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1. 发明授权

US5498710A Alkyl ether analogues of benzoporphyrin derivatives 失效
标题翻译：苯并卟啉衍生物的烷基醚类似物
公开(公告)号：US5498710A
公开(公告)日：1996-03-12
申请号：US231113
申请日：1994-04-22
申请人： Ravindra K. Pandey , Thomas J. Dougherty , Kevin M. Smith , Isabelle Meunier
发明人： Ravindra K. Pandey , Thomas J. Dougherty , Kevin M. Smith , Isabelle Meunier
IPC分类号： C07D487/22
CPC分类号： C07D487/22
摘要： Compounds having properties superior to known photosensitizers defined by the following chemical formula: ##STR1## including R groups R.sup.1, R.sup.2, R.sup.3, and R.sup.4, wherein R.sup.1 and R.sup.2 are methyl or --CH(O--(CH.sub.2).sub.n CH.sub.3)CH.sub.3 or are joined together to form the group D and wherein R.sup.3 and R.sup.4 are methyl or --CH(O--(CH.sub.2).sub.n CH.sub.3)CH.sub.3 or are joined together to form the group D; provided that one of R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 are joined together to form the group D wherein one of the remaining R groups is methyl and one of the remaining R groups is --CH(O--(CH.sub.2).sub.n CH.sub.3)CH.sub.3, where n is an integer of 5 through 7 and group D is: ##STR2## and R.sub.5 is independently at each occurrence --OR.sub.6 where R.sub.6 is lower alkyl of 1 through 7 carbon atoms or R.sub.6 is an amino acid residue.
摘要翻译：具有优于以下化学式定义的已知光敏剂的性质的化合物：包括R基团R 1，R 2，R 3和R 4的其中R 1和R 2是甲基或-CH（O-（CH 2）n CH 3）一起形成基团D，其中R 3和R 4是甲基或-CH（O-（CH 2）n CH 3）CH 3或连接在一起形成基团D; 条件是R 1和R 2或R 3和R 4中的一个连接在一起形成基团D，其中剩余的R基团之一是甲基，其余的R基团之一是-CH（O-（CH 2）n CH 3）CH 3，其中n 是5〜7的整数，D为：＆lt; IMAGE＆gt; R5各自独立地为-OR 6，其中R 6为1〜7个碳原子的低级烷基或者R6为氨基酸残基。

2. 发明授权

US5506255A Rhodoporphyrin and phylloerythrin related photosensitizers for photodynamic therapy 失效
标题翻译：铑卟啉和叶绿素相关光敏剂用于光动力疗法
公开(公告)号：US5506255A
公开(公告)日：1996-04-09
申请号：US160384
申请日：1993-12-01
申请人： Kevin M. Smith , Ravindra K. Pandey , Joseph M. Ryan , Nadine Jagerovic , Thomas J. Dougherty
发明人： Kevin M. Smith , Ravindra K. Pandey , Joseph M. Ryan , Nadine Jagerovic , Thomas J. Dougherty
IPC分类号： A61K41/00 , C07D487/22 , A61K31/40
CPC分类号： C07D487/22 , A61K41/0071
摘要： Novel photosensitizers related to rhodoporphyrins and phylloerythrin methyl ester, their preparation and use as photosensitizers for detection and treatment of tumors by photodynamic therapy. The novel photosensitizers accumulate and concentrate preferentially in tumor tissue, have strong light absorption in the 650 to 700 nm region and have reduced skin phototoxicity.
摘要翻译：与紫罗兰卟啉和叶绿菊酯甲酯相关的新型光敏剂，它们的制备和用作光敏剂用于通过光动力学治疗检测和治疗肿瘤。新型光敏剂积聚并优先集中在肿瘤组织中，在650〜700nm区域具有强光吸收，降低皮肤光毒性。

