RU2016112053A - Композиции для лечения гипертензии и/или фиброза - Google Patents

Композиции для лечения гипертензии и/или фиброза Download PDF

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RU2016112053A
RU2016112053A RU2016112053A RU2016112053A RU2016112053A RU 2016112053 A RU2016112053 A RU 2016112053A RU 2016112053 A RU2016112053 A RU 2016112053A RU 2016112053 A RU2016112053 A RU 2016112053A RU 2016112053 A RU2016112053 A RU 2016112053A
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compound
pharmaceutically acceptable
stereoisomer
acceptable salt
fibrosis
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RU2016112053A
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RU2661878C2 (ru
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Карен Аннетт ДАГГЕН
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Вектус Байосистемс Лимитед
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    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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Claims (51)

1. Соединение формулы:
Figure 00000001
где
А выбран из группы, состоящей из
Figure 00000002
Figure 00000003
и
Figure 00000004
,
Q независимо выбран из галогена, алкила, гидрокси, амино и замещенного амино;
n равняется 0, 1, 2, 3, 4 или 5;
R1, R3 и R4 независимо представляют собой С, СН, СН2, О, N, NH или S, и
R2 представляет собой С, СН, СН2, N, NH, C-CF3, CH-CF3 или C=O,
или его стереоизомер или фармацевтически приемлемая соль,
где, если n равняется 1, Q не может представлять собой гидрокси.
2. Соединение, или его стереоизомер или фармацевтически приемлемая соль по п. 1, где Q представляет собой галоген, выбранный из группы, состоящей из F, Cl, Br и I.
3. Соединение, или его стереоизомер или фармацевтически приемлемая соль по п. 1, где Q представляет собой замещенный амино формулы -NHW, и где
W выбран из -CN, -SO2(X)aY и -CO(X)aY,
а равняется 0 или 1,
X выбран из -NH- и -О-, и
Y выбран из -Н, -СН3, -СН2СН3, -СН2ОН и -СН2СН2ОН.
4. Соединение, или его стереоизомер или фармацевтически приемлемая соль по п. 1 или п. 3, где Q представляет собой замещенный амино, выбранный из группы, состоящей из -NHSO2CH3, -NHCOH, -NHCONHCH3, -NHCONHCH2CH3, -NHSO2NHCH3, -NHSO2NHCH2CH3, -NHCOCH3, -NHCOOCH3, -NHCOOCH2CH2OH, -NHCONH2 и -NHCN.
5. Соединение, или его стереоизомер или фармацевтически приемлемая соль по п. 1, где Q представляет собой алкил, выбранный из группы, состоящей из метила, этила, пропила, бутила и пентила.
6. Соединение, или его стереоизомер или фармацевтически приемлемая соль по п. 1, где А выбран из:
Figure 00000005
Figure 00000006
Figure 00000007
и
Figure 00000008
.
7. Соединение, или его стереоизомер или фармацевтически приемлемая соль по п. 1, где соединение выбрано из группы, состоящей из:
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
и
Figure 00000022
8. Фармацевтическая композиция, содержащая соединение, или его стереоизомер или фармацевтически приемлемую соль, по любому из пп. 1-7 и фармацевтически приемлемое вспомогательное средство.
9. Способ терапевтического лечения гипертензии или предгипертензии у субъекта, включающий введение субъекту соединения, или его стереоизомера или фармацевтически приемлемой соли, по любому из пп. 1-7 или композиции по п. 8.
10. Способ профилактического лечения фиброза у субъекта, включающий введение субъекту соединения, или его стереоизомера или фармацевтически приемлемой соли, по любому из пп. 1-7 или композиции по п. 8.
11. Способ терапевтического лечения фиброза у субъекта, включающий введение субъекту соединения, или его стереоизомера или фармацевтически приемлемой соли, по любому из пп. 1-7 или композиции по п. 8.
12. Способ терапевтического лечения гипертензии и фиброза у субъекта, включающий введение субъекту соединения, или его стереоизомера или фармацевтически приемлемой соли, по любому из пп. 1-7 или композиции по п. 8.
13. Способ лечения предгипертензии и фиброза у субъекта, включающий введение субъекту соединения, или его стереоизомера или фармацевтически приемлемой соли, по любому из пп. 1-7 или композиции по п. 8.
14. Способ по любому из пп. 10-13, где фиброз представляет собой фиброз миокарда или фиброз почки.
15. Способ по любому из пп. 10-13, где фиброз представляет собой фиброз почки и фиброз почки.
16. Применение соединения, или его стереоизомера или фармацевтически приемлемой соли, по любому из пп. 1-7 для изготовления лекарственного препарата для терапевтического лечения гипертензии или предгипертензии.
17. Применение соединения, или его стереоизомера или фармацевтически приемлемой соли по любому из пп. 1-7 для изготовления лекарственного препарата для профилактического лечения фиброза.
18. Применение соединения, или его стереоизомера или фармацевтически приемлемой соли по любому из пп. 1-7 для изготовления лекарственного препарата для терапевтического лечения фиброза.
19. Применение соединения, или его стереоизомера или фармацевтически приемлемой соли по любому из пп. 1-7 для изготовления лекарственного препарата для терапевтического лечения гипертензии и фиброза или предгипертензии и фиброза.
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