首页> 外国专利> CRYSTALLINE OF CARBAPENEM DERIVATIVE OR ITS HYDRATE, PREPARATION METHODS AND USES THEREOF

CRYSTALLINE OF CARBAPENEM DERIVATIVE OR ITS HYDRATE, PREPARATION METHODS AND USES THEREOF

机译:卡宾衍生物或其水合物的结晶,制备方法及其用途

摘要

The present invention relates to a crystalline form of carbapenems derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-((4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid_as represented by formula (I) or hydrate thereof and the preparation methods thereof, wherein said method comprise: dissolving the compound as represented by formula (I) by an aqueous solution of N,N′-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), and then adding a poor solvent dropwise to this solution, filtering and drying to obtain a crystal. Another method comprises: formulating the compound as represented by formula (I) as an aqueous suspension; after adjusting pH until complete dissolution, adding a mixed solvent of organic solvent/water with a certain volume ratio; adjusting pH to 5.4-7.0, cooling to low temperature, filtering and drying to obtain a crystal. The invention also relates to the use of the crystalline form of compound A or hydrate thereof in the preparation of a medicament for treating and/or preventing infectious diseases. The invention further relates to a pharmaceutical composition comprising the crystalline form of compound A or hydrate thereof and one or more pharmaceutical carriers and/or diluents.; embedded image
机译:本发明涉及碳青霉烯衍生物(4R,5S,6S)-6-((R)-1-羟乙基)-4-甲基-7-氧代-3-(((3S,5S)-5式(I)表示的-((4-氨基磺酰基苄基)氨基甲酰基)吡咯烷-3-基)硫基-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸或其水合物及其制备方法,其中所述方法包括:用N,N'-二甲基甲酰胺(DMF),二甲基亚砜(DMSO)的水溶液溶解式(I)表示的化合物,然后向该溶液中逐滴加入不良溶剂,过滤并干燥以获得晶体。另一种方法包括:将式(I)表示的化合物配制成水性悬浮液;调节pH至完全溶解后,加入一定体积比的有机溶剂/水混合溶剂。将pH调节至5.4-7.0,冷却至低温,过滤并干燥以获得晶体。本发明还涉及化合物A或其水合物的结晶形式在制备用于治疗和/或预防传染病的药物中的用途。本发明进一步涉及药物组合物,其包含化合物A或其水合物的结晶形式以及一种或多种药物载体和/或稀释剂。 “嵌入式图像”

著录项

  • 公开/公告号US2013079322A1

    专利类型

  • 公开/公告日2013-03-28

    原文格式PDF

  • 申请/专利权人 ZHENHUA HUANG;YANYAN DONG;

    申请/专利号US201113699550

  • 发明设计人 ZHENHUA HUANG;YANYAN DONG;

    申请日2011-05-20

  • 分类号C07D477/20;

  • 国家 US

  • 入库时间 2022-08-21 16:48:53

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