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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US5569759A Water soluble texaphyrin metal complex preparation 失效
标题翻译：水溶性泰克萨菲瑞金属配合物制剂
公开(公告)号：US5569759A
公开(公告)日：1996-10-29
申请号：US98514
申请日：1993-07-28
申请人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
发明人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
IPC分类号： A61K31/40 , A61K41/00 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/04 , A61L2/00 , A61P35/00 , A61P43/00 , C07D487/22 , C07H17/02 , C07H21/00
CPC分类号： A61K51/0485 , A61K41/0009 , A61K41/0038 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0036 , A61K49/0058 , A61K49/04 , A61K49/106 , A61K51/1093 , A61L2/0011 , C07D487/22 , C07H17/02 , C07H21/00
摘要： The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, and lanthanide) complexes of the hydroxy-substituted texaphyrin derivatives of the present invention have unusual water solubility and stability. They absorb light strongly in a physiologically important region (i.e. 690-880 nm). They have enhanced relaxivity and therefore are useful in magnetic resonance imaging. They form long-lived triplet states in high yield and act as photosensitizers for the generation of singlet oxygen. Thus, they are useful for inactivation or destruction of enveloped viruses, mononuclear or other cells infected with such viruses as well as tumor cells. They are water soluble, yet they retain sufficient lipophilicity so as to have greater affinity for lipid rich areas such as atheroma and tumors. They may be used for magnetic resonance imaging followed by photodynamic tumor therapy in the treatment of atheroma and tumors. These properties, coupled with their high chemical stability and appreciable solubility in water, add to their usefulness.
摘要翻译：本发明涉及保持亲油性的水溶性羟基取代的泰克萨菲瑞，合成这些化合物及其用途。这些膨胀的卟啉大环是二价和三价金属离子的有效螯合剂。本发明的羟基取代的泰克萨菲瑞衍生物的各种金属（例如，转变，主要和镧系元素）络合物具有不寻常的水溶性和稳定性。它们在生理上重要的区域（即690-880nm）中强烈吸收光。它们具有增强的放松性，因此在磁共振成像中是有用的。它们以高产率形成长寿命的三重态，并且作为产生单线态氧的光敏剂。因此，它们可用于灭活或破坏包封的病毒，感染了这种病毒以及肿瘤细胞的单核细胞或其他细胞。它们是水溶性的，但它们保持足够的亲脂性，以便对富含脂质的区域如动脉粥样化和肿瘤具有更大的亲和力。它们可用于磁共振成像，随后光动力学肿瘤治疗治疗动脉粥样化和肿瘤。这些性质加上其高的化学稳定性和在水中的明显的溶解度，增加了它们的用途。

6. 发明授权

US5432171A Water soluble texaphyrin metal complexes for viral deactivation 失效
标题翻译：水溶性泰克萨菲瑞金属配合物，用于病毒灭活
公开(公告)号：US5432171A
公开(公告)日：1995-07-11
申请号：US100093
申请日：1993-07-28
申请人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
发明人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
IPC分类号： A61K31/40 , A61K41/00 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/04 , A61L2/00 , A61P35/00 , A61P43/00 , C07D487/22 , C07H17/02 , C07H21/00
CPC分类号： A61K51/0485 , A61K41/0009 , A61K41/0038 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0036 , A61K49/0058 , A61K49/04 , A61K49/106 , A61K51/1093 , A61L2/0011 , C07D487/22 , C07H17/02 , C07H21/00
摘要： The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, and lanthanide) complexes of the hydroxy-substituted texaphyrin derivatives of the present invention have unusual water solubility and stability. They absorb light strongly in a physiologically important region (i.e. 690-880 nm). They have enhanced relaxivity and therefore are useful in magnetic resonance imaging. They form long-lived triplet states in high yield and act as photosensitizers for the generation of singlet oxygen. Thus, they are useful for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus as well as tumor cells. They are water soluble, yet they retain sufficient lipophilicity so as to have greater affinity for lipid rich areas such as atheroma and tumors. They may be used for magnetic resonance imaging followed by photodynamic tumor therapy in the treatment of atheroma and tumors. These properties, coupled with their high chemical stability and appreciable solubility in water, add to their usefulness.
摘要翻译：本发明涉及保持亲油性的水溶性羟基取代的泰克萨菲瑞，合成这些化合物及其用途。这些膨胀的卟啉大环是二价和三价金属离子的有效螯合剂。本发明的羟基取代的泰克萨菲瑞衍生物的各种金属（例如，转变，主要和镧系元素）络合物具有不寻常的水溶性和稳定性。它们在生理上重要的区域（即690-880nm）中强烈吸收光。它们具有增强的放松性，因此在磁共振成像中是有用的。它们以高产率形成长寿命的三重态，并且作为产生单线态氧的光敏剂。因此，它们可用于灭活或破坏感染了这种病毒以及肿瘤细胞的人类免疫缺陷病毒（HIV-1），单核细胞或其他细胞。它们是水溶性的，但它们保持足够的亲脂性，以便对富含脂质的区域如动脉粥样化和肿瘤具有更大的亲和力。它们可用于磁共振成像，随后光动力学肿瘤治疗治疗动脉粥样化和肿瘤。这些性质加上其高的化学稳定性和在水中的明显溶解度，增加了它们的用途。

