公开(公告)号：US20080032939A1

公开(公告)日：2008-02-07

申请号：US11901113

申请日：2007-09-13

申请人： Ravindra Pandey ,  Mahabeer Dobhal ,  Andrew Graham ,  Allan Oseroff

发明人： Ravindra Pandey ,  Mahabeer Dobhal ,  Andrew Graham ,  Allan Oseroff

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。

公开(公告)号：US20050222053A1

公开(公告)日：2005-10-06

申请号：US10975312

申请日：2004-10-28

申请人： Ravindra Pandey ,  Mahabeer Dobhal ,  Andrew Graham ,  Allan Oseroff

发明人： Ravindra Pandey ,  Mahabeer Dobhal ,  Andrew Graham ,  Allan Oseroff

IPC分类号： A61K31/70 ,  A61K31/704 ,  A61K36/24 ,  C07H15/24

CPC分类号： A61K31/70 ,  A61K31/704 ,  A61K36/24 ,  C07H15/24

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。

公开(公告)号：US20070134340A1

公开(公告)日：2007-06-14

申请号：US11471075

申请日：2006-06-20

申请人： Paras Prasad ,  Haridas Pudavar ,  Koichi Baba ,  Indrajit Roy ,  Tymish Ohulchanskyy ,  Ravindra Pandey ,  Allan Oseroff

发明人： Paras Prasad ,  Haridas Pudavar ,  Koichi Baba ,  Indrajit Roy ,  Tymish Ohulchanskyy ,  Ravindra Pandey ,  Allan Oseroff

IPC分类号： A61K31/555 ,  A61K31/409 ,  A61K9/14

CPC分类号： A61K9/14 ,  A61K9/146 ,  A61K31/409 ,  A61K31/4745 ,  A61K31/555 ,  A61K49/0021 ,  A61K49/0032 ,  A61K49/0036 ,  A61K49/0054 ,  A61K49/0067 ,  G01N33/5005 ,  G01N33/52

摘要： This invention provides nanocrystals or polymer doped nanocrystals of hydrophobic drug molecules as stably dispersed in an aqueous system which are prepared without stabilizers like surfactants and the like. In one embodiment, the drug is a tetra-pyrrole compound. An example is the hydrophobic photosensitizing anticancer drug 2-devinyl-2-(1-hexyloxyethyl)pyropheophorbide (HPPH). Pharmaceutical compositions comprising nanocrystals or polymer doped nanocrystals of hydrophobic drugs can be used for therapeutic purposes. For example pyropheophorbides such as HPPH can be used for photodynamic therapy. Drug efficacy of these nanocrystals were found to be comparable with that of same drug formulated in conventional delivery vehicles under in vitro and in vivo conditions.

摘要翻译： 本发明提供了稳定分散在水性体系中的疏水药物分子的纳米晶体或聚合物掺杂的纳米晶体，其不经过稳定剂如表面活性剂等制备。 在一个实施方案中，药物是四吡咯化合物。 一个例子是疏水性光敏抗癌药2-脱乙烯基-2-（1-己氧基乙基）焦脱镁叶绿素（HPPH）。 包含纳米晶体或疏水性药物的聚合物掺杂纳米晶体的药物组合物可用于治疗目的。 例如焦磷偏磷酸盐如HPPH可用于光动力疗法。 发现这些纳米晶体的药物效力与在体外和体内条件下在常规递送载体中配制的相同药物相当。

公开(公告)号：US20060198783A1

公开(公告)日：2006-09-07

申请号：US11353626

申请日：2006-02-14

申请人： Ravindra Pandey ,  Munawwar Sajjad ,  Suresh Pandey ,  Amy Gryshuk ,  Allan Oseroff ,  Hani Nabi

发明人： Ravindra Pandey ,  Munawwar Sajjad ,  Suresh Pandey ,  Amy Gryshuk ,  Allan Oseroff ,  Hani Nabi

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

CPC分类号： A61K51/0485 ,  C07D487/22 ,  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。

公开(公告)号：US20070149497A1

公开(公告)日：2007-06-28

申请号：US11452511

申请日：2006-06-14

申请人： Ravindra Pandey ,  Amy Gryshuk ,  Lalit Goswami ,  William Potter ,  Allan Oseroff

发明人： Ravindra Pandey ,  Amy Gryshuk ,  Lalit Goswami ,  William Potter ,  Allan Oseroff

