Meso-substituted tripyrrane compounds, compositions, and methods for
making and using the same
    24.
    发明授权
    Meso-substituted tripyrrane compounds, compositions, and methods for making and using the same 失效
    中间取代的三卤化合物,组合物及其制备和使用方法

    公开(公告)号:US5919923A

    公开(公告)日:1999-07-06

    申请号:US80989

    申请日:1998-05-19

    CPC分类号: C07D207/323

    摘要: The invention provides for tripyrrane compounds of the formula ##STR1## wherein: each Q represents, typically, an alkyl group, cycloalkyl group, aryl group, or a heteroaryl group; and each R represents hydrogen, an alkyl group, alcohol group, or a carbonyl-containing group. Additionally, there are described methods to prepare such compounds, for example, comprising the steps of:(a) reacting a compound of the formula:Q--CHO or Q--CH(OS)(OS')wherein S and S' are independently lower alkyl, an aryl group containing from 5 to 14 ring atoms, and --(CH.sub.2).sub.n -- where n=2-4;with a stoichiometric excess of a pyrrole having the formula: ##STR2## in the presence of a catalytic amount of an acid; (b) removing the unreacted pyrrole or any other solvents used in (a) by evaporation to form a residue; and(c) treating the residue to remove high molecular weight polymeric materials and the corresponding dipyrromethane by-product, leaving the desired compound.

    摘要翻译: 本发明提供下式的三吡咯化合物,其中:每个Q通常为烷基,环烷基,芳基或杂芳基; 并且每个R表示氢,烷基,醇基或含羰基。 此外,描述了制备这种化合物的方法,例如包括以下步骤:(a)使下式化合物:Q-CHO或Q-CH(OS)(OS')其中S和S'独立地 低级烷基,含有5至14个环原子的芳基和 - (CH 2)n - ,其中n = 2-4; 化学计量过量的具有下式的吡咯:在催化量的酸存在下; (b)通过蒸发除去(a)中使用的未反应的吡咯或任何其它溶剂以形成残余物; 和(c)处理残留物以除去高分子量聚合物材料和相应的二吡咯甲烷副产物,留下所需化合物。

    Porphocyanine and CNC-expanded porphyrins
    25.
    发明授权
    Porphocyanine and CNC-expanded porphyrins 失效
    芍丝苷和数控膨胀卟啉

    公开(公告)号:US5726304A

    公开(公告)日:1998-03-10

    申请号:US233632

    申请日:1994-04-26

    摘要: Compounds of the formula ##STR1## and the metalated forms and salts thereof; wherein n is an integer of 1-4; and wherein each P.sub.i is independently a pyrrole residue of the formula ##STR2## wherein each R.sub.ia and R.sub.ib is independently a noninterfering substituent, and wherein each Z.sub.i is independently a covalent bond; or is a meso bridging group of the formula ##STR3## or is an N-meso bridging group of the formula .dbd.N--.revreaction.--N.dbd.; or is a CC linkage of the formula ##STR4## or is a CNCCNC linkage of the formula ##STR5## wherein each R.sub.ic, R.sub.id, R.sub.ie, R.sub.if and R.sub.ig is independently a noninterfering substituent; or is a CNC linkage of the formula --CH.dbd.N--CH.dbd..revreaction..dbd.CH--N.dbd.CH-- wherein at least one Z.sub.i is said CNC linkage, are disclosed. These compounds are useful in photodynamic therapy and diagnosis. The metalated forms when the metal is paramagnetic are useful as MRI contrast agents.

    摘要翻译: 式“IMAGE”的化合物及其金属化形式和盐; 其中n为1-4的整数; 并且其中每个Pi独立地是下式的吡咯残基:其中每个R a和R b各自独立地为非干扰取代基,并且其中每个Z 1独立地为共价键; 或者是具有式“IMAGE”的中观桥连基团或者是式= N - > N-N的N-中间桥连基团。 或具有式“IMAGE”的isa CC键或是具有式“IMAGE”的CNCCNC连接,其中每个Ric,Rid,Rie,Rif和Rig独立地为非干扰取代基; 或者是公式CH = N-CH = - > < - = CH-N = CH-的CNC连接,其中至少一个Zi是所述CNC连接。 这些化合物可用于光动力疗法和诊断。 当金属顺磁时,金属化形式可用作MRI造影剂。

    Drug delivery systems for photodynamic therapy
    27.
    发明申请
    Drug delivery systems for photodynamic therapy 有权
    用于光动力治疗的药物输送系统

    公开(公告)号:US20070086973A1

    公开(公告)日:2007-04-19

    申请号:US11601559

    申请日:2006-11-17

    摘要: The invention is generally related to the field of photodynamic therapy by use of photosensitizers and stabilized formulations of the photosensitizers. These formulations may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer containing formulations and compositions of the invention comprise one or more block copolymers. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as photosensitizer drug delivery systems.