7. 发明授权

US5756726A Methods of producing singlet oxygen using compounds having improved functionalization 失效
标题翻译：使用具有改进的官能化的化合物生产单线态氧的方法
公开(公告)号：US5756726A
公开(公告)日：1998-05-26
申请号：US468935
申请日：1995-06-06
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 , C01B13/00
CPC分类号： C07D487/18 , A61K41/0038 , A61K41/0076 , C07D487/22
摘要： Novel texaphyrin compounds having improved functionalization are described. Metal complexes of these compounds are active as photosensitizers for the generation of singlet oxygen and thus are potentially useful for treatments performed with singlet oxygen. Several of the metallotexaphyrin complexes absorb light in the physiologically important range of 690-880 nm. The complexes form long-lived triplet states and thus may act as efficient photosensitizers for generation of singlet oxygen.
摘要翻译：描述了具有改进的功能化的新型泰克萨菲林化合物。这些化合物的金属络合物作为用于产生单线态氧的光敏剂是有活性的，因此可用于用单线态氧进行的处理。几种金属脱甲基吡啶络合物在690-880nm的生理重要范围内吸收光。络合物形成长寿命的三线态，因此可以作为产生单线态氧的有效光敏剂。

8. 发明授权

US5733903A Treatment of neoplastic tissue by water-soluble texaphyrine metal complexes 失效
标题翻译：通过水溶性泰克萨菲瑞金属配合物治疗肿瘤组织
公开(公告)号：US5733903A
公开(公告)日：1998-03-31
申请号：US679162
申请日：1996-07-10
申请人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
发明人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
IPC分类号： A61K31/40 , A61K41/00 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/04 , A61L2/00 , A61P35/00 , A61P43/00 , C07D487/22 , C07H17/02 , C07H21/00 , A61K31/715
CPC分类号： A61K51/0485 , A61K41/0009 , A61K41/0038 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0036 , A61K49/0058 , A61K49/04 , A61K49/106 , A61K51/1093 , A61L2/0011 , C07D487/22 , C07H17/02 , C07H21/00
摘要： The present invention relates to the use of water-soluble texaphyrin-diamagnetic metal complexes retaining lipophilicity as photosensitizers in the treatment of benign and malignant neoplastic tissue.
摘要翻译：本发明涉及在良性和恶性肿瘤组织的治疗中保持亲脂性的水溶性泰克萨菲瑞 - 抗磁性金属复合物作为光敏剂的用途。

9. 发明授权

US5504205A Reduced sp.sup.3 texaphyrins 失效
标题翻译：减少sp3泰克萨菲
公开(公告)号：US5504205A
公开(公告)日：1996-04-02
申请号：US280351
申请日：1994-07-26
申请人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
发明人： Jonathan L. Sessler , Gregory W. Hemmi , Tarak D. Mody
IPC分类号： A61K31/40 , A61K41/00 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/04 , A61L2/00 , A61P35/00 , A61P43/00 , C07D487/22 , C07H17/02 , C07H21/00
CPC分类号： A61K51/0485 , A61K41/0009 , A61K41/0038 , A61K41/0076 , A61K47/48069 , A61K49/0021 , A61K49/0036 , A61K49/0058 , A61K49/04 , A61K49/106 , A61K51/1093 , A61L2/0011 , C07D487/22 , C07H17/02 , C07H21/00
摘要： The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, and lanthanide) complexes of the hydroxy-substituted texaphyrin derivatives of the present invention have unusual water solubility and stability. They absorb light strongly in a physiologically important region (i.e. 690-880 nm). They have enhanced relaxivity and therefore are useful in magnetic resonance imaging. They form long-lived triplet states in high yield and act as photosensitizers for the generation of singlet oxygen. Thus, they are useful for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus as well as tumor cells. They are water soluble, yet they retain sufficient lipophilicity so as to have greater affinity for lipid rich areas such as atheroma and tumors. They may be used for magnetic resonance imaging followed by photodynamic tumor therapy in the treatment of atheroma and tumors. These properties, coupled with their high chemical stability and appreciable solubility in water, add to their usefulness.
摘要翻译：本发明涉及保持亲油性的水溶性羟基取代的泰克萨菲瑞，合成这些化合物及其用途。这些膨胀的卟啉大环是二价和三价金属离子的有效螯合剂。本发明的羟基取代的泰克萨菲瑞衍生物的各种金属（例如，转变，主要和镧系元素）络合物具有不寻常的水溶性和稳定性。它们在生理上重要的区域（即690-880nm）中强烈吸收光。它们具有增强的放松性，因此在磁共振成像中是有用的。它们以高产率形成长寿命的三重态，并且作为产生单线态氧的光敏剂。因此，它们可用于灭活或破坏感染了这种病毒以及肿瘤细胞的人类免疫缺陷病毒（HIV-1），单核细胞或其他细胞。它们是水溶性的，但它们保持足够的亲脂性，以便对富含脂质的区域如动脉粥样化和肿瘤具有更大的亲和力。它们可用于磁共振成像，随后光动力学肿瘤治疗治疗动脉粥样化和肿瘤。这些性质加上其高的化学稳定性和在水中的明显的溶解度，增加了它们的用途。

10. 发明授权

US5591422A Texaphyrin complexes having improved functionalization 失效
标题翻译：特拉法林复合物具有改进的功能化
公开(公告)号：US5591422A
公开(公告)日：1997-01-07
申请号：US468209
申请日：1995-06-06
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 , A61B5/055 , A61K49/00 , C07D257/00
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, radiosensitization and radiation therapy. 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。这些具有增强的稳定性的泰克萨菲瑞金属络合物可用于定位，放射增敏和放射治疗。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。

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