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1. 发明授权

US5567687A Texaphyrins and uses thereof 失效
标题翻译： Texaphyrins及其用途
公开(公告)号：US5567687A
公开(公告)日：1996-10-22
申请号：US310501
申请日：1994-09-21
申请人： Darren Magda , Jonathan L. Sessler , Brent Iverson , Petra L. Jansen , Meredith Wright , Tarak D. Mody , Gregory W. Hemmi
发明人： Darren Magda , Jonathan L. Sessler , Brent Iverson , Petra L. Jansen , Meredith Wright , Tarak D. Mody , Gregory W. Hemmi
IPC分类号： A61K41/00 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/04 , A61L2/00 , B01J31/02 , B01J31/16 , B01J31/18 , C07D487/22 , C07H21/00 , C12N15/113
CPC分类号： C07D487/22 , A61K41/0042 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0054 , A61K49/085 , A61K49/106 , A61K49/126 , A61K51/0485 , A61L2/0011 , B01J31/1658 , B01J31/1815 , C07H21/00 , C12N15/113 , B01J2531/025 , B01J2531/26 , B01J2531/27 , B01J2531/33 , B01J2531/37 , B01J2531/38 , B01J31/0201 , C12N2310/15 , C12N2310/321 , C12N2310/3511
摘要： A texaphyrin having substituents containing ethoxy groups, methods for using texaphyrins in photodynamic therapy, and cleavage of a polymer of deoxyribonucleic acid are disclosed. The in vivo treatment of tumors and atheroma is demonstrated using Lu(III)texaphyrin complexes. A preferred method of use is the site-specific cleavage of a polymer of deoxyribonucleic acid and a preferred texaphyrin is a derivatized texaphyrin having binding specificity, in particular, a texaphyrin covalently coupled to a site-directing molecule, preferably an oligonucleotide.
摘要翻译：公开了具有含乙氧基的取代基的泰克萨菲瑞，光动力学治疗中使用泰克萨菲瑞的方法和脱氧核糖核酸的聚合物的切割。使用Lu（III）泰克萨菲瑞复合物证明体内治疗肿瘤和动脉粥样硬化。优选的使用方法是脱氧核糖核酸的聚合物的位点特异性切割，优选的泰克萨菲瑞是具有结合特异性的衍生的泰克萨菲林，特别是共价偶联到位点定向分子，优选寡核苷酸的泰克萨菲林。

2. 发明授权

US5632970A Fluoresence detection using texaphyrins 失效
标题翻译：使用泰克萨菲瑞的荧光检测
公开(公告)号：US5632970A
公开(公告)日：1997-05-27
申请号：US486967
申请日：1995-06-07
申请人： Jonathan L. Sessler , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kr al , Darren Magda
发明人： Jonathan L. Sessler , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kr al , Darren Magda
IPC分类号： A61K31/40 , A61K31/407 , A61K41/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/00 , A61K51/04 , A61L2/00 , A61P35/02 , A61P43/00 , B01J31/06 , B01J31/16 , B01J31/18 , C07D487/22 , C07H21/00 , A61K31/555
CPC分类号： A61K51/0485 , A61K41/0038 , A61K41/0057 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0054 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/126 , A61L2/0011 , B01J31/1658 , B01J31/1805 , B01J31/1815 , C07D487/22 , C07H21/00 , B01J2531/025 , B01J2531/23 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/36 , B01J2531/37 , B01J2531/38 , B01J2531/72 , B01J2531/842 , B01J2531/845 , B01J2531/847 , B01J2531/96 , B01J31/061
摘要： Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocatization, and iv) indifference to the presence or absence of O.sub.2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.
摘要翻译：特拉法芬被提供用作辐射敏化剂。泰克萨菲瑞用作辐射敏化剂的有利特性包括：i）低的氧化还原电位，其允许辐射诱导的水合电子流向泰克萨菲瑞而不是中和羟基，允许羟基自由基引起细胞损伤，ii）相对稳定的泰克萨菲瑞基其易于共价修饰相邻的分子，导致进一步的细胞损伤，iii）内在的生物定位，以及iv）对O2的存在或不存在的冷漠。这些性质使得泰克萨菲瑞对于治疗实体性赘生物的缺氧区域特别有效。具有肿瘤或动脉粥样硬化的个体的治疗方法包括使用泰克萨菲林作为辐射敏化剂和作为光动力学肿瘤治疗的药剂，或者使用泰克萨菲瑞用于内部和外部电离辐射。提供了新的泰克萨菲标本。

