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    System and method to measure dissociation constants
    2.
    发明授权
    System and method to measure dissociation constants 有权
    测量离解常数的系统和方法

    公开(公告)号：US08859295B2

    公开(公告)日：2014-10-14

    申请号：US13214355

    申请日：2011-08-22

    Applicant: Richard Brown ,  Burleigh Hutchins ,  Ernesto Freire

    Inventor： Richard Brown ,  Burleigh Hutchins ,  Ernesto Freire

    IPC: G01N33/566 ,  G01N35/10 ,  G01N33/68

    CPC classification number: G01N21/6486 ,  G01N1/38 ,  G01N33/6803 ,  G01N35/1065 ,  G01N35/1072

    Abstract: A system and method for determining the dissociation constant for a particular ligand is disclosed. In accordance with certain embodiments, the method creates a chemical denaturation curve of a protein in the absence of the ligand. A particular point is selected from this curve, such as the point at which 90% of the protein is unfolded. The molarity of chemical denaturant is determined for this selected point. A one point test is then performed for the protein with a predetermined concentration of the particular ligand. The fraction of protein which is unfolded at this point is then used to determine the dissociation constant for the ligand. This constant is used to quickly determine whether a particular ligard is well suited to be considered a potential drug candidate against that protein target.

    Abstract translation: 公开了用于确定特定配体的解离常数的系统和方法。 根据某些实施方案，该方法在不存在配体的情况下产生蛋白质的化学变性曲线。 从该曲线中选择特定的点，例如90％蛋白质展开的点。 测定化学变性剂的摩尔浓度。 然后对具有预定浓度的特定配体的蛋白进行一点测试。 然后将此处展开的蛋白质的级分用于确定配体的解离常数。 该常数用于快速确定特定的基因是否非常适合被认为是针对该蛋白质靶标的潜在药物候选物。

    SYSTEM AND METHOD FOR pH FORMULATIONS
    4.
    发明申请
    SYSTEM AND METHOD FOR pH FORMULATIONS 审中-公开
    pH配方的系统和方法

    公开(公告)号：US20120045846A1

    公开(公告)日：2012-02-23

    申请号：US13214353

    申请日：2011-08-22

    Applicant: Richard Brown ,  Burleigh Hutchins ,  Ernesto Freire

    Inventor： Richard Brown ,  Burleigh Hutchins ,  Ernesto Freire

    IPC: G01N21/64 ,  C09K3/00

    CPC classification number: G01N21/6486 ,  G01N1/38 ,  G01N33/6803 ,  G01N35/1065 ,  G01N35/1072

    Abstract: A system and method for creating a buffer solution having a desired pH value is disclosed. The method uses two known buffer solutions, each with predetermined pH values, and determines a mathematical relationship which defines the amount of each known buffer solution needed to create the buffer solution with the desired pH. This method can then be used to create one or more denaturation graphs, which demonstrate the stability of a protein at a given pH level.

    Abstract translation: 公开了一种用于产生具有所需pH值的缓冲溶液的系统和方法。 该方法使用两个已知的缓冲溶液，每个具有预定的pH值，并确定数学关系，其定义了产生具有所需pH的缓冲溶液所需的每种已知缓冲溶液的量。 然后可以使用该方法来产生一个或多个变性图，其证明在给定pH水平下蛋白质的稳定性。

    SYSTEM FOR CREATION OF FORMULATIONS AND GENERATION OF DENATURATION GRAPHS
    5.
    发明申请
    SYSTEM FOR CREATION OF FORMULATIONS AND GENERATION OF DENATURATION GRAPHS 有权
    制作和制作遗传图谱系统

    公开(公告)号：US20120045367A1

    公开(公告)日：2012-02-23

    申请号：US13214361

    申请日：2011-08-22

    Applicant: Richard Brown ,  Burleigh Hutchins ,  Ernesto Freire

    Inventor： Richard Brown ,  Burleigh Hutchins ,  Ernesto Freire

    IPC: G01N33/50

    CPC classification number: G01N21/6486 ,  G01N1/38 ,  G01N33/6803 ,  G01N35/1065 ,  G01N35/1072

    Abstract: A system for automatically creating a denaturation curve is disclosed. In accordance with certain embodiments, a movement system including a unit having a plurality of cannulas is used. The cannulas are in fluid communication with a fluid system, which allows the cannulas to draw in and dispense fluid. A measurement system is included which draws fluid from a well into a detector to determine a characteristic of the fluid. A controller is used to control these systems and also to create a denaturation graph from the measured characteristics. In another embodiment, a plurality of formulations may be created using the system.

    Abstract translation: 公开了一种自动生成变性曲线的系统。 根据某些实施例，使用包括具有多个插管的单元的移动系统。 插管与流体系统流体连通，这允许插管吸入和分配流体。 包括测量系统，其将流体从井抽入检测器以确定流体的特性。 控制器用于控制这些系统，并且还可以根据测量的特征创建变性图。 在另一个实施方案中，可以使用该系统产生多种制剂。

    Beta-lactamase inhibitors and methods of use thereof
    6.
    发明申请
    Beta-lactamase inhibitors and methods of use thereof 有权
    β-内酰胺酶抑制剂及其使用方法

    公开(公告)号：US20050124580A1

    公开(公告)日：2005-06-09

    申请号：US10866179

    申请日：2004-06-10

    Applicant: Ernesto Freire ,  Patrick Ross ,  Yingxin Xiao ,  Raphael Ottenbrite ,  Irene Luque

    Inventor： Ernesto Freire ,  Patrick Ross ,  Yingxin Xiao ,  Raphael Ottenbrite ,  Irene Luque

    IPC: A61K20060101 ,  A61K31/381 ,  A61K31/69 ,  C07D327/04

    CPC classification number: A61K31/381 ,  C07D213/63 ,  C07D327/04 ,  C07F5/025 ,  G01N2800/52

    Abstract: The invention provides novel non-β-lactam inhibitors of β-lactamases. In particular, the invention provides boronic acid-based compounds set forth in the specification. These compounds may be used with β-lactam antibiotics to bacterial infection, particularly, β-lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial agents by themselves. The invention further provides methods of using such compounds. Finally, the invention provides a pharmaceutical composition comprising these compounds.

