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JP2005529069A5
JP2005529069A5 JP2003564039A JP2003564039A JP2005529069A5 JP 2005529069 A5 JP2005529069 A5 JP 2005529069A5 JP 2003564039 A JP2003564039 A JP 2003564039A JP 2003564039 A JP2003564039 A JP 2003564039A JP 2005529069 A5 JP2005529069 A5 JP 2005529069A5
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JP4073872B2 (ja
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Claims (31)

  1. 式(I):
    Figure 2005529069
     (式中、
    R1はヒドロキシ又はNHSO2R1A(式中、R1Aは(C1-8)アルキル、(C3-7)シクロアルキル又は{(C1-6)アルキル-(C3-7)シクロアルキル }(これらは全てハロ、シアノ、ニトロ、O-(C1-6)アルキル、アミド、アミノ又はフェニルで1〜3回適宜置換されている)であるか、又は、R1Aはハロ、シアノ、ニトロ、(C1-6)アルキル、O-(C1-6)アルキル、アミド、アミノ又はフェニルで1〜3回適宜置換されているC6又はC10アリールである)であり、
    R2はt-ブチル、-CH2-C(CH3)3又は-CH2-シクロペンチルであり、
    R3はt-ブチル又はシクロヘキシルであり、
    R4はシクロブチル、シクロペンチル又はシクロヘキシルである。)
    で表される化合物又はその医薬的に許容しうる塩。
  2. R1がヒドロキシ、NHSO2Me、NHSO2-シクロプロピル又はNHSO2Phである、請求項1に記載の式(I)で表される化合物。
  3. R1がNHSO2Me又はヒドロキシである、請求項2に記載の式(I)で表される化合物。
  4. R1がヒドロキシである、請求項3に記載の式(I)で表される化合物。
  5. R2がt-ブチル又はCH2-C(CH3)3である、請求項1〜4のいずれかに記載の式(I)で表される化合物。
  6. R2がCH2-C(CH3)3である、請求項5に記載の式(I)で表される化合物。
  7. R3がt-ブチルである、請求項1〜6のいずれかに記載の式(I)で表される化合物。
  8. R4がシクロペンチル又はシクロヘキシルである、請求項1〜7のいずれかに記載の式(I)で表される化合物。
  9. R4がシクロペンチルである、請求項8に記載の式(I)で表される化合物。
  10. R1がヒドロキシであり、R2がCH2-C(CH3)3であり、R3がt-ブチルであり、R4がシクロペンチルである、請求項1に記載の式(I)で表される化合物。
  11. R1がヒドロキシであり、R2及びR3がそれぞれt-ブチルであり、R4がシクロペンチルである、請求項1に記載の式(I)で表される化合物。
  12. R1がヒドロキシであり、R2がCH2-C(CH3)3であり、R3がシクロヘキシルであり、R4がシクロペンチルである、請求項1に記載の式(I)で表される化合物。
  13. R1がヒドロキシであり、R2がCH2-C(CH3)3であり、R3及びR4がそれぞれシクロヘキシルである、請求項1に記載の式(I)で表される化合物。
  14. R1がヒドロキシであり、R2がシクロペンチルメチルであり、R3がt-ブチルであり、R4がシクロブチルである、請求項1に記載の式(I)で表される化合物。
  15. R1がヒドロキシであり、R2がCH2-C(CH3)3であり、R3がt-ブチルであり、R4がシクロブチルである、請求項1に記載の式(I)で表される化合物。
  16. R1がNHSO2Meであり、R2がCH2-C(CH3)3であり、R3がt-ブチルであり、R4がシクロペンチルである、請求項1に記載の式(I)で表される化合物。
  17. R1がNHSO2Phであり、R2がCH2-C(CH3)3であり、R3がt-ブチルであり、R4がシクロペンチルである、請求項1に記載の式(I)で表される化合物。
  18. 医薬的に許容しうる担体媒体又は補助剤と混合した、請求項1〜17のいずれかに記載の式(I)で表される化合物又はその医薬的に許容しうる塩の抗C型肝炎ウイルス有効量を含む医薬組成物
  19. 1種以上のその他の抗HCV剤の治療的有効量を更に含む、請求項18に記載の医薬組成物。
  20. 前記その他の抗HCV剤がα-インターフェロン又はPEG化α-インターフェロンから選ばれる、請求項19に記載の医薬組成物。
  21. 前記その他の抗HCV剤がリバビリンである、請求項19又は20に記載の医薬組成物。
  22. 前記その他の抗HCV剤が、ヘリカーゼ阻害剤、NS2/3プロテアーゼ阻害剤及び配列内リボソーム進入部位(IRES)の阻害剤から選ばれる、請求項19、20又は21に記載の医薬組成物。
  23. 請求項1〜17のいずれかに記載の式(I)で表される化合物又はその医薬的に許容しうる塩の抗C型肝炎ウイルス的有効量を含む、哺乳類におけるC型肝炎ウイルス感染を治療又は予防するための医薬組成物。
  24. 請求項18〜22のいずれかに記載の組成物の抗C型肝炎ウイルス的有効量を含む、哺乳類におけるC型肝炎ウイルス感染を治療又は予防するための医薬組成物。
  25. 1種以上のその他の抗HCV剤と組み合わせた、請求項1〜17のいずれかに記載の式(I)で表される化合物又はその治療的に許容しうる塩の抗C型肝炎ウイルス的有効量を含む、哺乳類におけるC型肝炎ウイルス感染を治療又は予防するための医薬組成物。
  26. 前記その他の抗HCV剤がα-インターフェロン又はPEG化α-インターフェロンから選ばれる、請求項25に記載の医薬組成物。
  27. 前記その他の抗HCV剤がリバビリンである、請求項25又は26に記載の医薬組成物。
  28. 前記その他の抗HCV剤が、ヘリカーゼ阻害剤、NS2/3プロテアーゼ阻害剤及び配列内リボソーム進入部位(IRES)の阻害剤から選ばれる、請求項25、26又は27に記載の医薬組成物。
  29. C型肝炎ウイルス感染を治療又は予防する薬物を製造するための、請求項1〜17のいずれかに記載の式(I)で表される化合物の使用
  30. 前記その他の抗HCV剤がHCVポリメラーゼ阻害剤である、請求項19、20又は21に記載の医薬組成物。
  31. 前記その他の抗HCV剤がHCVポリメラーゼ阻害剤である、請求項25、26又は27に記載の医薬組成物。
JP2003564039A 2002-02-01 2003-01-24 Ｃ型肝炎阻害剤としての複素環式トリペプチド Expired - Fee Related JP4073872B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CA002369970A CA2369970A1 (en) 2002-02-01 2002-02-01 Hepatitis c inhibitor tri-peptides
PCT/CA2003/000091 WO2003064416A1 (en) 2002-02-01 2003-01-24 Heterocyclic tripeptides as hepatitis c inhibitors

