gene for DAHP synthase in Toxoplasma gondii, and their encoded enzymes, provide means to rationally design novel inhibitory compositions useful for prevention and treatment of apicomplexan related diseases. For example, triclosan is a lead compound. Delivery of inhibitors to microorganisms by short amino acid polymers demonstrates a novel method to treat active infections, and demonstrates a new approach for delivering antimicrobials to encysted, latent parasites. The shikimate pathway is essential for survival of the apicomplexan parasites Plasmodium falciparum, Toxoplasma gondii and Cryptosporidium parvum. Because it is absent in mammals, it is an appealing therapeutic target. Genes encoding the shikimate pathway enzymes in T. gondii are described. Putative AOX sequences were identified and sequenced from both type 1 and type 2 strains of C. parvum. The gene encodes a polypeptide of 336 amino acids and has a predicted N-terminal transit sequence similar to that found in proteins targeted to the mitochondria of other species. Alternative oxidase (AOX) is another target for new anti-microbial agents for C. parvum.
摘要翻译：一种apicomplexan Fab I基因和弓形虫中DAHP合酶基因及其编码的酶，提供合理设计可用于预防和治疗副作用相关疾病的新型抑制组合物的手段。例如，三氯生是铅化合物。通过短氨基酸聚合物递送微生物抑制剂表明了一种治疗活动性感染的新方法，并展示了一种将抗微生物剂递送至包埋的潜伏寄生虫的新方法。莽草酸通路对于复合寄生虫恶性疟原虫，弓形虫和隐孢子虫的生存至关重要。因为它在哺乳动物中不存在，这是一个有吸引力的治疗目标。描述了编码弓形虫中莽草酸通路酶的基因。鉴定并鉴定了来自小曲霉的1型和2型菌株的推定的AOX序列。该基因编码336个氨基酸的多肽，并且具有与靶向其他物种的线粒体的蛋白质中发现的N-末端转运序列相似的预测的N-末端转运序列。替代氧化酶（AOX）是新小型副抗菌剂的另一个目标。

35. 发明申请

WO2004016220A2 APICOMPLEXAN PATHWAYS, INHIBITIORS, AND DRUG DELIVERY 审中-公开
标题翻译： APICOMPLEXAN PATHWAYS，INHIBITIORS和DRUG DELIVERY
公开(公告)号：WO2004016220A2
公开(公告)日：2004-02-26
申请号：PCT/US2003/025571
申请日：2003-08-14
申请人： McLEOD, Rima, L. , MUI, Ernest, J. , SAMUEL, Benjamin, U. , MACK, Douglas, G. , KIRISITS, Michael, J. , WENDER, Paul , ROTHBARD, Jonathan , HEARN, Brian , ROBERTS, Craig, W. , RICE, David, W. , MUENCH, Stephen, P. , PRIGGE, Sean , CAMPBELL, Samantha, A. , COGGINS, John, R. , ROBERTS, Fiona , HENRIQUEZ, Fiona, L. , MILHOUS, Wilbur, K. , KYLE, Dennis, E.
发明人： McLEOD, Rima, L. , MUI, Ernest, J. , SAMUEL, Benjamin, U. , MACK, Douglas, G. , KIRISITS, Michael, J. , WENDER, Paul , ROTHBARD, Jonathan , HEARN, Brian , ROBERTS, Craig, W. , RICE, David, W. , MUENCH, Stephen, P. , PRIGGE, Sean , CAMPBELL, Samantha, A. , COGGINS, John, R. , ROBERTS, Fiona , HENRIQUEZ, Fiona, L. , MILHOUS, Wilbur, K. , KYLE, Dennis, E.
IPC分类号： A61K
CPC分类号： C12N9/001 , C12N9/88 , C12Q1/18
摘要： An apicomplexan Fab I gene and the gene for DAHP synthase in Toxoplasma gondii , and their encoded enzymes, provide means to rationally design novel inhibitory compositions useful for prevention and treatment of apicomplexan related diseases. For example, triclosan is a lead compound. Delivery of inhibitors to microorganisms by short amino acid polymers demonstrates a novel method to treat active infections, and demonstrates a new approach for delivering antimicrobials to encysted, latent parasites. The shikimate pathway is essential for survival of the apicomplexan parasites Plasmodium falciparum , Toxoplasma gondii and Cryptosporidium parvum . Because it is absent in mammals, it is an appealing therapeutic target. Genes encoding the shikimate pathway enzymes in T. gondii are described. Putative AOX sequences were identified and sequenced from both type 1 and type 2 strains of C. parvum . The gene encodes a polypeptide of 336 amino acids and has a predicted N-terminal transit sequence similar to that found in proteins targeted to the mitochondria of other species. Alternative oxidase (AOX) is another target for new anti-microbial agents for C. parvum .
摘要翻译：一种apicomplexan Fab I基因和弓形虫中DAHP合酶基因及其编码的酶，提供合理设计可用于预防和治疗副作用相关疾病的新型抑制组合物的手段。例如，三氯生是铅化合物。通过短氨基酸聚合物递送微生物抑制剂表明了一种治疗活动性感染的新方法，并展示了一种将抗微生物剂递送至包埋的潜伏寄生虫的新方法。痴呆途径对于复合寄生虫恶性疟原虫，弓形虫和隐孢子虫的生存至关重要。因为它在哺乳动物中不存在，这是一个有吸引力的治疗目标。描述了编码弓形虫中莽草酸通路酶的基因。鉴定并鉴定了来自小曲霉的1型和2型菌株的推定的AOX序列。该基因编码336个氨基酸的多肽，并且具有与靶向其他物种的线粒体的蛋白质中发现的N-末端转运序列相似的预测的N-末端转运序列。替代氧化酶（AOX）是新小型副抗菌剂的另一个目标。

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