3. 发明授权

US5580543A Method of magnetic resonance image enhancement 失效
标题翻译：磁共振图像增强方法
公开(公告)号：US5580543A
公开(公告)日：1996-12-03
申请号：US458267
申请日：1995-06-02
申请人： Jonathan L. Sessler , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kr al , Darren Magda
发明人： Jonathan L. Sessler , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kr al , Darren Magda
IPC分类号： A61K31/40 , A61K31/407 , A61K41/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/00 , A61K51/04 , A61L2/00 , A61P35/02 , A61P43/00 , B01J31/06 , B01J31/16 , B01J31/18 , C07D487/22 , C07H21/00 , G01N24/08 , A61K31/555
CPC分类号： A61K51/0485 , A61K41/0038 , A61K41/0057 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0054 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/126 , A61L2/0011 , B01J31/1658 , B01J31/1805 , B01J31/1815 , C07D487/22 , C07H21/00 , B01J2531/025 , B01J2531/23 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/36 , B01J2531/37 , B01J2531/38 , B01J2531/72 , B01J2531/842 , B01J2531/845 , B01J2531/847 , B01J2531/96 , B01J31/061
摘要： Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocalization, and iv) indifference to the presence or absence of O.sub.2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.
摘要翻译：特拉法芬被提供用作辐射敏化剂。泰克萨菲瑞用作辐射敏化剂的有利特性包括：i）低的氧化还原电位，其允许辐射诱导的水合电子流向泰克萨菲瑞而不是中和羟基，允许羟基自由基引起细胞损伤，ii）相对稳定的泰克萨菲瑞基其易于共价修饰相邻的分子，导致进一步的细胞损伤，iii）内在的生物定位，以及iv）不存在或不存在O 2。这些性质使得泰克萨菲瑞对于治疗实体性赘生物的缺氧区域特别有效。具有肿瘤或动脉粥样硬化的个体的治疗方法包括使用泰克萨菲林作为辐射敏化剂和作为光动力学肿瘤治疗的药剂，或者使用泰克萨菲瑞用于内部和外部电离辐射。提供了新的泰克萨菲标本。

4. 发明授权

US5587371A Texaphyrin-oligonucleotide conjugates 失效
标题翻译： Texaphyrin-寡核苷酸共轭物
公开(公告)号：US5587371A
公开(公告)日：1996-12-24
申请号：US458909
申请日：1995-06-02
申请人： Jonathan L. Sessler , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kr al , Darren Magda
发明人： Jonathan L. Sessler , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kr al , Darren Magda
IPC分类号： A61K31/40 , A61K31/407 , A61K41/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/00 , A61K51/04 , A61L2/00 , A61P35/02 , A61P43/00 , B01J31/06 , B01J31/16 , B01J31/18 , C07D487/22 , C07H21/00 , A61K31/715
CPC分类号： A61K51/0485 , A61K41/0038 , A61K41/0057 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0054 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/126 , A61L2/0011 , B01J31/1658 , B01J31/1805 , B01J31/1815 , C07D487/22 , C07H21/00 , B01J2531/025 , B01J2531/23 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/36 , B01J2531/37 , B01J2531/38 , B01J2531/72 , B01J2531/842 , B01J2531/845 , B01J2531/847 , B01J2531/96 , B01J31/061
摘要： Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocalization, and iv) indifference to the presence or absence of O.sub.2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.
摘要翻译：特拉法芬被提供用作辐射敏化剂。泰克萨菲瑞用作辐射敏化剂的有利特性包括：i）低的氧化还原电位，其允许辐射诱导的水合电子流向泰克萨菲瑞而不是中和羟基，允许羟基自由基引起细胞损伤，ii）相对稳定的泰克萨菲瑞基其易于共价修饰相邻的分子，导致进一步的细胞损伤，iii）内在的生物定位，以及iv）不存在或不存在O 2。这些性质使得泰克萨菲瑞对于治疗实体性赘生物的缺氧区域特别有效。具有肿瘤或动脉粥样硬化的个体的治疗方法包括使用泰克萨菲林作为辐射敏化剂和作为光动力学肿瘤治疗的药剂，或者使用泰克萨菲瑞用于内部和外部电离辐射。提供了新的泰克萨菲标本。

