JP2008509953A5 - - Google Patents

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Publication number
JP2008509953A5
JP2008509953A5 JP2007526360A JP2007526360A JP2008509953A5 JP 2008509953 A5 JP2008509953 A5 JP 2008509953A5 JP 2007526360 A JP2007526360 A JP 2007526360A JP 2007526360 A JP2007526360 A JP 2007526360A JP 2008509953 A5 JP2008509953 A5 JP 2008509953A5
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JP
Japan
Prior art keywords
compound
formula
anhydride
hydrate
preparing
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Withdrawn
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JP2007526360A
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JP2008509953A (ja
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Priority claimed from PCT/EP2005/008736 external-priority patent/WO2006018222A1/de
Publication of JP2008509953A publication Critical patent/JP2008509953A/ja
Publication of JP2008509953A5 publication Critical patent/JP2008509953A5/ja
Withdrawn legal-status Critical Current

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Claims (21)

  1. 下記式(I)の化合物の水和物。
    Figure 2008509953
  2. 化合物(I)の一水和物であることを特徴とする請求項1記載の式(I)の化合物の水和物。
  3. 化合物(I)の三水和物であることを特徴とする請求項1記載の式(I)の化合物の水和物。
  4. 下記式(I)の化合物の無水物。
    Figure 2008509953
  5. 式(I)の化合物のI型無水物として存在することを特徴とする請求項4記載の無水物。
  6. 式(I)の化合物のII型無水物として存在することを特徴とする請求項4記載の無水物。
  7. 式(I)の化合物のIII型無水物として存在することを特徴とする請求項4記載の無水物。
  8. 治療的に有効な量の請求項1〜2又は4〜6のいずれか1項に記載の式(I)の化合物の水和物又は無水物と、1種以上の医薬的に許容しうる賦形剤とを含有することを特徴とする医薬組成物。
  9. 請求項1〜2又は4〜6のいずれか1項に記載の式(I)の化合物の水和物又は無水物を含む、抗増殖活性を有する医薬組成物。
  10. 癌、感染症、炎症性疾患及び自己免疫性疾患の治療及び/又は予防用医薬組成物を調製するための、請求項1〜2又は4〜6のいずれか1項に記載の式(I)の化合物の水和物又は無水物の使用。
  11. polo様キナーゼを阻害するための医薬組成物を調製するための、請求項1〜2又は4〜6のいずれか1項に記載の式(I)の化合物の水和物又は無水物の使用。
  12. 前記polo様キナーゼがPLK-1であることを特徴とする請求項11記載の使用。
  13. 前記活性物質を経口、経腸、静脈内、腹膜投与又は注射によって投与する、請求項10〜12のいずれか1項に記載の使用。
  14. 下記式(I):
    Figure 2008509953
    の化合物の調製方法であって、下記式4:
    Figure 2008509953
    の化合物を、下記式9:
    Figure 2008509953
    の化合物と反応させることを特徴とする方法。
  15. 下記式9:
    Figure 2008509953
    の化合物の調製方法であって、下記式8:
    Figure 2008509953
    の化合物を、炭酸ジメチルによりメチル化することを特徴とする方法。
  16. 下記式3の化合物。
    Figure 2008509953
  17. 下記式4の化合物。
    Figure 2008509953
  18. 請求項2記載の式(I)の化合物の一水和物の調製方法であって、以下の工程:
    a)1−プロパノール又はイソプロパノールと水の溶媒混合物中の式(I)の化合物の溶液を調製する工程;
    b)前記溶媒混合物から前記式(I)の化合物の一水和物を結晶化する工程;及び
    c)前記式(I)の化合物の一水和物を単離する工程
    を含む、前記方法。
  19. 請求項18記載の式(I)の化合物の一水和物の調製方法であって、ステップa)において、前記式(I)の化合物の溶液が1−プロパノールと水の溶媒混合物中に調製される、前記方法。
  20. 請求項5記載の式(I)の化合物のI型無水物の調製方法であって、以下の工程:
    a)酢酸エチルとメチル-tert.-ブチルエーテル中の式(I)の化合物の溶液を調製する工程;
    b)前記溶媒混合物から前記式(I)の化合物のI型無水物を結晶化する工程;及び
    c)前記式(I)の化合物のI型無水物を単離する工程
    を含む、前記方法。
  21. 請求項6記載の式(I)の化合物のII型無水物の調製方法であって、以下の工程:
    a)酢酸エチル中の式(I)の化合物の溶液を調製する工程;
    b)酢酸エチルから前記式(I)の化合物のII型無水物を結晶化した後、ジエチルエーテルを添加する工程;及び
    c)前記式(I)の化合物のII型無水物を単離する工程
    を含む、前記方法。
JP2007526360A 2004-08-14 2005-08-11 4−[[(7r)−8−シクロペンチル−7−エチル−5,6,7,8−テトラヒドロ−5−メチル−4−6−オキソ−2−ピペリジニル]アミノ]−3−メトキシ−n−(1−メチル−4−ピペリジニル)ベンズアミドの水和物及び多形、その製造方法、並びにその薬物としての使用 Withdrawn JP2008509953A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04019366 2004-08-14
PCT/EP2005/008736 WO2006018222A1 (de) 2004-08-14 2005-08-11 Hydrate und polymorphe des 4-[[(7r)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-4-6-oxo-2-piperidinyl]amino]-3-methoxy-n-(1-methyl-4-piperidinyl)-benzamid, verfahren zu deren herstellung und deren verwendung als arzneimittel

Publications (2)

Publication Number Publication Date
JP2008509953A JP2008509953A (ja) 2008-04-03
JP2008509953A5 true JP2008509953A5 (ja) 2008-10-09

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JP2007526360A Withdrawn JP2008509953A (ja) 2004-08-14 2005-08-11 4−[[(7r)−8−シクロペンチル−7−エチル−5,6,7,8−テトラヒドロ−5−メチル−4−6−オキソ−2−ピペリジニル]アミノ]−3−メトキシ−n−(1−メチル−4−ピペリジニル)ベンズアミドの水和物及び多形、その製造方法、並びにその薬物としての使用

Country Status (19)

Country Link
US (3) US7728134B2 (ja)
EP (1) EP1778691A1 (ja)
JP (1) JP2008509953A (ja)
KR (1) KR101221864B1 (ja)
CN (1) CN101006090A (ja)
AR (1) AR052404A1 (ja)
AU (1) AU2005274340B2 (ja)
BR (1) BRPI0514351A2 (ja)
CA (1) CA2578098A1 (ja)
EA (1) EA011407B1 (ja)
EC (1) ECSP077249A (ja)
IL (1) IL181302A0 (ja)
MX (1) MX2007001854A (ja)
NO (1) NO20070752L (ja)
NZ (1) NZ553649A (ja)
PE (1) PE20060424A1 (ja)
TW (1) TWI370131B (ja)
UA (1) UA87865C2 (ja)
WO (1) WO2006018222A1 (ja)

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