IPC分类号： A61K31/555 ,  C07D487/22 ,  A61K31/409

CPC分类号： C07D471/22 ,  A61K41/0071 ,  A61K41/0076 ,  C09B47/00 ,  C09B69/108

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

公开(公告)号：US20060111565A1

公开(公告)日：2006-05-25

申请号：US11066511

申请日：2005-02-25

申请人： Ravindra Pandey ,  Andrei Kozyrev ,  Xiang Zheng

发明人： Ravindra Pandey ,  Andrei Kozyrev ,  Xiang Zheng

IPC分类号： C07D487/22

CPC分类号： C07D487/22

摘要： A compound having the structural formula: where R is H or lower alkyl of 1 through 12 carbon atoms. In general, the compounds of the invention are 132-Oxo-bacteriopyropheophorbide-a carboxylic acid and C1-C12 alkyl esters thereof. A method for the preparation of the carboxylic acid compounds of the invention includes the step of reacting bacteriopyropheophorbide-a alkyl ester with lithium hydroxide in tetrahydrofuran and water. A method of the invention for the preparation of the C1-C12 alkyl ester compounds of the invention includes the steps of reacting bacteriopyropheophorbide-a alkyl, especially methyl, ester with lithium hydroxide in tetrahydrofuran and water to obtain 132-Oxo-bacterio-pyropheophobide-a carboxylic acid followed by reacting the carboxylic acid with an acid chloride producing reagent to obtain the 132-Oxo-bacterio pyropheophobide-a acid chloride (compound 5) and reacting the 132-Oxo-bacterio pyropheophobide-a acid chloride with a C1-C12 alcohol to obtain a 132-Oxo-bacterio-pyropheophobide-a carboxylic acid C1-C12 alkyl ester (compound 6). The compounds of the invention may be used as long wavelength absorbing photosensitizers for photodynamic therapy.

摘要翻译： 具有以下结构式的化合物：其中R是H或1至12个碳原子的低级烷基。 一般而言，本发明的化合物是其中一个羧酸和一个C 1 -C 12烷基酯的十二烷基氧杂菌素。 制备本发明的羧酸化合物的方法包括使烷基酯与氢氧化锂在四氢呋喃和水中反应的步骤。 本发明的制备本发明的C 12 -C 12烷基酯化合物的方法包括以下步骤：使抑制甜菜碱 - 烷基，特别是甲基酯与 氢氧化锂在四氢呋喃和水中的溶液，得到13β-氧代 - 焦磷酸酯 - 羧酸，随后将羧酸与产生酰基氯的试剂反应，得到13重量％ > - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - > 12醇，得到13β-氧代 - 焦磷酸酯 - 羧酸C 1 -C 12烷基酯 （化合物6）。 本发明的化合物可用作光动力疗法的长波吸收光敏剂。

公开(公告)号：US20070053840A1

公开(公告)日：2007-03-08

申请号：US11479524

申请日：2006-06-30

申请人： Ravindra Pandey ,  Lalit Goswami ,  Joseph Spernyak ,  Peter Kanter ,  Richard Mazurchuk

发明人： Ravindra Pandey ,  Lalit Goswami ,  Joseph Spernyak ,  Peter Kanter ,  Richard Mazurchuk

IPC分类号： A61K49/10 ,  C07F5/00 ,  C07D487/22

CPC分类号： C07D487/22 ,  A61K41/0071 ,  A61K41/0076 ,  A61K49/124

摘要： 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).

摘要翻译： 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苯基CH 2 CH 2的细菌嘌呤酰亚胺 （N（CH 2 COOH）2））（CH 2 N（CH 2 COOH）（CH 3） （CH 2 CO 2）2）其基团或其与钆（III）的络合物 ）。

公开(公告)号：US20060204437A1

公开(公告)日：2006-09-14

申请号：US11431275

申请日：2006-05-10

申请人： Ravindra Pandey ,  Zachary Grossman ,  Peter Kanter ,  Thomas Dougherty

发明人： Ravindra Pandey ,  Zachary Grossman ,  Peter Kanter ,  Thomas Dougherty

IPC分类号： A61K51/00 ,  C07F13/00 ,  C07F5/00 ,  C07D487/22 ,  A61K31/555 ,  A61K49/12

CPC分类号： A61K51/0485 ,  A61K41/0071 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/10 ,  A61K51/0478 ,  C07D471/22 ,  C07D487/22

摘要： A compound comprising a chemical combination of a photodynamic tetra-pyrrolic compound with a plurality of radionuclide element atoms such that the compound may be used to enhance MR imaging and also be used as a photodynamic compound for use in photodynamic therapy to treat hyperproliferative tissue. The preferred compounds have the structural formula: where R1, R2, R2a R3, R3a R4, R5, R5a R6, R7, R7a, and R8 cumulatively contain at least two functional groups that will complex or combine with an MR imaging enhancing element or ion. The compound is intended to include such complexes and combinations and includes the use of such compounds for MR imaging and photodynamic therapy treatment of tumors and other hyperproliferative tissue.