RU2016130095A - Конъюгат анти-trop2 антитело-лекарственное средство - Google Patents

Конъюгат анти-trop2 антитело-лекарственное средство Download PDF

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RU2016130095A
RU2016130095A RU2016130095A RU2016130095A RU2016130095A RU 2016130095 A RU2016130095 A RU 2016130095A RU 2016130095 A RU2016130095 A RU 2016130095A RU 2016130095 A RU2016130095 A RU 2016130095A RU 2016130095 A RU2016130095 A RU 2016130095A
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cancer
crystalline form
benzylcarbamoyl
pyrazino
octahydro
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RU2016130095A
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RU2016130095A3 (ru
RU2705367C2 (ru
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Тосинори АГАЦУМА
Су ТАКАХАСИ
Дзун ХАСЕГАВА
Даисуке ОКАДЗИМА
Хирофуми ХАМАДА
Мики ЯМАГУТИ
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Дайити Санкио Компани, Лимитед
Саппоро Медикал Юниверсити
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    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
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    • 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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    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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Claims (8)

1. Кристаллическая форма 4-(((6S,9S)-1-(бензилкарбамоил)-2,9-диметил-4,7-диоксо-8-(хинолин-8-илметил)октагидро-1H-пиразино[2,1-c][1,2,4]триазин-6-ил)метил)фенилдигидрофосфата или его гидрата.
2. Кристаллическая форма гидрата 4-(((6S,9S)-1-(бензилкарбамоил)-2,9-диметил-4,7-диоксо-8-(хинолин-8-илметил)октагидро-1H-пиразино[2,1-c][1,2,4]триазин-6-ил)метил)фенилдигидрофосфата.
3. Кристаллическая форма по п.2, демонстрирующая дифракционный пик при угле дифракции (2θ±0,2°) 15,9° в порошковой рентгеновской дифракции.
4. Кристаллическая форма гидрата 4-(((6S,9S)-1-(бензилкарбамоил)-2,9-диметил-4,7-диоксо-8-(хинолин-8-илметил)октагидро-1H-пиразино[2,1-c][1,2,4]триазин-6-ил)метил)фенилдигидрофосфата, демонстрирующая пики при химических сдвигах (м.д.) 15,8, 56,4, 127,8, 157,4 и 168,6 в спектре твердотельного 13С ЯМР.
5. Способ получения кристаллической формы 4-(((6S,9S)-1-(бензилкарбамоил)-2,9-диметил-4,7-диоксо-8-(хинолин-8-илметил)октагидро-1H-пиразино[2,1-c][1,2,4]триазин-6-ил)метил)фенилдигидрофосфата или его гидрата, включающий стадию кристаллизации из растворителя, выбранного из группы, состоящей из спиртового растворителя, воды и их комбинации.
6. Фармацевтическая композиция, содержащая кристаллическую форму по любому одному из п.п.1-4 в качестве активного ингредиента.
7. Противоопухолевое средство, содержащее кристаллическую форму по любому одному из п.п.1-4 в качестве активного ингредиента.
8. Противоопухолевое средство по п.7, в котором опухоль представляет собой рак легких, рак молочной железы, рак желудка, рак поджелудочной железы, рак печени, рак матки, рак яичников, глиому, меланому, колоректальный рак, лимфому или рак крови.
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