JP2001500165A - アルツハイマー病及び痴呆の治療及び診断のための高選択的ブチリルコリンエステラーゼ阻害薬 - Google Patents
アルツハイマー病及び痴呆の治療及び診断のための高選択的ブチリルコリンエステラーゼ阻害薬Info
- Publication number
- JP2001500165A JP2001500165A JP11508849A JP50884999A JP2001500165A JP 2001500165 A JP2001500165 A JP 2001500165A JP 11508849 A JP11508849 A JP 11508849A JP 50884999 A JP50884999 A JP 50884999A JP 2001500165 A JP2001500165 A JP 2001500165A
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- bis
- serine
- benzyl
- compound
- simserin
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.老齢化又はアルツハイマー病に関連した認識障害の防止又は治療のための 方法であって、前記認識障害の危険性のある又は前記認識障害を有する患者を有 効量の高選択的ブチリルコリンエステラーゼ阻害薬で処置することから成る方法 。 2.前記ブチリルコリンエステラーゼ阻害薬が約15対1より大きいブチリル コリンエステラーゼ阻害対アセチルコリンエステラーゼ阻害の選択性比を有する 請求項1の方法。 3.前記ブチリルコリンエステラーゼ阻害薬が、シムセリン、N’−ノルシム セリン、N’−ベンジルノルフィソスチグミン、N’−ベンジルノルシムセリン 、N’−フェネチルノルフィソスチグミン、N’−フェネチルノルシムセリン、 N’−アリルノルフィソスチグミン、チアフィソベニン、チアシムセリン、シム スベニン、N8−ベンジルノルシムセリン、N8−ノルシムセリン、N1,N8−ビ スノルシムセリン、N1,N8−ビスベンジルノルフィソスチグミン、N1,N8− ビスベンジルノルフェンセリン、N1,N8−ビスベンジルノルシムセリン及びそ れらの医薬として許容可能な塩から成る群から選択される請求項2の方法。 4.前記ブチリルコリンエステラーゼ阻害薬がシムセリンである請求項3の方 法。 5.前記ブチリルコリンエステラーゼ阻害薬がN1,N8−ビスノルシムセリン である請求項3の方法。 6.N3−ベンジルノルシムセリンの式を有する化合物。 7.N8−ノルシムセリンの式を有する化合物。 8.N2,N8−ビスノルシムセリンの式を有する化合物。 9.N1,N8−ビスベンジルノルフィソスチグミンの式を有す る化合物。 10.N1,N8−ビスベンジルノルフェンセリンの式を有する化合物。 11.N1,N8−ビスベンジルノルシムセリンの式を有する化合物。 12.アルツハイマー病に関連した病変又は病状の存在の検出方法であって、 検出可能な標識と結合した高選択的ブチリルコリンエステラーゼ阻害薬を包含す る試薬で脳組織を処置し、それにより前記試薬が関連標識を検出することにより 検出される前記病変又は病状と選択的に結合することから成る方法。 13.前記試薬が患者にin vivoに投与され、脳組織中に入る医薬として許容 可能な処方物であって、前記標識が適切な脳スキャン装置により検出可能であり 、そして前記病変又は病状の存在が前記患者に脳スキャンを実行することにより 検出される請求項12の方法。 14.前記ブチリルコリンエステラーゼ阻害薬が炭素11標識を含有するシム セリンである請求項13の方法。 15.前記組織がスライドに固定され、前記標識が蛍光標識である請求項12 の方法。 16.ニューロン起始の細胞株又は組織からのβアミロイド前駆体タンパク質 の分泌及び剛性を低下させる方法であって、ニューロン起始の前記細胞株又は組 織に有効量の高選択的ブチリルコリンエステラーゼ阻害薬を投与することから成 る方法。 17.前記ブチリルコリンエステラーゼがシムセリン、N’−ノルシムセリン 、N’−ベンジルノルフィソスチグミン、N’−ベンジルノルシムセリン、N’ −フェネチルノルフィソスチグミン、N’−フェネチルノルシムセリン、N’− アリルノルフィソスチグミ ン、チアフィソベニン、チアシムセリン、シムスベニン、N8−ベンジルノルト ルセリン、N8−ベンジルノルシムセリン、N8−ノルトルセリン、N8−ノルシ ムセリン、N,N8−ビスノルフィソスチグミン、N,N8−ビスノルフェネセリ ン、N’,N8−ビスノルシムセリン及びそれらの医薬として許容可能な塩から 成る群から選択される請求項16の方法。 18.前記ブチリルコリンエステラーゼ阻害薬がシムセリンである請求項16 の方法。
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US5208797P | 1997-07-09 | 1997-07-09 | |
US60/052,087 | 1997-07-09 | ||
PCT/US1998/014063 WO1999002154A1 (en) | 1997-07-09 | 1998-07-09 | Highly selective butyrylcholinesterase inhibitors for the treatment and diagnosis of alzheimer's disease and dementias |
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JP (1) | JP4522499B2 (ja) |
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IL (2) | IL128877A0 (ja) |
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PL332078A1 (en) | 1999-08-30 |
AU8293198A (en) | 1999-02-08 |
MXPA04001462A (es) | 2005-04-29 |
IL128877A0 (en) | 2000-01-31 |
DE69832688T2 (de) | 2006-09-07 |
HUP0003852A2 (hu) | 2001-04-28 |
HUP0003852A3 (en) | 2003-04-28 |
US6683105B2 (en) | 2004-01-27 |
BR9806184A (pt) | 2001-06-19 |
IL128877A (en) | 2007-10-31 |
CZ297533B6 (cs) | 2007-01-03 |
AU749088B2 (en) | 2002-06-20 |
PL191402B1 (pl) | 2006-05-31 |
CZ81699A3 (cs) | 2000-01-12 |
US6410747B1 (en) | 2002-06-25 |
JP4522499B2 (ja) | 2010-08-11 |
DE69832688D1 (de) | 2006-01-12 |
CA2264750C (en) | 2009-06-16 |
DK0949920T3 (da) | 2006-04-18 |
ES2255170T3 (es) | 2006-06-16 |
EP0949920A1 (en) | 1999-10-20 |
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