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1. 发明授权

US07053210B2 Efficient synthesis of pyropheophorbide a and its derivatives 失效
标题翻译：高效合成焦脱镁叶绿酸a及其衍生物
公开(公告)号：US07053210B2
公开(公告)日：2006-05-30
申请号：US10613474
申请日：2003-07-02
申请人： Ravindra K. Pandey , Thomas J. Dougherty , Alexander J. Pallenberg
发明人： Ravindra K. Pandey , Thomas J. Dougherty , Alexander J. Pallenberg
IPC分类号： A61B5/055 , A61B10/00 , C07B47/00 , C07F5/10 , A61K31/555
CPC分类号： C07D471/22 , C07D487/22 , C07D491/22
摘要： A process for the preparation of pyropheophorbide a and its derivatives, including 3-devinyl-3-(1′-hexyloxy)ethyl-pyropheophorbide-a, otherwise known as HPPH, is provided. The process involves treating chlorin e6, in the form of its trimethyl ester, with a base, followed by heating to give pyropheophorbide a, which is converted to HPPH by treatment with acid, followed by hexyl alcohol under basic conditions.
摘要翻译：提供了制备焦脱镁叶绿酸a及其衍生物的方法，包括3-脱乙烯基-3-（1'-己氧基）乙基 - 焦脱镁叶绿酸a，也称为HPPH。该方法包括用碱处理其三甲酯形式的二氢卟酚，然后加热得到焦脱镁叶绿酸a，其通过用酸处理转化成HPPH，随后用己醇转化为HPPH 基本条件

2. 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-。

3. 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。

4. 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。

5. 发明申请

US20100144820A1 THERAPEUTIC HPPH DOSAGE FOR PDT 审中-公开
标题翻译： PDT治疗HPPH剂量
公开(公告)号：US20100144820A1
公开(公告)日：2010-06-10
申请号：US12448661
申请日：2007-09-27
申请人： Ravindra K. Pandey , Thomas J. Dougherty , William R. Potter
发明人： Ravindra K. Pandey , Thomas J. Dougherty , William R. Potter
IPC分类号： A61K31/409 , C07D487/22 , A61P35/00
CPC分类号： A61K31/41 , A61K41/0071
摘要： A method for treating cancer and other hyperproliferative tissues in humans that can be exposed to light comprising injection of HPPH at the equivalent to a dose of 0.05 to 0.11 mg/kg of body weight 24 hours post injection and exposing the tumor or other hyperproliferative tissue to 665±10 nm of light at 50 to 200 Joules/cm2.
摘要翻译：一种用于治疗可暴露于光的人类的癌症和其它过度增生组织的方法，包括以相当于注射后24小时0.05至0.11mg / kg体重的剂量注射HPPH并将肿瘤或其它过度增生组织暴露于在50至200焦耳/平方厘米的光照下为665±10nm。

6. 发明申请

US20100130909A1 TREATMENT OF BARRETT'S ESOPHAGUS USING PHOTODYNAMIC THERAPY 审中-公开
标题翻译：使用光化疗法治疗棒状病毒
公开(公告)号：US20100130909A1
公开(公告)日：2010-05-27
申请号：US12448662
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： A61M37/00 , A61K31/409
CPC分类号： A61K31/395 , A61N5/0601 , A61N5/062
摘要： A method for treatment of Barrett's esophagus comprising the steps of: injecting HPPH in a physiologically compatible medium into a patient having Barrett's esophagus 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 Barrett's esophagus tissue, and exposing the Barrett's esophagus 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：一种治疗巴雷特食管的方法，包括以下步骤：将HPPH在生理相容性培养基中注射入具有巴雷特食管组织的患者中，以提供3至5mg / m 2的体表面积的剂量水平，等待24小时 60小时以允许HPPH优先吸收到巴雷特食管组织中，并以约75至约200焦耳/厘米的能量将巴雷特食管组织暴露于波长约670±5nm的光。

7. 发明授权

US07166719B2 Fluorinated photosensitizers related to chlorins and bacteriochlorins for photodynamic therapy 有权
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：US07166719B2
公开(公告)日：2007-01-23
申请号：US10607922
申请日：2003-06-27
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。

