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    Preparation of prodrugs for selective drug delivery
    1.
    发明申请
    Preparation of prodrugs for selective drug delivery 审中-公开
    用于选择性药物递送的前药的制备

    公开(公告)号：US20050080260A1

    公开(公告)日：2005-04-14

    申请号：US10828558

    申请日：2004-04-21

    申请人： Randell Mills ,  Guo-Zhang Wu

    发明人： Randell Mills ,  Guo-Zhang Wu

    IPC分类号： C07C221/00 ,  C07C225/22 ,  C07D209/48 ,  C07D237/32 ,  C07D405/14 ,  C07D487/04 ,  C07D237/30 ,  C07C211/27

    CPC分类号： C07D209/48 ,  C07C221/00 ,  C07D237/32 ,  C07D405/14 ,  C07D487/04 ,  C07C225/22

    摘要： Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

    摘要翻译： 合成具有式A-B-C的化合物，其可用于例如药物递送的应用，其中A是化学发光部分，B是光致变色部分，C是其中A-B-C可以用作前药的生物活性部分。 形成前药的本发明的新型合成方法包括以下步骤：（1）形成二苯甲酮，（2）形成二芳基乙烯，（3）将邻苯二甲酰亚胺部分连接至乙烯的至少一个芳基以形成 邻苯二甲酰亚胺 - 乙烯共轭物，（4）缩合两个乙烯 - 邻苯二甲酰亚胺共轭物以形成邻苯二甲酰亚胺 - 戊二烯缀合物，（5）通过与肼反应形成本发明的载体化合物，将邻苯二甲酰亚胺转化为邻苯二甲酰肼 ）使载体化合物与药物的亲核部分反应形成相应的前药。 或者，可以通过使用卤素取代的二芳基乙烯以已知方法制备相应的阳离子无色染料样化合物来制备载体。 然后通过与亲核试剂反应保护阳离子化合物，并通过钯催化的胺化与氨基间苯二酰胺偶联以形成受保护的邻苯二甲酰亚胺 - 戊二烯缀合物。 将后者与肼回流以将其邻苯二甲酰亚胺转化为邻苯二甲酰肼并酸化以得到载体。 本发明的另一方面涉及这些化合物作为抗病毒剂用于治疗病毒感染如HIV的用途，以及用作治疗诸如肠，肺和乳腺癌的癌症的抗癌剂。

    Method and System of Computing and Rendering the Nature of the Excited Electronic States of Atoms and Atomic Ions
    3.
    发明申请
    Method and System of Computing and Rendering the Nature of the Excited Electronic States of Atoms and Atomic Ions 有权
    计算和渲染原子和原子的兴奋电子状态的方法和系统

    公开(公告)号：US20080034287A1

    公开(公告)日：2008-02-07

    申请号：US11596218

    申请日：2005-05-17

    申请人： Randell Mills

    发明人： Randell Mills

    IPC分类号： G06F17/11 ,  G06F3/14

    CPC分类号： G06F19/704 ,  G06F19/701 ,  G06F19/708 ,  Y10T436/24

    摘要： A method and system of physically solving the charge, mass, and current density functions of excited-state atoms and atomic ions using Maxwell's equations and computing and rendering the nature of excited-state electrons using the solutions. The results can be displayed on visual or graphical media. The display can be static or dynamic such that electron spin and rotation motion can be displayed in an embodiment. The displayed information is useful to anticipate reactivity and physical properties. The insight into the nature of excited-state electrons can permit the solution and display of those of other atoms and atomic ions and provide utility to anticipate their reactivity and physical properties as well as spectral absorption and emission to lead to new optical materials and light sources.

    摘要翻译： 使用麦克斯韦方程来物理地求解激发态原子和原子离子的电荷，质量和电流密度函数的方法和系统，并使用解决方案计算和渲染激发态电子的性质。 结果可以在视觉或图形媒体上显示。 显示器可以是静态的或动态的，使得在一个实施例中可以显示电子旋转和旋转运动。 显示的信息有助于预测反应性和物理性质。 对激发态电子的性质的洞察可以允许其他原子和原子离子的溶液和显示，并提供预期其反应性和物理性质以及光谱吸收和发射以产生新的光学材料和光源的效用 。

    Great-circle geodesic dome
    4.
    发明申请
    Great-circle geodesic dome 审中-公开
    大圆环测地球

    公开(公告)号：US20060135288A1

    公开(公告)日：2006-06-22

    申请号：US11296350

    申请日：2005-12-08

    申请人： Randell Mills

    发明人： Randell Mills

    IPC分类号： A63B37/12 ,  E04B7/08

    CPC分类号： E04B1/3211 ,  E04B7/105

    摘要： The present invention is a structural system and a method of fabricating the system comprised of finite elements called basis elements such as great circles or partial great circles to form a great-circle geodesic sphere, dome, or arch called a great sphere, dome, and arch, respectively. The structure is generated by forming a pattern of the basis element rotated at incremental angles about a rotational axis from an initial position to define a so-called primary component orbitsphere-cvf. The primary component orbitsphere defines a stationary pattern as well as a structural element called a secondary component orbitsphere-cvf that is constructed according to the pattern of the primary orbitsphere-cvf. The secondary component orbitsphere-cvf is initially oriented at the initial position and is incrementally rotated about the rotational axis to form the great-sphere-type structure.

    摘要翻译： 本发明是一种由诸如大圆或部分大圆之类的基本元素的有限元素构成的系统的结构体系和方法，以形成称为大球体，圆顶的大圆测地球，圆顶或拱。 拱，分别。 该结构是通过形成基本单元的图案来生成的，该图形基于从初始位置围绕旋转轴线以增量的角度旋转以限定所谓的主要分量轨道cvf。 主要组分轨道定义了固定模式以及根据主要轨道cvf的模式构建的称为次要分量轨道球的结构元素。 次级分量轨道cvf最初定位在初始位置，并且围绕旋转轴线逐渐旋转以形成大球型结构。

    Method and system of computing and rendering the nature of the chemical bond of hydrogen-type molecules and molecular ions
    7.
    发明申请
    Method and system of computing and rendering the nature of the chemical bond of hydrogen-type molecules and molecular ions 有权
    计算和呈现氢型分子和分子离子的化学键性质的方法和系统

    公开(公告)号：US20050209788A1

    公开(公告)日：2005-09-22

    申请号：US10893280

    申请日：2004-07-19

    申请人： Randell Mills

    发明人： Randell Mills

    IPC分类号： C01B3/00 ,  G01N31/00

    CPC分类号： G01N31/00 ,  C01B3/00 ,  Y10T436/24

    摘要： Provided is a system of computing and rendering a nature of a chemical bond based on physical, Maxwellian solutions of charge, mass, and current density functions of hydrogen-type molecules and molecular ions. The system includes a processor for processing Maxwellian equations representing charge, mass, and current density functions of hydrogen-type molecules and molecular ions and an output device in communication with the processor for displaying the nature of the chemical bond.

    摘要翻译： 提供了一种基于氢型分子和分子离子的电荷，质量和电流密度函数的物理，麦克斯韦解决方案来计算和呈现化学键性质的系统。 该系统包括处理器，用于处理表示氢型分子和分子离子的电荷，质量和电流密度函数的麦克斯韦方程，以及与处理器通信以显示化学键的性质的输出装置。