Cycloheptene compounds
    3.
    发明授权
    Cycloheptene compounds 失效
    环庚烯化合物

    公开(公告)号:US06638962B2

    公开(公告)日:2003-10-28

    申请号:US10050666

    申请日:2002-01-16

    IPC分类号: A61K314174

    摘要: Compound of formula (I): wherein: X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—, Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, T represents —CH(R5)—, —N(R5)— or —N(R5)CO—, V represents hydrogen or unsubstituted or substituted aryl or heteroaryl, A2 represents [C(R6)(R′6)]p, R7 and R8 are as defined in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as farnesyl transferase inhibitors.

    摘要翻译: 式(I)的化合物:其中:X表示键或亚烷基,CO,S(O)n,-S(O)n -A1,-CO-A1-,-AS(O)n-A'1 - 或-A1-CO-A'1-,Y表示芳基,杂芳基,环烷基或杂环烷基,每个未取代或取代的,R 1,R 2,R 3和R 4各自独立地表示氢或芳基,杂芳基,环烷基或杂环烷基, 每个未取代或取代的或R 1,R 2,R 3和R 4成对取代,一起形成键,或形成稠合苯环或稠合芳族或部分不饱和杂环,T表示-CH(R 5) - , - N( R5) - 或-N(R5)CO-,V表示氢或未取代或取代的芳基或杂芳基,A2表示[C(R6)(R'6)] p,R7和R8如说明书中所定义, 并且其与药学上可接受的酸或碱的加成盐和含有它们的药物可用作法呢基转移酶抑制剂。

    Motif of the beclin protein which interacts with anti-apoptotic members of the Bcl-2 protein family, and uses
    4.
    发明授权
    Motif of the beclin protein which interacts with anti-apoptotic members of the Bcl-2 protein family, and uses 失效
    与Bcl-2蛋白家族的抗凋亡成员相互作用的beclin蛋白的主题和用途

    公开(公告)号:US07919233B2

    公开(公告)日:2011-04-05

    申请号:US11883438

    申请日:2006-01-31

    IPC分类号: G01N33/574 G01N33/53

    摘要: The invention relates to a method of identifying modulators of programmed cell death, comprising an interaction between a motif of Beclin protein and an anti-apoptotic member of the family of Bcl-2 proteins and the detection of said interaction be means of fluorescence polarization. The modulators identified on the basis of said method are administered to cancer patients in order to induce apoptotic- and/or autophagic-type programmed cell death. The invention also relates to a motif of the Beclin protein which can interact with an anti-apoptic member of the family of Bcl-2 proteins and to the use thereof in order to induce programmed cell death in a cancer patient.

    摘要翻译: 本发明涉及鉴定程序性细胞死亡调节剂的方法,其包括Beclin蛋白的基序与Bcl-2蛋白家族的抗凋亡成员之间的相互作用以及所述相互作用的检测是荧光偏振的手段。 基于所述方法鉴定的调节剂被施用于癌症患者以诱导凋亡和/或自噬型程序性细胞死亡。 本发明还涉及可与Bcl-2蛋白家族的抗宿主成分相互作用的Beclin蛋白的主题及其在癌症患者中诱导程序性细胞死亡的用途。

    Peptides Which Interact with Anti-Apoptotic Members of the BCL-2 Protein Family, and Uses
    5.
    发明申请
    Peptides Which Interact with Anti-Apoptotic Members of the BCL-2 Protein Family, and Uses 失效
    与BCL-2蛋白家族的抗凋亡成员相互作用的肽及其用途

    公开(公告)号:US20090325883A1

    公开(公告)日:2009-12-31

    申请号:US11883400

    申请日:2006-01-31

    CPC分类号: C07K14/4747

    摘要: The invention lies within the field of seeking out and identifying new peptides which interact with anti-apoptotic members of the Bcl-2 protein family, by means of the two-hybrid system.The invention relates to a method of screening and identifying modulators of the protein interaction between those new peptides and anti-apoptotic members of the Bcl-2 protein family. The modulators identified on the basis of this method are administered to patients with cancer in order to bring about apoptotic-type and/or autophagic-type programmed cell death in those patients.

    摘要翻译: 本发明在寻求和鉴定与Bcl-2蛋白家族的抗凋亡成员相互作用的新型肽的领域中,借助于双杂交系统。 本发明涉及筛选和鉴定这些新肽和Bcl-2蛋白家族的抗凋亡成员之间的蛋白质相互作用的调节剂的方法。 基于该方法鉴定的调节剂被施用于患有癌症的患者,以便在那些患者中引起凋亡型和/或自噬型程序性细胞死亡。

    Motif of the Beclin Protein Which Interacts with Anti-Apoptotic Members of the Bcl-2 Protein Family, and Uses
    9.
    发明申请
    Motif of the Beclin Protein Which Interacts with Anti-Apoptotic Members of the Bcl-2 Protein Family, and Uses 失效
    与Bcl-2蛋白家族的抗凋亡成员相互作用的Beclin蛋白的主题及其用途

    公开(公告)号:US20090099072A1

    公开(公告)日:2009-04-16

    申请号:US11883438

    申请日:2006-01-31

    摘要: The invention relates to a method of identifying modulators of programmed cell death, comprising an interaction between a motif of Beclin protein and an anti-apoptotic member of the family of Bcl-2 proteins and the detection of said interaction be means of fluorescence polarisation. The modulators identified on the basis of said method are administered to cancer patients in order to induce apoptotic- and/or autophagic-type programmed cell death. The invention also relates to a motif of the Beclin protein which can interact with an anti-apoptic member of the family of Bcl-2 proteins and to the use thereof in order to induce programmed cell death in a cancer patient.

    摘要翻译: 本发明涉及鉴定程序性细胞死亡调节剂的方法,其包括Beclin蛋白的基序与Bcl-2蛋白家族的抗凋亡成员之间的相互作用以及所述相互作用的检测是荧光偏振的手段。 基于所述方法鉴定的调节剂被施用于癌症患者以诱导凋亡和/或自噬型程序性细胞死亡。 本发明还涉及可与Bcl-2蛋白家族的抗宿主成分相互作用的Beclin蛋白的主题及其在癌症患者中诱导程序性细胞死亡的用途。