B ring reduced-D ring oxidized tetrapyrrolic photosensitizers for photodynamic therapy and tumor imaging
    1.
    发明授权
    B ring reduced-D ring oxidized tetrapyrrolic photosensitizers for photodynamic therapy and tumor imaging 有权
    B环还原-D环氧化四吡咯光敏剂用于光动力疗法和肿瘤成像

    公开(公告)号:US08679459B2

    公开(公告)日:2014-03-25

    申请号:US12918238

    申请日:2009-02-19

    CPC分类号: C07D487/22

    摘要: Tetrapyrrolic photosensitizers and imaging agent compounds having A, B, C, and D rings and having a reduced B ring and an oxidized D ring. The compounds preferably have a purity of at least 95 percent and preferably have a fused system connected at an unsaturated carbon atom of the C ring nearest the D ring and at the unsaturated carbon atom between the C and D rings. The invention also includes a method of making the compounds at over 95 percent yield by starting with a B and D ring oxidized tetrapyrollic compound and dissolving it in a halogenated hydrocarbon solvent and treating it with sufficient nitroalkane solution of FeCl36H2O to oxidize the D ring and separating the resulting organic layer and drying.

    摘要翻译: 具有A,B,C和D环的四吡咯类光敏剂和成像剂化合物,并具有还原的B环和氧化的D环。 化合物优选具有至少95%的纯度,并且优选具有在C环的最接近D环的不饱和碳原子和C和D环之间的不饱和碳原子连接的稠合体系。 本发明还包括通过用B和D环氧化的四元醇化合物开始制备化合物百分之九十五以上的方法,并将其溶解在卤代烃溶剂中,并用足够的FeCl 3·6H 2 O的硝基烷烃溶液处理以氧化D环并分离 所得有机层并干燥。

    B RING REDUCED-D RING OXIDIZED TETRAPYROLLIC PHOTOSENSITIZERS FOR PHOTODYNAMIC THERAPY AND TUMOR IMAGING
    2.
    发明申请
    B RING REDUCED-D RING OXIDIZED TETRAPYROLLIC PHOTOSENSITIZERS FOR PHOTODYNAMIC THERAPY AND TUMOR IMAGING 有权
    用于光化学治疗和肿瘤成像的B环减少D环氧化的光致变色光敏剂

    公开(公告)号:US20110264027A1

    公开(公告)日:2011-10-27

    申请号:US12918238

    申请日:2009-02-19

    CPC分类号: C07D487/22

    摘要: Tetrapyrollic photosensitizers and imaging agent compounds having A, B, C, and D rings and having a reduced B ring and an oxidized D ring. The compounds preferably have a purity of at least 95 percent and preferably have a fused system connected at an unsaturated carbon atom of the C ring nearest the D ring and at the unsaturated carbon atom between the C and D rings. The invention also includes a method of making the compounds at over 95 percent yield by starting with a B and D ring oxidized tetrapyrollic compound and dissolving it in a halogenated hydrocarbon solvent and treating it with sufficient nitroalkane solution of FeCl3.6H2O to oxidize the D ring and separating the resulting organic layer and drying.

    摘要翻译: 具有A,B,C和D环并且具有还原的B环和氧化的D环的四味光敏剂和显影剂化合物。 化合物优选具有至少95%的纯度,并且优选具有在C环的最接近D环的不饱和碳原子和C和D环之间的不饱和碳原子连接的稠合体系。 本发明还包括一种通过用B和D环氧化的四羰基化合物开始制备化合物超过95%的方法,并将其溶解在卤代烃溶剂中并用足量的FeCl 3·6H 2 O的硝基烷烃溶液处理以氧化D环 并分离得到的有机层并干燥。

    Water soluble tetrapyrollic photosensitizers for photodynamic therapy
    3.
    发明授权
    Water soluble tetrapyrollic photosensitizers for photodynamic therapy 失效
    用于光动力疗法的水溶性四光镜光敏剂

    公开(公告)号:US07501509B2

    公开(公告)日:2009-03-10

    申请号:US11452511

    申请日:2006-06-14

    IPC分类号: C07B47/00 C09D48/22

    摘要: A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a phamaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.

    摘要翻译: 具有至少一个-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2或-N(CH 2 COOH)2基团的四酯类光敏剂化合物或其酯,所述四元醇化合物是二氢卟酚,细菌二氢卟酚,卟啉,焦脱镁叶绿素,嘌呤酰亚胺或细菌嘌呤酰亚胺。 理想地,化合物具有下式:或其药学上可接受的衍生物,其中R 1 -R 8和R 10是各种取代基,R 9是取代或未取代的-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2; 或-N(CH 2 COOH)2。 本发明还包括通过光注射化合物后用光处理的光动力学治疗方法和注射化合物后通过荧光成像的方法。

    Water soluble tetrapyrollic photosensitizers for photodynamic therapy
    4.
    发明授权
    Water soluble tetrapyrollic photosensitizers for photodynamic therapy 有权
    用于光动力疗法的水溶性四光镜光敏剂

    公开(公告)号:US07820143B2

    公开(公告)日:2010-10-26

    申请号:US12378751

    申请日:2009-02-19

    IPC分类号: A61B5/055

    摘要: A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a pharmaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.

