JP6740354B2 - オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 - Google Patents
オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法 Download PDFInfo
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Description
本出願は2015年10月5日出願の米国仮出願第62/237,342号の優先権を主張する。上記出願の全体の内容が、本明細書に完全に記述されるのと同様に、参照により援用される。
式中、Y1及びY2はCH及びNからなる群より独立に選択され、
XはH、ハロゲン基、及びアリールからなる群より選択され、
R1は、任意選択で置換されたチオヘテロアリール、ヒドロキシル置換(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、Y1はCHであり、
Y2はNであり、
Xはハロゲン基であり、
R1は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、Xはハロゲン基であり、
R1は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、XはHであり、
R1は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、XはHであり、
R1は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、R1は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、R1は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、Y3はCHまたはNであり、
R2は任意選択で置換された(2−アミノエチル)アリールである
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、Y3はCHであり、
R2は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、R2は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、Y4はCHまたはNであり、
R3は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、R2は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、R2は、任意選択で置換されたチオヘテロアリール、任意選択で置換された(2−アミノエチル)アリール、ハロゲン基、任意選択で置換されたチオシクロアルキルであり、上記シクロアルキルの1〜3の炭素原子が任意選択でO、S及びNからなる群より選択されるヘテロ原子によって置換された上記チオシクロアルキル、ならびにチオアリールからなる群より選択される
上記化合物、またはその塩、鏡像異性体、ラセミ体、それらの混合物、もしくはそれらの組み合わせが提供される。
式中、XはHまたはハロゲン基であり、
Z1はOであり、
R4は、H、任意選択で置換されたアルキル、Et、CF3、任意選択で置換されたシクロアルキル、任意選択で置換されたアリール、任意選択で置換されたヘテロアリール、及び
上記化合物が提供される。
合成スキームの例
スキーム1は式
オートファジーの流れ及びホスホリパーゼDの活性化剤
CNSへの浸透に関するリピンスキーの法則に従った分子量(MW)及び分配係数(log P)、すなわちMW≦400、log P≦5に基づいて、最適な脳への浸透を目的としてWHYKDシリーズの化合物を合成した。
誘導体の設計
いくつかの一連の誘導体を以下のリード化合物に基づいて合成した。
WHYKD化合物の検出及び結果
フォトダイオードアレイ(PDA)を用いてマウスの脳中のWHYKD8を検出した(図1)。試料は、時間ベースの分離したピーク(左図)によって且つ測定可能な曲線下面積(AUC)(挿入図)によって容易に検出された。
Claims (7)
- 以下の式:
- 請求項1に記載の化合物または薬学的に許容されるその塩を含む医薬組成物。
- 請求項1に記載の化合物または薬学的に許容されるその塩を含む、神経変性疾患治療用医薬組成物。
- 前記神経変性疾患がタンパク質症である、請求項3に記載の医薬組成物。
- 前記タンパク質症がタウオパチーである、請求項4に記載の医薬組成物。
- 前記神経変性疾患がアルツハイマー病である、請求項3に記載の医薬組成物。
- 請求項1に記載の化合物または薬学的に許容されるその塩を含む、細胞またはタンパク質凝集体に与えるためのオートファジーの流れの亢進用医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562237342P | 2015-10-05 | 2015-10-05 | |
US62/237,342 | 2015-10-05 | ||
PCT/US2016/055561 WO2017062500A2 (en) | 2015-10-05 | 2016-10-05 | Activators of autophagic flux and phospholipase d and clearance of protein aggregates including tau and treatment of proteinopathies |
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