Small molecule printing
    1.
    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

    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。

    Small molecule printing
    2.
    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

    IPC分类号: G01N3353

    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。

    Compositions and methods for promoting the generation of definitive endoderm
    3.
    发明授权
    Compositions and methods for promoting the generation of definitive endoderm 有权
    用于促进确定性内胚层的产生的组成和方法

    公开(公告)号:US08507274B2

    公开(公告)日:2013-08-13

    申请号:US12679406

    申请日:2010-02-05

    摘要: Certain embodiments disclosed herein are directed to a method of producing endoderm cells, such as definitive endoderm cells by exposing stem cells such as embryonic stem cells or induced pluripotent stem (iPS) cells to an effective amount of at least one compound described herein to differentiate the stem cells into the endoderm cells such as definitive endoderm cells. Differentated endoderm cells produced by the methods disclosed herein can be differentiated into pancreatic epithelium, and other endoderm derivatives such as thymus, liver, stomach, intestine and lung. Another aspect of the present invention relates to a method of producing pancreatic progenitor cells, such as Pdx1-positive pancreatic progenitor cells by exposing endoderm cells, such as definitive endoderm cells to an effective amount of at least one compound described herein to differentiate the definitive endoderm cells into Pdx1-positive pancreatic progenitor cells. Kits and compositions comprising Pdx1-positive pancreatic progenitor produced using the methods are also described.

    摘要翻译: 本文公开的某些实施例涉及通过将干细胞如胚胎干细胞或诱导的多能干(iPS)细胞暴露于有效量的本文所述的至少一种化合物来分化本发明的内胚层细胞,例如定形内胚层细胞, 干细胞进入内胚层细胞,如定形内胚层细胞。 通过本文公开的方法产生的分化的内胚层细胞可以分化成胰腺上皮和其它内胚层衍生物如胸腺,肝,胃,肠和肺。 本发明的另一方面涉及通过将内胚层细胞如定形内胚层细胞暴露于有效量的至少一种本文所述的化合物来分化定形内胚层来产生胰腺祖细胞如Pdx1阳性胰腺祖细胞的方法 细胞进入Pdx1阳性胰腺祖细胞。 还描述了使用该方法制备的包含Pdx1阳性胰腺祖细胞的组合物和组合物。

    Dioxanes and uses thereof
    8.
    发明申请
    Dioxanes and uses thereof 有权
    二恶烷及其用途

    公开(公告)号:US20080269245A1

    公开(公告)日:2008-10-30

    申请号:US11879466

    申请日:2007-07-17

    摘要: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.

    摘要翻译: 鉴于需要开发新型治疗剂及其有效的合成方法,本发明提供了新的通式(I)化合物及其药学上可接受的衍生物,其中R 1,R 2, O 2,R 3,N,X和Y如本文所定义。 本发明还提供包含式(I)化合物和药学上可接受的载体的药物组合物。 本发明还提供能够抑制组蛋白去乙酰化酶活性的化合物和用于治疗由组蛋白脱乙酰酶活性调节的病症(例如,癌症和原生动物感染)的方法,包括向有需要的受试者施用治疗有效量的式(I)化合物 。 本发明另外提供了调节Ure2p下游基因的葡萄糖敏感亚群的方法。 本发明还提供了制备本发明化合物的方法。