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JP2005529069A JP2005529069A (ja) 2005-09-29
JP2005529069A5 true JP2005529069A5 (ja) 2005-12-22
JP4073872B2 JP4073872B2 (ja) 2008-04-09

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Country Status (29)

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US (1) US20030191067A1 (ja)
EP (1) EP1474423B1 (ja)
JP (1) JP4073872B2 (ja)
KR (1) KR20040081167A (ja)
CN (1) CN1304416C (ja)
AR (1) AR038382A1 (ja)
AT (1) ATE369364T1 (ja)
AU (1) AU2003202348B2 (ja)
BR (1) BR0307517A (ja)
CA (1) CA2369970A1 (ja)
CO (1) CO5611112A2 (ja)
DE (1) DE60315420T2 (ja)
EA (1) EA007739B1 (ja)
EC (1) ECSP045224A (ja)
ES (1) ES2290425T3 (ja)
HR (1) HRP20040696A2 (ja)
MX (1) MXPA04007446A (ja)
MY (1) MY133719A (ja)
NO (1) NO326421B1 (ja)
NZ (1) NZ534730A (ja)
PE (1) PE20030854A1 (ja)
PL (1) PL371283A1 (ja)
RS (1) RS67104A (ja)
SA (1) SA03240006B1 (ja)
TW (1) TWI274056B (ja)
UA (1) UA77757C2 (ja)
UY (1) UY27638A1 (ja)
WO (1) WO2003064416A1 (ja)
ZA (1) ZA200406014B (ja)

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