5. 发明授权

US5583220A Pyrole nitrogen-substituted texaphyrins 失效
标题翻译：吡咯氮取代的泰克萨菲
公开(公告)号：US5583220A
公开(公告)日：1996-12-10
申请号：US449681
申请日：1995-05-24
申请人： Jonathan L. Sessler , Anthony M. Harriman , Richard A. Miller , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kral , Darren Magda
发明人： Jonathan L. Sessler , Anthony M. Harriman , Richard A. Miller , Tarak D. Mody , Gregory W. Hemmi , Vladimir A. Kral , Darren Magda
IPC分类号： A61K31/40 , A61K31/407 , A61K41/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/00 , A61K51/04 , A61L2/00 , A61P35/02 , A61P43/00 , B01J31/06 , B01J31/16 , B01J31/18 , C07D487/22 , C07H21/00
CPC分类号： A61K51/0485 , A61K41/0038 , A61K41/0057 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0054 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/126 , A61L2/0011 , B01J31/1658 , B01J31/1805 , B01J31/1815 , C07D487/22 , C07H21/00 , B01J2531/025 , B01J2531/23 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/36 , B01J2531/37 , B01J2531/38 , B01J2531/72 , B01J2531/842 , B01J2531/845 , B01J2531/847 , B01J2531/96 , B01J31/061
摘要： Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocalization, and iv) indifference to the presence or absence of O.sub.2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.
摘要翻译：特拉法芬被提供用作辐射敏化剂。泰克萨菲瑞用作辐射敏化剂的有利特性包括：i）低的氧化还原电位，其允许辐射诱导的水合电子流向泰克萨菲瑞而不是中和羟基，允许羟基自由基引起细胞损伤，ii）相对稳定的泰克萨菲瑞基其易于共价修饰相邻的分子，导致进一步的细胞损伤，iii）内在的生物定位，以及iv）不存在或不存在O 2。这些性质使得泰克萨菲瑞对于治疗实体性赘生物的缺氧区域特别有效。具有肿瘤或动脉粥样硬化的个体的治疗方法包括使用泰克萨菲林作为辐射敏化剂和作为光动力学肿瘤治疗的药剂，或者使用泰克萨菲瑞用于内部和外部电离辐射。提供了新的泰克萨菲标本。

6. 发明授权

US5969111A Texaphyrins substituted with imidazole are provided 失效
标题翻译：取代的泰克萨菲
公开(公告)号：US5969111A
公开(公告)日：1999-10-19
申请号：US775261
申请日：1997-02-04
申请人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody , Darren Magda , Vladimir A. Kral
发明人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody , Darren Magda , Vladimir A. Kral
IPC分类号： A61K41/00 , A61K47/48 , A61K49/00 , A61K51/04 , B01J31/06 , B01J31/16 , B01J31/18 , C07D487/22 , C07H21/00 , A61K31/40 , A61K31/555 , C07K2/00
CPC分类号： A61K47/48069 , A61K41/0038 , A61K41/0076 , A61K47/48023 , A61K49/0021 , A61K51/0485 , B01J31/1658 , B01J31/1815 , C07D487/22 , C07H21/00 , B01J2531/025 , B01J2531/36 , B01J2531/38 , B01J31/061
摘要： Texaphyrins substituted with imidazda are provided.
摘要翻译：提供了用咪唑代替的Texaphyrins。