3. 发明授权

US5591847A Long wavelength absorbing photosensitizers related to purpurin-18, bacteriopurpurin-18 and related compounds with imide linkages 失效
标题翻译：长紫外线吸收光紫外线吸收剂与紫草素-18，细菌尿素-18以及与酰亚胺连接的相关化合物
公开(公告)号：US5591847A
公开(公告)日：1997-01-07
申请号：US247866
申请日：1994-05-23
申请人： Ravindra K. Pandey , Thomas J. Dougherty , Kevin M. Smith , Fuu-Yau Shiau
发明人： Ravindra K. Pandey , Thomas J. Dougherty , Kevin M. Smith , Fuu-Yau Shiau
IPC分类号： A61K41/00 , C07D487/22 , C07D491/22
CPC分类号： C07D487/22 , A61K41/0071 , C07D491/22
摘要： Compounds having utility as light absorbing compounds, especially in the area of photodynamic therapy.Such compounds have the formula: ##STR1## where Z is .dbd.O or .dbd.NR.sub.6, where R.sub.6 is lower alkyl of from 1 to 8 carbon atoms or ##STR2## R.sub.1 is ##STR3## where R.sub.7 is ##STR4## or --ORS, where R.sub.8 is hydrogen or lower alkyl of 1 to 8 carbon atoms, or R.sub.7 is an amino acid residue connected at a nitrogen atom of such residue; R.sub.2 is lower alkyl or lower alkylene of from 2 to 4 carbon atoms or a formal or carbonyl containing group of from 1 to 4 carbon atoms; R.sub.3 and R.sub.4 are --H or --OR.sub.8 or are joined together so that each represents one-half of a chemical bond and R.sub.4 may be taken together with R.sub.5 to form .dbd.O; and R.sub.5 is ethyl or is taken together with R.sub.4 to form .dbd.O; provided that when Z is --O-- the sum of the number of carbon atoms in R.sub.1 through R.sub.5 is from 12 to 20 and when Z is .dbd.NR.sub.6, the sum of the number of carbon atoms in R.sub.1 through R.sub.6 is 8 to 20.
摘要翻译：具有作为光吸收化合物用途的化合物，特别是在光动力疗法领域。这样的化合物具有下式：其中Z是=或NR 6，其中R 6是1至8个碳原子的低级烷基或者其中R 7是<或>，或者-OR，其中 R8是氢或1〜8个碳原子的低级烷基，或R7是在这种残基的氮原子上连接的氨基酸残基; R 2是2至4个碳原子的低级烷基或低级亚烷基或含有1至4个碳原子的形式或含羰基的基团; R 3和R 4是-H或-OR 8或连接在一起，使得各自表示化学键的一半，并且R 4可以与R 5一起形成= O; 并且R 5是乙基或与R 4一起形成= O; 条件是当Z为-O-时，R 1至R 5中的碳原子数之和为12至20，当Z为NR 6时，R 1至R 6中的碳原子数之和为8至20。