    摘要翻译: 本发明通常通过使用光敏剂和光敏剂的稳定配方与光动力疗法领域相关。 这些制剂可用于递送光敏剂作为药物,农业或工业剂。 含有本发明制剂和组合物的光敏剂包含一种或多种嵌段共聚物。 此外,本发明涉及用于制备和应用所述制剂和组合物作为光敏药物递送系统的方法。

    Chiral separation of benzoporphyrin derivative mono-and di-acids by laser-induced fluorescence capillary electrophoresis
    28.
    发明授权
    Chiral separation of benzoporphyrin derivative mono-and di-acids by laser-induced fluorescence capillary electrophoresis 有权
    通过激光诱导荧光毛细管电泳手性分离苯并卟啉衍生物单酸和二酸

    公开(公告)号:US06878253B2

    公开(公告)日:2005-04-12

    申请号:US10026980

    申请日:2001-12-17

    IPC分类号: G01N27/447

    CPC分类号: G01N27/44747

    摘要: A method for the separation of benzoporphyrin derivative mono and diacid (BPD-MA, BPD-DA) enantiomers by Laser-Induced Fluorescence Capillary Electrophoresis has been developed. The limits of detection are 2.06×10−6 M, and the relative standard deviation for the separation was 2.90% to 4.64%. The BPD enantiomers can be quantitatively determined in the range of 10−2 to 10−5 mg mL−1. In comparison with HPLC, CE has better resolution and efficiency. This separation method was successfully applied to the BPD enantiomers obtained from a matrix of bovine serum and from liposomally formulated material as well as from studies with rat, dog and human microsomes.

    摘要翻译: 已经开发了通过激光诱导荧光毛细管电泳分离苯并卟啉衍生物单和二酸(BPD-MA,BPD-DA)对映异构体的方法。 检测限为2.06×10 -6 M,分离相对标准偏差为2.90%〜4.64%。 BPD对映体可以在10 -2至5 -5 mg / mL范围内定量测定。 与HPLC相比,CE具有更好的分辨率和效率。 该分离方法成功应用于从牛血清基质和脂质体配制物质以及从大鼠,狗和人微粒体研究中获得的BPD对映异构体。

    Wavelength-specific photosensitive compounds and expanded porphyrin-like
compounds and methods of use
    29.
    发明授权
    Wavelength-specific photosensitive compounds and expanded porphyrin-like compounds and methods of use 失效
    波长特异性光敏化合物和扩展的卟啉化合物及其使用方法

    公开(公告)号:US5405957A

    公开(公告)日:1995-04-11

    申请号:US968966

    申请日:1992-10-30

    摘要: A group of novel expanded porphyrin-like compounds, porphacyanine (Pc) and porphacyanine-like compounds, having absorption maxima in the range of 400-850 nanometers is useful in detecting and treating targeted tissues, cells and viruses. The use of the Pc of the invention permits the irradiation to comprise wavelengths other than those absorbed by blood. The Pc of the invention may also be conjugated to target-specific moieties such as immunoglobulins or fragments thereof to target specific tissues or cells for the radiation treatment. Use of these materials permits greater depth of treatment penetration and greater specificity in targeting tissues or cells. Coupled with an appropriate paramagnetic ion or radioisotope, the Pc of the invention is suitable for use in nuclear magnetic resonance imaging and radioimaging.

    摘要翻译: 一组新的扩增卟啉样化合物,卟菲花青(Pc)和卟菲花青样化合物,其吸收最大值在400-850纳米范围内,可用于检测和治疗靶向组织,细胞和病毒。 使用本发明的Pc允许照射包括不同于血液吸收的波长的波长。 本发明的Pc也可以与靶特异性部分例如免疫球蛋白或其片段缀合以靶向用于放射治疗的特定组织或细胞。 使用这些材料允许更高的治疗深度渗透和更高的特异性靶向组织或细胞。 与适当的顺磁离子或放射性同位素相结合,本发明的Pc适用于核磁共振成像和放射成像。

    Photosensitizing Diels-Alder porphyrin derivatives
    30.
    发明授权
    Photosensitizing Diels-Alder porphyrin derivatives 失效
    光敏狄尔斯 - 阿尔德卟啉衍生物

    公开(公告)号:US5308608A

    公开(公告)日:1994-05-03

    申请号:US940673

    申请日:1992-09-04

    摘要: A group of hydro-dibenzoporphyrins prepared by di-Diels-Alder additions at the A and C rings of the appropriate divinyl porphyrins have absorption maxima in the range of 700-820 nanometers and are photosensitizing agents. These compounds are useful in treating disorders or conditions which are subject to hematoporphyrin derivative (HPD) treatment in the presence of light, or in treating biological materials generally to destroy unwanted targets such as viruses, cells and tissues. The use of the compounds of the invention permits irradiation with wavelengths other than those absorbed by blood. The compounds of the invention may also be conjugated to ligands specific for receptors or to specific immunoglobulins or fragments thereof to home to target tissues or cells for the radiation treatment. Use of these materials permits lower levels of photosensitizer to be used, thus preventing side reactions which might destroy normal tissues.

    摘要翻译: 在适当的二乙烯基卟啉的A和C环上通过二狄尔斯 - 阿尔德添加剂制备的一组氢 - 二苯并卟啉具有700-820纳米的吸收最大值,并且是光敏剂。 这些化合物可用于治疗在光存在下经受血卟啉衍生物(HPD)治疗的病症或病症,或通常用于治疗生物材料以破坏不想要的靶,例如病毒,细胞和组织。 使用本发明的化合物允许用除了被血液吸收的那些以外的波长的照射。 本发明的化合物还可以与受体特异性配体或特异性免疫球蛋白或其片段缀合到用于放射治疗的靶组织或细胞的家中。 使用这些材料可以使用较低水平的光敏剂,从而防止可能破坏正常组织的副反应。