RU2007126483A - Гетероциклические ингибиторы аспартилпротеазы - Google Patents

Гетероциклические ингибиторы аспартилпротеазы Download PDF

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Publication number
RU2007126483A
RU2007126483A RU2007126483/04A RU2007126483A RU2007126483A RU 2007126483 A RU2007126483 A RU 2007126483A RU 2007126483/04 A RU2007126483/04 A RU 2007126483/04A RU 2007126483 A RU2007126483 A RU 2007126483A RU 2007126483 A RU2007126483 A RU 2007126483A
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medicament
treatment
preparation
inhibitor
compound according
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RU2007126483/04A
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RU2401658C2 (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
Уиль м 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. (US)
Фармакопие, Инк.
Шеринг Корпорейшн (US)
Шеринг Корпорейшн
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Publication of RU2007126483A publication Critical patent/RU2007126483A/ru
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Publication of RU2401658C2 publication Critical patent/RU2401658C2/ru

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    • 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
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Claims (15)

1. Соединение, выбранное из группы, состоящей из
Figure 00000001
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Figure 00000100
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Figure 00000115
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Figure 00000127
Figure 00000128
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Figure 00000130
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Figure 00000148
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Figure 00000160
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Figure 00000175
Figure 00000176
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Figure 00000179
Figure 00000180
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Figure 00000186
Figure 00000187
Figure 00000188
Figure 00000189
Figure 00000190
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Figure 00000192
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Figure 00000195
Figure 00000196
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Figure 00000198
Figure 00000199
Figure 00000200
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Figure 00000210
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Figure 00000221
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Figure 00000230
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Figure 00000250
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Figure 00000260
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Figure 00000264
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Figure 00000280
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Figure 00000310
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Figure 00000320
Figure 00000321
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Figure 00000325
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2. Фармацевтическая композиция, содержащая эффективное количество соединения по п.1 и фармацевтически эффективный носитель.
3. Фармацевтическая композиция по п.2, дополнительно содержащая эффективное количество ингибитора холинэстеразы или мускаринового агониста m1 или антагониста m2.
4. Фармацевтическая композиция по п.2, дополнительно содержащая эффективное количество ингибитора гамма-секретазы; ингибитора HMG-СоА редуктазы или нестероидного противовоспалительного агента.
5. Способ ингибирования аспартилпротеазы, содержащий введение пациенту, нуждающемуся в таком лечении, эффективного количества соединения по п.1.
6. Применение соединения по п.1 для приготовления лекарственного средства, предназначенного для лечения сердечно-сосудистых заболеваний, нарушений познавательной способности и нейродегенеративных заболеваний и способов ингибирования вируса иммунодефицита человека, плазмепсинов, катепсина D и протозойных ферментов.
7. Применение по п.6 для приготовления лекарственного средства для лечения нарушения познавательной способности или нейродегенеративного заболевания.
8. Применение по п.7 для приготовления лекарственного средства для лечения болезни Альцгеймера.
9. Применение соединения по п.1 в комбинации с ингибитором холинэстеразы для приготовления лекарственного средства для лечения нарушения познавательной способности или нейродегенеративного заболевания.
10. Применение по п.9 для приготовления лекарственного средства для лечения болезни Альцгеймера.
11. Применение соединения по п.1 в комбинации с ингибитором гамма-секретазы, ингибитором HMG-CoA редуктазы или нестероидным противоспалительным агентом для приготовления лекарственного средства для лечения нарушения познавательной способности или нейродегенеративного заболевания.
12. Применение по п.11 для приготовления лекарственного средства для лечения болезни Альцгеймера.
13. Применение по п.11, в котором указанным ингибитором HMG-CoA редуктазы является аторвастатин, ловастатин, симвастатин, правастатин, флувастатин или росувастатин.
14. Применение по п.11, в котором указанным нестероидным противовоспалительным агентом является ибупрофен, релафен или напроксен.
15. Применение соединения по п.1 в комбинации с одним или большим количеством соединений, выбранных из группы, состоящей из ингибитора холинэстеразы, мускаринового агониста m1 или антагониста m2, ингибитора гамма-секретазы, ингибитора HMG-CoA редуктазы и нестероидного противовоспалительного агента для приготовления лекарственного средства для лечения нарушения познавательной способности или нейродегенеративного заболевания.
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