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公开(公告)号:US09556426B2
公开(公告)日:2017-01-31
申请号:US12882484
申请日:2010-09-15
申请人: Juswinder Singh , Russell Colyn Petter , Deqiang Niu , Lixin Qiao , Arthur Kluge , Roy Lobb , Shomir Ghosh , Zhendong Zhu
发明人: Juswinder Singh , Russell Colyn Petter , Deqiang Niu , Lixin Qiao , Arthur Kluge , Roy Lobb , Shomir Ghosh , Zhendong Zhu
IPC分类号: C12N9/96 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , A61K47/48 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/22 , C07D231/12 , C07D239/42 , C07D239/48 , C07D333/68 , C07D401/12 , C07D403/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/04 , C07D498/04 , C12N9/12
CPC分类号: C07D487/04 , A61K47/545 , A61K47/62 , C07D213/72 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/22 , C07D231/12 , C07D239/42 , C07D239/48 , C07D333/68 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D495/04 , C07D498/04 , C12N9/1205 , C12N9/96
摘要: The invention relates to protein conjugates that contain a protein kinase containing a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.
摘要翻译: 本发明涉及含有ATP结合位点中含有半胱氨酸残基的蛋白激酶和与所述半胱氨酸残基共价和不可逆地结合的抑制剂的蛋白质缀合物,使得蛋白激酶的活性不可逆地被抑制。 本发明还涉及不可逆地抑制蛋白激酶的化合物。
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公开(公告)号:US20110117073A1
公开(公告)日:2011-05-19
申请号:US12882484
申请日:2010-09-15
申请人: Juswinder Singh , Russell Colyn Petter , Deqiang Niu , Lixin Qiao , Arthur Kluge , Roy Lobb , Shomir Ghosh , Zhendong Zhu
发明人: Juswinder Singh , Russell Colyn Petter , Deqiang Niu , Lixin Qiao , Arthur Kluge , Roy Lobb , Shomir Ghosh , Zhendong Zhu
IPC分类号: A61K38/45 , C12N9/12 , C07D403/14 , A61K31/497 , C07D213/66 , C07D239/42 , C07D487/04 , A61K31/502 , A61K31/44 , A61K31/506 , A61P9/00 , A61P35/00 , A61P25/28 , A61P19/00 , A61P11/06 , A61P37/02
CPC分类号: C07D487/04 , A61K47/545 , A61K47/62 , C07D213/72 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/22 , C07D231/12 , C07D239/42 , C07D239/48 , C07D333/68 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D495/04 , C07D498/04 , C12N9/1205 , C12N9/96
摘要: The invention relates to protein conjugates that contain a protein kinase containg a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.
摘要翻译: 本发明涉及蛋白质缀合物,其含有包含ATP结合位点中的半胱氨酸残基的蛋白激酶和与所述半胱氨酸残基共价和不可逆地结合的抑制剂,使得蛋白激酶的活性不可逆地被抑制。 本发明还涉及不可逆地抑制蛋白激酶的化合物。
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公开(公告)号:US20100185419A1
公开(公告)日:2010-07-22
申请号:US12554433
申请日:2009-09-04
IPC分类号: G06F17/50 , C07D209/52 , C07D215/12 , C07K14/00
摘要: The invention is an algorithm and method for designing an inhibitor that covalently binds a target polypeptide. The algorithm and method can be used to rapidly and efficiently convert reversible inhibitors into irreversible inhibitors.
摘要翻译: 本发明是用于设计共价结合靶多肽的抑制剂的算法和方法。 该算法和方法可用于快速有效地将可逆抑制剂转化为不可逆抑制剂。
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