RU2011147186A - 2, 5-дизамещенные арилсульфонамидные антагонисты ссr3 - Google Patents
2, 5-дизамещенные арилсульфонамидные антагонисты ссr3 Download PDFInfo
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Abstract
1. Соединение формулы Ia или его фармацевтически приемлемая соль, сольват, гидрат, стереоизомер или таутомер:где X представляет собой S, SO или SO;Y и Z представляют собой(i) Y представляет собой NR; и Z представляет собой =О, CORили Салкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; или(ii) Y представляет собой CH, CHF, CHCH, O, S или SO; и Z представляет собой водород или Салкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном;Rи Rнезависимо представляют собой галоген, Салкил или Сгалогеналкил;Rпредставляет собой CN или NO;Rпредставляет собой водород или Салкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; иRпредставляет собой водород или Салкил; иRпредставляет собой водород или Салкил.2. Соединение формулы I или его фармацевтически приемлемая соль, сольват, гидрат, стереоизомер или таутомер:где X представляет собой S, SO или SO;Y и Z представляют собой(i) Y представляет собой NR; и Z представляет собой =О или Салкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; или(ii) Y представляет собой CH, CHF, CHCH, O, S или SO; и Z представляет собой водород или Салкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном;Rи Rнезависимо представляют собой галоген, Салкил или Сгалогеналкил;Rпредставляет собой CN или NO;Rпредставляет собой водород или Салкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; иRпредставляет собой водород или Салкил.3. Соединение по п.1 или 2, где X представляет собой S.4. Соединение по п.1 или 2, где Rпредста�
Claims (31)
1. Соединение формулы Ia или его фармацевтически приемлемая соль, сольват, гидрат, стереоизомер или таутомер:
где X представляет собой S, SO или SO2;
Y и Z представляют собой
(i) Y представляет собой NR5; и Z представляет собой =О, CO2R6 или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; или
(ii) Y представляет собой CH2, CHF, CHCH3, O, S или SO2; и Z представляет собой водород или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном;
R1 и R2 независимо представляют собой галоген, С1-6 алкил или С1-6 галогеналкил;
R3 представляет собой CN или NO2;
R4 представляет собой водород или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; и
R5 представляет собой водород или С1-6 алкил; и
R6 представляет собой водород или С1-6 алкил.
2. Соединение формулы I или его фармацевтически приемлемая соль, сольват, гидрат, стереоизомер или таутомер:
где X представляет собой S, SO или SO2;
Y и Z представляют собой
(i) Y представляет собой NR5; и Z представляет собой =О или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; или
(ii) Y представляет собой CH2, CHF, CHCH3, O, S или SO2; и Z представляет собой водород или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном;
R1 и R2 независимо представляют собой галоген, С1-6 алкил или С1-6 галогеналкил;
R3 представляет собой CN или NO2;
R4 представляет собой водород или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; и
R5 представляет собой водород или С1-6 алкил.
3. Соединение по п.1 или 2, где X представляет собой S.
4. Соединение по п.1 или 2, где R3 представляет собой CN.
5. Соединение по п.1 или 2, где R3 представляет собой NO2.
6. Соединение формулы II или его фармацевтически приемлемая соль, сольват, гидрат, стереоизомер или таутомер:
где Y и Z представляют собой
(i) Y представляет собой NR5; и Z представляет собой =О или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном; или
(ii) Y представляет собой CH2, CHF, CHCH3, O, S или SO2; и Z представляет собой водород или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном;
R1 и R2 независимо представляют собой галоген, С1-6 алкил или С1-6 галогеналкил;
R4 представляет собой водород или С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном;
R5 представляет собой водород или С1-6 алкил;
при условии, что если Y представляет собой CH2, по крайней мере один из Z и R4 представляет собой С1-6 алкил, необязательно замещенный арилом, гидрокси, карбокси, алкокси, карбамоилом или галогеном.
7. Соединение по п.6, где Y представляет собой NR5.
8. Соединение по п.7, где R5 представляет собой H.
9. Соединение по п.7 или 8, где Z представляет собой =О.
10. Соединение по п.7 или 8, где Z представляет собой CH3.
11. Соединение по п.6, где Y представляет собой CH2.
12. Соединение по п.6, где Y представляет собой CHF.
13. Соединение по п.6, где Y представляет собой CHCH3.
14. Соединение по п.6, где Y представляет собой O.
15. Соединение по п.6, где Y представляет собой S.
16. Соединение по п.6, где Y представляет собой SO2.
17. Соединение по любому из пп. 12-16, где Z представляет собой H.
