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    B RING REDUCED-D RING OXIDIZED TETRAPYROLLIC PHOTOSENSITIZERS FOR PHOTODYNAMIC THERAPY AND TUMOR IMAGING
    42.
    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

    Applicant: Ravindra K. Pandey ,  Chao Liu ,  Mahabeer Dobhal ,  William Potter ,  Janet Morgan ,  Allan Oseroff ,  Stephanie Pincus

    Inventor： Ravindra K. Pandey ,  Chao Liu ,  Mahabeer Dobhal ,  William Potter ,  Janet Morgan ,  Allan Oseroff ,  Stephanie Pincus

    IPC: A61N5/00 ,  A61P35/00 ,  A61K51/04 ,  A61K49/00 ,  C07D487/22 ,  A61K49/04

    CPC classification number: C07D487/22

    Abstract: 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.

    Abstract translation: 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。

    Multi DTPA conjugated tetrapyrollic compounds for phototherapeutic contrast agents
    43.
    发明授权
    Multi DTPA conjugated tetrapyrollic compounds for phototherapeutic contrast agents 有权
    用于光疗治疗造影剂的多DTPA共轭四氢化合物

    公开(公告)号：US07897140B2

    公开(公告)日：2011-03-01

    申请号：US11479524

    申请日：2006-06-30

    Applicant: Ravindra K. Pandey ,  Lalit Goswami ,  Joseph Spernyak ,  Peter Kanter ,  Richard Mazurchuk

    Inventor： Ravindra K. Pandey ,  Lalit Goswami ,  Joseph Spernyak ,  Peter Kanter ,  Richard Mazurchuk

    IPC: A61K5/055

    CPC classification number: C07D487/22 ,  A61K41/0071 ,  A61K41/0076 ,  A61K49/124

    Abstract: Novel tetrapyrollic water soluble photosensitizing and imaging compounds and the methods of treating and imaging hyperproliferative tissue, e.g. tumors and hypervacularized tissue such as found in macular degeneration. Broadly, the compounds are tetrapyrollic photosensitizer compounds where the tetrapyrollic compound is a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide having 3 to 6 —CH2CONHphenylCH2CH(N(CH2COOH)2))(CH2N(CH2COOH)(CH2CH2N(CH2COOH)2)) groups or esters thereof or complexes thereof with gadolinium(III).

    Abstract translation: 新型四级水溶性光敏剂和成像化合物以及治疗和成像过度增生组织的方法，例如， 肿瘤和高血压组织，如发现于黄斑变性。 广泛地说，这些化合物是四级光敏剂化合物，其中四溴化合物是二氢卟酚，细菌二氢卟酚，卟啉，焦脱镁叶绿素，嘌呤酰亚胺或具有3至6个-CH 2 CONH苯基CH 2 CH（N（CH 2 COOH）2））（CH 2 CO 2）（CH 2 CH 2 N（CH 2 COOH） 2））或其酯或其与钆（III）的络合物。

    Porphyrin-based compounds for tumor imaging and photodynamic therapy
    44.
    发明申请
    Porphyrin-based compounds for tumor imaging and photodynamic therapy 有权
    卟啉基化合物用于肿瘤成像和光动力学治疗

    公开(公告)号：US20100184970A1

    公开(公告)日：2010-07-22

    申请号：US12462535

    申请日：2009-08-05

    Applicant: Ravindra K. Pandey ,  Munawwar Sajjad ,  Suresh Pandey ,  Amy Gryshuk ,  Allan Oseroff ,  Hani A. Nabi ,  Stephanie Pincus

    Inventor： Ravindra K. Pandey ,  Munawwar Sajjad ,  Suresh Pandey ,  Amy Gryshuk ,  Allan Oseroff ,  Hani A. Nabi ,  Stephanie Pincus

    IPC: C07D487/22

    CPC classification number: C07D487/22 ,  A61K51/0485 ,  C07H17/02

    Abstract: 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.

    Abstract translation: 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124I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
    45.
    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

    Applicant: Ravindra K. Pandey ,  Amy Gryshuk ,  Lalit Goswami ,  William Potter ,  Allan Oseroff

    Inventor： Ravindra K. Pandey ,  Amy Gryshuk ,  Lalit Goswami ,  William Potter ,  Allan Oseroff

    IPC: C07B47/00 ,  C09D48/22

    CPC classification number: C07D471/22 ,  A61K41/0071 ,  A61K41/0076 ,  C09B47/00 ,  C09B69/108

    Abstract: 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.

