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    HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF
    1.
    发明申请
    HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF 有权
    恶唑罗丹明衍生物及其应用

    公开(公告)号：US20110301573A1

    公开(公告)日：2011-12-08

    申请号：US13157105

    申请日：2011-06-09

    申请人： Abdelkri Habi ,  Denis Gravel ,  Luc Villeneuve ,  Hongsheng Su ,  Marc Vaillancourt

    发明人： Abdelkri Habi ,  Denis Gravel ,  Luc Villeneuve ,  Hongsheng Su ,  Marc Vaillancourt

    IPC分类号： A61M37/00

    CPC分类号： A61K35/28 ,  A61K35/14 ,  C07D311/82

    摘要： Methods for treating a bacterial infection in a tissue sample are described. Tissue samples that are harvested from a patient may be infected with bacteria. A rhodamine compound is mixed with the infected tissue sample to form a mixture. The mixture is then exposed to radiant energy to inhibit or kill the bacteria. The exposed mixture is then transplanted into the patient. Examples of rhodamine compounds include 2′-(6-dimethylamino-3-dimethylimino-3H-xanthen-9-yl) 4′,5′-dichloro-benzoic acid methyl ester hydrochloride; 4,5-dibromorhodamine 110 2-(2-methoxy ethoxy)ethyl ester hydrobromide; acetate salt of 2,7-dibromorhodamine B hexyl ester; acetate salt of 2,7-dibromorhodamine B methyl ester; 4,5-dibromorhodamine 6G hydrobromide; rhodamine B 3-bromopropyl; acetate salt 2,7-dibromo-4′-carboxytetramethylrosamine methyl ester; 4-bromo-5-phenyl rhodamine B methyl ester chloride; 2,7-dibromo-4,5-dimethyl rhodamine B methyl ester bromide; 2-bromo-7-ethynyl rhodamine B methyl ester bromide; and 4,5-dibromo-2,7-di-n-butyl rhodamine B methyl ester bromide.

    摘要翻译： 描述了用于治疗组织样品中的细菌感染的方法。 从患者收获的组织样品可能被细菌感染。 将罗丹明化合物与感染的组织样品混合以形成混合物。 然后将混合物暴露于辐射能以抑制或杀死细菌。 然后将暴露的混合物移植到患者体内。 罗丹明化合物的实例包括2' - （6-二甲基氨基-3-二甲基亚氨基-3H-呫吨-9-基）4'，5'-二氯 - 苯甲酸甲酯盐酸盐; 4,5-二溴罗丹胺110 2-（2-甲氧基乙氧基）乙酯氢溴酸盐; 2,7-二溴罗丹明B己基酯的乙酸盐; 乙酸盐2,7-二溴罗丹明B甲酯; 4,5-二溴罗丹明6G氢溴酸盐; 罗丹明B 3 - 溴丙基; 乙酸盐2,7-二溴-4'-羧基四甲基甲胺甲酯; 4-溴-5-苯基罗丹明B甲酯氯化物; 2,7-二溴-4,5-二甲基罗丹明B甲酯溴化物; 2-溴-7-乙炔基罗丹明B甲酯溴化物; 和4,5-二溴-2,7-二正丁基罗丹明B甲酯溴化物。

    Halogenated rhodamine derivatives and applications thereof
    2.
    发明授权
    Halogenated rhodamine derivatives and applications thereof 有权
    卤化罗丹明衍生物及其应用

    公开(公告)号：US08383672B2

    公开(公告)日：2013-02-26

    申请号：US13157105

    申请日：2011-06-09

    申请人： Abdelkrim Habi ,  Denis Gravel ,  Luc Villeneuve ,  Hongsheng Su ,  Marc Vaillancourt

    发明人： Abdelkrim Habi ,  Denis Gravel ,  Luc Villeneuve ,  Hongsheng Su ,  Marc Vaillancourt

