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1. 发明申请

WO2008080218A1 METHODS OF SELECTING AND PRODUCING MODIFIED TOXINS, CONJUGATES CONTAINING MODIFIED TOXINS AND USES THEREOF 审中-公开
标题翻译：选择和生产改性毒素的方法，含有改性毒素的缀合物及其用途
公开(公告)号：WO2008080218A1
公开(公告)日：2008-07-10
申请号：PCT/CA2007/002278
申请日：2007-12-17
申请人： OSPREY PHARMACEUTICALS, LTD. , SU, Hongsheng , COGGINS, Philip, J. , MCDONALD, John R. , MCINTOSH, Laura, M.
发明人： SU, Hongsheng , COGGINS, Philip, J. , MCDONALD, John R. , MCINTOSH, Laura, M.
IPC分类号： C12N15/62 , A61K47/48 , A61P11/00 , A61P29/00 , A61P37/06 , C07K14/245 , C07K14/25 , C07K14/475 , C07K14/52 , C07K16/00 , C07K19/00 , C12N1/21 , C12N15/13 , C12N15/18 , C12N15/19 , C12N15/56 , C12N15/63 , C12N9/24 , C12P21/02 , C12Q1/00 , C12Q1/68 , G01N33/68
CPC分类号： C07K16/1203 , A61K47/6415 , C07K14/25 , C07K2319/01 , C07K2319/55 , C12N15/01 , C12N15/1034 , G01N2333/25 , G01N2333/415
摘要： Methods for selecting and identifying modified toxins and conjugates thereof are provided. The methods are select for toxins that exhibit reduced toxicity to the host cell in which they are expressed. Methods of increasing production of toxins, such as the modified toxins, or conjugates thereof, also are provided. In particular, in the methods the toxins, or conjugates thereof, are produced in the presence of an inhibitor molecule. Also provided, are modified toxins and conjugates thereof. Such conjugates can be used in the treatment of various disease or disorders associated with proliferation, migration, and physiological activity of cells involved in immune or inflammatory responses.
摘要翻译：提供了用于选择和鉴定修饰的毒素及其缀合物的方法。该方法选择毒素表现出对它们表达的宿主细胞的毒性降低。还提供了增加毒素例如修饰的毒素或其缀合物的产生的方法。具体而言，在该方法中，毒素或其缀合物在抑制剂分子存在下产生。还提供了修饰的毒素及其缀合物。这样的缀合物可以用于治疗与增殖，迁移和参与免疫或炎症反应的细胞的生理活性有关的各种疾病或病症。

