Iridoid-saccharide compound and method of using same
    2.
    发明申请
    Iridoid-saccharide compound and method of using same 审中-公开
    吡啶糖类化合物及其使用方法

    公开(公告)号:US20080032939A1

    公开(公告)日:2008-02-07

    申请号:US11901113

    申请日:2007-09-13

    IPC分类号: A61K31/7048 A61P35/00

    CPC分类号: A61K31/7048

    摘要: A method for treatment of hyperproliferative tissue which by exposing the hyperproliferative tissue to a sufficient quantity of a purified iridoid compound to inhibit its growth, where the iridoid compound includes a polysubstituted cyclopenta(c)dihydropyran where the cyclopenta ring is substituted at its 2′ position with a ketofuryl group, where the numbering of the fused cyclopenta(c)dihydropyran ring structure includes heterocyclic oxygen, is counterclockwise and begins at the first carbon atom counterclockwise from the cyclopenta ring so that oxygen is in the 2 position in the pyran ring. The invention also includes the mouse iridoid compounds.

    摘要翻译: 一种用于治疗过度增殖组织的方法,其通过将过度增殖组织暴露于足量的纯化环烯醚萜类化合物以抑制其生长,其中环烯醚萜烯化合物包括多环取代的环戊二烯(c)二氢吡喃,其中环戊环在其2'位置被取代 其中稠合环戊二烯(c)二氢吡喃环结构的编号包括杂环氧的酮基呋喃基是逆时针方向,并且从环戊环逆时针开始于第一碳原子,使得氧在吡喃环中位于2位。 本发明还包括小鼠环烯醚萜类化合物。

    Porphyrin-based compounds for tumor imaging and photodynamic therapy
    3.
    发明申请
    Porphyrin-based compounds for tumor imaging and photodynamic therapy 审中-公开
    卟啉基化合物用于肿瘤成像和光动力学治疗

    公开(公告)号:US20060198783A1

    公开(公告)日:2006-09-07

    申请号:US11353626

    申请日:2006-02-14

    IPC分类号: A61K51/00 A61M36/14 C07H17/02

    摘要: This invention describes a first report on the synthesis of certain 124I-labelled photosensitizers related to chlorines and bacteriochlorins with long wavelength absorption in the range of 660-800 nm. In preliminary studies, these compounds show a great potential for tumor detection by positron emission tomography (PET) and treatment by photodynamic therapy (PDT). The development of tumor imaging or improved photodynamic therapy agent(s) itself represent an important step, but a dual function agent (PET imaging and PDT) provides the potential for diagnostic body scan followed by targeted therapy.

    摘要翻译: 本发明描述了关于在660-800nm范围内具有长波长吸收的氯和细菌二氢红素相关的某些124 I-标记的光敏剂的合成的第一报告。 在初步研究中,这些化合物通过正电子发射断层扫描(PET)和光动力学治疗(PDT)治疗显示出巨大的潜力。 肿瘤成像或改进的光动力治疗剂本身的发展本身就是重要的一步,但双重功能试剂(PET成像和PDT)提供诊断身体扫描的潜力,然后进行靶向治疗。

    Water soluble tetrapyrollic photosensitizers for photodynamic therapy
    4.
    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

    Iridoid-saccharide compound and method of using same
    5.
    发明申请
    Iridoid-saccharide compound and method of using same 审中-公开
    吡啶糖类化合物及其使用方法

    公开(公告)号:US20050222053A1

    公开(公告)日:2005-10-06

    申请号:US10975312

    申请日:2004-10-28

    摘要: A method for treatment of hyperproliferative tissue which by exposing the hyperproliferative tissue to a sufficient quantity of a purified iridoid compound to inhibit its growth, where the iridoid compound includes a polysubstituted cyclopenta(c)dihydropyran where the cyclopenta ring is substituted at its 2′ position with a ketofuryl group, where the numbering of the fused cyclopenta(c)dihydropyran ring structure includes heterocyclic oxygen, is counterclockwise and begins at the first carbon atom counterclockwise from the cyclopenta ring so that oxygen is in the 2 position in the pyran ring. The invention also includes the mouse iridoid compounds.