    IPC分类号： C07D311/88 ,  A61K31/35

    CPC分类号： A61K35/28 ,  A61K35/14 ,  C07D311/82

    摘要： Methods for treating a bacterial infection in a tissue sample are described. Tissue samples that are harvested from a patient may be infected with bacteria. A rhodamine compound is mixed with the infected tissue sample to form a mixture. The mixture is then exposed to radiant energy to inhibit or kill the bacteria. The exposed mixture is then transplanted into the patient. Examples of rhodamine compounds include 2′-(6-dimethylamino-3-dimethylimino-3H-xanthen-9-yl) 4′,5′-dichloro-benzoic acid methyl ester hydrochloride; 4,5-dibromorhodamine 110 2-(2-methoxy ethoxy)ethyl ester hydrobromide; acetate salt of 2,7-dibromorhodamine B hexyl ester; acetate salt of 2,7-dibromorhodamine B methyl ester; 4,5-dibromorhodamine 6G hydrobromide; rhodamine B 3-bromopropyl; acetate salt 2,7-dibromo-4′-carboxytetramethylrosamine methyl ester; 4-bromo-5-phenyl rhodamine B methyl ester chloride; 2,7-dibromo-4,5-dimethyl rhodamine B methyl ester bromide; 2-bromo-7-ethynyl rhodamine B methyl ester bromide; and 4,5-dibromo-2,7-di-n-butyl rhodamine B methyl ester bromide.

    摘要翻译： 描述了用于治疗组织样品中的细菌感染的方法。 从患者收获的组织样品可能被细菌感染。 将罗丹明化合物与感染的组织样品混合以形成混合物。 然后将混合物暴露于辐射能以抑制或杀死细菌。 然后将暴露的混合物移植到患者体内。 罗丹明化合物的实例包括2' - （6-二甲基氨基-3-二甲基亚氨基-3H-呫吨-9-基）4'，5'-二氯 - 苯甲酸甲酯盐酸盐; 4,5-二溴罗丹胺110 2-（2-甲氧基乙氧基）乙酯氢溴酸盐; 2,7-二溴罗丹明B己基酯的乙酸盐; 乙酸盐2,7-二溴罗丹明B甲酯; 4,5-二溴罗丹明6G氢溴酸盐; 罗丹明B 3 - 溴丙基; 乙酸盐2,7-二溴-4'-羧基四甲基甲胺甲酯; 4-溴-5-苯基罗丹明B甲酯氯化物; 2,7-二溴-4,5-二甲基罗丹明B甲酯溴化物; 2-溴-7-乙炔基罗丹明B甲酯溴化物; 和4,5-二溴-2,7-二正丁基罗丹明B甲酯溴化物。

    Halogenated rhodamine derivatives and applications thereof
    3.
    发明授权
    Halogenated rhodamine derivatives and applications thereof 有权
    卤化罗丹明衍生物及其应用

    公开(公告)号：US07560574B2

    公开(公告)日：2009-07-14

    申请号：US10297088

    申请日：2002-03-27

    申请人： Abdelkrim Habi ,  Denis Gravel ,  Luc Villeneuve ,  Hongsheng Su ,  Marc Vaillancourt

    发明人： Abdelkrim Habi ,  Denis Gravel ,  Luc Villeneuve ,  Hongsheng Su ,  Marc Vaillancourt

    IPC分类号： C07D311/88

    CPC分类号： A61K35/28 ,  A61K35/14 ,  C07D311/82

    摘要： Compounds of formula (I) wherein: one of R1, R2, R3, R4 and (R10)n represents halogen and each remaining R1, R2, R3, R4 and R10 group is independently selected from hydrogen, halogen, 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, and corresponding substituted groups; m=0-1; n=1-4, A is nil, O, or NH; R9 is alkylene; -Z is H, amino, dialkylamino, or a 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 R4 in combination with R7 or R8 represents alkylene, are useful alone or with a pharmaceutically acceptable carrier, as intermediates and as bactericides, antiviral agents and in treatment of immunologic disorders.

    摘要翻译： 式（I）化合物其中：R 1，R 2，R 3，R 4和（R 10）n中的一个表示卤素，并且各残基R 1，R 2，R 3，R 4和R 10基团独立地选自氢，卤素，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，烷基芳基烷基氨基，芳基芳烷基氨基，羟基，烷氧基，芳氧基，芳烷氧基，巯基，烷硫基，芳硫基，芳烷硫基，羧基，烷氧羰基，芳氧羰基，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 酰基，芳酰基，烷基，亚烷基，烯基，芳基，芳烷基，乙烯基，炔基和相应的取代基; m = 0-1; n = 1-4，A为无，O或NH; R9是亚烷基; -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R4与R7或R8组合 代表亚烷基，可单独使用或与药学上可接受的载体一起使用，作为中间体以及作为杀细菌剂，抗病毒剂和治疗免疫疾病。