4. 发明授权

US6103751A Carotene analogs of porphyrins, chlorins and bacteriochlorins as therapeutic and diagnostic agents 失效
标题翻译：卟啉类胡萝卜素类似物，二氢卟酚和细菌毒素作为治疗和诊断剂
公开(公告)号：US6103751A
公开(公告)日：2000-08-15
申请号：US102417
申请日：1998-06-22
申请人： Ravindra K. Pandey , William R. Potter , Thomas J. Dougherty
发明人： Ravindra K. Pandey , William R. Potter , Thomas J. Dougherty
IPC分类号： A61K49/00 , C07D487/22 , C07D519/00 , A61K31/40
CPC分类号： A61K49/0036 , A61K49/0052 , C07D487/22 , C07D519/00
摘要： A carotene conjugate of the formula: ##STR1## where R.sup.1 is hydrogen or methyl; R.sup.2 is: ##STR2## R.sup.3, R.sup.4 and R.sup.5 are independently, hydrogen, methyl or ethyl; R.sup.6 and R.sup.7 are independently --R.sup.13, --OR , --C(R.sup.6)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 ; R.sup.8 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken with R.sup.10 is .dbd.O; R.sup.9 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken with R.sup.10 is a chemical bond; R.sup.10 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O) , --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken together with R.sup.9 is a chemical bond or taken with R.sup.8 is .dbd.O; R.sup.11 is R.sup.13, or --OR.sup.13 ; R.sup.12 is --C(R.sup.13).sub.2 C(Y)--, --C(O)O(O)C--, --C(NR.sup.13)O(O)C--, or --C(O)N(R.sup.15)--C(O)--; R.sup.13 is, independently at each occurrence, hydrogen or lower alkyl of from 1 through about 10 carbon atoms; R.sup.14 is an amino acid residue, R.sup.15 is --R.sup.13, --R.sup.14, or --C(O)NHR.sup.13 ; R.sup.16 is, independently at each occurrence, hydrogen or lower alkyl of 1 to about 4 carbon atoms and Y is .dbd.O, .dbd.S, or 2H--.
摘要翻译：下式的胡萝卜素缀合物：其中R1是氢或甲基; R2是：R3，R4和R5独立地是氢，甲基或乙基; R6和R7独立地是-R13，-OR，-C（R6）（O），-C（R16）2OR13，-CH = CHR13或 - （CH2）R14; R8是-R13，-OR13，-C（R16）（O），-C（R16）2OR13，-CH = CHR13或 - （CH2）R14，或R10为= R9为-R13，-OR13，-C（R16）（O），-C（R16）2OR13，-CH = CHR13或 - （CH2）R14或R10为化学键; R 10为-R 13，-OR 13，-C（R 16）（O），-C（R 16）2 OR 13，-CH = CHR 13或 - （CH 2）R 14或与R 9一起为化学键， O; R11是R13或-OR13; R 12是-C（R 13）2 C（Y） - ， - C（O）O（O）C - ， - C（NR 13）O（O）C-或-C（O）N（R 15） O） - ; R 13在每次出现时独立地为氢或1至约10个碳原子的低级烷基; R14是氨基酸残基，R15是-R13，-R14或-C（O）NHR13; R 16在每次出现时独立地为氢或1至约4个碳原子的低级烷基，Y为= O，= S或2H-。

5. 发明授权

US5459159A Pyropheophorbides and their use in photodynamic therapy 失效
标题翻译：偏焦异构体及其在光动力疗法中的应用
公开(公告)号：US5459159A
公开(公告)日：1995-10-17
申请号：US239089
申请日：1994-05-05
申请人： Ravindra K. Pandey , Thomas J. Dougherty
发明人： Ravindra K. Pandey , Thomas J. Dougherty
IPC分类号： A61K31/40 , A61K41/00 , A61K51/04 , A61P31/12 , A61P35/00 , C07D487/22 , C07D519/00
CPC分类号： C07D487/22 , A61K41/0071 , A61K51/0485 , C07D519/00 , A61K2123/00
摘要： Pyropheophorbide compounds are injected into a host and accumulate in tumor tissue to a higher degree than surrounding normal tissues. When the pyropheophorbide compounds are exposed to a particular wavelength of light the compounds become cytotoxic and destroy the tumor or diseased tissue without causing irreversible normal tissue damage. The pyropheophorbide compounds have shown improved results as compared to drugs currently used in photodynamic therapy. Further, they absorb light further in the red, optimizing tissue penetration and are retained in the skin for short time periods relative to other drugs used in photodynamic therapy.
摘要翻译：将焦磷偏磷酸酯化合物注射到宿主中并在肿瘤组织中积聚到比周围正常组织更高的程度。当焦偏磷酸酯化合物暴露于特定波长的光时，化合物变成细胞毒性并破坏肿瘤或患病组织而不引起不可逆的正常组织损伤。与目前在光动力疗法中使用的药物相比，焦偏镁离子化合物显示出改善的结果。此外，它们进一步吸收红色的光，优化组织穿透，并相对于光动力疗法中使用的其他药物，在短时间内保留在皮肤中。

