EA199900769A1 - N-гидрокси-2-(алкил-, арил- или гетероарилсульфанил, -сульфинил или -сульфонил)-3-замещенные алкилов, арилов или гетероариламидов в качестве ингибиторов матриксных металлопротеиназ - Google Patents

N-гидрокси-2-(алкил-, арил- или гетероарилсульфанил, -сульфинил или -сульфонил)-3-замещенные алкилов, арилов или гетероариламидов в качестве ингибиторов матриксных металлопротеиназ

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Publication number
EA199900769A1
EA199900769A1 EA199900769A EA199900769A EA199900769A1 EA 199900769 A1 EA199900769 A1 EA 199900769A1 EA 199900769 A EA199900769 A EA 199900769A EA 199900769 A EA199900769 A EA 199900769A EA 199900769 A1 EA199900769 A1 EA 199900769A1
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Eurasian Patent Office
Prior art keywords
tnf
tace
mmps
tissue
enzymes
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EA199900769A
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English (en)
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EA001742B1 (ru
Inventor
Аранапакам Мудумбай Венкатесан
Джордж Теодор Гросу
Жами Мари Дэвис
Жанни Леа Бэйкер
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Американ Цианамид Компани
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Publication of EA199900769A1 publication Critical patent/EA199900769A1/ru
Publication of EA001742B1 publication Critical patent/EA001742B1/ru

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    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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Abstract

Матричные металлопротеиназы (MMPs) представляют собой группу ферментов, которые вовлечены в патологическую деструкцию соединительной ткани и основных мембран. Эти цинксодержащие эндопептидазы состоят из нескольких подгрупп ферментов, включая коллагеназы, стромелизины и желатиназы. Фермент, конвертирующий TNF-α (ТАСЕ), противовоспалительный цитокин, катализирует образование TNF-α из белка-предшественника TNF-α, связанного с мембраной. Поэтому предполагается, что небольшие молекулы, ингибирующие MMPs и ТАСЕ, вероятно, пригодны для лечения ряда болезненных состояний. В настоящем изобретении созданы низкомолекулярные непептидные ингибиторы матричных металлопротеиназ (MMPs) и фермента конвертирующего TNF-α (ТАСЕ) для лечения артрита, опухолевых метастазов, тканевого изъязвления, аномального заживления ран, болезни околозубной ткани, костных заболеваний, диабета (инсулинустойчивого) и HIV-инфекции, обладающий формулой (I), в которой Rи Rобразуют гетероциклическое кольцо, а А представляет собой S, S(O), или S(O), а Rи Rприведены в ней.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199900769A 1997-02-27 1998-02-17 N-гидрокси-2-(алкил-, арил- или гетероарилсульфанил, -сульфинил или -сульфонил)-3-замещенные алкилов, арилов или гетероариламидов в качестве ингибиторов матриксных металлопротеиназ EA001742B1 (ru)

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US80672897A 1997-02-27 1997-02-27
PCT/US1998/002987 WO1998037877A1 (en) 1997-02-27 1998-02-17 N-hydroxy-2-(alkyl, aryl or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors

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EA199900769A1 true EA199900769A1 (ru) 2000-04-24
EA001742B1 EA001742B1 (ru) 2001-08-27

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EA199900768A EA003836B1 (ru) 1997-02-27 1998-02-17 N-гидрокси-2-(алкил, арил или гетероарилсульфанил, сульфинил или сульфонил)-3-замещенный алкил, арил или гетероариламиды в качестве ингибиторов матричной металлопротеиназы

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