    Halogenated Rhodamine Derivatives and Applications Thereof
    4.
    发明申请
    Halogenated Rhodamine Derivatives and Applications Thereof 审中-公开
    卤代罗丹明衍生物及其应用

    公开(公告)号：US20090176869A1

    公开(公告)日：2009-07-09

    申请号：US12403819

    申请日：2009-03-13

    申请人： Abdelkrim Habi ,  Denis Gravel ,  Luc Villeneuve ,  Jean-Pierre Forte ,  Hongsheng Su ,  Marc Vaillancourt

    发明人： Abdelkrim Habi ,  Denis Gravel ,  Luc Villeneuve ,  Jean-Pierre Forte ,  Hongsheng Su ,  Marc Vaillancourt

    IPC分类号： A61K31/352 ,  C07D311/88 ,  A61P31/04

    CPC分类号： A61K35/28 ,  A61K35/14 ,  C07D311/82

    摘要： Compounds of formula I: in which one of R1, R2, R3, R4 and (R10)n represents halogen and each of the remaining R1, R2, R3, R4 and R10 groups is independently selected from hydrogen, halogen, amino, acylamino, dialkylamino, cycloalkylamino, azacycloalkyl, alkylcycloalkylamino, aroylamino, diarylamino, arylalkylamino, aralkylamino, alkylaralkylamino, arylaralkylamino, hydroxyl, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, hydroxysulfonyl, amidosulfonyl, dialkylamidosulfonyl, arylalkylamido-sulfonyl, formyl, acyl, aroyl, alkyl, alkylene, alkenyl, aryl, aralkyl, vinyl, alkynyl and corresponding substituted groups; m=0-1; n=1-4; A is nil, O or NH; R9 is alkylene, Z is H, amino, dialkylamino or trialkylamino salt; X is an anion; and R5, R6, R7 and R8 are independently selected from H and C1-6 alkyl, or R1 with R5 or R6, or R2 with R5 or R6, or R3 with R7 or R8 represents alkylene, optionally in association with a pharmaceutically acceptable carrier, which are useful as intermediates, and as bacteriocides, antiviral agents or in treating immunological disorders.

    摘要翻译： 式Ⅰ化合物其中R 1，R 2，R 3，R 4和R 10中的一个表示卤素，R 1，R 2，R 3，R 4和R 10各自独立地选自氢，卤素，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，芳酰基氨基，二芳基氨基，芳基烷基氨基，芳烷基氨基，烷基芳基烷基氨基，芳基芳基氨基，羟基，烷氧基，芳氧基，芳烷氧基，巯基，烷硫基，芳硫基，芳烷硫基，羧基，烷氧羰基，芳氧羰基，芳烷氧羰基，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，芳基烷基酰氨基 - 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，炔基和相应的取代基; m = 0-1; n = 1-4; A为零，O或NH; R9是亚烷基，Z是H，氨基，二烷基氨基或三烷基氨基盐; X是阴离子; 并且R 5，R 6，R 7和R 8独立地选自H和C 1-6烷基，或R 1与R 5或R 6，或R 2与R 5或R 6，或R 3与R 7或R 8表示亚烷基，任选地与药学上可接受的载体 ，其可用作中间体，以及作为杀细菌剂，抗病毒剂或用于治疗免疫学疾病。

    Nucleic acid sequences and expression systems for heparinase II and heparinase III derived from Flavobacterium heparinum
    6.
    发明授权
    Nucleic acid sequences and expression systems for heparinase II and heparinase III derived from Flavobacterium heparinum 失效
    肝素肝素肝素II和肝素酶III的核酸序列和表达系统

    公开(公告)号：US5919693A

    公开(公告)日：1999-07-06

    申请号：US900951

    申请日：1997-07-25

    申请人： Hongsheng Su ,  Francoise Blain ,  Clark Bennett ,  Kangfu Gu ,  Joseph Zimmermann ,  Roy Musil

    发明人： Hongsheng Su ,  Francoise Blain ,  Clark Bennett ,  Kangfu Gu ,  Joseph Zimmermann ,  Roy Musil

