JP2016199546A5 - - Google Patents
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- JP2016199546A5 JP2016199546A5 JP2016089950A JP2016089950A JP2016199546A5 JP 2016199546 A5 JP2016199546 A5 JP 2016199546A5 JP 2016089950 A JP2016089950 A JP 2016089950A JP 2016089950 A JP2016089950 A JP 2016089950A JP 2016199546 A5 JP2016199546 A5 JP 2016199546A5
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- 239000008194 pharmaceutical composition Substances 0.000 claims 20
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004429 atoms Chemical group 0.000 claims 4
- 150000002678 macrocyclic compounds Chemical class 0.000 claims 4
- 125000004450 alkenylene group Chemical group 0.000 claims 3
- 125000004419 alkynylene group Chemical group 0.000 claims 3
- 150000001413 amino acids Chemical class 0.000 claims 3
- 125000000732 arylene group Chemical group 0.000 claims 3
- 230000000875 corresponding Effects 0.000 claims 3
- 125000002993 cycloalkylene group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004474 heteroalkylene group Chemical group 0.000 claims 3
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 3
- 239000000816 peptidomimetic Substances 0.000 claims 3
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 229920001184 polypeptide Polymers 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Claims (21)
- 式(I)のペプチドミメティック大環状化合物を含む医薬組成物であって:
各々のA、C、D、及びEは、独立して、天然又は非天然アミノ酸であり;
各々のBは、天然又は非天然アミノ酸、アミノ酸アナログ、
各々のR1及びR2は、独立して、−H、非置換であるかハロ−で置換されたアルキル、アルケニル、アルキニル、アリールアルキル、シクロアルキル、シクロアルキルアルキル、ヘテロアルキル、又はヘテロシクロアルキルであり;
各々のR3は、独立して、水素、非置換であるかR5で置換されたアルキル、アルケニル、アルキニル、アリールアルキル、ヘテロアルキル、シクロアルキル、ヘテロシクロアルキル、シクロアルキルアルキル、シクロアリール、又はヘテロシクロアリールであり;
各々のL1 、L3及びL4は、独立して、各々が非置換であるかR5で置換されたアルキレン、アルケニレン、アルキニレン、ヘテロアルキレン、シクロアルキレン、ヘテロシクロアルキレン、シクロアリーレン、ヘテロシクロアリーレン、又は[−R4−K−R4−]nであり;
L 2 は、各々が非置換であるかR 5 で置換されたアルキレン、アルケニレン、アルキニレン、ヘテロアルキレン、シクロアルキレン、ヘテロシクロアルキレン、又は[−R 4 −K−R 4 −]nであり;
Kは、O、S、SO、SO2、CO、CO2、又はCONR3であり;
各R4は、アルキレン、アルケニレン、アルキニレン、ヘテロアルキレン、シクロアルキレン、ヘテロシクロアルキレン、アリーレン、又はヘテロアリーレンであり;
各R5は、独立して、ハロゲン、アルキル、−OR6、−N(R6)2、−SR6、−SOR6、−SO2R6、−CO2R6、蛍光部分、放射性同位体、又は治療剤であり;
各R6は、独立して、−H、アルキル、アルケニル、アルキニル、アリールアルキル、シクロアルキルアルキル、ヘテロシクロアルキル、蛍光部分、放射性同位体、又は治療剤であり;
R7は、−H、非置換であるかR5で置換されたアルキル、アルケニル、アルキニル、アリールアルキル、シクロアルキル、ヘテロアルキル、シクロアルキルアルキル、ヘテロシクロアルキル、シクロアリール、又はヘテロシクロアリール、又はD残基を有する環状構造の一部であり;
R8は、−H、非置換であるかR5で置換されたアルキル、アルケニル、アルキニル、アリールアルキル、シクロアルキル、ヘテロアルキル、シクロアルキルアルキル、ヘテロシクロアルキル、シクロアリール、又はヘテロシクロアリール、又はE残基を有する環状構造の一部であり;
vは、1〜1000の整数であり;
wは、1〜1000の整数であり;
xは、0〜10の整数であり;
yは、0〜10の整数であり;
zは、0〜10の整数であり;そして
nは、1〜5の整数である)。 - R 1 及びR 2 の少なくとも1つは、非置換であるかハロ−で置換されたアルキル、アルケニル、アルキニル、アリールアルキル、シクロアルキル、シクロアルキルアルキル、ヘテロアルキル、又はヘテロシクロアルキルである、請求項1に記載の医薬組成物。
