首页> 外国专利> Crystalline polymorph of (-)-4-4-4-4-(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl-methoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-(S)-1-ethyl-2(S)-hydroxylpropyl-3H-1,2,4-triazol-3-one and its use as a fungicide

Crystalline polymorph of (-)-4-4-4-4-(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl-methoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-(S)-1-ethyl-2(S)-hydroxylpropyl-3H-1,2,4-triazol-3-one and its use as a fungicide

机译:(-)-4- [4- [4- [4-[[[(2R-顺式)-5-(2,4-二氟苯基)四氢-5-(1H-1,2,4-三唑- 1-基甲基)呋喃-3-基]-甲氧基]苯基] -1-哌嗪基]苯基-2,4-二氢-2-[(S)-1-乙基-2(S)-羟丙基] -3H-1 ,2,4-三唑-3-一及其作为杀菌剂的用途

摘要

A crystalline polymorph of (-)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4 -triazol-1-ylmethyl)furan-3-yl]-methoxy]phenyl]-1-piperazinyl]phenyl-2 ,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one (refer to the formula shown). The described polymorph has an x-ray powder diffraction pattern expressed in terms of "d" spacing and relative intensities ("RI") (refer to the table shown). The polymorph has a lower impurity content and more consistent product quality i.e., more consistent physical characteristics including more consistent colour, rate of dissolution and ease of handling; as well as a longer term stability compared to its amorphous form. The polymorphs are useful for the treatment and prevention of fungal infections in mammals.
机译:(-)-4- [4- [4- [4-[[[(2R-顺式)-5-(2,4-二氟苯基)四氢-5-(1H-1,2,4-三唑) -1-基甲基)呋喃-3-基]-甲氧基]苯基] -1-哌嗪基]苯基-2,4-二氢-2-[(S)-1-乙基-2(S)-羟丙基] -3H- 1,2,4-三唑-3-一(请参见所示的式)。所述多晶型物具有以“ d”间距和相对强度(“ RI”)表示的X射线粉末衍射图(参见所示表)。该多晶型物具有较低的杂质含量和更一致的产品质量,即更一致的物理特性,包括更一致的颜色,溶解速率和易于处理;以及与无定形形式相比的长期稳定性。该多晶型物可用于治疗和预防哺乳动物的真菌感染。

著录项

  • 公开/公告号NZ503662A

    专利类型

  • 公开/公告日2002-10-25

    原文格式PDF

  • 申请/专利权人 SCHERING CORPORATION;

    申请/专利号NZ19980503662

  • 申请日1998-10-05

  • 分类号C07D405/14;A61K31/496;A61P31/00;A01N43/653;

  • 国家 NZ

  • 入库时间 2022-08-22 00:43:59

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