    摘要翻译: 具有至少一个-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2或-N(CH 2 COOH)2基团的四酯类光敏剂化合物或其酯,所述四元醇化合物是二氢卟酚,细菌二氢卟酚,卟啉,焦脱镁叶绿素,嘌呤酰亚胺或细菌嘌呤酰亚胺。 理想地,化合物具有下式:或其药学上可接受的衍生物,其中R 1 -R 8和R 10是各种取代基,R 9是取代或未取代的-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2; 或-N(CH 2 COOH)2。 本发明还包括通过光注射化合物后用光处理的光动力学治疗方法和注射化合物后通过荧光成像的方法。

    WATER SOLUBLE TETRAPYROLLIC PHOTOSENSITIZERS FOR PHOTODYNAMIC THERAPY
    5.
    发明申请
    WATER SOLUBLE TETRAPYROLLIC PHOTOSENSITIZERS FOR PHOTODYNAMIC THERAPY 审中-公开
    水溶性光敏光敏剂光解动力疗法

    公开(公告)号:US20110091390A1

    公开(公告)日:2011-04-21

    申请号:US12912033

    申请日:2010-10-26

    IPC分类号: A61K49/00 A61P35/00

    摘要: A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a pharmaceutically acceptable derivative thereof, wherein R1—R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.

    摘要翻译: 具有至少一个-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2或-N(CH 2 COOH)2基团的四酯类光敏剂化合物或其酯,所述四元醇化合物是二氢卟酚,细菌二氢卟酚,卟啉,焦脱镁叶绿素,嘌呤酰亚胺或细菌嘌呤酰亚胺。 理想地,化合物具有下式:或其药学上可接受的衍生物,其中R 1 -R 8和R 10是各种取代基,R 9是取代或未取代的-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2; 或-N(CH 2 COOH)2。 本发明还包括通过光注射化合物后用光处理的光动力学治疗方法和注射化合物后通过荧光成像的方法。

    Water soluble tetrapyrollic photosensitizers for photodynamic therapy
    6.
    发明申请
    Water soluble tetrapyrollic photosensitizers for photodynamic therapy 有权
    用于光动力疗法的水溶性四光镜光敏剂

    公开(公告)号:US20090162289A1

    公开(公告)日:2009-06-25

    申请号:US12378751

    申请日:2009-02-19

    摘要: A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a pharmaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.

    摘要翻译: 具有至少一个-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2或-N(CH 2 COOH)2基团的四酯类光敏剂化合物或其酯,所述四元醇化合物是二氢卟酚,细菌二氢卟酚,卟啉,焦脱镁叶绿素,嘌呤酰亚胺或细菌嘌呤酰亚胺。 理想地,化合物具有下式:或其药学上可接受的衍生物,其中R 1 -R 8和R 10是各种取代基,R 9是取代或未取代的-CH 2 CH 2 CON(CH 2 CON(CH 2 COOH)2)2; 或-N(CH 2 COOH)2。 本发明还包括通过光注射化合物后用光处理的光动力学治疗方法和注射化合物后通过荧光成像的方法。

    Adduct of fluorescent dye and tumor avid tetrapyrrole
    7.
    发明授权
    Adduct of fluorescent dye and tumor avid tetrapyrrole 有权
    荧光染料和肿瘤病毒四吡咯的加合物

    公开(公告)号:US07947729B2

    公开(公告)日:2011-05-24

    申请号:US11632433

    申请日:2005-07-13

    IPC分类号: C07B47/00 C07D487/22

    摘要: A compound having preferential localization in tumor tissue relative to normal tissue, a preferential electromagnetic absorption at a wavelength between about 660 and 900 nm, and a fluorescence at a wavelength shifted from the preferential absorption by at least +30 nm and preferably at least +50 nm. The compound further preferably destroys tumor tissue in which it is absorbed when exposed to light at its preferential absorption wavelength. In a preferred embodiment of the invention, the compound is a conjugate of a tumor avid tetrapyrrole compound with a fluorescent dye, and more preferably the fluorescent dye is an indocyanine dye such as indocyanine green. The tumor avid tetrapyrrole compound is preferably a porphyrin derivative selected from the group consisting of chlorins, bacteriochlorins, purpurins and derivatives thereof.

    摘要翻译: 相对于正常组织在肿瘤组织中优先定位的化合物,在约660和900nm之间的波长处的优先电磁吸收以及波长从优选吸收偏移至少±30nm,优选至少+50nm的荧光 nm。 该化合物进一步优选地破坏在其优先吸收波长下暴露于光时被吸收的肿瘤组织。 在本发明的一个优选实施方案中,化合物是肿瘤病毒四吡咯化合物与荧光染料的缀合物,更优选荧光染料是吲哚菁染料,如吲哚菁绿。 肿瘤病毒四吡咯化合物优选为选自二卟啉,细菌二氢卟酚,紫草素及其衍生物的卟啉衍生物。

