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1. 发明授权

US08383672B2 Halogenated rhodamine derivatives and applications thereof 有权
标题翻译：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。

2. 发明申请

US20110301573A1 HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF 有权
标题翻译：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。

3. 发明申请

US20110021616A1 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：US20110021616A1
公开(公告)日：2011-01-27
申请号：US12786280
申请日：2010-05-24
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： A61K31/352 , A61P31/04
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 rhodmaine 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 of 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。与感染的组织样品混合罗丹明酸化合物以形成混合物。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; 2,7-二溴-4'-羧基四甲基甲胺甲酯的乙酸盐; 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。

4. 发明申请

US20120136338A1 IMMUNOLOGIC COMPOUNDS FOR PREVENTION, PROTECTION, PROPHYLAXIS OR TREATMENT OF IMMUNOLOGICAL DISORDERS, INFECTIONS AND CANCER 审中-公开
标题翻译：用于预防，保护，预防或治疗免疫缺陷病毒，感染和癌症的免疫化学物质
公开(公告)号：US20120136338A1
公开(公告)日：2012-05-31
申请号：US13366099
申请日：2012-02-03
申请人： DENIS CLAUDE ROY , Marc Vaillancourt , Luc Villeneuve
发明人： DENIS CLAUDE ROY , Marc Vaillancourt , Luc Villeneuve
IPC分类号： A61M5/00 , A61P37/00 , A61P31/00 , A61P35/00 , A61P31/12 , A61P35/02 , A61P31/10 , A61P33/02 , A61P31/18 , A61P31/14 , A61P31/22 , A61K35/12 , A61P33/00
CPC分类号： A61K31/353 , A61K31/365 , A61K35/28 , A61K38/193 , A61K38/2013 , A61K38/21 , A61K39/0008 , A61K39/0011 , A61K41/0019 , A61K41/0057 , A61K2039/5154 , C09B11/24 , Y02A50/414 , A61K2300/00
摘要： The present invention provides for methods of treating a cancer patient. In one methods, cancer cells are harvested from a patient. A therapeutic amount of a rhodamine derivative is then added to the harvested cancer cells. The harvested cells and the rhodamine derivative are then irradiated with a suitable wavelength and intensity for the selective killing of the cancer cells. The irradiated cancer cells are then mixed with antigen presenting cells to form a mixture. The mixture of cancer and antigen presenting cells are then injected into the patient. The present invention also provides for methods of inhibiting or treating an immunological disorder, infection, or a cancer in an individual.
摘要翻译：本发明提供了治疗癌症患者的方法。在一种方法中，从患者收获癌细胞。然后将治疗量的罗丹明衍生物加入到所获得的癌细胞中。然后用合适的波长和强度照射收获的细胞和罗丹明衍生物，用于选择性杀死癌细胞。然后将照射的癌细胞与抗原呈递细胞混合以形成混合物。然后将癌症和抗原呈递细胞的混合物注射到患者体内。本发明还提供了抑制或治疗个体的免疫学障碍，感染或癌症的方法。

5. 发明授权

US07560574B2 Halogenated rhodamine derivatives and applications thereof 有权
标题翻译：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。

6. 发明申请

US20090176869A1 Halogenated Rhodamine Derivatives and Applications Thereof 审中-公开
标题翻译：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。

7. 发明申请

US20070098732A1 Immunologic compounds for prevention, protection, prophylaxis or treatment of immunological disorders, infections and cancer 审中-公开
标题翻译：用于预防，保护，预防或治疗免疫疾病，感染和癌症的免疫化合物
公开(公告)号：US20070098732A1
公开(公告)日：2007-05-03
申请号：US10581718
申请日：2004-12-02
申请人： Denis Roy , Marc Vaillancourt , Luc Villeneuve
发明人： Denis Roy , Marc Vaillancourt , Luc Villeneuve
IPC分类号： A61K39/00 , A61K31/365 , A61K31/353
CPC分类号： A61K31/353 , A61K31/365 , A61K35/28 , A61K38/193 , A61K38/2013 , A61K38/21 , A61K39/0008 , A61K39/0011 , A61K41/0019 , A61K41/0057 , A61K2039/5154 , C09B11/24 , Y02A50/414 , A61K2300/00
摘要： The present invention relates to the use of PDT-treated cells (whole or fragments thereof) and/or supernatant thereof in the preparation of vaccines for immunoprotection or immunomodulation. More particularly, the use of PDT-treated cells (whole or fragments thereof) and/or supernatant thereof in the preparation of an immunologic compound for prevention, protection, prophylaxis or treatment of an immunological disorder, infection and/or a cancer in an individual, which comprises treatment of the individual cells or components thereof with a photoactivatable molecule selected from the group consisting of compounds I to XVIII, wherein the photoactivatable molecule is activated by a light of appropriate wavelength, thereby activating the photoactivatable molecule and causing prevention, protection, prophylaxis or treatment of the immunological disorder, infection and/or a cancer.
摘要翻译：本发明涉及PDT处理的细胞（其全部或其片段）和/或上清液在免疫保护或免疫调节疫苗的制备中的用途。更具体地说，PDT处理的细胞（其全部或其片段）和/或其上清液在制备免疫化合物中用于预防，保护，预防或治疗个体中的免疫疾病，感染和/或癌症的用途其包括用选自化合物I至XVIII的可光活化分子处理单个细胞或其组分，其中可光活化分子由适当波长的光激活，由此活化可光活化分子并引起预防，保护，预防或治疗免疫学疾病，感染和/或癌症。

8. 发明授权

US4402941A Veterinary composition for preventing feline urological syndrome and litter product containing the composition 失效
标题翻译：用于预防猫泌尿综合征的兽药组合物和含有该组合物的垃圾产品
公开(公告)号：US4402941A
公开(公告)日：1983-09-06
申请号：US302685
申请日：1981-09-15
申请人： Marc Vaillancourt
发明人： Marc Vaillancourt
IPC分类号： A61K33/00 , A61K33/14 , A61K36/00
CPC分类号： A61K36/00 , A01K1/0152
摘要： A veterinary composition for preventing feline urological syndrome in cats, comprising from 25 to 75% by weight of green plant powder, from 15 to 45% of a urine acidifying agent, from 9.5 to 28.5% by weight of a soft diuretic agent and from 0.5 to 1.5% of a calcium chelating agent, based on the total weight of the composition. A method for administering such a veterinary composition to a cat is also disclosed comprising using a veterinary litter comprising particles of wood or of wood derivatives covered with 0.1 to 4% by weight of the above veterinary composition based on the total weight of the particles. An animal using this litter composed of particles covered with an external layer of medicine impregnates its paws, part of its fur and its muzzle with medicine without noticing it and then unconsciously ingests the medicine when it cleans itself by licking its paws and fur.
摘要翻译：一种用于预防猫的猫泌尿综合征的兽用组合物，其包含25至75重量％的绿色植物粉末，15至45％的尿酸化剂，9.5至28.5重量％的软利尿剂和0.5 至1.5％的钙螯合剂，基于组合物的总重量。还公开了向猫施用这种兽医组合物的方法，其包括使用含有基于所述颗粒总重量的上述兽药组合物的0.1至4重量％的木材或木材衍生物颗粒的兽用垫料。使用这种由外部药物覆盖的颗粒组成的垃圾的动物，将其爪子，毛皮及其枪口的一部分药物浸没在药物中，而不注意它，然后通过舔其爪子和毛皮自动吸收药物。

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