ANGIOGENESIS AND VASCULAR PERMEABILITY MODULATORS AND INHIBITORS
    1.
    发明授权
    ANGIOGENESIS AND VASCULAR PERMEABILITY MODULATORS AND INHIBITORS 有权
    调制器和血管生成和血管通透性的抑制剂

    公开(公告)号:EP1250155B1

    公开(公告)日:2008-04-16

    申请号:EP00990365.9

    申请日:2000-12-22

    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, Src family tyrosine kinase protein inhibitors, and nucleic acids capable of expression of Src or modified Src protein, Yes protein or modified Yes protein, and Src family tyrosine kinase protein inhibitors, or mixtures thereof. The invention also describes methods for inhibiting VP using an inactive Src or Yes protein or a mixture thereof, or CSK protein or modified CSK protein, or nucleic acids encoding therefor, or by using chemical Src family tyrosine kinase inhibitors such as PP1, PP2, PD173955, AGL1872, PD162531, Radicicol R2146, and Geldanamycin, 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.

    METHOD OF TREATMENT OF MYOCARDIAL INFARCTION
    4.
    发明公开
    METHOD OF TREATMENT OF MYOCARDIAL INFARCTION 审中-公开
    VEFAHREN用于治疗心肌梗塞

    公开(公告)号:EP1567160A2

    公开(公告)日:2005-08-31

    申请号:EP03790028.9

    申请日:2003-11-18

    IPC分类号: A61K31/519 A61K38/45

    摘要: Myocardial infarction in a mammal is treated by administering to the mammal a therapeutically effective amount of a chemical Src family tyrosine kinase protein inhibitor and the use of such inhibitor compounds for the preparation of a medicament for treating myocardial infarction. Myocardial infarction can be prevented by administering to the mammal a prophylactic amount of the inhibitor. The inhibitor preferably is an inhibitor of Src protein selected from the group consisting of a pyrazolopyrimidine class Src family tyrosine kinase inhibitor, a macrocyclic dienone class Src family tyrosine kinase inhibitor, a pyrido[2,3-d]pyrimidine class Src family tyrosine kinase inhibitor, a 4-anilino-3-quinolinecarbonitrile class Src family tyrosine kinase inhibitor, and a mixture thereof. The Src family tyrosine kinase inhibitors can be used to prepare medicaments for the treatment of myocardial infarction. Also disclosed are articles of manufacture containing a chemical Src family tyrosine kinase inhibitor.

    METHODS FOR INHIBITING ANGIOGENESIS AND TUMOR GROWTH
    5.
    发明公开
    METHODS FOR INHIBITING ANGIOGENESIS AND TUMOR GROWTH 审中-公开
    方法用于抑制血管生成和肿瘤生长

    公开(公告)号:EP1272173A1

    公开(公告)日:2003-01-08

    申请号:EP01922734.7

    申请日:2001-03-27

    IPC分类号: A61K31/16

    摘要: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-αvβ3 are inhibited by an inhibitor compound of formula (I): wherein G?1 and G2¿ are each independently NH-C(O)-O-R1, -NH-C(O)-O-(CH¿2?)v-(C6H4)-X?3¿, -NH-C(O)-NH-(CH¿2?)v-(C6H4)-X?3¿, -O-C(O)-NH-(CH¿2?)v-(C6H4)-X?3¿,-O-C(O)-O-(CH¿2?)v-(C6H4)-X?3¿, or NH-C(O)-CH¿2?-(C6H4)-X?3; Y1 and Y2¿ are each independently OH, C¿1?-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl, benzyl, or NH2; R?1 is C¿1-C4 alkyl; X?1 and X2¿ are each independently halo or C¿1?-C4 alkoxy; X?3¿ is halo, nitro, C¿1?-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, Y?1 is C¿1-C4 hydroxyalkyl; and when n is 0, Y2 is C1 C4 hydroxyalkyl.