18. Соединение по любому из пп. 11-16, где Z представляет собой CH3.
19. Соединение по п.6, где R1 и R2 представляют собой Cl.
20. Соединение по п.6, где R1 и R2 представляют собой CH3.
21. Соединение по п.6, где R1 и R2 представляют собой CF3.
22. Соединение по п.6, где R4 представляет собой H.
24. Фармацевтическая композиция, включающая соединение по любому из пп.1, 2 и 6 и один или несколько фармацевтически приемлемых носителей или эксципиентов.
25. Способ лечения, профилактики или улучшения одного или нескольких симптомов связанного с CCR3 нарушения, заболевания или состояния у субъекта, включающий введение субъекту терапевтически эффективного количества соединения по любому из пп.1, 2 и 6 или композиции по п.24.
26. Способ по п.25, где нарушение или заболевание представляет собой воспалительное или иммунорегулируемое нарушение или заболевание.
27. Способ по п.25, где нарушение или заболевание представляет собой астму, ринит, аллергическое заболевание или аутоиммунную патологию.
28. Способ по п.25, где нарушение или заболевание представляет собой ВИЧ, гранулему легких или болезнь Альцгеймера.
29. Способ по п.25, где соединение или композицию вводят перорально, парентерально или наружно.
30. Способ по п.25, где соединение или композицию вводят в сочетании со вторым терапевтическим агентом.
31. Способ модулирования активности CCR3, включающий контактирование рецептора CCR3 с соединением по любому из пп.1, 2 и 6 или композиции по п.24.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17162609P | 2009-04-22 | 2009-04-22 | |
US61/171,626 | 2009-04-22 | ||
PCT/US2010/031832 WO2010123959A2 (en) | 2009-04-22 | 2010-04-21 | 2,5-disubstituted arylsulfonamide ccr3 antagonists |
Publications (2)
Publication Number | Publication Date |
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RU2011147186A true RU2011147186A (ru) | 2013-05-27 |
RU2527165C2 RU2527165C2 (ru) | 2014-08-27 |
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Application Number | Title | Priority Date | Filing Date |
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RU2011147186/04A RU2527165C2 (ru) | 2009-04-22 | 2010-04-21 | 2, 5-дизамещенные арилсульфонамидные антагонисты ссr3 |
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US (4) | US8318747B2 (ru) |
EP (2) | EP2421830B1 (ru) |
JP (1) | JP5847702B2 (ru) |
KR (2) | KR20120013403A (ru) |
CN (1) | CN102459177B (ru) |
AR (1) | AR076362A1 (ru) |
AU (1) | AU2010239340B2 (ru) |
BR (1) | BRPI1014669A2 (ru) |
CA (1) | CA2758968C (ru) |
CL (1) | CL2011002617A1 (ru) |
CO (1) | CO6470792A2 (ru) |
CR (1) | CR20110535A (ru) |
DK (1) | DK2749554T3 (ru) |
EC (1) | ECSP11011473A (ru) |
ES (2) | ES2664984T3 (ru) |
HK (2) | HK1162475A1 (ru) |
HU (1) | HUE038507T2 (ru) |
IL (4) | IL215840A (ru) |
MX (2) | MX2011011080A (ru) |
MY (1) | MY162440A (ru) |
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NZ (2) | NZ595823A (ru) |
PE (2) | PE20150925A1 (ru) |
RU (1) | RU2527165C2 (ru) |
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PE20150925A1 (es) | 2009-04-22 | 2015-06-14 | Axikin Pharmaceuticals Inc | Antagonistas de ccr3 de arilsulfonamida 2,5-disustituida |
HUE025699T2 (en) * | 2010-03-02 | 2016-04-28 | Axikin Pharmaceuticals Inc | Isotopically enriched arylsulfonamide derivatives as CCR3 antagonists |
NZ587490A (en) * | 2010-08-20 | 2013-03-28 | Greentide Ltd | Anti-Microbial Compounds containing compounds with a sugar substituent |
CN103298786B (zh) * | 2010-10-11 | 2016-01-20 | 埃克希金医药品有限公司 | 芳基磺酰胺盐ccr3拮抗剂 |
US9487476B2 (en) * | 2011-10-12 | 2016-11-08 | Yale University | Catechol diethers as potent anti-HIV agents |
US10213421B2 (en) | 2012-04-04 | 2019-02-26 | Alkahest, Inc. | Pharmaceutical formulations comprising CCR3 antagonists |
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BR112019020798A2 (pt) * | 2017-04-05 | 2020-04-28 | Alkahest Inc | métodos e composições para tratamento de danos associados ao envelhecimento usando inibidores de ccr3 |
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