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    Small molecule printing
    2.
    发明申请
    Small molecule printing 审中-公开
    小分子印刷

    公开(公告)号：US20050095639A1

    公开(公告)日：2005-05-05

    申请号：US10998867

    申请日：2004-11-29

    申请人： Stuart L. Schreiber ,  Gavin MacBeath ,  Angela Koehler ,  Paul Hergenrother ,  Kristopher Depew

    发明人： Stuart L. Schreiber ,  Gavin MacBeath ,  Angela Koehler ,  Paul Hergenrother ,  Kristopher Depew

    IPC分类号： B01J19/00 ,  C07B61/00 ,  C07C311/49 ,  C40B30/04 ,  C40B40/04 ,  C40B50/14 ,  C40B60/14 ,  G01N33/543 ,  C12Q1/68 ,  G01N33/53

    CPC分类号： G01N31/00 ,  B01J19/0046 ,  B01J2219/00387 ,  B01J2219/00454 ,  B01J2219/00459 ,  B01J2219/005 ,  B01J2219/00533 ,  B01J2219/00605 ,  B01J2219/0061 ,  B01J2219/00612 ,  B01J2219/00626 ,  B01J2219/00637 ,  B01J2219/0072 ,  C07B2200/11 ,  C07C311/49 ,  C40B30/04 ,  C40B40/04 ,  C40B50/14 ,  C40B60/14 ,  G01N33/54353 ,  Y10S436/809

    摘要： The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with a selected chemical moiety capable of interacting with a desired chemical compound to form an attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; and (3) delivering said one or more types of compounds to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest comprising: (1) providing an array of compounds, wherein the array has a density of at least 1000 spots per cm2; (2) contacting the array with one of more types of biological macromolecules of interest; and (3) determining the interaction of specific small molecule-biological macromolecule partners.

    摘要翻译： 本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。 在一个方面，提供了一种组合物，其包含连接到固体支持物上的一种或多种类型化学化合物的阵列，其中化合物阵列的密度为至少1000个点/ cm 2。 在特别优选的实施方案中，这些化合物通过共价相互作用连接到固体支持物上。 通常，这些本发明的阵列通过以下方式产生：（1）提供固体支持物，其中所述固体支持物用能够与所需化学化合物相互作用以形成附着物的选定化学部分官能化; （2）提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; 和（3）将所述一种或多种类型的化合物递送到固体支持物，由此形成阵列，并且化合物阵列具有至少1000个点/ cm 2的密度。 另一方面，本发明提供利用这些阵列鉴定感兴趣的生物大分子的小分子伴侣的方法，包括：（1）提供化合物阵列，其中阵列的密度至少为1000个点/ 2 ; （2）使阵列与感兴趣的多种生物大分子之一接触; 和（3）确定特定小分子 - 生物大分子伴侣的相互作用。

    Analogues of N-acetylardeemin, method of preparation and uses thereof
    3.
    发明授权
    Analogues of N-acetylardeemin, method of preparation and uses thereof 失效
    N-乙酰胆碱的类似物，其制备方法及其用途

    公开(公告)号：US6147076A

    公开(公告)日：2000-11-14

    申请号：US749908

    申请日：1996-11-15

    申请人： Samuel J. Danishefsky ,  Kristopher Depew ,  Stephen P. Marsden ,  William Bornmann ,  Ting Chao Chou ,  Andrej Zatorski

    发明人： Samuel J. Danishefsky ,  Kristopher Depew ,  Stephen P. Marsden ,  William Bornmann ,  Ting Chao Chou ,  Andrej Zatorski

    IPC分类号： C07D487/14 ,  A61K31/495 ,  A61K31/505 ,  A61P35/02 ,  C07D487/22

    CPC分类号： C07D487/22

    摘要： The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 R.sub.6 and R.sub.7 are independently hydrogen, OH, NH.sub.2, SH, halogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, alkylmercapto, alkylamino, dialkylamino, alkoxy, phenyl, etc.; wherein R.sub.0 and R.sub.2 are independently hydrogen, OH, linear or branched chain alkyl, --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.2 OH, --CR.sub.3 R.sub.3 --CH(OH)R.sub.4 or --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4 ; wherein R.sub.3 and R.sub.4 are independently hydrogen, halogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, phenyl, etc.; wherein R.sub.5 is hydrogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, phenyl, etc.; and wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.9 linear or branched chain acyl, benzoyl, etc.; with the proviso that (a) when R.sub.2 is --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.2 OH, --CR.sub.3 R.sub.3 --CH(OH)R.sub.4 or --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4, then R.sub.2 is hydrogen; (b) when R.sub.0 is --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.2 OH, --CR.sub.3 R.sub.3 --CH(OH)R.sub.4 or --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4, then R.sub.2 is OH; and (c) when (i) R.sub.0 or R.sub.2 is --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4, (ii) R.sub.3 and R.sub.5 are CH.sub.3 and (iii) R.sub.4 is hydrogen, then R.sub.1, R.sub.6 and R.sub.7 are not all hydrogen. Also provided are related compounds and compositions, and methods of inhibiting the growth of multidrug resistant cells by means of MDR reversal, collateral sensitivity and quantitative synergism.

    摘要翻译： 本发明提供具有以下结构的化合物：其中R 1 R 6和R 7独立地为氢，OH，NH 2，SH，卤素，C 1 -C 9直链或支链烷基，烷基巯基，烷基氨基，二烷基氨基，烷氧基，苯基等; 其中R 0和R 2独立地是氢，OH，直链或支链烷基，-CR 3 R 3 -CH（O）CH 2，-CR 3 R 3 -CH 2 CH 3，-CR 3 R 3 -CH 2 CH 2 OH，-CR 3 R 3 -CH（OH）R 4或-CR 3 R 3 -CH = CHR 4 ; 其中R 3和R 4独立地是氢，卤素，C 1 -C 9直链或支链烷基，苯基等; 其中R5是氢，C1-C9直链或支链烷基，苯基等; 并且其中R8是氢，C1-C9直链或支链酰基，苯甲酰基等; 条件是（a）当R 2为-CR 3 R 3 -CH（O）CH 2，-CR 3 R 3 -CH 2 CH 3，-CR 3 R 3 -CH 2 CH 2 OH，-CR 3 R 3 -CH（OH）R 4或-CR 3 R 3 -CH = CHR 4时，则R2为氢; （b）当R 0是-CR 3 R 3 -CH（O）CH 2，-CR 3 R 3 -CH 2 CH 3，-CR 3 R 3 -CH 2 CH 2 OH，-CR 3 R 3 -CH（OH）R 4或-CR 3 R 3 -CH = CHR 4时，则R2是OH; 和（c）当（i）R 0或R 2为-CR 3 R 3 -CH = CHR 4时，（ⅱ）R 3和R 5为CH 3，（ⅲ）R 4为氢，则R 1，R 6和R 7不全为氢。 还提供了相关的化合物和组合物，以及通过MDR逆转，附着敏感性和定量协同作用抑制多药耐药细胞生长的方法。