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21. 发明专利

CA2432992A1 FAB I AND INHIBITION OF APICOMPLEXAN PARASITES 未知
公开(公告)号：CA2432992A1
公开(公告)日：2002-06-27
申请号：CA2432992
申请日：2001-12-20
申请人： MCLEOD RIMA , PRIGGE SEAN , MUI ERNEST J , KIRISITS MICHAEL J , SAMUEL BENJAMIN U , RICE DAVID W , ROBERTS CRAIG W , MACK DOUGLAS G , MUENCH STEPHEN P , RAFFERTY JOHN B , KYLE DENNIS E , LYONS RUSSEL E , MILHOUS WILBUR K
发明人： MCLEOD RIMA , PRIGGE SEAN , MUI ERNEST J , KIRISITS MICHAEL J , SAMUEL BENJAMIN U , RICE DAVID W , ROBERTS CRAIG W , MACK DOUGLAS G , MUENCH STEPHEN P , RAFFERTY JOHN B , KYLE DENNIS E , LYONS RUSSEL E , MILHOUS WILBUR K
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 , A61K38/00
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.

22. 发明专利

IL92101A Amidine derivatives and pharmaceutical compositions containing the same 未知
公开(公告)号：IL92101A
公开(公告)日：1995-11-27
申请号：IL9210189
申请日：1989-10-24
申请人： TIDWELL RICHARD R , GERATZ DIETER , HALL JAMES EDWIN , KYLE DENNIS E , GROGL MAX , OHEMENG KWASI A
IPC分类号： A61K31/155 , A61K31/41 , A61P11/00 , A61P33/02 , A61P33/10 , A61P43/00 , C07C257/18 , C07C323/60 , C07D233/20 , C07D239/22 , C07D239/24 , C07C323/29 , C07D233/12 , C07D239/06 , C07D234/04 , A61K31/395
摘要： New pentamidine analogue compounds and compositions containing the new analogues are disclosed. Methods for the treatment of, and prophylaxis against, Pneumocystis carinii pneumonia, and methods for treating leishmaniasis, giardiasis, and malaria using the new analogues are also disclosed.

23. 发明专利

NO894222L 未知
公开(公告)号：NO894222L
公开(公告)日：1990-04-26
申请号：NO894222
申请日：1989-10-24
申请人： TIDWELL RICHARD R , GERATZ J DIETER , OHEMENG KWASI A , HALL JAMES EDWIN , KYLE DENNIS E , GROGL MAX
发明人： TIDWELL RICHARD R , GERATZ J DIETER , HALL JAMES EDWIN , KYLE DENNIS E , GROGL MAX , OHEMENG KWASI A
IPC分类号： A61K31/155 , A61K31/41 , A61P11/00 , A61P33/02 , A61P33/10 , A61P43/00 , C07C257/18 , C07C323/60 , C07D233/20 , C07D239/22 , C07D239/24
摘要： New pentamidine analogue compounds and compositions containing the new analogues are disclosed. Methods for the treatment of, and prophylaxis against, Pneumocystis carinii pneumonia, and methods for treating leishmaniasis, giardiasis, and malaria using the new analogues are also disclosed.

24. 发明专利

CA2001359A1 METHODS FOR THE TREATMENT AND PROPHYLAXIS OF PNEUMOCYSTIS CARINII PNEUMONIA AND OTHER DISEASES AND COMPOUNDS AND FORMULATIONS FOR USE IN SAID METHODS 未知
公开(公告)号：CA2001359A1
公开(公告)日：1990-04-25
申请号：CA2001359
申请日：1989-10-24
申请人： TIDWELL RICHARD R , GERATZ J DIETER , HALL JAMES E , KYLE DENNIS E , GROGL MAX , OHEMENG KWASI A
发明人： TIDWELL RICHARD R , GERATZ J DIETER , HALL JAMES E , KYLE DENNIS E , GROGL MAX , OHEMENG KWASI A
IPC分类号： A61K31/155 , A61K31/41 , A61P11/00 , A61P33/02 , A61P33/10 , A61P43/00 , C07C257/18 , C07C323/60 , C07D233/20 , C07D239/22 , C07D239/24
摘要： New pentamidine analogue compounds and compositions containing the new analogues are disclosed. Methods for the treatment of, and prophylaxis against, Pneumocystis carinii pneumonia, and methods for treating leishmaniasis, giardiasis, and malaria using the new analogues are also disclosed.

