RU2011151611A - Композиции для модуляции киназного каскада и способы их применения - Google Patents

Композиции для модуляции киназного каскада и способы их применения Download PDF

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RU2011151611A
RU2011151611A RU2011151611/04A RU2011151611A RU2011151611A RU 2011151611 A RU2011151611 A RU 2011151611A RU 2011151611/04 A RU2011151611/04 A RU 2011151611/04A RU 2011151611 A RU2011151611 A RU 2011151611A RU 2011151611 A RU2011151611 A RU 2011151611A
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polymorph
dsc
acetone
morpholinoethoxy
pyridin
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Джереми Э. КОУДИ
Дэвид Г. Мл. ХЭНГАУЭР
Пол К. ИСБЕСТЕР
Грант Дж. ПАЛМЕР
Дебасис ПАТРА
Джонатон Сэлсбери
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КАЙНЕКС ФАРМАСЬЮТИКАЛС ЭлЭлСи
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/59—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with at least one of the bonds being to sulfur
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    • C07—ORGANIC CHEMISTRY
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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Abstract

1. Полиморф мезилатной соли 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-N-бензилацетамида (Форма A), характеризующийся структурой дифракции рентгеновских лучей, в основном подобной представленной на фиг.7.2. Полиморф мезилатной соли 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-N-бензилацетамида (Форма A), характеризующийся структурой дифракции рентгеновских лучей, включающей пики в приблизительно 22,7, 19,7, 18,9 и 16,3 градусов 2θ.3. Полиморф мезилатной соли 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-N-бензилацетамида (Форма A), характеризующийся термограммой дифференциальной сканирующей калориметрии (DSC), имеющей единственное максимальное значение при приблизительно 164 при измерении прибором Mettler 822DSC.4. Полиморф по п.1, дополнительно характеризующийся термограммой дифференциальной сканирующей калориметрии (DSC), имеющей единственное максимальное значение при приблизительно 164 при измерении прибором Mettler 822DSC.5. Полиморф по п.2, дополнительно характеризующийся термограммой дифференциальной сканирующей калориметрии (DSC), имеющей единственное максимальное значение при приблизительно 164 при измерении прибором Mettler 822DSC.6. Полиморф по любому из пп.1-5, полученный способом очистки, включающим стадию перекристаллизации сырого препарата указанной соли из ацетона.7. Полиморф по п.6, причем количество указанного используемого ацетона составляет более чем 64 объема.8. Фармацевтическая композиция, включающая полиморф по п.6 и фармацевтически приемлемый эксципиент или носитель.9. Способ лечения или профилактики заболевания или состояния у пациента, включающий стадия введения указанному пациенту фармацевтической композиции по п.8, причем указан

Claims (13)

1. Полиморф мезилатной соли 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-N-бензилацетамида (Форма A), характеризующийся структурой дифракции рентгеновских лучей, в основном подобной представленной на фиг.7.
2. Полиморф мезилатной соли 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-N-бензилацетамида (Форма A), характеризующийся структурой дифракции рентгеновских лучей, включающей пики в приблизительно 22,7, 19,7, 18,9 и 16,3 градусов 2θ.
3. Полиморф мезилатной соли 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-N-бензилацетамида (Форма A), характеризующийся термограммой дифференциальной сканирующей калориметрии (DSC), имеющей единственное максимальное значение при приблизительно 164 при измерении прибором Mettler 822e DSC.
4. Полиморф по п.1, дополнительно характеризующийся термограммой дифференциальной сканирующей калориметрии (DSC), имеющей единственное максимальное значение при приблизительно 164 при измерении прибором Mettler 822e DSC.
5. Полиморф по п.2, дополнительно характеризующийся термограммой дифференциальной сканирующей калориметрии (DSC), имеющей единственное максимальное значение при приблизительно 164 при измерении прибором Mettler 822e DSC.
6. Полиморф по любому из пп.1-5, полученный способом очистки, включающим стадию перекристаллизации сырого препарата указанной соли из ацетона.
7. Полиморф по п.6, причем количество указанного используемого ацетона составляет более чем 64 объема.
8. Фармацевтическая композиция, включающая полиморф по п.6 и фармацевтически приемлемый эксципиент или носитель.
9. Способ лечения или профилактики заболевания или состояния у пациента, включающий стадия введения указанному пациенту фармацевтической композиции по п.8, причем указанное заболевание или состояние выбраны из рака, потери слуха, остеопороза, ожирения, диабета, глазных заболеваний, инсульта, атеросклероза, нейропатической боли, гепатита B и аутоиммунного заболевания.
10. Способ получения полиморфа по любому из пп.1-5, включающий стадию добавления метансульфоновой кислоты к 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-N-бензилацетамиду в ацетоне.
11. Способ по п.10, в котором количество указанного ацетона составляет более чем 64 объема.
12. Способ по п.11, в котором количество указанного ацетона составляет более чем 64 и менее чем 100 объемов.
13. Способ по п.12, в котором количество указанного ацетона составляет 80 объемов.
RU2011151611/04A 2009-05-19 2010-05-19 Композиции для модуляции киназного каскада и способы их применения RU2569299C2 (ru)

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US12/468,694 US7935697B2 (en) 2006-12-28 2009-05-19 Compositions for modulating a kinase cascade and methods of use thereof
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US8309549B2 (en) 2012-11-13
US20090318450A1 (en) 2009-12-24
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US8901297B2 (en) 2014-12-02
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