JP2018109050A5 - - Google Patents

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JP2018109050A5
JP2018109050A5 JP2018034436A JP2018034436A JP2018109050A5 JP 2018109050 A5 JP2018109050 A5 JP 2018109050A5 JP 2018034436 A JP2018034436 A JP 2018034436A JP 2018034436 A JP2018034436 A JP 2018034436A JP 2018109050 A5 JP2018109050 A5 JP 2018109050A5
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Claims (5)

  1. 以下の構造を持つC−5修飾アミノカルボニルピリミジン:
    Figure 2018109050
    式中、
    R’は、−H、−Ac、−Bz−C(O)CHOCHおよび−SiMetBuからなる群より選択され;
    R”は、H、DMT、及び三リン酸(−P(O)(OH)−O−P(O)(OH)−O−P(O)(OH))又はその塩からなる群より選択され;
    Xは、−H、−OH、−OMe、−O−アリル、−F、−OEt、−OPr、−OCHCHOCH、及び−アジドからなる群より選択され;
    Rは、−(CH−RX1からなる群より選択され;
    X1は:
    Figure 2018109050
    からなる群より選択され;
    *は、RX1基の(CHへの付加点を示し;
    X4は、分岐鎖又は直鎖の低級アルキル(C1−C20)からなる群より選択され;そして、
    n=0〜10である。
  2. 以下の構造を持つC−5修飾アミノカルボニルピリミジン:
    Figure 2018109050
    式中、
    R’は、−H、−Ac、−Bz、−C(O)CH OCH および−SiMe tBuからなる群より選択され;
    R”は、H、DMT、及び三リン酸(−P(O)(OH)−O−P(O)(OH)−O−P(O)(OH) )又はその塩からなる群より選択され;
    Xは、−H、−OH、−OMe、−O−アリル、−F、−OEt、−OPr、−OCH CH OCH 、及び−アジドからなる群より選択され;
    Rは、−(CH −R X1 からなる群より選択され;
    X1 は:
    Figure 2018109050
    からなる群より選択され;
    *は、R X1 基の(CH への付加点を示し;
    X4 は、分岐鎖又は直鎖の低級アルキル(C1−C20)からなる群より選択され;そして、
    n=0〜10である。
  3. 以下の構造を持つC−5修飾アミノカルボニルピリミジンの3’−ホスホロアミダイト:
    Figure 2018109050
    式中、
    R”は、H、DMT、及び三リン酸(−P(O)(OH)−O−P(O)(OH)−O−P(O)(OH))又はその塩からなる群より選択され;
    Xは、−H、−OH、−OMe、−O−アリル、−F、−OEt、−OPr、−OCHCHOCH、及び−アジドからなる群より選択され;
    Rは、−(CH−RX1からなる群より選択され;
    X1は:
    Figure 2018109050
    及び
    Figure 2018109050
    からなる群より選択され;
    *は、RX1基の(CHへの付加点を示し;
    X4は、分岐鎖又は直鎖の低級アルキル(C1−C20)からなる群より選択され;そして、
    n=0〜10である。
  4. 以下の構造を持つC−5修飾アミノカルボニルピリミジンの5’−三リン酸:
    Figure 2018109050
    式中、
    R’は、−H、−Ac、−Bz−C(O)CHOCHおよび−SiMetBuからなる群より選択され;
    Xは、−H、−OH、−OMe、−O−アリル、−F、−OEt、−OPr、−OCHCHOCH、及び−アジドからなる群より選択され;
    Rは、−(CH−RX1からなる群より選択され;
    X1は:
    Figure 2018109050
    及び
    Figure 2018109050
    からなる群より選択され;
    *は、RX1基の(CHへの付加点を示し;
    X4は、分岐鎖又は直鎖の低級アルキル(C1−C20)からなる群より選択され;そして、
    n=0〜10である。
  5. n=0、1又は2である、請求項1から4のいずれかに記載されるC−5修飾アミノカルボニルピリミジン。
JP2018034436A 2010-04-12 2018-02-28 5位修飾ピリミジンとその使用 Active JP7025818B2 (ja)

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US32314510P 2010-04-12 2010-04-12
US61/323,145 2010-04-12

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JP2013505029A Active JP6012591B2 (ja) 2010-04-12 2011-04-12 β−NGFに対するアプタマー及びβ−NGF介在疾患及び障害の治療におけるその使用
JP2013505056A Active JP5901610B2 (ja) 2010-04-12 2011-04-12 5位修飾ピリミジンとその使用
JP2016041782A Active JP6352324B2 (ja) 2010-04-12 2016-03-04 5位修飾ピリミジンとその使用
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US (7) US20110275794A1 (ja)
EP (3) EP2558478B1 (ja)
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KR (4) KR20130043099A (ja)
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