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RU2011103741A - Композиции и способы лечения заболевания сетчатки - Google Patents

Композиции и способы лечения заболевания сетчатки Download PDF

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RU2011103741A
RU2011103741A RU2011103741/04A RU2011103741A RU2011103741A RU 2011103741 A RU2011103741 A RU 2011103741A RU 2011103741/04 A RU2011103741/04 A RU 2011103741/04A RU 2011103741 A RU2011103741 A RU 2011103741A RU 2011103741 A RU2011103741 A RU 2011103741A
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compound according
pharmaceutically acceptable
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acceptable salt
aryl
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Томас А. ДЖОРДАН (US)
Томас А. ДЖОРДАН
Джон И. ДАУЛИНГ (US)
Джон И. ДАУЛИНГ
Джон Клиффорд ЧАБАЛА (US)
Джон Клиффорд ЧАБАЛА
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Ньюрон Системз Инк., (Us)
Ньюрон Системз Инк.,
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Abstract

1. Соединение формулы IIIa: !(IIIa) ! или фармацевтически приемлемая соль соединения IIIa, где ! L представляет собой представляет ординарную связь или CH2; ! X, Y и Z, каждый независимо представляет собой N, NH, O, S, CB, CH или отсутствует, так что один из X, Y и Z представляет собой N или NH; p равно 0, 1, 2 или 3; B представляет собой атом галогена, гидроксил, карбамоил, арил или амино; ! A представляет собой ! ; и ! D представляет собой неразветвленный низший алкил. ! 2. Соединение по п.1, где один из X или Z представляет собой N, а оставшийся X или Z представляет собой O; ! Y отсутствует; ! p равно 1; ! B представляет собой атом галогена, гидроксил, карбамоил, арил или амино; ! L представляет собой одинарную связь или CH2; ! A представляет собой ! ; и ! D представляет собой неразветвтленный низший алкил. ! 3. Соединение по п.2, где L представляет собой одинарную связь. ! 4. Соединение по п.3, где X представляет собой O, и Z представляет собой N. ! 5. Соединение по п.3, где X представляет собой N, и Z представляет собой O. ! 6. Соединение по п.4 или 5, где B представляет собой арил. ! 7. Соединение по п.6, где B представляет собой фенил. ! 8. Соединение по п.3, где D представляет собой CH3. ! 9. Соединение по п.8, выбранное из ! , , ! или его фармацевтически приемлемая соль. ! 10. Соединение по п.9, которое представляет собой ! ! или его фармацевтически приемлемая соль. ! 11. Соединение по п.9, которое представляет собой ! ! или его фармацевтически приемлемая соль. ! 12. Фармацевтическая композиция, содержащая соединение по п.1 и фармацевтически приемлемый носитель. ! 13. Фармацевтическая композиция по п. 12, содержащая соединение, выбранное из !, ! или его фармацевтически приемлемую соль и фармацевти

Claims (16)

1. Соединение формулы IIIa:
Figure 00000001
(IIIa)
или фармацевтически приемлемая соль соединения IIIa, где
L представляет собой представляет ординарную связь или CH2;
X, Y и Z, каждый независимо представляет собой N, NH, O, S, CB, CH или отсутствует, так что один из X, Y и Z представляет собой N или NH; p равно 0, 1, 2 или 3; B представляет собой атом галогена, гидроксил, карбамоил, арил или амино;
A представляет собой
Figure 00000002
; и
D представляет собой неразветвленный низший алкил.
2. Соединение по п.1, где один из X или Z представляет собой N, а оставшийся X или Z представляет собой O;
Y отсутствует;
p равно 1;
B представляет собой атом галогена, гидроксил, карбамоил, арил или амино;
L представляет собой одинарную связь или CH2;
A представляет собой
Figure 00000002
; и
D представляет собой неразветвтленный низший алкил.
3. Соединение по п.2, где L представляет собой одинарную связь.
4. Соединение по п.3, где X представляет собой O, и Z представляет собой N.
5. Соединение по п.3, где X представляет собой N, и Z представляет собой O.
6. Соединение по п.4 или 5, где B представляет собой арил.
7. Соединение по п.6, где B представляет собой фенил.
8. Соединение по п.3, где D представляет собой CH3.
9. Соединение по п.8, выбранное из
Figure 00000003
,
Figure 00000004
,
или его фармацевтически приемлемая соль.
10. Соединение по п.9, которое представляет собой
Figure 00000003
или его фармацевтически приемлемая соль.
11. Соединение по п.9, которое представляет собой
Figure 00000004
или его фармацевтически приемлемая соль.
12. Фармацевтическая композиция, содержащая соединение по п.1 и фармацевтически приемлемый носитель.
13. Фармацевтическая композиция по п. 12, содержащая соединение, выбранное из
Figure 00000003
,
Figure 00000004
или его фармацевтически приемлемую соль и фармацевтически приемлемый носитель.
14. Соединение, которое представляет собой
Figure 00000003
или его фармацевтически приемлемая соль.
15. Соединение, которое представляет собой
Figure 00000004
или его фармацевтически приемлемая соль.
16. Применение соединения по п.9 в производстве лекарственного средства для лечения дегенерации желтого пятна и других форм заболевания сетчатки, этиология которых включает накопление А2Е и/или липофусцина в ткани сетчатки у субъекта, причем указанное лекарственное средство снижает уровень накопления А2Е по отношению к уровню накопления А2Е у субъекта в отсутствии лекарственного средства.
RU2011103741/04A 2005-05-26 2011-02-02 Композиции и способы лечения заболевания сетчатки RU2011103741A (ru)

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