发明申请
US20050026840A1 Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or pertidomimetics
失效
蛋白激酶抑制剂包含与肽或百日咳模拟物缀合的ATP模拟物
- 专利标题: Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or pertidomimetics
- 专利标题(中): 蛋白激酶抑制剂包含与肽或百日咳模拟物缀合的ATP模拟物
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申请号: US10764288申请日: 2004-01-23
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公开(公告)号: US20050026840A1公开(公告)日: 2005-02-03
- 发明人: Nurit Livnah , Tamar Yechezkel , Yosef Salitra , Boris Perlmutter , Onsat Ohne , Ilana Cohen , Pninit Litman , Hanoch Senderowitz
- 申请人: Nurit Livnah , Tamar Yechezkel , Yosef Salitra , Boris Perlmutter , Onsat Ohne , Ilana Cohen , Pninit Litman , Hanoch Senderowitz
- 优先权: ILIL144583 20010726
- 主分类号: C12N9/99
- IPC分类号: C12N9/99 ; A61K38/00 ; A61K47/48 ; A61K49/00 ; A61P3/04 ; A61P3/10 ; A61P7/00 ; A61P9/10 ; A61P25/00 ; A61P29/00 ; A61P35/00 ; A61P37/02 ; A61P43/00 ; C07K5/11 ; C07K7/02 ; C07K7/06 ; C07K7/08 ; A61K38/08
摘要:
The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention preferably serve as PKB inhibitors with improved activity and selectivity. Novel ATP mimetic compounds, particularly isoquinoline derivatives, conjugated with peptides or peptidomimetics are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.