RU2461551C2 - Азолкарбоксамидное соединение или его фармацевтически приемлемая соль - Google Patents

Азолкарбоксамидное соединение или его фармацевтически приемлемая соль Download PDF

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RU2461551C2
RU2461551C2 RU2010120676/04A RU2010120676A RU2461551C2 RU 2461551 C2 RU2461551 C2 RU 2461551C2 RU 2010120676/04 A RU2010120676/04 A RU 2010120676/04A RU 2010120676 A RU2010120676 A RU 2010120676A RU 2461551 C2 RU2461551 C2 RU 2461551C2
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carboxamide
phenyl
thiazole
pharmaceutically acceptable
methoxyethyl
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RU2010120676/04A
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RU2010120676A (ru
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Кейзо СУГАСАВА (JP)
Кейзо СУГАСАВА
Кенити КАВАГУТИ (JP)
Кенити КАВАГУТИ
Такахо НОМУРА (JP)
Такахо НОМУРА
Сунитиро МАЦУМОТО (JP)
Сунитиро Мацумото
Такаси СИН (JP)
Такаси Син
Хиденори АЗАМИ (JP)
Хиденори АЗАМИ
Томоаки АБЕ (JP)
Томоаки АБЕ
Акира СУГА (JP)
Акира СУГА
Рюси СЕО (JP)
Рюси Сео
Масаюки ТАНАХАСИ (JP)
Масаюки Танахаси
Тору ВАТАНАБЕ (JP)
Тору ВАТАНАБЕ
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Астеллас Фарма Инк.
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Abstract

Обеспечение терапевтического и/или профилактического средства от частого мочеиспускания, частых позывов на мочеиспускание и недержания мочи, связанных с различными заболеваниями нижнего мочеполового тракта, включая повышенную активность мочевого пузыря, различных заболеваний нижнего мочеполового тракта, сопровождающихся болью в нижнем мочеполовом тракте, таких как интерстициальный цистит, хронический простатит и подобные, и различных заболеваний, сопровождающихся болью, на основании отличного ингибиторного действия в отношении trkA рецептора. Подтверждено, что новое азолкарбоксамидное соединение или его фармацевтически приемлемая соль, в котором тиазольное кольцо или оксазольное кольцо связано с бензольным кольцом, пиридиновым кольцом, пиридазиновым кольцом, тиофеновым кольцом, пиразольным кольцом или пиррольным кольцом через карбоксамид, или его соль обладают высокой активностью ингибирования trkA рецептора, и было обнаружено, что их можно использовать в качестве терапевтического и/или профилактического средства, которое является отличным, в том что касается эффективности и безопасности, от частого мочеиспускания, частых позывов на мочеиспускание и недержания мочи, связанных с различными заболеваниями нижнего мочеполового тракта, включая повышенную активность мочевого пузыря, различных заболеваний нижнего мочеполового тракта, сопровождающихся болью в нижнем мочеполовом тракте, таких как интерстициальный цистит, хронический простатит и подобные, и различных заболеваний, сопровождающихся болью, таким образом, было создано настоящее изобретение. 4 н. и 20 з.п. ф-лы, 1195 пр., 215 табл.

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Claims (24)

