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

    IPC分类号: C07D311/88 A61K31/35

    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。

    Compact dual receiver architecture for point to point radio
    3.
    发明授权
    Compact dual receiver architecture for point to point radio 有权
    紧凑型双接收机架构,用于点对点无线电

    公开(公告)号:US08275071B2

    公开(公告)日:2012-09-25

    申请号:US11750209

    申请日:2007-05-17

    IPC分类号: H03K9/00 H04L27/00

    摘要: A radio frequency receiver comprising a receiver module, an intermediate frequency (“IF”) module, a synthesizer module and a controller module. The receiver module receives a radio frequency signal and provides a baseband in-phase signal and a baseband quadrature signal, eliminates a sideband of the in-phase and quadrature signals to create a first and a second signal, downconverts the first and second signal to a first and a second IF signal, and selects one of the first or second IF signals. The IF module receives the first or second IF signal, performs analog-to-digital conversion on the first or second IF signal, and demodulates the digitally converted IF signal. The synthesizer module receives a programmable reference signal, downconverts the reference signal to an IF feedback signal, downconverts the reference signal to a baseband feedback signal, provides the IF feedback signal to the IF module, and provides the baseband feedback signal to the receiver module. The controller module samples the digitally converted IF signal and provides the programmable reference signal to the synthesizer module to thereby provide a demodulated output signal.

    摘要翻译: 一种射频接收机,包括接收机模块,中频(“IF”)模块,合成器模块和控制器模块。 接收器模块接收射频信号并提供基带同相信号和基带正交信号,消除同相和正交信号的边带以产生第一和第二信号,将第一和第二信号下变频到 第一和第二IF信号,并且选择第一IF信号或第二IF信号中的一个。 IF模块接收第一或第二IF信号,对第一或第二IF信号执行模数转换,并对数字转换的IF信号进行解调。 合成器模块接收可编程参考信号,将参考信号下变频为IF反馈信号,将参考信号下变频为基带反馈信号,向IF模块提供IF反馈信号,并将基带反馈信号提供给接收机模块。 控制器模块对数字转换的IF信号进行采样,并将可编程参考信号提供给合成器模块,从而提供解调的输出信号。

    Compact Dual Receiver Architecture for Point to Point Radio
    4.
    发明申请
    Compact Dual Receiver Architecture for Point to Point Radio 有权
    用于点对点无线电的紧凑型双接收机架构

    公开(公告)号:US20080285684A1

    公开(公告)日:2008-11-20

    申请号:US11750209

    申请日:2007-05-17

    IPC分类号: H04L27/00

    摘要: A radio frequency receiver comprising a receiver module, an intermediate frequency (“IF”) module, a synthesizer module and a controller module. The receiver module receives a radio frequency signal and provides a baseband in-phase signal and a baseband quadrature signal eliminates a sideband of the in-phase and quadrature signals to create a first and a second signal, downconverts the first and second signal to a first and a second IF signal, and selects one of the first or second IF signals. The IF module receives the first or second IF signal, performs analog-to-digital conversion on the first or second IF signal, and demodulates the digitally converted. If signal The synthesizer module receives a programmable reference signal, downconverts the reference signal to an IF feedback signal, downconverts the reference signal to a baseband feedback signal provides the IF feedback signal to the IF module, and provides the baseband feedback signal to the receiver module. The controller module samples the digitally converted IF signal and provides the programmable reference signal to the synthesizer module to thereby provide a demodulated output signal.

    摘要翻译: 一种射频接收机,包括接收机模块,中频(“IF”)模块,合成器模块和控制器模块。 接收器模块接收射频信号并提供基带同相信号,并且基带正交信号消除同相和正交信号的边带以产生第一和第二信号,将第一和第二信号下变频到第一和第二信号 和第二IF信号,并且选择第一IF信号或第二IF信号中的一个。 IF模块接收第一或第二IF信号,在第一或第二IF信号上执行模数转换,并对数字转换进行解调。 如果信号合成器模块接收到可编程参考信号,将参考信号下变频为IF反馈信号,将参考信号下变频为基带反馈信号,将IF反馈信号提供给IF模块,并将基带反馈信号提供给接收机模块 。 控制器模块对数字转换的IF信号进行采样,并将可编程参考信号提供给合成器模块,从而提供解调的输出信号。

    Compact Dual Receiver Architecture for Point to Point Radio
    5.
    发明申请
    Compact Dual Receiver Architecture for Point to Point Radio 审中-公开
    用于点对点无线电的紧凑型双接收机架构

    公开(公告)号:US20130089130A1

    公开(公告)日:2013-04-11

    申请号:US13626813

    申请日:2012-09-25

    IPC分类号: H03D9/00 H04B17/00

    摘要: A radio frequency receiver comprising a receiver module, an intermediate frequency (“IF”) module, a synthesizer module and a controller module. The receiver module receives a radio frequency signal and provides a baseband in-phase signal and a baseband quadrature signal, eliminates a sideband of the in-phase and quadrature signals to create a first and a second signal, downconverts the first and second signal to a first and a second IF signal, and selects one of the first or second IF signals. The IF module receives the first or second IF signal, performs analog-to-digital conversion on the first or second IF signal, and demodulates the digitally converted IF signal. The synthesizer module receives a programmable reference signal, downconverts the reference signal to an IF feedback signal, downconverts the reference signal to a baseband feedback signal, provides the IF feedback signal to the IF module, and provides the baseband feedback signal to the receiver module. The controller module samples the digitally converted IF signal and provides the programmable reference signal to the synthesizer module to thereby provide a demodulated output signal.

