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公开(公告)号：US20110091390A1
公开(公告)日：2011-04-21
申请号：US12912033
申请日：2010-10-26
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-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。
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公开(公告)号：US20090162289A1
公开(公告)日：2009-06-25
申请号：US12378751
申请日：2009-02-19
IPC分类号： A61K31/409 , A61P35/00 , A61K49/00 , A61K49/06
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-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。
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3.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
IPC分类号： A61K5/055
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 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。
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公开(公告)号：US07501509B2
公开(公告)日：2009-03-10
申请号：US11452511
申请日：2006-06-14
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 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.
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。
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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
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6.发明申请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：US20070053840A1
公开(公告)日：2007-03-08
申请号：US11479524
申请日：2006-06-30
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 ）。
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公开(公告)号：US20110223102A1
公开(公告)日：2011-09-15
申请号：US12677381
申请日：2008-09-11
申请人： Ravindra K. Pandey , Suresh Pandey , Lalit Goswami , Allan Oseroff , Shipra Dubey , Munawwar Sajjad , Stephanie Pincus
发明人： Ravindra K. Pandey , Suresh Pandey , Lalit Goswami , Allan Oseroff , Shipra Dubey , Munawwar Sajjad , Stephanie Pincus
IPC分类号： A61K51/04 , A61K49/00 , A61K31/30 , A61K31/409 , A61K38/12 , A61K31/437 , A61K31/506 , A61P35/00 , A61P43/00
CPC分类号： C07K7/06 , A61B5/02007 , A61B5/416 , A61K41/0071 , A61K47/54 , A61K47/64 , A61K49/0032 , A61K49/0036 , A61K49/0056 , A61K51/082 , A61K51/088
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。
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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
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-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。
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