RU2401658C2 - Гетероциклические ингибиторы аспартилпротеазы - Google Patents

Гетероциклические ингибиторы аспартилпротеазы Download PDF

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RU2401658C2
RU2401658C2 RU2007126483A RU2007126483A RU2401658C2 RU 2401658 C2 RU2401658 C2 RU 2401658C2 RU 2007126483 A RU2007126483 A RU 2007126483A RU 2007126483 A RU2007126483 A RU 2007126483A RU 2401658 C2 RU2401658 C2 RU 2401658C2
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Russia
Prior art keywords
aspartylprotease
heterocyclic
inhibitors
васе
compound according
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RU2007126483A
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English (en)
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RU2007126483A (ru
Inventor
Жаонинг ЖУ (US)
Жаонинг Жу
Брайан МАККИТРИК (US)
Брайан МАККИТРИК
Жонг-Юе СУН (US)
Жонг-Юе СУН
Юанзан К. ЙЕ (US)
Юанзан К. ЙЕ
Йоханнес Х. ФОЙГТ (US)
Йоханнес Х. ФОЙГТ
Кори СТРИКЛЭНД (US)
Кори СТРИКЛЭНД
Элизабет М. СМИТ (US)
Элизабет М. СМИТ
Эндрю СТЭМФОРД (US)
Эндрю СТЭМФОРД
Уильям Дж. ГРИНЛИ (US)
Уильям Дж. ГРИНЛИ
Роберт МАЦЦОЛА (US)
Роберт МАЦЦОЛА
Джон КОЛДУЭЛЛ (US)
Джон КОЛДУЭЛЛ
Джейрид КАММИНГ (US)
Джейрид КАММИНГ
Лингйан ВАНГ (US)
Лингйан ВАНГ
Юшенг ВУ (US)
Юшенг Ву
Ульрих ИЗЕРЛО (US)
Ульрих Изерло
Тао ГУО (US)
Тао ГУО
Туй Кс. Х. ЛЕ (US)
Туй Кс. Х. ЛЕ
Керт В. ЗАЙОНЦ (US)
Керт В. ЗАЙОНЦ
Суреш Д. БАБУ (US)
Суреш Д. БАБУ
Рейчел К. ХАНТЕР (US)
Рейчел К. ХАНТЕР
Мишель Л. МОРРИС (US)
Мишель Л. МОРРИС
Хуижонг ГУ (US)
Хуижонг ГУ
Ганг КВИАН (US)
Ганг КВИАН
Дейвит ТЭДЕССИ (US)
Дейвит ТЭДЕССИ
Original Assignee
Фармакопие, Инк.
Шеринг Корпорейшн
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Publication of RU2007126483A publication Critical patent/RU2007126483A/ru
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
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    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Abstract

Изобретение относится к новым 5-6-членным азотсодержащим гетероциклическим соединениям, выбранным из производных пиридина, пиримидина, имидазолина, оксадиазолина, таким, как, например,
Figure 00000389
Figure 00000755
Figure 00000756
,
которые обладают ингибирующей активностью в отношении аспартилпротеазы, такой как ВАСЕ-1. Изобретение также относится к фармацевтической композиции, способу ингибирования аспартилпротеазы и применению соединений для приготовления лекарственного средства, предназначенного для лечения состояния, опосредованного аспартилпротеазой, такой как ВАСЕ-1. 4 н.з. п. ф-лы, 1 табл.

Description

Текст описания приведен в факсимильном виде.
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Claims (4)

1. Соединение, выбранное из группы, состоящей из
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и
Figure 00000754
2. Фармацевтическая композиция, обладающая ингибирующей активностью в отношении аспартилпротеазы, такой, как ВАСЕ-1, содержащая эффективное количество соединения по п.1 и фармацевтически эффективный носитель.
3. Способ ингибирования аспартилпротеазы введением эффективного количества соединения по п.1.
4. Применение соединения по п.1 для приготовления лекарственного средства, предназначенного для лечения заболеваний, опосредованных аспартилпротеазой, такой, как ВАСЕ-1.
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