专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2011104055-A1 优先权日:2002-05-31 标题:Substituted n-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies 发明人:SNOW ALAN; WEIGELE MANFRED; LARSEN LESLEY; NGUYEN BETH; LAKE THOMAS; CASTILLO GERARDO; SANDERS VIRGINIA; WEAVERS REX T; LORIMER STEPHEN; LARSEN DAVID; COFFEN DAVID L; COFFEN CHARLOTTE 权利人:SNOW ALAN; WEIGELE MANFRED; LARSEN LESLEY; NGUYEN BETH; LAKE THOMAS; CASTILLO GERARDO; SANDERS VIRGINIA; WEAVERS REX T; LORIMER STEPHEN; LARSEN DAVID; COFFEN DAVID L; COFFEN CHARLOTTE 摘要:Compounds and their pharmaceutically acceptable salts, their synthesis and labeling, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided. Also provided is the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of amyloid and synuclein.
专利号:WO-2009081259-A1 优先权日:2007-12-21 标题 :Phenoxy-pyridyl derivatives 发明人:BARTA NANCY SUE; CAMPBELL BRIAN MICHAEL; DOUNAY AMY BETH; GRAY DAVID LAWRENCE FIRMAN; ZORN STEVIN HOWARD 权利人:PFIZER; BARTA NANCY SUE; CAMPBELL BRIAN MICHAEL; DOUNAY AMY BETH; GRAY DAVID LAWRENCE FIRMAN; ZORN STEVIN HOWARD 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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