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    Heterocyclic NF-kB Inhibitors
    8.
    发明申请
    Heterocyclic NF-kB Inhibitors 审中-公开
    杂环NF-kB抑制剂

    公开(公告)号：US20070219190A1

    公开(公告)日：2007-09-20

    申请号：US11686263

    申请日：2007-03-14

    申请人： Johann Leban ,  Daniel Vitt

    发明人： Johann Leban ,  Daniel Vitt

    IPC分类号： A61K31/538 ,  A61K31/53 ,  A61K31/52 ,  A61K31/496 ,  A61K31/473 ,  A61K31/4545 ,  C07D417/14

    CPC分类号： C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

    摘要： The present invention relates to compounds of the general formula(Ig) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, wherein R1 independently represents H, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, or heteroaryl; R2 independently represents NR3R5, R3 independently represents H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 independently represents H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 independently represents H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 independently represents H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1; q is 0, or 1; X is CO, CS, or SO2.

    摘要翻译： 本发明涉及通式（Ig）的化合物或其药学上可接受的盐与酸或碱或其药学上可接受的前药或立体异构体，其中R 1独立地表示H，烷基， 环烷基，羟基烷基，卤代烷基，卤代烷氧基，芳基或杂芳基; R 2独立地表示NR 3 R 5，R 3独立地表示H，COR 6， SO 2，SO 2，SO 2，SOR 6，SO 2，R 6， ，SO 3 R 6，烷基，环烷基，烷氧基，-NH 2，烷基胺，-NR 7 COR 卤素，-OH，-SH，烷硫基，羟基烷基，卤代烷基，卤代烷氧基，芳基或杂芳基; R 5独立地表示H，COR 6，CO 2，R 6，SOR 6， SO 2 SO 2，SO 3 S 6，烷基，环烷基烷氧基，-NH 2， 2，烷基胺，-NR 7 COR 6，卤素，-OH，-SH，烷硫基，羟基烷基，卤代烷基，卤代烷氧基，芳基或杂芳基; R 6独立地表示H，烷基，环烷基，-NH 2，烷基胺，芳基或杂芳基; R 7独立地表示H，烷基，环烷基，烷氧基，-OH，-SH，烷硫基，羟基烷基，芳基或杂芳基; p为0或1; q为0或1; X是CO，CS或SO 2。

    Method of identifying candidate molecules
    9.
    发明授权
    Method of identifying candidate molecules 有权
    识别候选分子的方法

    公开(公告)号：US06727100B1

    公开(公告)日：2004-04-27

    申请号：US09693731

    申请日：2000-10-20

    申请人： Daniel Vitt ,  Stefan Busemann ,  Ulrich Dauer

    发明人： Daniel Vitt ,  Stefan Busemann ,  Ulrich Dauer

    IPC分类号： G06F1900

    CPC分类号： G06F19/704 ,  C40B50/02 ,  G06F19/707

    摘要： A method of identifying candidate molecules expected to be biologically active comprises the following steps: Creating a set consisting of different molecules; to each of said molecules of said set, assigning a descriptor representing a predetermined number of molecular properties; mapping said set of molecules onto points of a two-dimensional grid with regard to a predetermined similarity relation of the respective assigned descriptors such that the grid distance between grid points of two molecules is a measure for the similarity of said two molecule descriptors; forming a three-dimensional surface over said grid of molecules, said surface representing the distribution of biological activity of the molecules on the grid approximatively according to a predetermined quality criterion; selecting from said three-dimensional surface candidate molecules satisfying a predetermined criterion with respect to their biological activity.

    摘要翻译： 鉴定预期具有生物活性的候选分子的方法包括以下步骤：创建由不同分子组成的组; 分配给所述组的所述分子，分配表示预定数量的分子性质的描述符; 将所述分子集合相对于各个分配的描述符的预定相似关系映射到二维网格的点，使得两个分子的网格点之间的网格距离是所述两个分子描述符的相似性的量度; 在所述分子网格上形成三维表面，所述表面根据预定质量标准近似表示网格上分子的生物活性分布; 从相对于其生物活性满足预定标准的所述三维表面候选分子进行选择。