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    • 4. 发明专利
    • Antisense oligonucleotides directed against connective tissue growth factor and uses thereof
    • NZ601660A
    • 2014-05-30
    • NZ60166009
    • 2009-08-25
    • EXCALIARD PHARMACEUTICALS INCISIS PHARMACEUTICALS INC
    • DEAN NICHOLAS MFOULKES J GORDONO’DONNELL NIALLBENNETT C FRANKFREIER SUSAN M
    • A61K48/00C12N15/113
    • 601660 Disclosed is a compound which comprises a modified oligonucleotide consisting of 12 -30 linked nucleosides, at least a 12 nucleobase sequence portion of which is complementary to nucleotides within the region selected from nucleotides 718-751, 1388-1423, 2728-2797, 1394-1423, 1659-1689, 2100-2129 and 1399-1423 of SEQ ID NO: 9, wherein the modified oligonucleotide comprises (a) a gap segment consisting of linked deoxynucleosides; (b) a 5’ wing segment consisting of linked modified nucleosides; and (c) a 3’ wing segment consisting of linked modified nucleosides; wherein the gap segment is positioned between the 5’ wing segment and the 3’ wing segment and wherein each modified nucleoside within each wing segment comprises a modified sugar. Further disclosed is a compound which comprises a modified oligonucleotide consisting of 12 - 30 linked nucleosides, at least a 12 nucleobase sequence portion of which is complementary to nucleotides within the region selected from nucleotides 1457-1689, 2120-2147,2267-2301,553-611,1469-1508 and 1559-1605 of SEQ ID NO: 9, wherein the modified oligonucleotide comprises (a) a gap segment consisting of linked deoxynucleosides; (b) a 5’ wing segment consisting of linked modified nucleosides; and (c) a 3’ wing segment consisting of linked modified nucleosides; wherein the gap segment is positioned between the 5’ wing segment and the 3’ wing segment and wherein each modified nucleoside within each wing segment comprises a modified sugar; and wherein the compound demonstrates at least 60% inhibition in a human connective tissue growth factor expression assay.