Methods for inhibiting angiogenesis and tumor growth
    1.
    发明授权
    Methods for inhibiting angiogenesis and tumor growth 有权
    抑制血管生成和肿瘤生长的方法

    公开(公告)号:US07368478B2

    公开(公告)日:2008-05-06

    申请号:US11439918

    申请日:2006-05-24

    摘要: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-αvβ3 are inhibited by an inhibitor compound of formula: wherein G1 and G2 are each independently —NH—C(O)—O—(CH2)v—(C6H4)—X3 ; Y1 and Y2 are each independently —OH or C1-C4 alkoxy; X1 and X2 are each independently halo or C1-C4 alkoxy; X3 is fluoro, 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 1; t is an integer having a value of 0 or 1; p and r are each 2, and v is 1; with the proviso that when A is H, t is 0, and when A is a covalent bond, t is 1.

    摘要翻译: 血管生成,肿瘤生长和金属蛋白酶2(MMP2)与整联蛋白α3β3的相互作用被下式的抑制剂化合物抑制:其中G 1, (O)-O-(CH 2)2 - (C 1 -C 6) 6 H 4)-X 3; Y 1和Y 2各自独立地为-OH或C 1 -C 4烷氧基; X 1和X 2各自独立地为卤素或C 1 -C 4烷氧基; X 3是氟,硝基,C 1 -C 4烷基,C 1 -C 4 烷氧基或C 1 -C 4全氟烷基; Z是-C≡C - , - C 6 H 4 - ,顺式-CH-CH-,反式-CH-CH-,顺式-CH 2 -CH-CH-CH 2 - ,反式-CH 2 -CH-CH 2 CH 2 - ,1,4 顺式-1,3-环己基,反式-1,3-环己基,顺式-1,4-环己基或反式-1,4-环己基; A是H或共价键; m和n分别为1; t是值为0或1的整数; p和r各自为2,v为1; 条件是当A为H时,t为0,当A为共价键时,t为1。

    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

    摘要: 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
    3.
    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

    IPC分类号: A01N3718

    CPC分类号: C07C237/22 C07C271/22

    摘要: 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.

    摘要翻译: 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。

    Methods and compositions useful for modulation of angiogenesis using tyrosine kinase Src
    4.
    发明授权
    Methods and compositions useful for modulation of angiogenesis using tyrosine kinase Src 失效
    使用酪氨酸激酶Src调节血管发生的方法和组合物

    公开(公告)号:US07585841B2

    公开(公告)日:2009-09-08

    申请号:US11230995

    申请日:2005-09-19

    IPC分类号: A61K38/00

    摘要: The present invention describes methods for modulating angiogenesis in tissues using Src protein, modified Src protein, and nucleic acids encoding for such. Particularly the invention describes methods for inhibiting angiogenesis using an inactive Src protein, or nucleic acids encoding therefor, or for potentiating angiogenesis using an active Src protein, or nucleic acids encoding therefor. The invention also describes the use of gene delivery systems for providing nucleic acids encoding for the Src protein, or modified forms thereof.

    摘要翻译: 本发明描述了使用Src蛋白质,修饰的Src蛋白质和编码这种蛋白质的核酸调节组织中血管生成的方法。 特别地,本发明描述了使用无活性Src蛋白或其编码的核酸抑制血管生成或使用活性Src蛋白增强血管发生或编码其的核酸抑制血管发生的方法。 本发明还描述了使用基因递送系统提供编码Src蛋白的核酸或其修饰形式。

    Methods and compositions useful for modulation of angiogenesis and vascular permeability using SRC or Yes tyrosine kinases
    6.
    发明授权
    Methods and compositions useful for modulation of angiogenesis and vascular permeability using SRC or Yes tyrosine kinases 有权
    用于调节血管生成和血管通透性的方法和组合物使用SRC或是酪氨酸激酶

    公开(公告)号:US06685938B1

    公开(公告)日:2004-02-03

    申请号:US09470881

    申请日:1999-12-22

    IPC分类号: A61K3845

    摘要: The present invention describes methods for modulating vascular permeability (VP) in tissues using Src or modified Src protein, Yes protein or modified Yes protein, or mixtures thereof, and nucleic acids capable of expression such proteins. In particular, the invention describes methods for inhibiting VP using an inactive Src or Yes protein or a mixture thereof, or nucleic acids encoding therefor, or for potentiating VP using an active, Src or Yes protein or a mixture thereof, or nucleic acids encoding therefor. Related compositions and articles of manufacture are also disclosed.

    摘要翻译: 本发明描述了使用Src或修饰的Src蛋白质,Yes蛋白质或修饰的Yes蛋白质或其混合物以及能够表达这种蛋白质的核酸调节组织中血管通透性(VP)的方法。 特别地,本发明描述了使用无活性Src或Yes蛋白质或其混合物或其编码的核酸抑制VP或使用活性,Src或Yes蛋白质或其混合物或其编码的核酸来增强VP的方法 。 还公开了相关的组合物和制品。