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ES2285735T3 - Modelo molecular para inhibidores de vla-4. - Google Patents

Modelo molecular para inhibidores de vla-4. Download PDF

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Publication number
ES2285735T3
ES2285735T3 ES97934288T ES97934288T ES2285735T3 ES 2285735 T3 ES2285735 T3 ES 2285735T3 ES 97934288 T ES97934288 T ES 97934288T ES 97934288 T ES97934288 T ES 97934288T ES 2285735 T3 ES2285735 T3 ES 2285735T3
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Spain
Prior art keywords
inhibitors
vla
molecular model
methods
molecular
Prior art date
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Expired - Lifetime
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ES97934288T
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English (en)
Inventor
Juswinder Singh
Zhongli Zheng
Peter Sprague
Vlijmen Herman W T Van
Alfredo C Castro
Steven P Adams
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Biogen Inc
Biogen MA Inc
Original Assignee
Biogen Idec Inc
Biogen Idec MA Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/40—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
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    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/415—1,2-Diazoles
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Abstract

Un método para identificar un compuesto químico que tiene un valor de la CI50 menor que aproximadamente 100 µM en un ensayo de unión directa a VLA-4, comprendiendo dicho método las etapas siguientes: a) seleccionar un estructura de un compuesto experimental que ha de ser evaluada en cuanto a actividad de VLA-4; b) obtener mediante programas de ordenador o experimentalmente una estructura tridimensional de dicho compuesto experimental; c) evaluar si la estructura tridimensional de dicho compuesto experimental se adapta a un modelo farmacóforo; y d) determinar si dicho compuesto experimental tiene un valor de la CI50 menor que aproximadamente 100 µM en un ensayo de unión directa a VLA-4; en donde dicha estructura de compuesto experimental comprende NEG ("N") (Ver tabla) y al menos tres características seleccionadas del grupo que consiste en: (Ver tabla)
ES97934288T 1996-07-25 1997-07-24 Modelo molecular para inhibidores de vla-4. Expired - Lifetime ES2285735T3 (es)

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JP2005520171A (ja) * 2001-04-10 2005-07-07 トランス　テック　ファーマ，インコーポレイテッド ドラッグディスカバリーに関する、プローブ、システム、および方法
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