    Abstract translation: 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。

    Nanoparticles for two-photon activated photodynamic therapy and imaging
    46.
    发明申请
    Nanoparticles for two-photon activated photodynamic therapy and imaging 审中-公开
    纳米粒子用于双光子激活光动力治疗和成像

    公开(公告)号：US20090035576A1

    公开(公告)日：2009-02-05

    申请号：US11900334

    申请日：2007-09-10

    Applicant: Paras N. Prasad ,  Sehoon Kim ,  Tymish Y. Ohulchanskyy ,  Ravindra K. Pandey

    Inventor： Paras N. Prasad ,  Sehoon Kim ,  Tymish Y. Ohulchanskyy ,  Ravindra K. Pandey

    IPC: B32B5/16

    CPC classification number: A61K41/0071 ,  A61K41/008 ,  A61K49/0021 ,  A61K49/0093 ,  C01B33/141 ,  G01N33/582 ,  G01N33/585 ,  Y10T428/2982

    Abstract: The present invention provides organically modified silica (ORMOSIL) nanoparticles into which have been incorporated two-photon absorption dye molecules. The two photon absorption dye displays a unique aggregation induced fluorescence enhancement behavior. As a result ORMOSIL nanoparticles with high amounts of the dye can be prepared. These particles can be used for imaging. In one embodiment, the nanoparticles can additionally have incorporated therein a photosensitizer. The photosensitzer can be activated by intraparticle fluorescence resonance energy transfer (FRET) from the dye aggregates resulting in enhanced fluorescence and singlet oxygen generation from photosensitizer under two-photon excitation conditions. Such nanoparticles can be used for photodynamic therapy applications.

    Abstract translation: 本发明提供了已经掺入双光子吸收染料分子的有机改性二氧化硅（ORMOSIL）纳米颗粒。 两个光子吸收染料显示出独特的聚集诱导的荧光增强行为。 因此，可以制备具有大量染料的ORMOSIL纳米颗粒。 这些颗粒可用于成像。 在一个实施方案中，纳米颗粒另外可以掺入光敏剂。 光敏剂可以通过来自染料聚集体的颗粒内荧光共振能量转移（FRET）来激活，从而在双光子激发条件下从光敏剂产生增强的荧光和单线态氧产生。 这种纳米颗粒可用于光动力疗法应用。

    Nanoparticles for two-photon activated photodynamic therapy and imaging
    47.
    发明申请
    Nanoparticles for two-photon activated photodynamic therapy and imaging 审中-公开
    纳米粒子用于双光子激活光动力治疗和成像

    公开(公告)号：US20080233051A1

    公开(公告)日：2008-09-25

    申请号：US11983845

    申请日：2007-11-13

    Applicant: Paras N. Prasad ,  Sehoon Kim ,  Tymish Y. Ohulchanskyy ,  Ravindra K. Pandey

    Inventor： Paras N. Prasad ,  Sehoon Kim ,  Tymish Y. Ohulchanskyy ,  Ravindra K. Pandey

    IPC: A61K9/14 ,  A61K31/695 ,  A61K49/00

    CPC classification number: A61K31/695 ,  A61K41/0071 ,  A61K41/008 ,  A61K49/0021 ,  A61K49/0093

    Abstract: The present invention provides organically modified silica (ORMOSIL) nanoparticles into which have been incorporated two-photon absorption dye molecules. The two photon absorption dye displays a unique aggregation induced fluorescence enhancement behavior. As a result ORMOSIL nanoparticles with high amounts of the dye can be prepared. These particles can be used for imaging. In one embodiment, the nanoparticles can additionally have incorporated therein a photosensitizer. The photosensitizer can be activated by intraparticle fluorescence resonance energy transfer (FRET) from the dye aggregates resulting in enhanced fluorescence and singlet oxygen generation from photosensitizer under two-photon excitation conditions. Such nanoparticles can be used for photodynamic therapy applications.

    Abstract translation: 本发明提供了已经掺入双光子吸收染料分子的有机改性二氧化硅（ORMOSIL）纳米颗粒。 两个光子吸收染料显示出独特的聚集诱导的荧光增强行为。 因此，可以制备具有大量染料的ORMOSIL纳米颗粒。 这些颗粒可用于成像。 在一个实施方案中，纳米颗粒另外可以掺入光敏剂。 可以通过来自染料聚集体的颗粒内荧光共振能量转移（FRET）来激活光敏剂，从而在双光子激发条件下从光敏剂产生增强的荧光和单线态氧产生。 这种纳米颗粒可用于光动力疗法应用。

    B ring reduced-D ring oxidized tetrapyrrolic photosensitizers for photodynamic therapy and tumor imaging
    49.
    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

    Applicant: Ravindra K. Pandey ,  Chao Liu ,  Mahabeer Dobhal ,  William Potter ,  Janet Morgan ,  Stephanie Pincus

    Inventor： Ravindra K. Pandey ,  Chao Liu ,  Mahabeer Dobhal ,  William Potter ,  Janet Morgan ,  Allan Oseroff

    IPC: A61B5/055 ,  C07B47/00 ,  C07D487/22

    CPC classification number: C07D487/22

    Abstract: 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.

    Abstract translation: 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。

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