2. 发明申请

WO2002079183A1 HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF 审中-公开
标题翻译：恶唑罗丹明衍生物及其应用
公开(公告)号：WO2002079183A1
公开(公告)日：2002-10-10
申请号：PCT/CA2002/000438
申请日：2002-03-27
申请人： THERATECHNOLOGIES INC. , HABI, Abdelkrim , GRAVEL, Denis , VILLENEUVE, Luc , FORTÉ, Jean-Pierre , SU, Hongsheng , VAILLANCOURT, Marc
发明人： HABI, Abdelkrim , GRAVEL, Denis , VILLENEUVE, Luc , FORTÉ, Jean-Pierre , SU, Hongsheng , VAILLANCOURT, Marc
IPC分类号： C07D311/82
CPC分类号： C07D311/82
摘要： Novel compounds of the formula (I) wherein: one of R1, R2, R3, R4, and (R10)n represents an halogen atom and each of the remaining R1, R2, R3, R4, and each of the remaining R10 group is independently selected in the group constituted by hydrogen, halogen atoms, an amino, acylamino, dialkylamino, cycloalkylamino, azacycloalkyl, alkylcycloalkylamino, aroylamino, diarylamino, arylalkylamino, aralkylamino, alkylaralkylamino, arylaralkylamino, hydroxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, hydroxysulfonyl, amidosulfonyl, dialkylamidosulfonyl, arylalkylamidosulfonyl, formyl, acyl, aroyl, alkyl, alkylene, alkenyl, aryl, aralkyl, vinyl, alkynyl group and by the corresponding substituted groups; - m = 0 - 1; n = 1-4, A is nil, O, or NH; R9 represents an alkylene group; -Z is H, amino, dialkylamino, or trialkylamino salt; X- is an anion; R5, R6, R7 and R8 are independently H or C1-C6 alkyl or R1 in combination with R5 or R6, or R2 in combination with R5 or R6, or R3 in combination with R7 or R8, or R4in combination with R7 or R8 represents an alkylene, alone or in association with a pharmaceutically acceptable carrier. These compounds, which are usefull as intermediate and as bactericides, as antiviral agent and in the treatment of immunologic disoders.
摘要翻译：式（I）的新型化合物其中：R 1，R 2，R 3，R 4和（R 10）中的一个表示卤素原子，剩余的R 1，R 2，R 3，R 4及其余R 10基中的每一个为在由氢，卤素原子，氨基，酰氨基，二烷基氨基，环烷基氨基，氮杂环烷基，烷基环烷基氨基，芳酰氨基，二芳基氨基，芳基烷基氨基，芳烷基氨基，烷基烷基氨基，芳基芳基氨基，羟基，烷氧基，芳氧基，芳烷氧基，巯基，，芳烷硫基，羧基，烷氧基羰基，芳氧基羰基，芳烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，氰基，羟基磺酰基，酰氨基磺酰基，二烷基氨基磺酰基，芳基烷基氨基磺酰基，甲酰基，酰基，芳酰基，烷基，亚烷基，烯基，芳基，芳烷基，乙烯基，炔基相应的取代基; - m = 0-1; n = 1-4，A为无，O或NH; R9表示亚烷基; -Z是H，氨基，二烷基氨基或三烷基氨基盐; X-是阴离子; R5，R6，R7和R8独立地是H或C1-C6烷基或R1与R5或R6组合，或R2与R5或R6组合，或R3与R7或R8组合，或R4in与R7或R8的组合表示单独或与药学上可接受的载体结合的亚烷基。这些化合物可用作中间体和杀菌剂，作为抗病毒剂和治疗免疫学解码器。

3. 发明申请

WO2008080218A9 METHODS OF SELECTING AND PRODUCING MODIFIED TOXINS, CONJUGATES CONTAINING MODIFIED TOXINS AND USES THEREOF 审中-公开
标题翻译：选择和生产改性毒素的方法，含有改性毒素的结合物及其用途
公开(公告)号：WO2008080218A9
公开(公告)日：2008-08-28
申请号：PCT/CA2007002278
申请日：2007-12-17
申请人： OSPREY PHARMACEUTICALS LTD , SU HONGSHENG , COGGINS PHILIP J , MCDONALD JOHN R , MCINTOSH LAURA M
发明人： SU HONGSHENG , COGGINS PHILIP J , MCDONALD JOHN R , MCINTOSH LAURA M
IPC分类号： C12N15/62 , A61K47/48 , A61P11/00 , A61P29/00 , A61P37/06 , C07K14/245 , C07K14/25 , C07K14/475 , C07K14/52 , C07K16/00 , C07K19/00 , C12N1/21 , C12N9/24 , C12N15/13 , C12N15/18 , C12N15/19 , C12N15/56 , C12N15/63 , C12P21/02 , C12Q1/00 , C12Q1/68 , G01N33/68
CPC分类号： C07K16/1203 , A61K47/6415 , C07K14/25 , C07K2319/01 , C07K2319/55 , C12N15/01 , C12N15/1034 , G01N2333/25 , G01N2333/415
摘要： Methods for selecting and identifying modified toxins and conjugates thereof are provided. The methods are select for toxins that exhibit reduced toxicity to the host cell in which they are expressed. Methods of increasing production of toxins, such as the modified toxins, or conjugates thereof, also are provided. In particular, in the methods the toxins, or conjugates thereof, are produced in the presence of an inhibitor molecule. Also provided, are modified toxins and conjugates thereof. Such conjugates can be used in the treatment of various disease or disorders associated with proliferation, migration, and physiological activity of cells involved in immune or inflammatory responses.
摘要翻译：提供了选择和鉴定修饰毒素及其缀合物的方法。这些方法是选择对宿主细胞表现出降低的毒性的毒素。还提供了增加毒素生产的方法，例如修饰的毒素或其缀合物。特别地，在该方法中，毒素或其结合物在抑制剂分子的存在下产生。还提供了修饰的毒素及其缀合物。这种缀合物可以用于治疗与涉及免疫或炎症反应的细胞的增殖，迁移和生理活性相关的各种疾病或病症。