1. Соединение, которое выбрано из группы, включающей:
2-морфолин-4-ил-N-[2-(пиридин-3-илкарбамоил)фенил]-1,3-оксазол-4-карбоксамид,
2-(4-этоксипиперидин-1-ил)-N-[2-(тетрагидро-2Н-пиран-4-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид,
2-[(2-метоксиэтил)(метил)амино]-N-[2-(пиридин-3-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид,
2-[(3S)-3-метоксипирролидин-1-ил]-N-[2-(пиридин-3-илкарбамоил)фенил]-1,3-оксазол-4-карбоксамид,
2-[(2-метоксиэтил)(метил)амино]-N-[2-(тетрагидро-2H-пиран-4-илкарбамоил)фенил]-1,3-оксазол-4-карбоксамид,
N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-2-[4-(пиримидин-2-илокси)пиперидин-1-ил]-1,3-тиазол-4-карбоксамид,
4-[({2-[4-(пиримидин-2-илокси)пиперидин-1-ил]-1,3-тиазол-4-ил}карбонил)амино]-N-(тетрагидро-2Н-пиран-4-ил)никотинамид,
2-[(2-метоксиэтил)(метил)амино]-N-[4-метокси-2-(пиридин-3-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид,
2-[метил(тетрагидро-2Н-пиран-4-илметил)амино]-N-[4-(морфолин-4-илметил)-2-(тетрагидро-2Н-пиран-4-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид,
N-(2-[(2-метоксиэтил)карбамоил]-4-{[(2S)-2-метилморфолин-4-ил]метил}фенил)-2-[(3S)-3-метоксипирролидин-1-ил]-1,3-тиазол-4-карбоксамид,
N-{4-[(3,3-диметилморфолин-4-ил)метил]-2-[(2-метоксиэтил)карбамоил]фенил}-2-[(3S)-3-метоксипирролидин-1-ил]-1,3-тиазол-4-карбоксамид,
2-(3-метоксиазетидин-1-ил)-N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-1,3-тиазол-4-карбоксамид,
2-(3-метоксиазетидин-1-ил)-N-[2-{[(1R)-2-метокси-1-метилэтил]карбамоил}-4-(морфолин-4-илметил)фенил]-1,3-тиазол-4-карбоксамид,
N-{4-(этоксиметил)-2-[(2-метоксиэтил)карбамоил]фенил}-2-[(3S)-3-метоксипирролидин-1-ил]-1,3-тиазол-4-карбоксамид,
N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-2-[(2-метоксиэтил)(метил)амино]-1,3-тиазол-4-карбоксамид и
2-[(3S)-3-фторпирролидин-1-ил]-N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-1,3-тиазол-4-карбоксамид
или его фармацевтически приемелмая соль.
2. Фармацевтическая композиция, обладающая ингибирующей активностью в отношении trkA рецептора, содержащая соединение или его фармацевтически приемлемая соль по п.1 и фармацевтически приемлемый эксципиент.
3. Фармацевтическая композиция по п.2, которая представляет собой профилактическое и/или терапевтическое средство от частого мочеиспускания, частых позывов на мочеиспускание, недержания мочи и боли в нижнем мочеполовом тракте, связанной с различными заболеваниями нижнего мочеполового тракта, и различных заболеваний, сопровождающихся болью.
4. Фармацевтическая композиция по п.3, где заболевание нижнего мочеполового тракта представляет собой повышенную активность мочевого пузыря, интерстициальный цистит или хронический простатит.
5. Применение соединения или его фармацевтически приемлемой соли по п.1 для получения профилактического и/или терапевтического средства от частого мочеиспускания, частых позывов на мочеиспускание, недержания мочи и боли в нижнем мочеполовом тракте, связанной с различными заболеваниями нижнего мочеполового тракта, и различных заболеваний, сопровождающихся болью.
6. Применение по п.5, где заболевание нижнего мочеполового тракта представляет собой повышенную активность мочевого пузыря, интерстициальный цистит или хронический простатит.
7. Способ профилактики и/или лечения частого мочеиспускания, частых позывов на мочеиспускание, недержания мочи и боли в нижнем мочеполовом тракте, связанной с различными заболеваниями нижнего мочеполового тракта, и различных заболеваний, сопровождающихся болью, включающий введение пациенту эффективного количества соединения или его фармацевтически приемлемой соли по п.1.
8. Способ профилактики и/или лечения по п.7, где заболевание нижнего мочеполового тракта представляет собой повышенную активность мочевого пузыря, интерстициальный цистит или хронический простатит.
9. Соединение по п.1, представляющее собой 2-морфолин-4-ил-N-[2-(пиридин-3-илкарбамоил)фенил]-1,3-оксазол-4-карбоксамид, или его фармацевтически приемлемая соль.
10. Соединение по п.1, представляющее собой 2-(4-этоксипиперидин-1-ил)-N-[2-(тетрагидро-2Н-пиран-4-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
11. Соединение по п.1, представляющее собой 2-[(2-метоксиэтил)(метил)амино]-N-[2-(пиридин-3-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
12. Соединение по п.1, представляющее собой 2-[(3S)-3-метоксипирролидин-1-ил]-N-[2-(пиридин-3-илкарбамоил)фенил]-1,3-оксазол-4-карбоксамид, или его фармацевтически приемлемая соль.
13. Соединение по п.1, представляющее собой 2-[(2-метоксиэтил)(метил)амино]-N-[2-(тетрагидро-2Н-пиран-4-илкарбамоил)фенил]-1,3-оксазол-4-карбоксамид, или его фармацевтически приемлемая соль.
14. Соединение по п.1, представляющее собой N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-2-[4-(пиримидин-2-илокси)пиперидин-1-ил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
15. Соединение по п.1, представляющее собой 4-[({2-[4-(пиримидин-2-илокси)пиперидин-1-ил]-1,3-тиазол-4-ил}карбонил)амино]-N-(тетрагидро-2Н-пиран-4-ил)никотинамид, или его фармацевтически приемлемая соль.
16. Соединение по п.1, представляющее собой 2-[(2-метоксиэтил)(метил)амино]-N-[4-метокси-2-(пиридин-3-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
17. Соединение по п.1, представляющее собой 2-[метил(тетрагидро-2Н-пиран-4-илметил)амино]-N-[4-(морфолин-4-илметил)-2-(тетрагидро-2Н-пиран-4-илкарбамоил)фенил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
18. Соединение по п.1, представляющее собой N-(2-[(2-метоксиэтил)карбамоил]-4-{[(2S)-2-метилморфолин-4-ил]метил}фенил)-2-[(3S)-3-метоксипирролидин-1-ил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
19. Соединение по п.1, представляющее собой N-{4-[(3,3-диметилморфолин-4-ил)метил]-2-[(2-метоксиэтил)карбамоил]фенил}-2-[(3S)-3-метоксипирролидин-1-ил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
20. Соединение по п.1, представляющее собой 2-(3-метоксиазетидин-1-ил)-N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
21. Соединение по п.1, представляющее собой 2-(3-метоксиазетидин-1-ил)-N-[2-{[(1R)-2-метокси-1-метилэтил]карбамоил}-4-(морфолин-4-илметил)фенил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
22. Соединение по п.1, представляющее собой N-{4-(этоксиметил)-2-[(2-метоксиэтил)карбамоил]фенил}-2-[(3S)-3-метоксипирролидин-1-ил]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
23. Соединение по п.1, представляющее собой N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-2-[(2-метоксиэтил)(метил)амино]-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
24. Соединение по п.1, представляющее собой 2-[(3S)-3-фторпирролидин-1-ил]-N-{2-[(2-метоксиэтил)карбамоил]-4-(морфолин-4-илметил)фенил}-1,3-тиазол-4-карбоксамид, или его фармацевтически приемлемая соль.
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