6. 发明申请

US20100137396A1 TREATMENT OF ESOPHAGEAL HIGH GRADE DYSPLASIA USING PHOTODYNAMIC THERAPY 审中-公开
标题翻译：使用光化疗法治疗高脂肪高血压病
公开(公告)号：US20100137396A1
公开(公告)日：2010-06-03
申请号：US12448660
申请日：2007-09-27
申请人： Ravindra K. Pandey , Thomas J. Dougherty , David A. Bellnier , Hector R. Nava
发明人： Ravindra K. Pandey , Thomas J. Dougherty , David A. Bellnier , Hector R. Nava
IPC分类号： A61K31/407 , A61P35/00
CPC分类号： A61K31/409
摘要： A method for treatment of esophageal high grade dysplasia comprising the steps of: injecting HPPH in a physiologically compatible medium into a patient having high grade dysplasia tissue to provide a dose level of 3 through 5 mg/m2 of body surface area, waiting for a time period of 24 through 60 hours to permit preferential absorption of the HPPH into esophageal cancer tissue, and exposing the esophageal cancer tissue to light at a wavelength of about 670±5 nm at an energy of from about 75 to about 200 Joules/cm.
摘要翻译：一种治疗食管高级别发育不良的方法，包括以下步骤：将HPPH在生理相容性培养基中注入具有高度发育不良组织的患者，以提供3至5mg / m 2的体表面积的剂量水平，等待一段时间时间为24至60小时，以允许优先吸收HPPH进入食管癌组织，并以约75至约200焦耳/厘米的能量将食管癌组织暴露于波长约670±5nm的光。

7. 发明授权

US07097826B2 Chlorin and bacteriochlorin-based difunctional aminophenyl DTPA and N2S2 conjugates for MR contrast media and radiopharmaceuticals 有权
标题翻译：用于MR造影剂和放射性药物的二氢卟酚和细菌二氢卟酚基二官能氨基苯基DTPA和N2S2共轭物
公开(公告)号：US07097826B2
公开(公告)日：2006-08-29
申请号：US10177129
申请日：2002-06-21
申请人： Ravindra K. Pandey , Zachary Grossman , Peter Kanter , Thomas J. Dougherty
发明人： Ravindra K. Pandey , Zachary Grossman , Peter Kanter , Thomas J. Dougherty
IPC分类号： A61B5/055
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.
摘要翻译：包括光动力四吡咯化合物与多个放射性核素元素原子的化学组合的化合物，使得该化合物可用于增强MR成像，并且还可用作光动力学化合物用于光动力学治疗以治疗过度增生组织。优选的化合物具有以下结构式：其中R 1，R 2，R 2，R 3，R 3， R 5，R 5，R 5a，R 6，R 5，R 5，R 5， R 7，R 7a和R 8累积含有至少两个将与MR成像增强元件或离子复合或组合的官能团。该化合物旨在包括这种复合物和组合，并且包括使用这些化合物用于肿瘤和其它过度增生组织的MR成像和光动力治疗治疗。

8. 发明授权

US06534040B2 Chlorin and bacteriochlorin-based aminophenyl DTPA and N2S2 conjugates for MR contrast media and radiopharmaceuticals 有权
标题翻译：用于MR造影剂和放射性药物的二氢卟酚和细菌氯胺基氨基苯基DTPA和N2S2缀合物
公开(公告)号：US06534040B2
公开(公告)日：2003-03-18
申请号：US09739155
申请日：2000-12-18
申请人： Ravindra K. Pandey , Zachary Grossman , Peter Kanter , Thomas J. Dougherty
发明人： Ravindra K. Pandey , Zachary Grossman , Peter Kanter , Thomas J. Dougherty
IPC分类号： C07D48722
CPC分类号： A61K51/0478 , A61K41/0071 , A61K49/085 , A61K51/0485 , C07D471/22 , C07D487/22
摘要： Compositions that are a chemical combination of porphyrins, chlorins, bacteriochlorins, and related tetra-pyrrolic compounds with radioactive elements such as Technetium99, Gadolinium, Indium111 and radioactive iodine. When the element can form cations, the compound is usually a chelate with the porphyrin or chlorin structure. When the element forms anions, the compound is usually a direct chemical combination of the radioactive element into the porphyrin or chlorin structure. The invention further includes the method of using the compounds of the invention for diagnostic imaging of hyperproliferative tissue such as tumors and new blood vessel growth as is associated with the wet form of age related macular degeneration and methods of making the compounds. Compounds for MRI contrast imaging of the invention are usually Tc99, In111 or Gd(III) complexes of compounds of the formula:
摘要翻译：组合物是卟啉，二氢卟酚，细菌色素和与放射性元素相关的四吡咯化合物如锝99，钆，铟111和放射性碘的化学组合。当元素可以形成阳离子时，化合物通常是具有卟啉或二氢卟酚结构的螯合物。当元素形成阴离子时，化合物通常是放射性元素与卟啉或二氢卟酚结构的直接化学组合。本发明还包括使用本发明的化合物用于诊断超增殖组织如肿瘤和新血管生长的成像的方法，其与湿性形式的年龄相关性黄斑变性相关联，以及制备该化合物的方法。本发明的MRI造影成像的化合物通常是下式化合物的Tc99，In111或Gd（III）络合物：

