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1.发明公开CHRYSTALS INCLUDING A MALIC ACID SALT OF N-[2-(DIETHYLAMINO)ETHYL]-5-[(5-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOLE-3-YLIDENE)METHYL]-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXAMIDE, PROCESSES FOR ITS PREPARATION AND COMPOSITIONS THEREOF 有权晶体中N- [2-（二乙基氨基）乙基] -5的苹果酸盐 - [（5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基）甲基] -2,4-二甲基 -1H-吡咯-3-甲酰胺，其制备方法和组合物THEREFORE
公开(公告)号：EP1419151A1
公开(公告)日：2004-05-19
申请号：EP02759342.5
申请日：2002-08-13
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention provides crystals, and compositions thereof, wherein the crystals include a malic acid salt of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. Methods of preparing such crystals are also disclosed.
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2.发明授权CHRYSTALS INCLUDING A MALIC ACID SALT OF N-[2-(DIETHYLAMINO)ETHYL] -5-[(5-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOLE-3-YLIDENE)METHYL] -2,4-DIMETHYL-1H-PYRROLE-3-CARBOXAMIDE, PROCESSES FOR ITS PREPARATION AND COMPOSITIONS THEREOF 有权晶体中N- [2-（二乙基氨基）乙基] -5的苹果酸盐 - [（5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基）甲基] -2,4-二甲基 -1H-吡咯-3-甲酰胺，其制备方法和组合物THEREFORE
公开(公告)号：EP1419151B1
公开(公告)日：2014-02-26
申请号：EP02759342.5
申请日：2002-08-13
IPC分类号： C07D403/06
CPC分类号： C07D403/06
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公开(公告)号：EP3168218B1
公开(公告)日：2018-11-14
申请号：EP16196036.4
申请日：2002-08-13
IPC分类号： C07D403/06 , A61K31/404 , A61P35/00
CPC分类号： C07D403/06
摘要： The present invention provides crystals, and compositions thereof, wherein the crystals include a malic acid salt of N-[2-(diethylamino)ethyl]5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. Methods of preparing such crystals are also disclosed.
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4.发明公开A CRYSTAL COMPRISING AN L-MALIC ACID SALT OF N-[2-(DIETHYLAMINO)ETHYL]-5-[(5-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE)METHYL]-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXAMIDE FOR USE AS A MEDICAMENT 审中-公开晶体含有N- [2-（二乙基氨基）乙基] -5的苹果酸盐 - [（5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基）甲基] -2,4- 二甲基-1H-吡咯-3-甲酰胺，用作药物
公开(公告)号：EP3168218A1
公开(公告)日：2017-05-17
申请号：EP16196036.4
申请日：2002-08-13
IPC分类号： C07D403/06 , A61K31/404 , A61P35/00
CPC分类号： C07D403/06
摘要： The present invention provides a crystal comprising the L-malic acid salt of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, wherein the crystal has characteristic diffraction peaks at 13.2 and 24.2 degrees two-theta in a powder X-ray diffraction pattern, for use as a medicament.
摘要翻译： 本发明提供一种晶体，其包括N- [2-（二乙基氨基）乙基] -5的L-苹果酸盐 - [（5-氟-1,2-二氢-2-氧代-3H-吲哚-3-亚基 基）甲基] -2,4-二甲基-1H-吡咯-3-甲酰胺，worin晶体具有在13.2和24.2度2θ的粉末X-射线衍射图案，其用作药物的特征衍射峰。
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公开(公告)号：EP0892792B1
公开(公告)日：2001-11-21
申请号：EP97915865.6
申请日：1997-03-28
发明人： PEARLMAN, Bruce, A. , PERRAULT, William, R. , BARBACHYN, Michael, R. , MANNINEN, Peter, R. , TOOPS, Dana, S. , HOUSER, David, J. , FLECK, Thomas, J.
IPC分类号： C07D263/24 , C07D263/20 , C07D413/10 , C07D487/04 , C07D413/04
CPC分类号： C07D487/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/20 , C07D263/24 , C07D413/04 , C07D413/10
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公开(公告)号：EP0892792A1
公开(公告)日：1999-01-27
申请号：EP97915865.0
申请日：1997-03-28
发明人： PEARLMAN, Bruce, A. , PERRAULT, William, R. , BARBACHYN, Michael, R. , MANNINEN, Peter, R. , TOOPS, Dana, S. , HOUSER, David, J. , FLECK, Thomas, J.
CPC分类号： C07D487/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/20 , C07D263/24 , C07D413/04 , C07D413/10
摘要： The present invention includes processes for producing 5-hydroxymethyl substituted oxazolidinone alcohols (III) from carbamates (IIA) or a trifluoroacetamide (IIB) using a dihydroxy compound (I) or glycidol (IV) starting material and for the transformation of the hydroxymethyl substituted oxazolidinone alcohols (III) to the corresponding amino compounds, 5-aminomethyl substituted oxazolidinone amines (VII) which are acylated to form commercially useful antibacterial 5-acylamidomethyl substituted oxazolidinone (VIII).
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