4. 发明申请

WO02079183A8 HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF 审中-公开
标题翻译：恶唑罗丹明衍生物及其应用
公开(公告)号：WO02079183A8
公开(公告)日：2003-02-20
申请号：PCT/CA0200438
申请日：2002-03-27
申请人： THERATECHNOLOGIES INC , HABI ABDELKRIM , GRAVEL DENIS , VILLENEUVE LUC , SU HONGSHENG , VAILLANCOURT MARC
发明人： HABI ABDELKRIM , GRAVEL DENIS , VILLENEUVE LUC , SU HONGSHENG , VAILLANCOURT MARC
IPC分类号： A61K31/352 , A61N5/06 , A61P31/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , C07D311/82 , C07D493/10
CPC分类号： C07D311/82
摘要： Novel compounds of the formula (I) wherein: one of R1, R2, R3, R4, and (R10)n represents an halogen atom and each of the remaining R1, R2, R3, R4, and each of the remaining R10 group is independently selected in the group constituted by hydrogen, halogen atoms, an amino, acylamino, dialkylamino, cycloalkylamino, azacycloalkyl, alkylcycloalkylamino, aroylamino, diarylamino, arylalkylamino, aralkylamino, alkylaralkylamino, arylaralkylamino, hydroxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, hydroxysulfonyl, amidosulfonyl, dialkylamidosulfonyl, arylalkylamidosulfonyl, formyl, acyl, aroyl, alkyl, alkylene, alkenyl, aryl, aralkyl, vinyl, alkynyl group and by the corresponding substituted groups; - m = 0 - 1; n = 1-4, A is nil, O, or NH; R9 represents an alkylene group; -Z is H, amino, dialkylamino, or trialkylamino salt; X- is an anion; R5, R6, R7 and R8 are independently H or C1-C6 alkyl or R1 in combination with R5 or R6, or R2 in combination with R5 or R6, or R3 in combination with R7 or R8, or R4in combination with R7 or R8 represents an alkylene, alone or in association with a pharmaceutically acceptable carrier. These compounds, which are usefull as intermediate and as bactericides, as antiviral agent and in the treatment of immunologic disoders.
摘要翻译：式（I）的新型化合物其中：R 1，R 2，R 3，R 4和（R 10）中的一个表示卤素原子，剩余的R 1，R 2，R 3，R 4及其余R 10基中的每一个为在由氢，卤素原子，氨基，酰氨基，二烷基氨基，环烷基氨基，氮杂环烷基，烷基环烷基氨基，芳酰氨基，二芳基氨基，芳基烷基氨基，芳烷基氨基，烷基烷基氨基，芳基芳基氨基，羟基，烷氧基，芳氧基，芳烷氧基，巯基，，芳烷硫基，羧基，烷氧基羰基，芳氧基羰基，芳烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，氰基，羟基磺酰基，酰氨基磺酰基，二烷基氨基磺酰基，芳基烷基氨基磺酰基，甲酰基，酰基，芳酰基，烷基，亚烷基，烯基，芳基，芳烷基，乙烯基，炔基相应的取代基; - m = 0-1; n = 1-4，A为无，O或NH; R9表示亚烷基; -Z是H，氨基，二烷基氨基或三烷基氨基盐; X-是阴离子; R5，R6，R7和R8独立地是H或C1-C6烷基或R1与R5或R6组合，或R2与R5或R6组合，或R3与R7或R8组合，或R4in与R7或R8的组合表示单独或与药学上可接受的载体结合的亚烷基。这些化合物可用作中间体和杀菌剂，作为抗病毒剂和治疗免疫学解码器。

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