发明授权
US09139615B2 High-affinity, dimeric inhibitors of PSD-95 as efficient neuroprotectants against ischemic brain damage and for treatment of pain
有权
PSD-95的高亲和性二聚抑制剂作为抗缺血性脑损伤和治疗疼痛的有效神经保护剂
- 专利标题： High-affinity, dimeric inhibitors of PSD-95 as efficient neuroprotectants against ischemic brain damage and for treatment of pain
- 专利标题（中）： PSD-95的高亲和性二聚抑制剂作为抗缺血性脑损伤和治疗疼痛的有效神经保护剂
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申请号： US14116862申请日： 2012-05-11
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公开(公告)号： US09139615B2公开(公告)日： 2015-09-22
- 发明人: Anders Bach , Kristian Stromgaard
- 申请人： Anders Bach , Kristian Stromgaard
- 申请人地址： DK Copenhagen
- 专利权人： University of Copenhagen
- 当前专利权人： University of Copenhagen
- 当前专利权人地址： DK Copenhagen
- 代理机构： Gifford, Krass, Sprinkle, Anderson & Citkowski, P.C.
- 优先权： EP11165994 20110513
- 国际申请： PCT/EP2012/058762 WO 20120511
- 国际公布： WO2012/156308 WO 20121122
- 主分类号： C07K7/06
- IPC分类号： C07K7/06
摘要：
The invention provides novel potent inhibitors of the ternary protein complex of nNOS, PSD-95, and the NMDA receptor and pharmaceutical compositions comprising the inhibitors for prophylaxis and/or treatment of excitotoxic-related disease and chronic pain conditions in a subject. The inhibitors are dimeric PSD-95 inhibitors comprising a first peptide or peptide analogue linked to a second peptide or peptide analogue by a linker, wherein the first and the second peptide or peptide analogue comprise at least four amide-bonded residues having a sequence YTXV (SEQ ID NO: 5) or YSXV (SEQ ID NO: 6), wherein a. Y is selected from among E, Q, and A, or an analogue thereof, and b. X is selected from among A, Q, D, N, N-Me-A, N-Me-Q, N-Me-D, and N-Me-N or an analogue thereof, and wherein a Cell Penetrating Peptide (CPP) is linked to the linker or to an amino acid side chain of the first and second peptide or peptide analogue. The linker can be a PEG or NPEG linker.
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