- R 1 及びR 2 の少なくとも1つは、非置換であるかハロ−で置換されたアルキルである、請求項1に記載の医薬組成物。
- D及びEの少なくとも1つは、式[−L 1 −S−L 2 −S−L 3 −]の追加の大環状化合物形成リンカーに結合している、請求項1に記載の医薬組成物。
- 前記ペプチドミメティック大環状化合物の二次構造は、対応する非大環状ポリペプチドの対応する二次構造より安定である、請求項1に記載の医薬組成物。
- 前記ペプチドミメティック大環状化合物は、α−ヘリックスを含む、請求項1に記載の医薬組成物。
- 前記α−ヘリックスは、1ターンから5ターンを含む、請求項4に記載の医薬組成物。
- [−L 1 −S−L 2 −S−L 3 −]の長さは、α−ヘリックス1ターンあたり約5オングストローム〜約9オングストロームである、請求項4に記載の医薬組成物。
- [−L 1 −S−L 2 −S−L 3 −]の長さは、約5個の炭素−炭素結合〜約13個の炭素−炭素結合の長さにほぼ等しい、請求項4に記載の医薬組成物。
- 前記大環状化合物は、約17個の原子〜25個の原子の環又は約29個の原子〜約37個の原子の環を含む、請求項6に記載の医薬組成物。
- x+y+zは、少なくとも3である、請求項1に記載の医薬組成物。
- L 2 は[−R 4 −K−R 4 −]nである、請求項1に記載の医薬組成物。
- R 4 はアリレンである、請求項12に記載の医薬組成物。
- KはCOである、請求項13に記載の医薬組成物。
- R 4 はフェニレンであり、且つnは1である、請求項14に記載の医薬組成物。
- L 1 及びL 3 はアルキレンである、請求項15に記載の医薬組成物。
- L 1 及びL 3 はメチレンである、請求項15に記載の医薬組成物。
- R 1 及びR 2 の少なくとも1つは水素である、請求項15に記載の医薬組成物。
- L 2 は、各々が非置換であるかR 5 で置換されたアリール、シクロアリーレン、又はヘテロシクロアリーレンである、請求項1に記載の医薬組成物。
- R 1 及びR 2 の少なくとも1つはメチルである、請求項1に記載の医薬組成物。
- 前記α−ヘリックスは、対応する非大環状ポリペプチドのα−ヘリックスより安定である、請求項6に記載の医薬組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US87481906P | 2006-12-14 | 2006-12-14 | |
US60/874,819 | 2006-12-14 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2014163070A Division JP5931975B2 (ja) | 2006-12-14 | 2014-08-08 | ビス−スルフヒドリル大環状化系 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2016199546A JP2016199546A (ja) | 2016-12-01 |
JP2016199546A5 true JP2016199546A5 (ja) | 2017-03-16 |
JP6259861B2 JP6259861B2 (ja) | 2018-01-10 |
Family
ID=39536693
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009541617A Expired - Fee Related JP5656407B2 (ja) | 2006-12-14 | 2007-12-14 | ビス−スルフヒドリル大環状化系 |
JP2014163070A Expired - Fee Related JP5931975B2 (ja) | 2006-12-14 | 2014-08-08 | ビス−スルフヒドリル大環状化系 |
JP2016089950A Expired - Fee Related JP6259861B2 (ja) | 2006-12-14 | 2016-04-27 | ビス−スルフヒドリル大環状化系 |
Family Applications Before (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009541617A Expired - Fee Related JP5656407B2 (ja) | 2006-12-14 | 2007-12-14 | ビス−スルフヒドリル大環状化系 |
JP2014163070A Expired - Fee Related JP5931975B2 (ja) | 2006-12-14 | 2014-08-08 | ビス−スルフヒドリル大環状化系 |
Country Status (10)
Country | Link |
---|---|
US (5) | US7960506B2 (ja) |
EP (2) | EP2094721B1 (ja) |
JP (3) | JP5656407B2 (ja) |
CN (2) | CN101636407B (ja) |
AU (1) | AU2007333846B2 (ja) |
BR (1) | BRPI0720306A2 (ja) |
CA (1) | CA2686827C (ja) |
HK (1) | HK1137184A1 (ja) |
IL (1) | IL199301A (ja) |
WO (1) | WO2008076904A1 (ja) |
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- 2007-12-14 EP EP07869296.9A patent/EP2094721B1/en not_active Not-in-force
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