EA200100970A1 - Аминопроизводные как ингибиторы протеазы - Google Patents

Аминопроизводные как ингибиторы протеазы

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Publication number
EA200100970A1
EA200100970A1 EA200100970A EA200100970A EA200100970A1 EA 200100970 A1 EA200100970 A1 EA 200100970A1 EA 200100970 A EA200100970 A EA 200100970A EA 200100970 A EA200100970 A EA 200100970A EA 200100970 A1 EA200100970 A1 EA 200100970A1
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EA
Eurasian Patent Office
Prior art keywords
ring
atoms
atom
heteroatom
formula
Prior art date
Application number
EA200100970A
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English (en)
Other versions
EA004807B1 (ru
Inventor
Джон О. Линк
Арнольд Дж. Мартелли
Валерий Мартичонок
Джон У. Пэттерсон
Оливер Л. Сондерс
Шейла Зипфель
Original Assignee
Аксис Фармасьютикалз, Инк.
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Application filed by Аксис Фармасьютикалз, Инк. filed Critical Аксис Фармасьютикалз, Инк.
Publication of EA200100970A1 publication Critical patent/EA200100970A1/ru
Publication of EA004807B1 publication Critical patent/EA004807B1/ru

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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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Abstract

Настоящее изобретение касается новых алканоилзамещенных гетероциклических производных, являющихся ингибиторами цистеинпротеазы, или их фармацевтически приемлемых солей и их N-оксидов, их использования в качестве терапевтических средств и способов их изготовления в соответствии с формулой (I), в которой А представляет собой гетеромоноциклическое кольцо, содержащее от 5 до 6 входящих в кольцо атомов, или конденсированную гетероциклическую систему, содержащую от 8 до 14 входящих в состав колец атомов, в которой каждое кольцо содержит от 5 до 7 атомов; Xпредставляет собой входящий в состав кольца атом углерода, а каждый входящий в состав кольца атом, не являющийся X, представляет собой атом углерода или гетероатом, при условии, что (i) по меньшей мере один, входящий в состав кольца атом представляет собой гетероатом и (ii) если А представляет собой гетеромоноциклический радикал, содержащий 5 атомов, входящих в состав кольца, то не более двух входящих в состав кольца атомов, входящих в А, представляют собой гетероатомы; n представляет собой 0, 1, 2 или 3; Xпредставляет собой =С или -СН-; Xпредставляет собой связь или дивалентную группу формулы (а) или (b); R- Rтаковы, как они определены в заявке на изобретение.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200100970A 1999-03-15 2000-03-15 Аминопроизводные как ингибиторы протеазы EA004807B1 (ru)

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US12442199P 1999-03-15 1999-03-15
PCT/US2000/006885 WO2000055144A1 (en) 1999-03-15 2000-03-15 Amine derivatives as protease inhibitors

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EA200100970A1 true EA200100970A1 (ru) 2002-04-25
EA004807B1 EA004807B1 (ru) 2004-08-26

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US (2) US6576630B1 (ru)
EP (1) EP1161422A1 (ru)
JP (1) JP2002539201A (ru)
KR (1) KR20010110670A (ru)
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