8. 再颁专利

USRE39094E1 Pyropheophorbides and their use in photodynamic therapy 有权
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：USRE39094E1
公开(公告)日：2006-05-09
申请号：US10384895
申请日：2003-03-07
申请人： Ravindra K. Pandey , Thomas J. Dougherty
发明人： Ravindra K. Pandey , Thomas J. Dougherty
IPC分类号： A61K31/409 , C07D487/22
CPC分类号： A61K51/0485 , A61K41/0071 , A61K2123/00 , C07D487/22 , C07D519/00
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 mad 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线，相对于光动力治疗中使用的其他药物，优化组织穿透时间短于皮肤的时间。

9. 发明授权

US5952366A Alkyl ether analogs of chlorins having an N-substituted imide ring 失效
标题翻译：具有N-取代的酰亚胺环的二氢卟酚的烷基醚类似物
公开(公告)号：US5952366A
公开(公告)日：1999-09-14
申请号：US102394
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： C07D487/22 , A61K31/409 , A61K41/00 , A61P35/00 , C07D519/00 , A61K31/40
CPC分类号： C07D519/00 , A61K41/0071
摘要： Compounds having the generic formula: ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are independently alkyl of 3 through about 10 carbon atoms; provided that, R.sup.1 and R.sup.2 together contain at least six carbon atoms. The compounds have utility in photodynamic therapy in treatment of tumors and other diseases. The invention includes a method of treatment by contacting a tumor with the compound and then exposing the tumor to light.
摘要翻译：具有以下通式的化合物：其中R 1，R 2和R 3独立地为3至约10个碳原子的烷基; 条件是R 1和R 2一起含有至少6个碳原子。该化合物在光动力疗法中可用于治疗肿瘤和其他疾病。本发明包括通过使肿瘤与化合物接触然后将肿瘤暴露于光来治疗的方法。

10. 发明授权

US5864035A Synthesis of isoimide of chlorins and bacteriochlorins and their use for diagnosis and treatment of cancer 失效
标题翻译：二氢卟酚和细菌二氢卟酚的异构酰亚胺的合成及其在癌症诊断和治疗中的应用
公开(公告)号：US5864035A
公开(公告)日：1999-01-26
申请号：US812029
申请日：1997-03-06
申请人： Ravindra K. Pandey , Andrei N. Kozyrev , Thomas J. Dougherty
发明人： Ravindra K. Pandey , Andrei N. Kozyrev , Thomas J. Dougherty
IPC分类号： A61K41/00 , C07D471/22 , C07D491/22 , C07D487/22
CPC分类号： C07D471/22 , 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 NR.sub.14 ; R.sub.14 is alkyl or substituted alkyl; R.sub.1 is an amino acid group, a polyamine group, a polyether group or OR.sub.13 where R.sub.13 is alkyl; R.sub.4 through R.sub.11 are --H, --OH alkyl, alkoxy, alkenyl, alkylene, aryl, or aryloxy, or a carbonyl containing group, wherein carbon containing groups may be substituted with carbonyl, hydroxy, phosphoro, carboxy, halo, sulfo, amino and ether substituents, provided that; R.sub.4 may be taken together with R.sub.7 to form .dbd.O; R.sub.8 may be taken together with R.sub.9 to form .dbd.O; R.sub.10 may be taken together with R.sub.11 to form .dbd.O; and R.sub.4 and R.sub.7 may together form a chemical bond and R.sub.8 and R.sub.11 may together form a chemical bond; and R.sub.12 is hydrogen or lower alkyl; provided that if one z is O, the other z is --NR.sub.14.
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。这些化合物具有下式：其中z为= O或NR14; R14是烷基或取代的烷基; R1是氨基酸基团，多胺基团，聚醚基团或OR13，其中R13是烷基; R4至R11是-H，-OH烷基，烷氧基，烯基，亚烷基，芳基或芳氧基或含羰基，其中含碳基团可以被羰基，羟基，磷酰基，羧基，卤素，磺基，氨基和醚取代基，条件是 R4可以与R7一起形成= O; R8可以与R9一起形成= O; R10可以与R11一起形成= O; 并且R 4和R 7可以一起形成化学键，并且R 8和R 11可以一起形成化学键; 和R 12是氢或低级烷基; 条件是如果一个z是O，另一个Z是-NR 14。

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