发明名称 ANTISENSE NUCLEIC ACID DERIVATIVE
摘要 <p>PURPOSE:To obtain a new derivative useful as an active ingredient of an antiviral or an antitumor agent. CONSTITUTION:The objective compound of formula I [(k) is 0-20; (m) is 0 or 1; (n) is 4-29; X is OH, methyl, etc.; Y and Z are O or S; R<1> to R<3> are H, 1-6C alkyl, etc.; D and B are nucleotide unit residues of adenine (A), guanine (G), cytosine (C) and thymine (T), with the proviso that (m) is 0 when (k) is 0 and the base sequence containing the B is a base sequence complementary to tumorous gene or viral gene] or its salt, e.g. 5'-O-(4,4'-dimethoxytrityl)- TGGGAGGTGGGTCTG. This compound of formula I is obtained by reacting, e.g. a compound of formula II (D' is base such as A, G or C) as a starting raw material with a protecting reagent, a deprotecting reagent, etc., providing a compound of formula III (A<1> is OH or mercapto-protecting group; A<2> is protecting group of OH), then reacting the resultant compound with a compound of formula IV (Hal is halogen), deprotecting the prepared compound, affording a compound of formula V, then reacting the deprotected compound with a chlorophosphoramidite and further subjecting the obtained compound to condensing reaction with an oligodeoxynucleotide(ODN) of formula VI.</p>
申请公布号 JPH05213986(A) 申请公布日期 1993.08.24
申请号 JP19910301744 申请日期 1991.11.18
申请人 SANKYO CO LTD 发明人 FURUKAWA HIDEHIKO;MOMOTA KENJI;TAKIGUCHI HIROSHI;HOTODA HITOSHI;KANEKO MASAKATSU
分类号 A61K31/70;A61K47/48;A61P31/12;A61P35/00;C07H21/00;C07H21/04;C12N15/00;C12N15/09;C12N15/113 主分类号 A61K31/70
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