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    • 35. 发明授权
    • Synthesis of long wavelength absorbing photosensitizers
    • 合成长波吸收光敏剂
    • US6093739A
    • 2000-07-25
    • US196761
    • 1998-11-20
    • Claire K. JohnsonDavid Dolphin
    • Claire K. JohnsonDavid Dolphin
    • C07D471/22A61K31/40
    • C07D471/22
    • The present invention provides for novel therapeutic macrocycle compounds useful in photodynamic therapy that are based on the chlorin ring system. The macrocycle compounds have, in many cases, wavelengths of activation at about 670 nm, characteristics of chlorins, and are stabilized against oxidation by the attachment to the chlorin ring of a structure that comprises one or more exocyclic rings that contribute at least one nitrogen atom. Protonation or covalent modification of this nitrogen atom, or other covalent modification of the one or more exocyclic rings permits optimization of pharmacalogically relevant properties including, for example, solubility. Representative chlorins include the pyridochlorins depicted as follows ##STR1##
    • 本发明提供了用于基于二氢卟酚环系统的光动力疗法中的新型治疗性大环化合物。 在大多数情况下,大环化合物在大约670nm具有激活波长,二氢卟酚的特征,并且通过连接到含有一个或多个有助于至少一个氮原子的环外环的结构的二氢卟酚环而稳定化 。 该氮原子的质子化或共价修饰或一个或多个环外环的其它共价修饰允许优化药理学相关性质,包括例如溶解度。 代表性的二氢卟酚包括如下所示的吡啶二氢卟酚
    • 36. 发明授权
    • 5,15-diarylbenzochlorin-7-one compounds
    • 5,15-二芳基苯并三氮杂-7-酮化合物
    • US5656756A
    • 1997-08-12
    • US235174
    • 1994-04-29
    • David DolphinRoss Boyle
    • David DolphinRoss Boyle
    • C07D487/22A61K31/40
    • C07D487/22
    • A novel 5,15-diarylbenzochlorin-7-one compound having the formula (I) or (II): ##STR1## wherein M is a metal. A novel method for synthesizing the compound of formula (I) comprises the steps of:a. cyclizing a meso-(formylvinyl) 5,15-diarylporphyrin to form a cyclization reaction mixture, andb. oxidizing said reaction mixture to form the 5,15-diarylbenzochlorin-7-one of formula (I).A novel method for synthesizing the compound of formula (II) comprises the cyclizing and oxidizing steps listed above and, either prior to or after the oxidizing step, adding the step of demetallating the compound.
    • 具有式(I)或(II)的新的5,15-二芳基苯并二氢卟酚-7-酮化合物:其中M是金属。 合成式(I)化合物的新方法包括以下步骤:a。 环化内消旋(甲酰基乙烯基)5,15-二芳基卟啉以形成环化反应混合物,和b。 氧化所述反应混合物以形成式(I)的5,15-二芳基苯并二氢吡喃-7-酮。 用于合成式(II)化合物的新方法包括上述环化和氧化步骤,并且在氧化步骤之前或之后,加入脱金属化合物的步骤。
    • 40. 发明授权
    • Meso-substituted tripyrrane compounds, compositions, and methods for
making and using the same
    • 中间取代的三卤化合物,组合物及其制备和使用方法
    • US6022981A
    • 2000-02-08
    • US313030
    • 1999-05-17
    • Christian BrucknerRoss W. BoyleDavid Dolphin
    • Christian BrucknerRoss W. BoyleDavid Dolphin
    • A61K31/409A61K41/00A61K49/00A61P43/00C07D207/32C07D207/323C07D487/22C09B57/00C07D403/06
    • C07D207/323
    • 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.
    • 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。