    IPC分类号： C12N15/09 ,  C07K16/40 ,  C12N1/21 ,  C12N9/88 ,  C12N15/60 ,  C12N15/74 ,  C12P21/08 ,  C12R1/19 ,  C12N15/63

    CPC分类号： C12Y402/02007 ,  C12N15/74 ,  C12N9/88

    摘要： The present invention describes the isolation and sequence of genes from Flavobacterium heparinum encoding heparin and heparan sulfate degrading enzymes, heparinase II and heparinase III (EC 4.2.2.8). It further describes a method of expressing and an expression for heparinases I, II and III using a modified ribosome binding region derived from a promoter from glycosaminoglycan lyase genes of F. heparinum. Also, a multi-step protein purification method incorporating cell disruption, cation exchange chromatography, affinity chromatography and hydroxylapatite chromatography is outlined. Antibodies against a post-translational modification moiety common to Flavobacterium heparinum proteins and a method to obtain antibodies specific to these moieties and to the amino acid sequences of heparinases I, II and III are described.

    摘要翻译： 本发明描述了编码肝素黄肝素和硫酸乙酰肝素降解酶，肝素酶II和肝素酶III（EC 4.2.2.8）的基因的分离和序列。 它进一步描述了使用衍生自肝素肝素的糖胺聚糖裂解酶基因的启动子的修饰的核糖体结合区域来表达和表达肝素酶I，II和III的方法。 此外，概述了掺入细胞破碎，阳离子交换层析，亲和层析和羟基磷灰石层析的多步蛋白质纯化方法。 描述了针对肝炎黄杆菌蛋白质共同的翻译后修饰部分的抗体以及获得对这些部分和肝素酶I，II和III的氨基酸序列特异性的抗体的方法。

    Nucleic acid sequences and expression systems for heparinase II and heparinase III derived from Flavobacterium heparinum
    8.
    发明授权
    Nucleic acid sequences and expression systems for heparinase II and heparinase III derived from Flavobacterium heparinum 失效
    肝素肝素肝素II和肝素酶III的核酸序列和表达系统

    公开(公告)号：US5681733A

    公开(公告)日：1997-10-28

    申请号：US258639

    申请日：1994-06-10

    申请人： Hongsheng Su ,  Francoise Blain ,  Clark Bennett ,  Kangfu Gu ,  Joseph Zimmermann ,  Roy Musil

    发明人： Hongsheng Su ,  Francoise Blain ,  Clark Bennett ,  Kangfu Gu ,  Joseph Zimmermann ,  Roy Musil

    IPC分类号： C12N15/09 ,  C07K16/40 ,  C12N1/21 ,  C12N9/88 ,  C12N15/60 ,  C12N15/74 ,  C12P21/08 ,  C12R1/19

    CPC分类号： C12Y402/02007 ,  C12N15/74 ,  C12N9/88

    摘要： The present invention describes the isolation and sequence of genes from Flavobacterium heparinum encoding heparin and heparan sulfate degrading enzymes, heparinase II and heparinase III (EC 4.2.2.8). It further describes a method of expressing and an expression for heparinases I, II and III using a modified ribosome binding region derived from a promoter from glycosaminoglycan lyase genes of F. heparinum. Also, a multi-step protein purification method incorporating cell disruption, cation exchange chromatography, affinity chromatography and hydroxylapatite chromatography is outlined. Antibodies against a post-translational modification moiety common to Flavobacterium heparinum proteins and a method to obtain antibodies specific to these moieties and to the amino acid sequences of heparinases I, II and III are described.

    摘要翻译： 本发明描述了编码肝素黄肝素和硫酸乙酰肝素降解酶，肝素酶II和肝素酶III（EC 4.2.2.8）的基因的分离和序列。 它进一步描述了使用衍生自肝素肝素的糖胺聚糖裂解酶基因的启动子的修饰的核糖体结合区域来表达和表达肝素酶I，II和III的方法。 此外，概述了掺入细胞破碎，阳离子交换层析，亲和层析和羟基磷灰石层析的多步蛋白质纯化方法。 描述了针对肝炎黄杆菌蛋白质共同的翻译后修饰部分的抗体以及获得对这些部分和肝素酶I，II和III的氨基酸序列特异性的抗体的方法。