25. 发明专利

FI895039A0 未知
公开(公告)号：FI895039A0
公开(公告)日：1989-10-24
申请号：FI895039
申请日：1989-10-24
申请人： TIDWELL RICHARD R , GERATZ J DIETER , HALL JAMES EDWIN , KYLE DENNIS E , GROGL MAX , OHEMENG KWASI A
发明人： TIDWELL RICHARD R , GERATZ J DIETER , HALL JAMES EDWIN , KYLE DENNIS E , GROGL MAX , OHEMENG KWASI A
IPC分类号： A61K31/155 , A61K31/41 , A61P11/00 , A61P33/02 , A61P33/10 , A61P43/00 , C07C257/18 , C07C323/60 , C07D233/20 , C07D239/22 , C07D239/24 , C07C
摘要： New pentamidine analogue compounds and compositions containing the new analogues are disclosed. Methods for the treatment of, and prophylaxis against, Pneumocystis carinii pneumonia, and methods for treating leishmaniasis, giardiasis, and malaria using the new analogues are also disclosed.

26. 发明申请

WO2009055650A3 POLYACRYLATE NANOPARTICLE DRUG DELIVERY 审中-公开
标题翻译：聚丙烯酸纳米颗粒药物递送
公开(公告)号：WO2009055650A3
公开(公告)日：2009-06-04
申请号：PCT/US2008081080
申请日：2008-10-24
申请人： UNIV SOUTH FLORIDA , TUROS EDWARD , CORMIER RYAN , KYLE DENNIS E
发明人： TUROS EDWARD , CORMIER RYAN , KYLE DENNIS E
IPC分类号： A61F13/00
CPC分类号： A61K9/5138 , A61K9/5192
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：通过聚丙烯酸酯纳米颗粒用于治疗药物（例如氯喹）耐药性疟疾的药物递送抗性逆转剂。还提供了环丙沙星的聚丙烯酸酯纳米颗粒用于治疗炭疽的药物递送。

27. 发明申请

WO2002049576A3 FAB I AND INHIBITION OF APICOMPLEXAN PARASITES 审中-公开
公开(公告)号：WO2002049576A3
公开(公告)日：2002-06-27
申请号：PCT/US2001/049738
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： A61K38/00
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.

28. 发明申请

WO2003068736A3 MIXED STEROIDAL 1,2,4,5-TETRAOXANE COMPOUNDS AND METHODS OF MAKING AND USING THEREOF 审中-公开
公开(公告)号：WO2003068736A3
公开(公告)日：2003-08-21
申请号：PCT/US2003/003516
申请日：2003-02-07
申请人： U.S. ARMY MEDICAL RESEARCH AND MATERIAL COMMAND , SOLAJA, Bogdan , MILHOUS, Wilbur , OPSENICA, Dejan, M. , POCSFALVI, Gabriella , KYLE, Dennis, E.
发明人： SOLAJA, Bogdan , MILHOUS, Wilbur , OPSENICA, Dejan, M. , POCSFALVI, Gabriella , KYLE, Dennis, E.
IPC分类号： A01N45/00
摘要： Disclosed herein are mixed steroidal tetraoxanes having the following structural Formula (I), wherein n is 0, 1, 2, or 3; R is H; ethanoyl, propanoyl, or benzoyl; R1 is H, methyl, ethyl, or isopropyl; R2 is H, methyl, or ethyl; R3 is H, methyl, or ethyl; R4 is H, methyl, ethyl, tert -butyl, phenyl, p -hydroxyphenyl, p -methoxyphenyl, or p -nitrophenyl, or Formula (a), wherein Y is C 1 -C 4 straight or branched-chain alkoxy, or Formula (b), wherein W is N, R5 is hydrogen, methyl, ethyl, or n -propyl, isopropyl, or methyl ethanoate 2-yl, and R6 is hydrogen, methyl, ethyl, or n -propyl, or R5 and R6 are part of a pyrrolidine or piperidine ring; X is a C 1 -C 4 straight or branched-chain alkoxy, a primary amino, a N -akylamino wherein the alkyl is a straight-chain alkyl groups containing from 1 to 4 carbon atoms, methyl ethanoate-2-yl, N -phenylamino, p -nitrophenyl, N , N -dimethylamino, N , N -diethylamino, N , N -di( n -propyl)amino, N -pyrrolidino, or N -piperidino as single compounds, and any mixture of all possible stereoisomers at C(4’’). n may be 0, 1, 2, or 3, and methods of making and using thereof. As disclosed herein, the mixed steroidal tetraoxanes of the present invention exhibit antimalarial, antibacterial, and antiproliferative activity. Thus, as disclosed herein, the mixed steroidal tetraoxanes of the present invention may be used to treat, prevent, or inhibit malaria, bacterial infections, and diseases and disorders associated with cell proliferation in a subject.

