JP2021001188A - App選択的bace阻害のための組成物およびそのための使用 - Google Patents
App選択的bace阻害のための組成物およびそのための使用 Download PDFInfo
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- JP2021001188A JP2021001188A JP2020152650A JP2020152650A JP2021001188A JP 2021001188 A JP2021001188 A JP 2021001188A JP 2020152650 A JP2020152650 A JP 2020152650A JP 2020152650 A JP2020152650 A JP 2020152650A JP 2021001188 A JP2021001188 A JP 2021001188A
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- secretase
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- 0 CN(C1=O)C(N)=NC1(*)c1cc(*)c(*)cc1 Chemical compound CN(C1=O)C(N)=NC1(*)c1cc(*)c(*)cc1 0.000 description 2
- ZGTOUHBXYWEGQP-UHFFFAOYSA-N Cc1cc(C(C(CC2)CCC2c2cncnc2)(C(N2C)=O)N=C2N=C)ccc1OC(F)F Chemical compound Cc1cc(C(C(CC2)CCC2c2cncnc2)(C(N2C)=O)N=C2N=C)ccc1OC(F)F ZGTOUHBXYWEGQP-UHFFFAOYSA-N 0.000 description 1
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/70—One oxygen atom
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- A61K31/4164—1,3-Diazoles
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- A61K31/4164—1,3-Diazoles
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Abstract
Description
(式中、R2およびR3は上記で定められるとおりであり、R4は、場合によってはハロゲン化されるピリジニル、ピリミジニルまたはオキサゾリルであり、R4は、ハロゲン(例えばF)である。)に従う構造を有し得る。特に好ましい態様において、本化合物は、式IV〜XII:
の何れか1つに従う構造を有する。
合成プロトコール:
企図される化合物は、当技術分野で公知の様々な方法を使用して調製され得、これらは全て本明細書中での使用に適切とみなされる。さらなる特に適切な方法は、一般に、様々な置換基を適応させるために僅かに改変を行い、米国特許出願公開第2014/0371283号明細書に記載のような合成プロトコールに従う。
Claims (24)
- R4がハロゲン化ピリジニルである、請求項1に記載の化合物。
- R4がピリミジニルである、請求項1に記載の化合物。
- R4がオキサゾリルである、請求項1に記載の化合物。
- R2がハロゲン化アルコキシ基である、請求項1〜4の何れか1項に記載の化合物。
- R3がHまたは任意選択でハロゲン化されていてもよい低級アルキルである、請求項1〜4の何れか1項に記載の化合物。
- R2がハロゲン化アルコキシ基である、請求項1に記載の化合物。
- R3がHである、請求項1に記載の化合物。
- R3が、ハロゲン化された低級アルキルである、請求項1に記載の化合物。
- 薬学的に許容可能な担体と組み合わせて請求項1〜16の何れか1項に記載の化合物を含む、医薬組成物。
- 患者に投与された場合に患者においてBACEを阻害するのに有効な量で前記化合物が存在する、請求項17に記載の医薬組成物。
- 経口投与用または注射用に製剤化されている、請求項17または請求項18に記載の医薬組成物。
- 神経学的状態の処置に適切な第2の医薬品をさらに含む、請求項17に記載の医薬組成物。
- 前記神経学的状態がアルツハイマー病である、請求項20に記載の医薬組成物。
- 薬剤の製造における、請求項1〜16の何れか1項に記載の化合物の使用。
- 前記薬剤が神経変性疾患の処置のためのものである、請求項22に記載の使用。
- 前記薬剤が患者におけるBACE活性の低下のためのものである、請求項22に記載の使用。
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US201562210945P | 2015-08-27 | 2015-08-27 | |
US62/210,945 | 2015-08-27 |
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JP2018530646A Division JP2018525447A (ja) | 2015-08-27 | 2016-08-29 | App選択的bace阻害のための組成物およびそのための使用 |
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JP2018530646A Pending JP2018525447A (ja) | 2015-08-27 | 2016-08-29 | App選択的bace阻害のための組成物およびそのための使用 |
JP2020152650A Pending JP2021001188A (ja) | 2015-08-27 | 2020-09-11 | App選択的bace阻害のための組成物およびそのための使用 |
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JP2018530646A Pending JP2018525447A (ja) | 2015-08-27 | 2016-08-29 | App選択的bace阻害のための組成物およびそのための使用 |
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US (1) | US11142505B2 (ja) |
EP (1) | EP3341362B1 (ja) |
JP (2) | JP2018525447A (ja) |
KR (1) | KR20180090778A (ja) |
CN (1) | CN108349905A (ja) |
AU (1) | AU2016311502B2 (ja) |
CA (2) | CA3096896A1 (ja) |
WO (1) | WO2017035529A1 (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
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KR102051485B1 (ko) * | 2013-02-12 | 2019-12-03 | 버크 인스티튜트 포 리서치 온 에이징 | Bace 매개 app 처리과정을 조절하는 히단토인 |
CA3096896A1 (en) * | 2015-08-27 | 2017-03-02 | Nantneuro, Llc | 5,5'-disubstituted aminohydantoin compounds and compositions useful for inhibition of bace and the treatment of associated diseases |
EP3759079A4 (en) * | 2018-03-01 | 2021-11-17 | The Regents Of The University Of California | AMYLOID PROTEINSELECTIVE BACE INHIBITORS (ASBIS) FOR ALZHEIMER'S MORBUS |
US11926599B1 (en) | 2023-10-23 | 2024-03-12 | King Faisal University | 1-(2-chlorobenzylideneamino)-5,5-diphenylimidazolidine-2,4-dione as an antimicrobial compound |
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- 2016-08-29 AU AU2016311502A patent/AU2016311502B2/en active Active
- 2016-08-29 CN CN201680053449.1A patent/CN108349905A/zh active Pending
- 2016-08-29 KR KR1020187008350A patent/KR20180090778A/ko not_active Application Discontinuation
- 2016-08-29 EP EP16840254.3A patent/EP3341362B1/en active Active
- 2016-08-29 US US15/755,496 patent/US11142505B2/en active Active
- 2016-08-29 WO PCT/US2016/049271 patent/WO2017035529A1/en active Application Filing
- 2016-08-29 CA CA2996542A patent/CA2996542C/en active Active
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2020
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US11142505B2 (en) | 2021-10-12 |
CN108349905A (zh) | 2018-07-31 |
EP3341362A1 (en) | 2018-07-04 |
CA3096896A1 (en) | 2017-03-02 |
US20190077766A1 (en) | 2019-03-14 |
AU2016311502A1 (en) | 2018-03-15 |
WO2017035529A1 (en) | 2017-03-02 |
EP3341362B1 (en) | 2023-07-05 |
CA2996542C (en) | 2020-12-29 |
WO2017035529A9 (en) | 2017-08-24 |
KR20180090778A (ko) | 2018-08-13 |
CA2996542A1 (en) | 2017-03-02 |
JP2018525447A (ja) | 2018-09-06 |
EP3341362A4 (en) | 2019-06-12 |
AU2016311502B2 (en) | 2019-07-18 |
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