首页> 外国专利> Polymorphic forms of (s)-1-cyanobutan-2-yl (s)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl) phenyl) ureido) phenyl) ethylcarbamate

Polymorphic forms of (s)-1-cyanobutan-2-yl (s)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl) phenyl) ureido) phenyl) ethylcarbamate

机译:(s)-1-氰基丁-2-基(s)-1-(3-(3-(3-甲氧基-4-(恶唑-5-基)苯基)脲基)苯基)氨基甲酸乙酯的多晶型物

摘要

Disclosed is the polymorphic Form A1 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate wherein said polymorph comprises less than about 5 percent by weight of amorphous form and wherein the polymorph has a peak position at about 20.7 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation. Also disclosed is the polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein the polymorph has a peak position at about 4.1 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation. A process for preparing polymorphic form A1 or B2 is also disclosed. Also disclosed is the use of either polymorphic form A1 or B2 in the manufacture of a medicament for treating IMPDH-mediated diseases in a patient.
机译:公开了(S)-1-氰基丁烷-2-基(S)-1-(3-(3-(3-甲氧基-4-(恶唑-5-基)苯基)脲基)苯基)多晶型物A1氨基甲酸乙酯,其中所述多晶型物包含小于约5重量%的无定形形式,并且其中所述多晶型物在使用Cu Kα辐射获得的X射线粉末衍射图中在约20.7度2-θ处具有峰位置。还公开了(S)-1-氰基丁烷-2-基(S)-1-(3-(3-(3-甲氧基-4-(恶唑-5-基)苯基)脲基)苯基的多晶型形式B2。氨基甲酸乙酯),其中在使用Cu Kα辐射获得的X射线粉末衍射图中,多晶型物在约4.1度2-θ处具有峰位置。还公开了制备多晶型物A1或B2的方法。还公开了多晶型形式A1或B2在制备用于治疗患者的IMPDH介导的疾病的药物中的用途。

著录项

  • 公开/公告号NZ564252A

    专利类型

  • 公开/公告日2011-04-29

    原文格式PDF

  • 申请/专利权人 VERTEX PHARMACEUTICALS INCORPORATED;

    申请/专利号NZ20060564252

  • 发明设计人 BLYTHE TODD A;VLAHOVA PETINKA;

    申请日2006-05-25

  • 分类号C07D263/32;A61K31/421;A61P35;

  • 国家 NZ

  • 入库时间 2022-08-21 18:05:07

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