    摘要翻译: 一种用于治疗过度增殖组织的方法,其通过将过度增殖组织暴露于足量的纯化环烯醚萜类化合物以抑制其生长,其中环烯醚萜烯化合物包括多环取代的环戊二烯(c)二氢吡喃,其中环戊环在其2'位置被取代 其中稠合环戊二烯(c)二氢吡喃环结构的编号包括杂环氧的酮基呋喃基是逆时针方向,并且从环戊环逆时针开始于第一碳原子,使得氧在吡喃环中位于2位。 本发明还包括小鼠环烯醚萜类化合物。

    MULTIMODALITY AGENTS FOR TUMOR IMAGING AND THERAPY
    6.
    发明申请
    MULTIMODALITY AGENTS FOR TUMOR IMAGING AND THERAPY 审中-公开
    用于肿瘤成像和治疗的多功能剂

    公开(公告)号:US20110223102A1

    公开(公告)日:2011-09-15

    申请号:US12677381

    申请日:2008-09-11

    摘要: A compound that is a conjugate of an antagonist to an integrin expressed by a tumor cell and at least one of a tumor avid tetrapyrollic photosensitizer, a fluorescent dye, and a radioisotope labeled moiety wherein the radioisotope is 11C, 18F, 64Cu, 124I, 99Tc, 111In or GdIII and its method of use for diagnosing, imaging and/or treating hyperproliferative tissue such as tumors. Preferably the photosensitizer is a tumor avid tetrapyrollic photosensitizer, e.g. a porphyrin, chlorin or bacteriochlorin, e.g. pheophorbides and pyropheophorbides. Such conjugates have extreme tumor avidity and can be used to inhibit or completely destroy the tumor by light absoption. The integrin is usually αvβ3, α5β1, αvβ5, α4β1, or α2β1. Preferably, the antagonist is an RGD peptide or another antagonist that may be synthetic such as a 4-{2-(3,4,5,6-tetra-hydropyrimidin-2-ylamino)ethyloxy}-benzoyl]amino-2-(S)-amino-ethyl-sulfonylamino group. Such compounds provide tumor avidity and imaging ability thus permitting selective and clear tumor imaging.

    摘要翻译: 作为拮抗剂与由肿瘤细胞表达的整联蛋白结合的化合物,以及至少一种肿瘤病毒四级光敏剂,荧光染料和放射性同位素标记部分,其中放射性同位素为11C,18F,64Cu,124I,99Tc ,111In或GdIII及其用于诊断,成像和/或治疗过度增生组织如肿瘤的方法。 优选地,光敏剂是肿瘤急性四分光敏光敏剂,例如。 卟啉,二氢卟酚或细菌二氢卟酚。 脱镁叶绿素和焦偏镁偏磷酸盐。 这种缀合物具有极端的肿瘤亲合力,可用于通过光吸收抑制或完全破坏肿瘤。 整合素通常为αv&bgr; 3,α5和bgr; 1,αv&bgr; 5,α4和bgr; 1或α2和bgr; 1。 优选地,拮抗剂是可以是合成的RGD肽或另一种拮抗剂,例如4- {2-(3,4,5,6-四 - 嘧啶-2-基氨基)乙氧基} - 苯甲酰基]氨基-2-( S) - 氨基 - 乙基 - 磺酰基氨基。 这样的化合物提供了肿瘤亲合力和成像能力,从而允许选择性和清晰的肿瘤成像。

    Water soluble tetrapyrollic photosensitizers for photodynamic therapy
    7.
    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。

    Adduct of fluorescent dye and tumor avid tetrapyrrole
    10.
    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。