7. 发明授权

US5888997A Radiation sensitization using texaphyrins 失效
标题翻译：使用泰克萨菲的辐射敏化
公开(公告)号：US5888997A
公开(公告)日：1999-03-30
申请号：US795393
申请日：1997-02-04
申请人： Jonathan L. Sessler , Anthony Harriman , Richard A. Miller , Darren Magda , Tarak D. Mody , Gregory W. Hemmi
发明人： Jonathan L. Sessler , Anthony Harriman , Richard A. Miller , Darren Magda , Tarak D. Mody , Gregory W. Hemmi
IPC分类号： A61K41/00 , A61K47/48 , A61K49/00 , A61K51/04 , A61L2/00 , B01J31/06 , B01J31/16 , B01J31/18 , C07D487/22 , C07H21/00 , A61K31/555
CPC分类号： A61K41/0038 , A61K41/0057 , A61K41/0076 , A61K47/48023 , A61K47/48069 , A61K49/0021 , A61K49/0054 , A61K49/0058 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/126 , A61K51/0485 , A61L2/0011 , B01J31/1658 , B01J31/1805 , B01J31/1815 , C07D487/22 , C07H21/00 , B01J2531/025 , B01J2531/23 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/36 , B01J2531/37 , B01J2531/38 , B01J2531/72 , B01J2531/842 , B01J2531/845 , B01J2531/847 , B01J2531/96 , B01J31/061
摘要： The invention relates to the field of radiation sensitizers and the use of texaphyrins for radiation sensitization and other conditions for which X-ray radiation has proven to be therapeutic.
摘要翻译：本发明涉及辐射敏化剂领域，以及使用泰克萨菲精对辐射敏化和X射线辐射已被证明是治疗性的其他条件。

8. 发明授权

US06375930B2 Membrane incorporation of texaphyrins 失效
标题翻译：丝裂霉素的膜结合
公开(公告)号：US06375930B2
公开(公告)日：2002-04-23
申请号：US08975090
申请日：1997-11-20
申请人： Stuart W. Young , Meredith Wright , Jonathan L. Sessler , Tarak D. Mody , Darren Magda
发明人： Stuart W. Young , Meredith Wright , Jonathan L. Sessler , Tarak D. Mody , Darren Magda
IPC分类号： A61B55055
CPC分类号： B82Y5/00 , A61K41/0076 , A61K47/554 , A61K47/6901 , A61K47/6911 , A61K49/085 , A61K49/1896
摘要： Compositions having a texaphyrin-lipophilic molecule conjugate loaded into a biological vesicle and methods for imaging, diagnosis and treatment using the loaded vesicle are provided. For example, liposomes or red blood cells loaded with a paramagnetic texaphyrin-lipophilic molecule conjugate have utility as a blood pool contrast agent, facilitating the enhancement of normal tissues, magnetic resonance angiography, and marking areas of damaged endothelium by their egress through fenestrations or damaged portions of the blood vascular system. Liposomes or cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate can be photolysed, allowing for a photodynamic therapy effect at the site of lysis. Availability of red blood cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate provides a method for delivering a photodynamic therapeutic agent to a desired site with a high concentration of oxygen. By presenting the agent in this way, it is expected that a patient will experience less toxicity.
摘要翻译：提供了具有加载到生物囊泡中的泰克萨菲瑞 - 亲脂性分子缀合物的组合物以及使用加载的囊泡进行成像，诊断和治疗的方法。例如，装载有顺磁性泰克萨菲瑞 - 亲脂性分子缀合物的脂质体或红细胞具有作为血液池造影剂的效用，有利于正常组织的增强，磁共振血管造影术，以及通过开窗口或损伤引起的出血损伤的内皮标记区域部分血管系统。可以光密化具有感光性泰克萨菲瑞 - 亲脂性分子缀合物的脂质体或细胞，从而在裂解部位产生光动力学治疗效果。载有感光性泰克萨菲瑞 - 亲脂性分子缀合物的红细胞的可获得性提供了一种将光动力治疗剂递送至具有高浓度氧的所需部位的方法。通过以这种方式呈现代理，预期患者的毒性将较低。