29. 发明申请

WO2003068736A2 MIXED STEROIDAL 1,2,4,5-TETRAOXANE COMPOUNDS AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译：混合固体1,2,4,5-四氯乙烯化合物及其制备和使用方法
公开(公告)号：WO2003068736A2
公开(公告)日：2003-08-21
申请号：PCT/US2003/003516
申请日：2003-02-07
申请人： U.S. ARMY MEDICAL RESEARCH AND MATERIAL COMMAND , SOLAJA, Bogdan , MILHOUS, Wilbur , OPSENICA, Dejan, M. , POCSFALVI, Gabriella , KYLE, Dennis, E.
发明人： SOLAJA, Bogdan , MILHOUS, Wilbur , OPSENICA, Dejan, M. , POCSFALVI, Gabriella , KYLE, Dennis, E.
IPC分类号： C07D
CPC分类号： C07J21/00 , C07J41/0061
摘要： Disclosed herein are mixed steroidal tetraoxanes having the following structural Formula (I), wherein n is 0, 1, 2, or 3; R is H; ethanoyl, propanoyl, or benzoyl; R1 is H, methyl, ethyl, or isopropyl; R2 is H, methyl, or ethyl; R3 is H, methyl, or ethyl; R4 is H, methyl, ethyl, tert -butyl, phenyl, p -hydroxyphenyl, p -methoxyphenyl, or p -nitrophenyl, or Formula (II), wherein Y is C 1 -C 4 straight or branched-chain alkoxy, or Formula (III), wherein W is N, R5 is hydrogen, methyl, ethyl, or n -propyl, isopropyl, or methyl ethanoate 2-yl, and R6 is hydrogen, methyl, ethyl, or n -propyl, or R5 and R6 are part of a pyrrolidine or piperidine ring; X is a C 1 -C 4 straight or branched-chain alkoxy, a primary amino, a N -akylamino wherein the alkyl is a straight-chain alkyl groups containing from 1 to 4 carbon atoms, methyl ethanoate-2-yl, N -phenylamino, p -nitrophenyl, N , N -dimethylamino, N , N -diethylamino, N , N -di( n -propyl)amino, N -pyrrolidino, or N -piperidino as single compounds, and any mixture of all possible stereoisomers at C(4’’). n may be 0, 1, 2, or 3, and methods of making and using thereof. As disclosed herein, the mixed steroidal tetraoxanes of the present invention exhibit antimalarial, antibacterial, and antiproliferative activity. Thus, as disclosed herein, the mixed steroidal tetraoxanes of the present invention may be used to treat, prevent, or inhibit malaria, bacterial infections, and diseases and disorders associated with cell proliferation in a subject.
摘要翻译：本文公开了具有以下结构式I的混合甾族四恶烷，其中n为0,1,2或3 R为H乙酰基，丙酰基或苯甲酰基，R 1为H，甲基，乙基或异丙基，R 2为H，甲基或乙基R 3为H，甲基或R 4为H，甲基，乙基，叔丁基，苯基，对羟基苯基，对甲氧基苯基或对硝基苯基或式II，其中Y为C 1 -C 4直链或支链，链烷氧基或式III，其中W是N，R 5是氢，甲基，乙基或正丙基，异丙基或甲基乙酸酯2-基，并且R 6是氢，甲基，乙基或正丙基，或R 5 并且R 6是吡咯烷或哌啶环的一部分，X是C 1 -C 4直链或支链烷氧基，伯氨基，N-烷基氨基，其中烷基是含有1至4个碳原子的直链烷基，甲基乙酸酯-2-基，N-苯基氨基，对硝基苯基，N，N-二甲基氨基，N，N-二乙基氨基，N，N-二 - 丙基氨基，N-吡咯烷子基或N-哌啶子基作为单一化合物，所有可能的立体声在C4“somers。 n可以是0,1,2或3，以及其制备和使用方法。如本文所公开的，本发明的混合甾族四恶烷显示抗疟疾，抗细菌和抗增殖活性。因此，如本文所公开的，本发明的混合甾族四恶烷可用于治疗，预防或抑制疟疾，细菌感染以及与受试者中细胞增殖相关的疾病和病症。

30. 发明申请

WO0249576A9 FAB I AND INHIBITION OF APICOMPLEXAN PARASITES 审中-公开
标题翻译： FAB I和APICOMPLEXAN PARASITES的抑制
公开(公告)号：WO0249576A9
公开(公告)日：2003-04-24
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 , A61K38/00
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：发现和表征apicomplexan Fab I基因和编码酶以及三氯生作为铅化合物的发现，提供合理设计可用于预防和治疗复合物相关疾病的新型抑制组合物的手段。

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