RU2007133802A - Кристаллические формы производной имидазола - Google Patents

Кристаллические формы производной имидазола Download PDF

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RU2007133802A
RU2007133802A RU2007133802/04A RU2007133802A RU2007133802A RU 2007133802 A RU2007133802 A RU 2007133802A RU 2007133802/04 A RU2007133802/04 A RU 2007133802/04A RU 2007133802 A RU2007133802 A RU 2007133802A RU 2007133802 A RU2007133802 A RU 2007133802A
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ethyl
imidazo
pyridin
carbonyl
dimethyl
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RU2007133802/04A
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RU2357968C1 (ru
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Наоаки ХАРУТА (JP)
Наоаки ХАРУТА
Томоки КАТО (JP)
Томоки КАТО
Чжэн Джейн ЛИ (US)
Чжэн Джейн ЛИ
Тойохару НУМАТА (JP)
Тойохару Нумата
Эндрю Винсент ТРАСК (GB)
Эндрю Винсент Траск
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Пфайзер Инк. (US)
Пфайзер Инк.
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Claims (12)

1. Практически чистая, кристаллическая, полиморфная форма A N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)-фенил]этил}амино)карбонил]-4-метилбензолсульфонамида, которая характеризуется порошковой рентгенограммой, полученной при Cu Kα излучении, включающей основные пики при 2-Тета° 9,8, 13,2, 13,4, 13,7, 14,1, 17,5, 19,0, 21,6, 24,0 и 25,7 +/- 0,2.
2. Полиморфная форма N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метил-бензолсульфонамида по п.1, которая дополнительно характеризуется дифференциальной сканирующей калориметрией (ДСК) с эндотермическим эффектом при температуре около 160˚C.
3. Фармацевтическая композиция, включающая полиморфную форму A N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)-фенил]этил}амино)карбонил]-4-метилбензолсульфонамида по пп.1-2, вместе с одним или более фармацевтически приемлемыми наполнителями.
4. Полиморфная форма A N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метил-бензолсульфонамида по пп.1-2 для применения в качестве лекарственного препарата.
5. Применение полиморфной формы A N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метилбензолсульфонамида по пп.1-2, или фармацевтической композиции по п.3, для получения лекарственного препарата для лечебной, паллиативной или профилактической терапии боли, воспаления, остеоартрита или ревматоидного артрита.
6. Способ терапии боли, воспаления, остеоартрита или ревматоидного артрита, который включает введение эффективного количества полиморфной формы A N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метил-бензолсульфонамида по пп.1-2, или фармацевтической композиции по п.3, животному, включая человека, в случае необходимости такой терапии.
7. Практически чистая, кристаллическая, полиморфная форма B N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)-фенил]этил}амино)карбонил]-4-метилбензолсульфонамида, которая характеризуется порошковой рентгенограммой, полученной при Cu Kα излучении, включающей основные пики при 2-Тета˚ 6,3, 11,3, 12,8, 13,0, 13,5, 14,5, 15,6, 20,5, 23,0 and 25,8 +/- 0,2.
8. Полиморфная форма B N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метил-бензолсульфонамида по п.7, которая дополнительно характеризуется дифференциальной сканирующей калориметрией (ДСК) с эндотермическим эффектом при температуре около 178˚C.
9. Фармацевтическая композиция, включающая полиморфную форму В N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)-фенил]этил}амино)карбонил]-4-метилбензолсульфонамида по пп.7-8, вместе с одним или более фармацевтически приемлемыми наполнителями.
10. Полиморфная форма В N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метил-бензолсульфонамида по пп.7-8 для применения в качестве лекарственного препарата.
11. Применение полиморфной формы В N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метилбензолсульфонамида по пп.7-8, или фармацевтической композиции по п.9, для получения лекарственного препарата для лечебной, паллиативной или профилактической терапии боли, воспаления, остеоартрита или ревматоидного артрита.
12. Способ терапии боли, воспаления, остеоартрита или ревматоидного артрита, который включает введение эффективного количества полиморфной формы В N-[({2-[4-(2-этил-4,6-диметил-1H-имидазо[4,5-c]пиридин-1-ил)фенил]этил}амино)карбонил]-4-метил-бензолсульфонамида по пп.7-8, или фармацевтической композиции по п.9, животному, включая человека, в случае необходимости такой терапии.
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