9. 发明授权

US5601802A Methods of MRI enhancement using compounds having improved functionalization 失效
标题翻译：使用具有改进功能化的化合物进行MRI增强的方法
公开(公告)号：US5601802A
公开(公告)日：1997-02-11
申请号：US486886
申请日：1995-06-07
申请人： Gregory W. Hemmi , Jonathan L. Sessler , Tarak D. Mody
发明人： Gregory W. Hemmi , Jonathan L. Sessler , Tarak D. Mody
IPC分类号： A61K41/00 , C07D487/18 , C07D487/22 , C07D225/00 , G01N24/08
CPC分类号： C07D487/18 , A61K41/0038 , A61K41/0076 , C07D487/22
摘要： Texaphyrin metal complexes having improved functionalization include the addition of electron-donating groups to positions 2, 7, 12, 15, 18 and/or 21 and/or the addition of electron-withdrawing groups to positions 15 and/or 18 of the macrocycle. Electron-donating groups at positions 2, 7, 12, 15, 18 and/or 21 contribute electrons to the aromatic .pi. system of the macrocycle which stabilizes the metal complex to demetallation and the imine bonds to hydrolysis. These texaphyrin metal complexes having enhanced stability are useful for localization, magnetic resonance imaging, radiosensitization, radiation therapy, fluorescence imaging, photodynamic therapy, RNA hydrolysis, DNA photocleavage, and applications requiring singlet oxygen production for cytotoxicity. Electron-withdrawing groups at positions 15 and/or 18 render the macrocycle more readily reduced, i.e. the redox potential is lower and the macrocycle more readily gains an electron to form a radical. Such texaphyrins having a low redox potential are useful for radiation sensitization applications.
摘要翻译：具有改进的功能化的特拉法林金属络合物包括向位置2,7,12,15,18和/或21添加给电子基团和/或向大环化合物的位置15和/或18添加吸电子基团。位置2,7,12,15,18和/或21上的供体基团向大环化合物的芳族π系统贡献电子，这使得金属络合物稳定化以脱金属，并且亚胺键合到水解。具有增强的稳定性的这些泰克萨菲瑞金属络合物可用于定位，磁共振成像，放射增敏，放射治疗，荧光成像，光动力学治疗，RNA水解，DNA光切割以及需要单线态氧产生细胞毒性的应用。位置15和/或18处的吸电子基团使得大环化合物更容易降低，即氧化还原电位较低，大环化合物更容易获得电子以形成基团。具有低氧化还原电位的这种泰克萨菲瑞对于辐射敏化应用是有用的。

10. 发明授权

US5599928A Texaphyrin compounds having improved functionalization 失效
标题翻译：具有改进功能化的Texaphyrin化合物
公开(公告)号：US5599928A
公开(公告)日：1997-02-04
申请号：US459333
申请日：1995-06-02
申请人： Gregory W. Hemmi , Jonathan L. Sessler , Tarak D. Mody
发明人： Gregory W. Hemmi , Jonathan L. Sessler , Tarak D. Mody
IPC分类号： A61K31/40 , A61K41/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/00 , A61K51/04 , A61L2/00 , A61P35/00 , C07D487/22 , C07H21/00
CPC分类号： C07D487/22 , A61K41/0009 , A61K41/0038 , A61K41/0076 , A61K49/0021 , A61K49/106 , A61K51/04 , A61K51/0485 , A61K51/1093 , A61L2/0011 , C07H21/00 , A61K2121/00
摘要： Texaphyrin metal complexes having improved functionalization include the addition of electron-donating groups to positions 2, 7, 12, 15, 18 and/or 21 and/or the addition of electron-withdrawing groups to positions 15 and/or 18 of the macrocycle. Electron-donating groups at positions 2, 7, 12, 15, 18 and/or 21 contribute electrons to the aromatic .pi. system of the macrocycle which stabilizes the metal complex to demetallation and the imine bonds to hydrolysis. The addition of substituents to the 12 and 21 positions of the macrocycle offer steric protection for the imine bonds against possible in vivo enzyme hydrolysis. Electron-withdrawing groups at positions 15 and/or 18 render the macrocycle more readily reduced, i.e. the redox potential is lower and the macrocycle more readily gains an electron to form a radical. Such texaphyrins having a low redox potential and imine bond stabilization are useful in a variety of applications.
摘要翻译：具有改进的功能化的特拉法林金属络合物包括向位置2,7,12,15,18和/或21添加给电子基团和/或向大环化合物的位置15和/或18添加吸电子基团。位置2,7,12,15,18和/或21上的供体基团向大环化合物的芳族π系统贡献电子，这使得金属络合物稳定化以脱金属，并且亚胺键合到水解。在大环的12位和21位添加取代基可提供针对可能的体内酶水解的亚胺键的空间保护。位置15和/或18处的吸电子基团使得大环化合物更容易降低，即氧化还原电位较低，大环化合物更容易获得电子以形成基团。具有低氧化还原电位和亚胺键稳定性的这种泰克萨菲瑞可用于各种应用。

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