发明授权
US07175828B2 Modulators of β-amyloid peptide aggregation comprising D-amino acids
失效
包含D-氨基酸的β-淀粉样肽聚集体的调节剂
- 专利标题: Modulators of β-amyloid peptide aggregation comprising D-amino acids
- 专利标题(中): 包含D-氨基酸的β-淀粉样肽聚集体的调节剂
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申请号: US10677076申请日: 2003-09-30
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公开(公告)号: US07175828B2公开(公告)日: 2007-02-13
- 发明人: Mark A. Findeis , Malcolm L. Gefter , Gary F. Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
- 申请人: Mark A. Findeis , Malcolm L. Gefter , Gary F. Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
- 申请人地址: US MA Waltham
- 专利权人: Praecis Pharmaceuticals, Inc.
- 当前专利权人: Praecis Pharmaceuticals, Inc.
- 当前专利权人地址: US MA Waltham
- 代理机构: Lahive & Cockfield, LLP
- 代理商 Giulio A. DeConti, Jr.; Maria Laccotripe Zacharakis
- 主分类号: A61K38/08
- IPC分类号: A61K38/08 ; A61K38/10 ; A61K38/16 ; C07K7/06
摘要:
Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3–5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a β amyloid peptide, preferably a retro-inverso isomer of Aβ17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
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