    ADDUCT OF FLUORESCENT DYE AND TUMOR AVID TETRAPYRROLE
    8.
    发明申请
    ADDUCT OF FLUORESCENT DYE AND TUMOR AVID TETRAPYRROLE 有权
    荧光染色和肿瘤血小板衍生物的添加

    公开(公告)号:US20090043090A1

    公开(公告)日:2009-02-12

    申请号:US11632433

    申请日:2005-07-13

    IPC分类号: C09B47/00 C09B47/04

    摘要: A compound having preferential localization in tumor tissue relative to normal tissue, a preferential electromagnetic absorption at a wavelength between about 660 and 900 nm, and a fluorescence at a wavelength shifted from the preferential absorption by at least +30 nm and preferably at least +50 nm. The compound further preferably destroys tumor tissue in which it is absorbed when exposed to light at its preferential absorption wavelength. In a preferred embodiment of the invention, the compound is a conjugate of a tumor avid tetrapyrrole compound with a fluorescent dye, and more preferably the fluorescent dye is an indocyanine dye such as indocyanine green. The tumor avid tetrapyrrole compound is preferably a porphyrin derivative selected from the group consisting of chlorins, bacteriochlorins, purpurins and derivatives thereof.

    摘要翻译: 相对于正常组织在肿瘤组织中优先定位的化合物,在约660和900nm之间的波长处的优先电磁吸收以及波长从优选吸收偏移至少±30nm,优选至少+50nm的荧光 nm。 该化合物进一步优选地破坏在其优先吸收波长下暴露于光时被吸收的肿瘤组织。 在本发明的一个优选实施方案中,化合物是肿瘤病毒四吡咯化合物与荧光染料的缀合物,更优选荧光染料是吲哚菁染料,如吲哚菁绿。 肿瘤病毒四吡咯化合物优选为选自二卟啉,细菌二氢卟酚,紫草素及其衍生物的卟啉衍生物。

    Water soluble tetrapyrollic photosensitizers for photodynamic therapy
    9.
    发明申请
    Water soluble tetrapyrollic photosensitizers for photodynamic therapy 失效
    用于光动力疗法的水溶性四光镜光敏剂

    公开(公告)号:US20070149497A1

    公开(公告)日:2007-06-28

    申请号:US11452511

    申请日:2006-06-14

    摘要: A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a pharmaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.

    摘要翻译: 具有至少一个侧基-CH 2 CH 2 CON(CH 2 CH 2)(CH 2)2 CH 3的四级光敏剂化合物, COOH)2)2或-N(CH 2 COOH)2个基团或其酯,所述四酯化合物为 二氢卟酚,细菌二氢卟酚,卟啉,焦脱镁叶绿素,紫苏酰亚胺或细菌草甘膦酰亚胺。 该化合物具有下式:或其药学上可接受的衍生物,其中R 1 -R 8和R 10是各种取代基, 取代或未取代的-CH 2 CH 2 CON(CH 2 CH 2 CON(CH 2)2 CH 2) 2 CO 2)2)2

    Focal plane array mount for a fiber optic detector system and related
method of assembly
    10.
    发明授权
    Focal plane array mount for a fiber optic detector system and related method of assembly 失效
    用于光纤检测器系统的焦平面阵列安装和相关的组装方法

    公开(公告)号:US5337389A

    公开(公告)日:1994-08-09

    申请号:US69811

    申请日:1993-06-01

    IPC分类号: G02B6/36 G02B6/42

    CPC分类号: G02B6/3624

    摘要: A mount for supporting a silicon v-groove array that contains delicate opal fibers. Optical fibers are arranged in a planar silicon v-groove array to form a focal plane array, which is connected to a first L-bracket. The focal plane array and the first L-bracket combination are attached to a second L-bracket via a shock/vibration isolation pad. The second L-bracket includes an extended cylinder which is threaded so that a strain relief can be screwed directly into the second L-bracket and the fibers extending out the first L-bracket can be fed through the second L-bracket and directly into a monocoil. The second L-bracket also includes space to attach front, side and top covers over the focal plane array. In a related method, the silicon v-groove array is epoxied to the first L-bracket. After preparation of the focal plane array, e.g. polishing of the fibers, is completed, the focal plane array/first bracket combination is connected to the second L-bracket, with the pad therebetween. The covers are then attached to the L-bracket.

    摘要翻译: 用于支撑包含精细光纤的硅V形槽阵列的支架。 光纤布置在平面硅V型槽阵列中以形成连接到第一L型支架的焦平面阵列。 焦平面阵列和第一L形支架组合通过冲击/振动隔离垫连接到第二L支架。 第二个L形托架包括一个延伸的圆柱体,该圆柱体是螺纹的,使得应变消除件可以直接拧入到第二个L形支架中,而从第一个L形托架伸出的纤维可以通过第二个L形支架进给,并直接进入 单油 第二个L形支架还包括在焦平面阵列上安装前,侧和顶盖的空间。 在相关方法中,将硅V型槽阵列环氧化为第一L型支架。 在准备焦平面阵列之后,例如, 光纤的抛光完成后,焦平面阵列/第一支架组合连接到第二L形支架,垫片在其间。 然后将盖子连接到L型支架上。