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RU2007143505A - Производные ацетилена - Google Patents

Производные ацетилена Download PDF

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RU2007143505A
RU2007143505A RU2007143505/04A RU2007143505A RU2007143505A RU 2007143505 A RU2007143505 A RU 2007143505A RU 2007143505/04 A RU2007143505/04 A RU 2007143505/04A RU 2007143505 A RU2007143505 A RU 2007143505A RU 2007143505 A RU2007143505 A RU 2007143505A
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compound
formula
free base
addition salt
acid addition
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RU2007143505/04A
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Ральф ГЛАТТАР (DE)
Ральф ГЛАТТАР
Томас Й. ТРОКСЛЕР (CH)
Томас Й. ТРОКСЛЕР
Томас ЦОЛЛЕР (FR)
Томас Цоллер
Йоахим НОЦУЛАК (DE)
Йоахим Ноцулак
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Новартис АГ (CH)
Новартис Аг
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Abstract

1. Соединение формулы (I) ! ! в которой ! R1 обозначает водород или алкил; ! R2 обозначает незамещенный или замещенный гетероцикл или ! R2 обозначает незамещенный или замещенный арил; ! R3 обозначает алкил или галоген; ! Х обозначает ординарную связь или алкандиильную группу, в которую необязательно включены один или большее количество атомов кислорода, или карбонильных групп, или карбонилоксигрупп в форме свободного основания или соли присоединения с кислотой. ! 2. Соединение формулы (I) по п.1, в которой Х обозначает ординарную связь. ! 3. Соединение формулы (I) по п.1 или 2, в которой R3 обозначает хлор. ! 4. Трансизомер соединения формулы (I) по любому из предыдущих пунктов. ! 5. Способ получения соединения формулы (I) по п.1 или его соли, который включает стадии реакции соединения формулы (II) ! ! в которой R1 и R3 являются такими, как определено в п.1, с соединением формулы (III) ! ! в которой Х и R2 являются такими, как определено в п.1, и выделения полученного соединения формулы (I) в форме свободного основания или соли присоединения с кислотой. ! 6. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения в качестве фармацевтического средства. ! 7. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей и нервной системы, полностью или частично опосредуемых mGluR5. ! 8. Фармацевтическая композиция,

Claims (11)

1. Соединение формулы (I)
Figure 00000001
в которой
R1 обозначает водород или алкил;
R2 обозначает незамещенный или замещенный гетероцикл или
R2 обозначает незамещенный или замещенный арил;
R3 обозначает алкил или галоген;
Х обозначает ординарную связь или алкандиильную группу, в которую необязательно включены один или большее количество атомов кислорода, или карбонильных групп, или карбонилоксигрупп в форме свободного основания или соли присоединения с кислотой.
2. Соединение формулы (I) по п.1, в которой Х обозначает ординарную связь.
3. Соединение формулы (I) по п.1 или 2, в которой R3 обозначает хлор.
4. Трансизомер соединения формулы (I) по любому из предыдущих пунктов.
5. Способ получения соединения формулы (I) по п.1 или его соли, который включает стадии реакции соединения формулы (II)
Figure 00000002
в которой R1 и R3 являются такими, как определено в п.1, с соединением формулы (III)
Figure 00000003
в которой Х и R2 являются такими, как определено в п.1, и выделения полученного соединения формулы (I) в форме свободного основания или соли присоединения с кислотой.
6. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения в качестве фармацевтического средства.
7. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей и нервной системы, полностью или частично опосредуемых mGluR5.
8. Фармацевтическая композиция, включающая соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой совместно с фармацевтическим носителем или разбавителем.
9. Применение соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей и нервной системы, полностью или частично опосредуемых mGluR5.
10. Применение соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой для приготовления фармацевтической композиции, предназначенной для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей и нервной системы, полностью или частично опосредуемых mGluR5.
11. Способ лечения нарушений, связанных с нерегулярностью глутаматергической передачи сигнала и нарушений нервной системы, полностью или частично опосредуемых mGluR5, способ включает введение субъекту, нуждающемуся в таком лечении, терапевтически эффективного количества соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой.
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