JP2014518212A5 - 化合物及び組成物 - Google Patents

化合物及び組成物 Download PDF

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JP2014518212A5
JP2014518212A5 JP2014515939A JP2014515939A JP2014518212A5 JP 2014518212 A5 JP2014518212 A5 JP 2014518212A5 JP 2014515939 A JP2014515939 A JP 2014515939A JP 2014515939 A JP2014515939 A JP 2014515939A JP 2014518212 A5 JP2014518212 A5 JP 2014518212A5
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compound according
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JP2014518212A (ja
JP6068457B2 (ja
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Priority claimed from PCT/US2012/042178 external-priority patent/WO2012174064A1/en
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  1. 式(1)の構造を有する化合物:
    Figure 2014518212
    Xは、1)C(R)(R)、又は2)酸素であり;
    Tは、1)CH、2)CHCH、又は3)存在せず;
    とRは、独立して、1)−CH、又は2)−CHCHであり;
    は、1)水素、2)−CH、又は3)−CHCHであり;
    は、1)水素、又は2)−CHであり;
    とRは、それぞれ独立して、1)水素、2)−CH、又は3)−CHCHであり;
    とRは、それぞれ独立して、1)水素、2)重陽子、3)ヒドロキシル、4)フルオロ、5)アルコキシ、6)低級アルキル、又は7)低級ハロアルキルであり;
    とRは、オキソ(=O)として統合してもよく、
    Bは、1)
    Figure 2014518212
    Figure 2014518212
    Figure 2014518212
    7)シクロアルキル、又は8)低級ハロアルキルであり;
    、R、R、R、及びRは、それぞれ独立して、1)水素、2)低級アルキル、3)低級ハロアルキル、4)ハロゲン、5)ニトロ、6)ヒドロキシ、7)アルコキシ、8)ニトリル、9)カルボキシアミド、10)アリールカルボニル、11)カルバモイル、12)アミジル、13)アミノ、14)アルキルカルボニル、15)ウレア、又は16)−C(NOH)NHであり;
    、R、及びRは、1)−CR、又は2)窒素であるが、R、R、及びRの少なくとも1つは窒素であり;
    Zは、1)酸素、又は2)硫黄である;
    並びに、これらの薬学的に許容される塩、溶媒和物、及び水和物。
  2. XがCRである請求項1に記載の化合物。
  3. とRがオキソ(=O)として統合した請求項2に記載の化合物。
  4. がヒドロキシルで、Rが水素である請求項2に記載の化合物。
  5. とRが、それぞれ独立してメチル又はエチルである請求項2に記載の化合物。
  6. とRが、それぞれメチルである請求項2に記載の化合物。
  7. が水素又はメチルである請求項2に記載の化合物。
  8. がメチルである請求項7に記載の化合物。
  9. とRの双方がメチルである請求項1に記載の化合物。
  10. がメチル又は水素である請求項1に記載の化合物。
  11. がメチルである請求項10に記載の化合物。
  12. TがCHである請求項1に記載の化合物。
  13. とRが独立して水素又はメチルである請求項1に記載の化合物。
  14. とRがそれぞれ水素である請求項13に記載の化合物。
  15. 薬学的に許容される担体中に請求項1に記載の化合物の治療的有効量を含む組成物
  16. 前記化合物が(4−(トリフルオロメチル)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノン(化合物16)である請求項1に記載の化合物
  17. 前記化合物が(4−(トリフルオロメトキシ)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノン(化合物29)である請求項1に記載の化合物
  18. 前記化合物が(S)−(4−(トリフルオロメチル)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノール(化合物15)である請求項1に記載の化合物
  19. 前記化合物が(3−フルオロ−4−(トリフルオロメチル)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノン(化合物74)である請求項1に記載の化合物
  20. 前記化合物が(4−フルオロフェニル)((1R,6S)−1,2,2,6−テトラメチルシクロヘキシル)メタノン(化合物62)である請求項1に記載の化合物
  21. 前記化合物が2−(トリフルオロメチル)−4−((1R,6S)−2,2,6−トリメチルシクロヘキサンカルボニル)ベンゾニトリル(化合物61)である請求項1に記載の化合物
  22. 前記化合物が2−フルオロ−4−((1R,6S)−2,2,6−トリメチルシクロヘキサンカルボニル)ベンゾニトリル(化合物45)である請求項1に記載の化合物
JP2014515939A 2011-06-14 2012-06-13 化合物及び組成物 Expired - Fee Related JP6068457B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161520709P 2011-06-14 2011-06-14
US61/520,709 2011-06-14
US201161562689P 2011-11-22 2011-11-22
US61/562,689 2011-11-22
US201161564453P 2011-11-29 2011-11-29
US61/564,453 2011-11-29
PCT/US2012/042178 WO2012174064A1 (en) 2011-06-14 2012-06-13 Opsin-binding ligands, compositions and methods of use

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JP2014518212A JP2014518212A (ja) 2014-07-28
JP2014518212A5 true JP2014518212A5 (ja) 2015-08-06
JP6068457B2 JP6068457B2 (ja) 2017-01-25

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US (3) US9133082B2 (ja)
EP (1) EP2720539B1 (ja)
JP (2) JP6068457B2 (ja)
CN (2) CN106431988A (ja)
AU (2) AU2012271728B2 (ja)
BR (1) BR112013032199A2 (ja)
CA (1) CA2838974A1 (ja)
EA (2) EA026121B1 (ja)
HK (1) HK1199793A1 (ja)
WO (1) WO2012174064A1 (ja)

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