9. 发明授权

US4968715A Use of purified hematoporphyrin trimers in photodynamic therapy 失效
标题翻译：在光动力学治疗中使用纯化的血卟啉三聚体
公开(公告)号：US4968715A
公开(公告)日：1990-11-06
申请号：US343865
申请日：1989-04-26
申请人： Thomas J. Dougherty , Ravindra K. Pandey
发明人： Thomas J. Dougherty , Ravindra K. Pandey
IPC分类号： C07D487/22 , A61K31/40 , A61K39/44 , A61K41/00 , A61P35/00 , C07D519/00
CPC分类号： C07D519/00 , A61K31/40 , A61K41/0071
摘要： Pure dimer and trimer compounds of hematoporphyrin are prepared and shown to be effective agents in photodynamic therapy. The compounds of the invention are of the formula ##STR1## wherein each X is independently 1-hydroxyethyl or vinyl and wherein R is H or lower alkyl. The compounds of the invention can be conjugated to targeting substances such as immunoglobulins or to labels.
摘要翻译：制备血卟啉的纯二聚体和三聚体化合物，并显示为光动力学治疗中的有效试剂。本发明的化合物具有下式：其中每个X独立地为1-（4-羟基苯基）羟乙基或乙烯基，其中R为H或低级烷基。本发明的化合物可以与靶向物质例如免疫球蛋白缀合，或与标记缀合。

10. 再颁专利

USRE43274E1 Fluorinated photosensitizers related to chlorins and bacteriochlorins for photodynamic therapy 失效
标题翻译：与二氢卟酚和细菌毒素相关的氟光敏剂用于光动力疗法
公开(公告)号：USRE43274E1
公开(公告)日：2012-03-27
申请号：US12321729
申请日：2009-01-23
申请人： Ravindra K. Pandey , William R. Potter , Thomas J. Dougherty
发明人： Ravindra K. Pandey , William R. Potter , Thomas J. Dougherty
IPC分类号： C09B47/04
CPC分类号： C07D471/22 , A61K41/0071 , A61K41/0076 , C09B47/00 , C09B69/108
摘要： Provided herein are compounds for detection, diagnosis and treatment of target tissues or target compositions, including hyperproliferative tissues such as tumors, using photodynamic methods. In particular, photosensitizer compounds that collect in hyperproliferative tissue are provided. In another embodiment, compounds that absorb light at a wavelength of from about 700 to about 850 nm are provided. In a further embodiment, compounds that are detectable by magnetic resonance imaging are provided.
摘要翻译：本文提供了使用光动力学方法检测，诊断和治疗靶组织或靶组合物的化合物，包括过度增殖组织如肿瘤。特别地，提供了在过度增殖组织中收集的光敏剂化合物。在另一个实施方案中，提供了吸收波长为约700至约850nm的光的化合物。在另一个实施方案中，提供了可通过磁共振成像检测的化合物。

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