THERAPEUTIC METHODS AND COMPOSITIONS INVOLVING ALLOSTERIC KINASE INHIBITION
    16.
    发明申请
    THERAPEUTIC METHODS AND COMPOSITIONS INVOLVING ALLOSTERIC KINASE INHIBITION 有权
    涉及多发性激素抑制的治疗方法和组合物

    公开(公告)号:US20140296268A1

    公开(公告)日:2014-10-02

    申请号:US13577431

    申请日:2011-02-07

    CPC classification number: C07D403/12 C07D239/46

    Abstract: The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.

    Abstract translation: 本发明涉及抑制淋巴管生成,血管发生和/或肿瘤生长的方法和组合物。 所述方法包括使肿瘤与(i)稳定处于非活性状态的蛋白激酶的化合物接触,和(ii)不是处于活性状态的蛋白激酶的ATP竞争性抑制剂。

    Compositions And Methods For Reducing Cancer And Inflammation
    17.
    发明申请
    Compositions And Methods For Reducing Cancer And Inflammation 审中-公开
    用于减少癌症和炎症的组合物和方法

    公开(公告)号:US20100278837A1

    公开(公告)日:2010-11-04

    申请号:US12720348

    申请日:2010-03-09

    Abstract: This invention relates to the discovery of the convergence of diverse receptors and signaling pathways on the PI3gamma dependent activation of VLA4 (integrin a4b1). In particular, the invention relates to the role of myeloid cells in tumor inflammation and metastasis. The invention provides methods for inhibiting cancer in a subject comprising administering to a subject having cancer that comprises endothelial cells a therapeutically effective amount of a PI-3-kinase gamma inhibitor that reduces at least one of (a) adhesion of myeloid cells to the endothelial cells, (b) migration of myeloid cells into the cancer, (c) growth of the cancer, (d) activation of integrin a4b1 that is comprised on the myeloid cells, and (e) clustering of integrin a4b1 that is comprised on the myeloid cells.

    Abstract translation: 本发明涉及多种受体和信号传导途径对VLA4(整联蛋白a4b1)的PI3γ依赖性激活的收敛的发现。 特别地,本发明涉及骨髓细胞在肿瘤炎症和转移中的作用。 本发明提供了抑制受试者癌症的方法,其包括对具有包含内皮细胞癌症的受试者施用治疗有效量的PI-3-激酶γ抑制剂,其减少以下中的至少一种:(a)骨髓细胞粘附于内皮 细胞,(b)骨髓细胞迁移到癌症中,(c)癌症的生长,(d)骨髓细胞上的整合素a4b1的活化,和(e)包含在骨髓中的整联蛋白a4b1的聚集 细胞。

    Methods for inhibiting angiogenesis and tumor growth

    公开(公告)号:US07115660B2

    公开(公告)日:2006-10-03

    申请号:US10240142

    申请日:2001-03-27

    CPC classification number: A61K31/195 A61K31/165 A61K31/27

    Abstract: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-αvβ3 are inhibited by an inhibitor compound of formula (I): wherein G1 and G2 are each independently NH—C(O)—O—R1, —NH—C(O)—O—(CH2)v—(C6H4)—X3, —NH—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—O—(CH2)v—(C6H4)—X3, or NH—C(O)—CH2—(C6H4)—X3; Y1 and Y2 are each independently OH, C1–C4 alkyl, C1–C4 hydroxyalkyl, C1–C4 alkoxy, phenyl, benzyl, or NH2; R1 is C1–C4 alkyl; X1 and X2 are each independently halo or C1–C4 alkoxy; X3 is halo, nitro, C1–C4 alkyl, C1–C4 alkoxy, or C1–C4 perfluoroalkyl; Z is —C≡C—, —C6H4—, cis-CH═CH—, trans CH═CH—, cis-CH2—CH═CH—CH2—, trans —CH2—CH═CH—CH2—, 1,4-naphthyl, cis-1,3-cyclohexyl, trans-1, 3-cyclohexyl, cis-1,4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each independently an integer having a value of 0 or 1; t is an integer having a value of 0 or 1; and p, r, and v are each independently an integer having a value of 1 or 2; with provisos that when A is H, t is O; when A is a covalent bond, t is 1; when m is 0, Y1 is C1–C4 hydroxyalkyl; and when n is 0, Y2 is C1 C4 hydroxyalkyl.

    Inhibition of angiogenesis and tumor growth
    20.
    发明授权
    Inhibition of angiogenesis and tumor growth 失效
    抑制血管生成和肿瘤生长

    公开(公告)号:US06803383B2

    公开(公告)日:2004-10-12

    申请号:US10240141

    申请日:2002-09-27

    CPC classification number: C07C237/22 C07C271/22

    Abstract: Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.

    Abstract translation: 提供通式(II)抑制肿瘤生长和血管生成的化合物。 这些化合物包括与中心芳族连接核心结合的甘氨酰赖氨酸衍生物。

Patent Agency Ranking