RU2020131276A - Терапевтические соединения и композиции - Google Patents

Терапевтические соединения и композиции Download PDF

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RU2020131276A
RU2020131276A RU2020131276A RU2020131276A RU2020131276A RU 2020131276 A RU2020131276 A RU 2020131276A RU 2020131276 A RU2020131276 A RU 2020131276A RU 2020131276 A RU2020131276 A RU 2020131276A RU 2020131276 A RU2020131276 A RU 2020131276A
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alkyl
aryl
heteroaryl
heterocyclyl
cycloalkyl
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RU2020131276A
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Роберт А. ХРУСЬЦЕЛЬ
Роберт К. ГЭДВУД
Нил Дж. ХЭЙВОРД
Майкл Дж. МЕЛЬНИК
Мануэль НАВИА
Тони Дж. ПОЭЛЬ
Кэтрин А. СТЮАРТ
Франс Л. СТАССЕН
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Экзитера Фармасьютикалз Инк.
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Claims (24)

1. Соединение формулы (I):
Figure 00000001
(I),
или его фармацевтически приемлемая соль, где
R1 представляет собой H или -C1-6 алкил;
R2 представляет собой H, –C1-6 алкил, –CO2R5, –C(O)NR9R10, –CN, –SOqR5, –OR5, –CHN(OR5) или гетероарил;
R3 представляет собой H или -C1-6 алкил;
A представляет собой связь, C1-6 алкилен, C2-6 алкинилен или C2-6 алкинилен;
R4 представляет собой циклоалкил, арил, гетероарил или гетероциклил, каждый из которых замещен 0-3 R6;
каждый R5 независимо представляет собой H, -C1-6 алкил, аралкил или арил, замещенный 0-3 -NH2 или R6;
каждый R6 независимо представляет собой галоген, гидрокси, циано, нитро, –C1-6 алкил, –C1-6 алкокси, –NHR10, –NR9R10, –C(O)R11, –C(O)OR11, –C(O)NR9R10, –C(NR8)(N(R8)2), –SOqR11, –SO2NR9R10, –NHC(O)OR11, –NHC(O)R11, –OC(O)R11, арил, гетероарил, аралкил, циклоалкил, гетероаралкил, гетероциклил или гетероциклилалкил, или
две R6 группы, взятые вместе с атомами, к которым они присоединены, образуют 5-7-членное кольцо;
X представляет собой –C(O)O–, –OC(O)–, –C(O)S(O)2–, –S(O)2C(O)–, –C(O)N(R5)– или –N(R5)C(O) –;
Y представляет собой –C1-6 алкил, циклоалкил, арил, гетероарил или гетероциклил, каждый из которых замещен 0-3 –NH2 или R6;
R7 представляет собой H, –C1-6 алкил, циклоалкил, арил, гетероарил или гетероциклил, каждый из которых замещен 0-3 –NH2 или R6;
каждый R8 независимо представляет собой H, –C1-6 алкил, –C(O)R5, –C(O)OR5, арил, гетероарил, аралкил, гетероаралкил, гетероциклил или гетероциклилалкил;
каждый R9 и R10 независимо представляет собой –C1-6 алкил, циклоалкил, гетероциклил, арил или гетероарил, или
R9 и R10 вместе образуют необязательно замещенное 5-7-членное кольцо;
каждый R11 независимо представляет собой H, –C1-10 алкил, аралкил или арил;
q равно целому числу от 0 до 2; и
n равно целому числу от 0 до 2.
2. Соединение по п. 1, где R1 представляет собой H.
3. Соединение по п. 1, где R2 представляет собой –CO2R5, где R5 представляет собой H или –C1-6 алкил.
4. Соединение по п. 1, где A представляет собой C1-6 алкилен.
5. Соединение по п. 1, где R4 представляет собой арил или гетероарил.
RU2020131276A 2014-02-07 2015-02-04 Терапевтические соединения и композиции RU2020131276A (ru)

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