发明授权
US08586599B2 Polymorphic forms of 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof
有权
6-(1-甲基-1H-吡唑-4-基)-2- {3- [5-(2-吗啉-4-基 - 乙氧基) - 嘧啶-2-基] - 苄基} -2H的多晶型 哒嗪-3-酮磷酸二氢盐及其制备方法
- 专利标题: Polymorphic forms of 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof
- 专利标题(中): 6-(1-甲基-1H-吡唑-4-基)-2- {3- [5-(2-吗啉-4-基 - 乙氧基) - 嘧啶-2-基] - 苄基} -2H的多晶型 哒嗪-3-酮磷酸二氢盐及其制备方法
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申请号: US13141142申请日: 2009-11-24
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公开(公告)号: US08586599B2公开(公告)日: 2013-11-19
- 发明人: Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Eva Kriegbaum , Frank Stieber , Cristina Donini
- 申请人: Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Eva Kriegbaum , Frank Stieber , Cristina Donini
- 申请人地址: DE Darmstadt
- 专利权人: Merck Patent GmbH
- 当前专利权人: Merck Patent GmbH
- 当前专利权人地址: DE Darmstadt
- 代理机构: Millen, White, Zelano & Branigan, P.C.
- 优先权: EP08022253 20081222
- 国际申请: PCT/EP2009/008358 WO 20091124
- 国际公布: WO2010/072295 WO 20100701
- 主分类号: A61K31/501
- IPC分类号: A61K31/501 ; A61K31/5377 ; C07D413/14 ; C07D403/14
摘要:
The present invention relates to 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate, its solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
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