    Abstract translation: 本发明提供了β-内酰胺酶的新型非β-内酰胺抑制剂。 特别地，本发明提供了说明书中阐述的基于硼酸的化合物。 这些化合物可以与β-内酰胺抗生素一起用于细菌感染，特别是β-内酰胺抗生素抗性细菌感染。 这些化合物本身也是抗菌剂。 本发明还提供了使用这些化合物的方法。 最后，本发明提供包含这些化合物的药物组合物。

    Inhibitors of plasmepsins
    7.
    发明申请
    Inhibitors of plasmepsins 有权
    血浆素抑制剂

    公开(公告)号：US20050037953A1

    公开(公告)日：2005-02-17

    申请号：US10471655

    申请日：2002-03-15

    Applicant: Ernesto Freire ,  Azia Nezami ,  Yoshiaki Kiso

    Inventor： Ernesto Freire ,  Azia Nezami ,  Yoshiaki Kiso

    IPC: A61K31/198 ,  A61K31/366 ,  A61K31/426 ,  A61K38/05 ,  A61K38/06 ,  C07C237/20 ,  A61K38/00

    CPC classification number: C07C237/20 ,  A61K31/198 ,  A61K31/366 ,  A61K31/426 ,  A61K38/05 ,  A61K38/06 ,  Y02A50/411

    Abstract: Compounds and methods for the inhibition of anti-malarial target aspartyl protease plasmepsins (e.g. Plasmepsin I, Plasmepsin II, Plasmepsin IV and HAP) are provided. The compounds are based on allophenylnorstatine substituted at positions R1-R4, such that R1 is isoquinoline, carboxyl, naphtalene, phenyl, phenol, benzene, an amino acid, and derivatives thereof; R2 and R3 are aliphatic groups; and R4 is indan, naphthalene, benzylamine, phenyl, phenol, cyclopentane, tert-butylamine, or derivatives thereof. The compounds may be used to inhibit Plasmepsin II, to kill malarial parasites, and to treat malaria in a patient. Certain of the substituted allophenylnorstatine-based compounds also exhibit inhibitory activity against Cathepsin D.

    Abstract translation: 提供了用于抑制抗疟疾靶标天冬氨酰蛋白酶plasmepsin（例如Plasmepsin I，Plasmepsin II，Plasmepsin IV和HAP）的化合物和方法。 这些化合物基于在R1-R4位置被取代的异氰酸酯基，其中R 1是异喹啉，羧基，萘，苯基，苯酚，苯，氨基酸及其衍生物; R2和R3是脂族基团; R4为茚满，萘，苄胺，苯基，苯酚，环戊烷，叔丁胺或其衍生物。 该化合物可用于抑制Plasmepsin II，杀死疟疾寄生虫，并治疗患者的疟疾。 某些取代的基于异氰酸酯基的化合物也表现出对组织蛋白酶D的抑制活性。

    Method for the prediction of binding targets and the design of ligands
    8.
    发明授权
    Method for the prediction of binding targets and the design of ligands 失效
    结合靶的预测方法和配体的设计

    公开(公告)号：US06226603B1

    公开(公告)日：2001-05-01

    申请号：US09089097

    申请日：1998-06-02

    Applicant: Ernesto Freire ,  Irene Luque

    Inventor： Ernesto Freire ,  Irene Luque

    IPC: G06N312

    CPC classification number: G06F19/16 ,  C07K1/00 ,  C07K2299/00 ,  G06F19/18

    Abstract: A computer-based method for the identification of binding targets in proteins and other macromolecules. More particularly, the invention includes an algorithm aimed at predicting binding targets in proteins. This algorithm, named Woolford, requires knowledge of the high resolution structure of the protein but no knowledge of the location or identity of natural binding sites or ligands. Binding targets in the protein are identified and classified according to their expected optimal affinities. Binding targets can be located at the protein surface or at internal surfaces that become exposed as a result of partial unfolding, conformational changes, subunit dissociation, or other events. The entire protein is mapped according to the binding potential of its constituent atoms. Once binding targets are identified, optimal ligands are designed and progressively built by the addition of individual atoms that complement structurally and energetically the selected target.

    Abstract translation: 一种基于计算机的方法，用于鉴定蛋白质和其他大分子中的结合目标。 更具体地，本发明包括旨在预测蛋白质中的结合靶的算法。 该名称为Woolford的算法需要知道蛋白质的高分辨率结构，但不知道天然结合位点或配体的位置或身份。 根据其预期的最佳亲和力来鉴定和分类蛋白质中的结合目标。 结合靶可以位于蛋白质表面或由于部分展开，构象变化，亚基解离或其他事件而变得暴露的内表面。 根据其组成原子的结合电位对整个蛋白进行定位。 一旦确定了结合目标，则通过添加在结构上和能量上补充所选靶的各个原子来设计和逐步构建最佳配体。

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