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1.发明授权Methods of producing singlet oxygen using compounds having improved functionalization 失效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
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。
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2.发明授权Treatment of neoplastic tissue by water-soluble texaphyrine metal complexes 失效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
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。
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公开(公告)号：US5504205A
公开(公告)日：1996-04-02
申请号：US280351
申请日：1994-07-26
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。
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公开(公告)号：US5994535A
公开(公告)日：1999-11-30
申请号：US31239
申请日：1998-02-26
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 , C07F9/6524
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 is directed to methods for synthesizing water soluble hydroxy-substituted texaphyrins retaining lipophilicity. The synthesis comprises condensing a diformyltripyrrole with an ortho-phenylenediamine to give a nonaromatic texaphyrin having at least one hydroxy substituent, and oxidizing the condensation product to form an aromatic texaphyrin metal complex having at least one hydroxy substituent. These expanded porphyrin-like macrocycles may be used for magnetic resonance imaging and for photodynamic therapy in the treatment of atheroma and tumors.
摘要翻译： 本发明涉及合成保持亲油性的水溶性羟基取代的泰克萨菲瑞的方法。 合成方法包括将二甲基三吡咯与邻苯二胺缩合，得到具有至少一个羟基取代基的非芳族泰克萨菲林，并氧化缩合产物以形成具有至少一个羟基取代基的芳族泰克萨菲瑞金属络合物。 这些扩大的卟啉大环可用于磁共振成像和光动力疗法治疗动脉粥样化和肿瘤。
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公开(公告)号：US5801229A
公开(公告)日：1998-09-01
申请号：US713701
申请日：1996-09-13
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。
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公开(公告)号：US5599923A
公开(公告)日：1997-02-04
申请号：US196964
申请日：1994-02-15
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 including the addition of electron donating groups to positions 12, 15, 18 and/or 21 and/or the addition of electron withdrawing groups to positions 15 or 18 of the macrocycle. Electron donating groups at positions 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 tumor therapy and applications requiring singlet oxygen production for cytotoxicity. Electron withdrawing groups at positions 15 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 radiosensitization applications.
摘要翻译： 特拉法林金属配合物具有改进的官能化，包括向位置12,15,18和/或21添加给电子基团和/或向大环的位置15或18添加吸电子基团。 位置12,15,18和/或21处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， 磁共振成像，放射增敏，放射治疗，荧光成像，光动力学肿瘤治疗和需要单线态氧产生细胞毒性的应用。 位置15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可用于放射增敏应用。
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公开(公告)号：US5475104A
公开(公告)日：1995-12-12
申请号：US112786
申请日：1993-08-25
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 , C07F15/00
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。
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8.发明授权
公开(公告)号：US5439570A
公开(公告)日：1995-08-08
申请号：US112871
申请日：1993-08-25
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 , C07C27/00
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。
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公开(公告)号：US5256399A
公开(公告)日：1993-10-26
申请号：US880078
申请日：1992-05-07
IPC分类号： A61K41/00 , C07D487/22 , G01N24/08 , A61K31/555
CPC分类号： C07D487/22 , A61K41/0038 , A61K41/0071 , A61K41/0076 , A61K47/48069 , Y10S436/806 , Y10S514/836 , Y10T436/24
摘要： The present invention involves a novel tripyrrole dimethine-derived "expanded porphyrin" (texaphyrin), the synthesis of such compounds, their analogs or derivatives and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Metal complexes of these compounds are active as photosensitizers for the generation of singlet oxygen and thus potentially for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus and tumor cells as well. A variety of texaphyrin derivatives have been produced and many more are readily obtainable. Various metal (e.g., transition, main group, and lanthanide) complexes with the texaphyrin and texaphyrin derivatives of the present invention have unusual water solubility and stability which render them particularly useful. These metallotexaphyrin complexes have optical properties making them unique as compared to existing porphyrin-like or other macrocycles. For example, they absorb light strongly in a physiolThis invention was made in part with government support under the National Science Foundation Presidential Young Investigator Award (1986) to J. L. Sessler, grant CHE-8552768. The government has certain rights in the invention.
摘要翻译： 本发明涉及一种新型的三吡咯二聚苯胺衍生的“膨胀卟啉”（泰克萨菲林），这些化合物的合成，其类似物或衍生物及其用途。 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。 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，因此潜在地用于灭活或破坏人类免疫缺陷病毒（HIV-1），单核细胞或其它感染这种病毒和肿瘤细胞的细胞。 已经生产了多种泰克萨菲林衍生物，并且更容易获得更多。 与本发明的泰克萨菲瑞和泰克萨菲瑞衍生物的各种金属（例如，过渡态，主族和镧系元素）复合物具有不寻常的水溶性和稳定性，这使得它们特别有用。 这些金属脱甲基吡啶络合物具有光学性质，使其与现有的卟啉样或其它大环化合物相比是独特的。 例如，它们在生理上重要的区域（即690-880nm）中强烈吸收光。 这些复合物也以高产率形成长寿命的三线态，并且作为形成单线态氧的有效光敏剂。 这些性质加上它们的高化学稳定性和在极性介质如水中的可溶性，增加了它们的用途。
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10.发明授权Process for preparing expanded porphyrins: large porphyrin-like tripyrroledimethine-derived macrocycles 失效制备膨胀卟啉的方法：大卟啉样的tripyrroledimethine衍生的大环化合物
公开(公告)号：US5162509A
公开(公告)日：1992-11-10
申请号：US539975
申请日：1990-06-18
IPC分类号： A61K41/00 , C07D487/22
CPC分类号： C07D487/22 , A61K41/0038 , A61K41/0076 , A61K47/48069
摘要： The present invention involves a novel tripyrrole dimethine-derived "expanded porphyrin" (texaphyrin), the synthesis of such compounds, their analogs or derivatives and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Metal complexes of these compounds are active as photosensitizers for the generation of singlet oxygen and thus potentially for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus and tumor cells as well. A variety of texaphyrin derivatives have been produced and many more are readily obtainable. Various metal (e.g., transition, main group, and lanthanide) complexes with the texaphyrin and texaphyrin derivatives of the present invention have unusual water solubility and stability which render them particularly useful. These metallotexaphyrin complexes have optical properties making them unique as compared to existing porphyrin-like or other macrocycles. For example, they absorb light strongly in a physilogically important region (i.e. 690-880 nm). These complexes also form long-lived triplet states in high yield and act as efficient photosensitizers for the formation of singlet oxygen. These properties, coupled with their high chemical stability and appreciable solubility in polar media such as water, add to their usefulness.
摘要翻译： 本发明涉及一种新型的三吡咯二聚苯胺衍生的“膨胀卟啉”（泰克萨菲林），这些化合物的合成，其类似物或衍生物及其用途。 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。 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，因此潜在地用于灭活或破坏人类免疫缺陷病毒（HIV-1），单核细胞或其它感染这种病毒和肿瘤细胞的细胞。 已经生产了多种泰克萨菲林衍生物，并且更容易获得更多。 与本发明的泰克萨菲瑞和泰克萨菲瑞衍生物的各种金属（例如，过渡态，主族和镧系元素）复合物具有不寻常的水溶性和稳定性，这使得它们特别有用。 这些金属脱甲基吡啶络合物具有光学性质，使其与现有的卟啉样或其它大环化合物相比是独特的。 例如，它们在物理重要的区域（即690-880nm）中强烈吸收光。 这些复合物也以高产率形成长寿命的三线态，并且作为形成单线态氧的有效光敏剂。 这些性质加上它们的高化学稳定性和在极性介质如水中的可溶性，增加了它们的用途。
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