Processing

Please wait...

Settings

Settings

Goto Application

1. WO2005063294 - INHIBITOR FOR THE FORMATION OF ϝ-SECRETASE COMPLEX

Publication Number WO/2005/063294
Publication Date 14.07.2005
International Application No. PCT/JP2004/019628
International Filing Date 28.12.2004
IPC
A61K 31/35 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/47 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
A61K 31/724 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
716Glucans
724Cyclodextrins
A61K 45/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
A61P 25/28 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 43/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
CPC
A61K 31/135
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
135having aromatic rings ; , e.g. ketamine, nortriptyline
A61K 31/35
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/47
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
A61K 31/724
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
716Glucans
724Cyclodextrins
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants
  • 興和株式会社 KOWA COMPANY, LTD. [JP]/[JP] (AllExceptUS)
  • 日産化学工業株式会社 NISSAN CHEMICAL INDUSTRIES, LTD. [JP]/[JP] (AllExceptUS)
  • 浦野 泰臣 URANO, Yasuomi [JP]/[JP] (UsOnly)
  • 浜窪 隆雄 HAMAKUBO, Takao [JP]/[JP] (UsOnly)
  • 児玉 龍彦 KODAMA, Tatsuhiko [JP]/[JP] (UsOnly)
Inventors
  • 浦野 泰臣 URANO, Yasuomi
  • 浜窪 隆雄 HAMAKUBO, Takao
  • 児玉 龍彦 KODAMA, Tatsuhiko
Agents
  • 佐伯 憲生 SAEKI, Norio
Priority Data
60/532,92330.12.2003US
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) INHIBITOR FOR THE FORMATION OF ϝ-SECRETASE COMPLEX
(FR) INHIBITEUR DE FORMATION DE COMPLEXE $G(G)-SECRETASE
(JA) γ-セクレターゼ複合体形成阻害剤
Abstract
(EN)
It is intended to provide an inhibitor for the formation of a ϝ-secretase complex which comprises a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator as the active ingredient; and use of a cholesterol synthesis inhibitor or a protein geranylgeranylation regulator for producing the same. It is also intended to provide a method of screening a substance having an effect of inhibiting the formation of an active complex of ϝ-secretase which comprises assaying the activity of inhibiting cholesterol synthesis or quantifying cholesterol accumulated in lipid rafts in cells. It is also intended to provide a method of screening a cholesterol synthesis inhibitor, a protein geranylgeranylation regulator or an HMG-CoA reductase inhibitor which comprises assaying the effect of inhibiting the formation of an active complex of ϝ-secretase. Moreover, it is intended to provide a method of screening an effect of a test substance on ϝ-secretase which comprises measuring the distribution of constituents (niscastrin, APH-1, Pen-2 and so on) required by ϝ-secretase for the formation of its active complex in cells.
(FR)
L'invention concerne un inhibiteur de formation de complexe $g(g)-secrétase qui comprend un inhibiteur de synthèse de cholestérol ou un régulateur de géranylgéranylation de protéine en tant que principe actif; et l'utilisation d'un inhibiteur de synthèse de cholestérol ou d'un régulateur de géranylgéranylation de protéine afin de produire cet inhibiteur. L'invention concerne également un procédé de criblage d'une substance présentant un effet d'inhibition de la formation d'un complexe actif de $g(g)-secrétase qui consiste à analyser l'activité d'inhibition de la synthèse de cholestérol ou de quantifier le cholestérol accumulé dans des radeaux lipidiques de cellules. L'invention concerne également un procédé de criblage d'un inhibiteur de synthèse de cholestérol, d'un régulateur de géranylgéranylation de protéine ou d'un inhibiteur de réductase HMG-CoA qui consiste à analyser l'effet d'inhibition de la formation d'un complexe actif de $g(g)-secrétase. En outre, ce procédé de criblage produit un effet d'une substance de test sur la $g(g)-secrétase qui consiste à mesurer la répartition des constituants (niscastrine, APH-1, Pen-2 etc.) nécessaires à la $g(g)-secrétase pour la formation de son complexe actif dans les cellules.
(JA)
 本発明は、コレステロール合成阻害剤、又は蛋白ゲラニルゲラニル化抑制剤を有効成分とするγ−セクレターゼ複合体形成阻害剤、及びそれを製造するためのコレステロール合成阻害剤、又は蛋白ゲラニルゲラニル化抑制剤の使用を提供する。また、本発明は、コレステロールの合成阻害活性を測定すること、又は細胞の脂質ラフトにおけるコレステロールの蓄積量を測定することからなるγ−セクレターゼの活性複合体の形成を阻害する作用を有する物質をスクリーニングする方法に関する。また、本発明は、γ−セクレターゼの活性複合体の形成を阻害する作用を測定することからなるコレステロール合成阻害剤、蛋白ゲラニルゲラニル化抑制剤、又はHMG−CoA還元酵素阻害剤をスクリーニングする方法に関する。さらに、本発明は、細胞内におけるγ−セクレターゼが、その活性複合体を形成するに必要とされるニカストリン(nicastrin)、APH−1、Pen−2などの構成成分の細胞内における分布を測定することにより、被検物質のγ−セクレターゼに対する作用をスクリーニングする方法に関する。
Also published as
US2007161700
Latest bibliographic data on file with the International Bureau