    摘要翻译: 一种射频接收机,包括接收机模块,中频(IF)模块,合成器模块和控制器模块。 接收器模块接收射频信号并提供基带同相信号和基带正交信号,消除同相和正交信号的边带以产生第一和第二信号,将第一和第二信号下变频到 第一和第二IF信号,并且选择第一IF信号或第二IF信号中的一个。 IF模块接收第一或第二IF信号,对第一或第二IF信号执行模数转换,并对数字转换的IF信号进行解调。 合成器模块接收可编程参考信号,将参考信号下变频为IF反馈信号,将参考信号下变频为基带反馈信号,向IF模块提供IF反馈信号,并将基带反馈信号提供给接收机模块。 控制器模块对数字转换的IF信号进行采样,并将可编程参考信号提供给合成器模块,从而提供解调的输出信号。

    Halogenated rhodamine derivatives and applications thereof
    7.
    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

    IPC分类号: C07D311/88

    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
    8.
    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

    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。

    Rhodamine derivatives for photodynamic therapy of cancer and in vitro
purging of the leukemias
    9.
    发明授权

    公开(公告)号:US5773460A

    公开(公告)日:1998-06-30

    申请号:US674247

    申请日:1996-07-01

    CPC分类号: C07D311/82 A61K41/0057

    摘要: The present invention relates to novel photoactivable rhodamine derivatives for enhancing high quantum-yield production and singlet oxygen generation upon irradiation with light while maintaining desirable differential retention of rhodamine between normal and cancer cells. Representative derivatives are 2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid methyl ester hydrochloride; 2-(4, 5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid ethyl ester hydrochloride; 2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid octyl ester hydrochloride; 2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride; 2-(6-ethyl amino-3-ethyl imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride; and photoactivable derivatives thereof. These derivatives are utilized in an amount to achieve appropriate intracellular levels of the derivative when irradiation of a suitable wavelength and intensity is applied to photoactivate the derivative and thereby induce cell killing.

    摘要翻译: 本发明涉及用于在照射光时提高高量子产率产生和单线态氧产生的新型可光致发光罗丹明衍生物,同时保持罗丹明在正常癌细胞与癌细胞之间的期望差异保留。 代表性的衍生物是2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸甲酯盐酸盐; 2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸乙酯盐酸盐; 2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸辛酯盐酸盐; 2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸正丁酯盐酸盐; 2-(6-乙基氨基-3-乙基亚氨基-3H-呫吨-9-基) - 苯甲酸正丁酯盐酸盐; 和其可光活化的衍生物。 当照射适当的波长和强度以光激活衍生物并由此诱导细胞杀伤时,这些衍生物用量达到适当的细胞内水平的衍生物。

    Novel rhodamine derivatives for photodynamic therapy of cancer and in
vitro purging of the leukemias
    10.
    发明授权
    Novel rhodamine derivatives for photodynamic therapy of cancer and in vitro purging of the leukemias 失效
    用于光动力治疗癌症和体外清除白血病的新型罗丹明衍生物

    公开(公告)号:US5556992A

    公开(公告)日:1996-09-17

    申请号:US300179

    申请日:1994-09-02

    IPC分类号: A61K41/00 C07D311/82

    CPC分类号: C07D311/82 A61K41/0057

    摘要: The present invention relates to novel photoactivable rhodamine derivatives for enhancing high quantum-yield production and singlet oxygen generation upon irradiation with light while maintaining desirable differential retention of rhodamine between normal and cancer cells, said derivatives are selected from the group consisting of 4,5-dibromorhodamine 123 (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid methyl ester hydrochloride); 4, 5-dibromorhodamine 123 (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid ethyl ester hydrochloride); 4, 5-dibromorhodamine 123 (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid octhyl ester hydrochloride); 4,5-dibromorhodamine 110 n-butyl ester (2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride); Rhodamine B n-butyl ester (2-(6-ethyl amino-3-ethyl imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride); and photoactivable derivatives thereof; whereby photoactivation of the derivatives induces cell killing while unactivated derivatives are substantially non-toxic to cells. Also, the present invention relates to the use of the photoactivable derivatives of the present invention for the photodynamic therapy of a cancer patient by destroying human cancer cells, wherein appropriate intracellular levels of the derivatives are achieved and irradiation with light of a suitable wavelength is applied. The present invention also relates to a method for the photodynamic therapy of a patient suffering from leukemias, disseminated multiple myelomas or lymphomas.

    摘要翻译: 本发明涉及用于在照射光时增强高量子产率产生和单线态氧的新型可光致发光罗丹明衍生物,同时保持罗丹明在正常癌细胞与癌细胞之间的期望差异保留,所述衍生物选自4,5- 二溴罗丹明123(2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸甲酯盐酸盐); 4,5-二溴罗丹明123(2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸乙酯盐酸盐); 4,5-二溴罗丹明123(2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸辛酯盐酸盐); 4,5-二溴罗丹明110正丁基酯(2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸正丁酯盐酸盐); 罗丹明B正丁酯(2-(6-乙基氨基-3-乙基亚氨基-3H-呫吨-9-基) - 苯甲酸正丁酯盐酸盐); 及其可光活化衍生物; 由此衍生物的光活化诱导细胞杀伤,而未活化的衍生物对细胞基本上无毒性。 此外,本发明涉及本发明的可光反应衍生物在癌症患者的光动力治疗中的用途,其通过破坏人类癌细胞,其中实现了衍生物的适当的细胞内水平并且适用于适当波长的光的照射 。 本发明还涉及一种患有白血病,弥散性多发性骨髓瘤或淋巴瘤的患者的光动力疗法的方法。