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    Small molecule printing
    1.
    发明授权
    Small molecule printing 失效
    小分子印刷

    公开(公告)号：US06824987B1

    公开(公告)日：2004-11-30

    申请号：US09567910

    申请日：2000-05-10

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

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

    IPC分类号： G01N3353

    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的组合物，其中化合物阵列的密度为至少1000个斑点/ 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，并且所述化合物阵列的密度至少为1000个点/ cm 2。 另一方面，本发明提供了利用这些阵列来识别感兴趣的生物大分子的小分子配偶体的方法，包括：（1）提供化合物阵列，其中阵列的密度至少为1000个点/ cm 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。

    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。

    Compounds for the Treatment of Neurodegeneration and Stroke
    3.
    发明申请
    Compounds for the Treatment of Neurodegeneration and Stroke 审中-公开
    用于治疗神经退行性疾病和中风的化合物

    公开(公告)号：US20070032496A1

    公开(公告)日：2007-02-08

    申请号：US11460073

    申请日：2006-07-26

    申请人： Paul Hergenrother ,  Karson Putt ,  Xianjun Liu

    发明人： Paul Hergenrother ,  Karson Putt ,  Xianjun Liu

    IPC分类号： A61K31/50 ,  C07D237/02

    CPC分类号： C07D213/74 ,  A61K31/50 ,  C07D237/14 ,  C07D237/16 ,  C07D237/20

    摘要： Compounds and related methods for synthesis, and the use of compounds for the treatment of neurodegenerative diseases are disclosed. Compounds are disclosed in connection with PARG and/or PARP inhibition. Therapeutic applications are relevant for preventing or inhibiting neurological cell death for a variety of neurodegenerative conditions including Parkinson's disease, ischemia, and stroke. Also disclosed is a high-throughput screen for identifying compounds capable of inhibiting PARG and/or PARP.

    摘要翻译： 公开了用于合成的化合物和相关方法以及用于治疗神经变性疾病的化合物的用途。 关于PARG和/或PARP抑制公开了化合物。 治疗应用涉及预防或抑制神经细胞死亡的各种神经变性疾病，包括帕金森病，局部缺血和中风。 还公开了用于鉴定能够抑制PARG和/或PARP的化合物的高通量筛选。

    Selective Apoptotic Induction in Cancer Cells Including Activation of Procaspase-3
    5.
    发明申请
    Selective Apoptotic Induction in Cancer Cells Including Activation of Procaspase-3 审中-公开
    选择性凋亡诱导癌细胞包括激活的Procaspase-3

    公开(公告)号：US20070049602A1

    公开(公告)日：2007-03-01

    申请号：US11420425

    申请日：2006-05-25

    申请人： Paul Hergenrother ,  Karson Putt ,  Grace Chen ,  Jennifer Pearson

    发明人： Paul Hergenrother ,  Karson Putt ,  Grace Chen ,  Jennifer Pearson

    IPC分类号： A61K31/495 ,  C07D241/04

    CPC分类号： A61K31/495 ,  A61P35/00 ,  C07D295/15 ,  C12Q1/37 ,  G01N33/502 ,  G01N33/574 ,  G01N2333/96466 ,  G01N2510/00 ,  G01N2800/52

    摘要： Compounds and related methods for synthesis, and the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3, and particular embodiments are capable of direct activation of procaspase-3 and procaspase-7 to the effector forms of caspase-3 and caspase-7. Procaspase-3 levels can vary among cancer cell types; several types have relatively high levels and can have increased susceptibility to chemotherapy by compounds and methods herein. Therapeutic applications are relevant for a variety of cancer conditions and cell types, e.g. breast, lung, brain, colon, renal, adrenal, melanoma, and others.

    摘要翻译： 公开了合成的化合物和相关方法，以及化合物在治疗中用于治疗癌症和选择性诱导细胞凋亡的用途。 公开了与胱天蛋白酶（procaspase）如procaspase-3的修饰有关的化合物，特定实施方案能够将胱天蛋白酶-3和胱天蛋白酶-7的效应物形式直接活化于胱天蛋白酶-3和胱天蛋白酶-7。 Procaspase-3水平可能因癌细胞类型而异; 几种类型具有相对较高的水平，并且可以通过本文的化合物和方法增加对化学疗法的易感性。 治疗应用与各种癌症状况和细胞类型有关，例如， 乳腺，肺，脑，结肠，肾，肾上腺，黑素瘤等。

    Space environmentally durable polyimides and copolyimides
    7.
    发明申请
    Space environmentally durable polyimides and copolyimides 失效
    空间环保的聚酰亚胺和共聚酰亚胺

    公开(公告)号：US20050137383A1

    公开(公告)日：2005-06-23

    申请号：US10988407

    申请日：2004-11-08

    申请人： John Connell ,  Joseph Smith ,  Paul Hergenrother ,  Kent Watson ,  Craig Thompson

    发明人： John Connell ,  Joseph Smith ,  Paul Hergenrother ,  Kent Watson ,  Craig Thompson

    IPC分类号： C08G73/10 ,  C08G69/26

    CPC分类号： C08G73/1071 ,  C08G73/10 ,  C08G73/1014 ,  C08G73/1039 ,  C08G73/1057 ,  C08G73/1067

    摘要： Polyimides displaying low color in thin films, atomic oxygen resistance, vacuum ultraviolet radiation resistance, solubility in organic solvents in the imide form, high glass transition (Tg) temperatures, and high thermal stability are provided. The poly(amide acid)s, copoly(amide acid)s, polyimides and copolyimides are prepared by the reaction of stoichiometric ratios of an aromatic dianhydride with diamines which contain phenylphosphine oxide groups in polar aprotic solvents. Controlled molecular weight oligomeric (amide acid)s and imides can be prepared by offsetting the stoichiometry according to the Carothers equation using excess diamine and endcapping with aromatic anhydrides The polyimide materials can be processed into various material forms such as thin films, fibers, foams, threads, adhesive film, coatings, dry powders, and fiber coated prepreg, and uses include thin film membranes on antennas, second-surface mirrors, thermal optical coatings, and multi-layer thermal insulation (MLI) blanket materials.

    摘要翻译： 提供在薄膜中显示低色的聚酰亚胺，原子氧电阻，真空紫外线辐射抗性，在酰亚胺形式的有机溶剂中的溶解度，高玻璃化转变温度和高热稳定性。 聚（酰胺酸），共聚（酰胺酸），聚酰亚胺和共聚酰亚胺通过芳族二酐与极性非质子溶剂中含有苯基氧化膦基团的二胺的化学计量比的反应来制备。 控制分子量低聚（酰胺酸）和酰亚胺可以通过使用过量的二胺和用芳族酸酐封端根据Carothers方程来抵消化学计量来制备。聚酰亚胺材料可以加工成各种材料形式，例如薄膜，纤维，泡沫， 螺纹，粘合剂膜，涂料，干粉和纤维涂层预浸料，并且包括天线上的薄膜膜，第二表面反射镜，热光学涂层和多层保温（MLI）覆盖材料。