Upatinib-pyroglutamate amorphous substance as well as preparation method and application thereof
The invention relates to an amorphous substance of upatinib-pyroglutamate as well as a preparation method and application of the amorphous substance. The invention belongs to the field of medicinal chemistry, and overcomes the defects of poor water solubility of medicines and solubility and curative...
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| creator | SONG WEIGUO XU GUANGMING WEI LIUYA QIAO YANAN SUN LE LI FAHUI ZHONG WENDA FENG KAIRUI |
| description | The invention relates to an amorphous substance of upatinib-pyroglutamate as well as a preparation method and application of the amorphous substance. The invention belongs to the field of medicinal chemistry, and overcomes the defects of poor water solubility of medicines and solubility and curative effect of medicinal salts in the prior art. The preparation method comprises the following steps: dissolving upatinib and pyroglutamic acid in a first solvent, fully reacting, evaporating to remove the solvent, adding a second solvent, collecting a solid when turbidity appears, and drying to obtain white powder, namely the amorphous substance. Compared with upatinib L-tartrate, glutarate and L-di-p-methyl benzoyl tartrate in the prior art, the solubility of the amorphous substance disclosed by the invention is remarkably improved, and the anti-inflammatory activity is also improved.
本发明涉及一种乌帕替尼-焦谷氨酸盐的无定形物及其制备方法与应用。本发明属于药物化学领域，解决现有技术中药物水溶性差及药用盐溶解度及疗效方面存在的缺陷。本发明将乌帕替尼、焦谷氨酸溶于第一溶剂中，充分反应后，蒸除溶剂，加入第二溶剂，出现混浊，收集固体、干燥得白色粉末即为 |
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本发明涉及一种乌帕替尼-焦谷氨酸盐的无定形物及其制备方法与应用。本发明属于药物化学领域，解决现有技术中药物水溶性差及药用盐溶解度及疗效方面存在的缺陷。本发明将乌帕替尼、焦谷氨酸溶于第一溶剂中，充分反应后，蒸除溶剂，加入第二溶剂，出现混浊，收集固体、干燥得白色粉末即为</description><language>chi ; eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2024</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20240126&DB=EPODOC&CC=CN&NR=117447481A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20240126&DB=EPODOC&CC=CN&NR=117447481A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>SONG WEIGUO</creatorcontrib><creatorcontrib>XU GUANGMING</creatorcontrib><creatorcontrib>WEI LIUYA</creatorcontrib><creatorcontrib>QIAO YANAN</creatorcontrib><creatorcontrib>SUN LE</creatorcontrib><creatorcontrib>LI FAHUI</creatorcontrib><creatorcontrib>ZHONG WENDA</creatorcontrib><creatorcontrib>FENG KAIRUI</creatorcontrib><title>Upatinib-pyroglutamate amorphous substance as well as preparation method and application thereof</title><description>The invention relates to an amorphous substance of upatinib-pyroglutamate as well as a preparation method and application of the amorphous substance. The invention belongs to the field of medicinal chemistry, and overcomes the defects of poor water solubility of medicines and solubility and curative effect of medicinal salts in the prior art. The preparation method comprises the following steps: dissolving upatinib and pyroglutamic acid in a first solvent, fully reacting, evaporating to remove the solvent, adding a second solvent, collecting a solid when turbidity appears, and drying to obtain white powder, namely the amorphous substance. Compared with upatinib L-tartrate, glutarate and L-di-p-methyl benzoyl tartrate in the prior art, the solubility of the amorphous substance disclosed by the invention is remarkably improved, and the anti-inflammatory activity is also improved.
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本发明涉及一种乌帕替尼-焦谷氨酸盐的无定形物及其制备方法与应用。本发明属于药物化学领域，解决现有技术中药物水溶性差及药用盐溶解度及疗效方面存在的缺陷。本发明将乌帕替尼、焦谷氨酸溶于第一溶剂中，充分反应后，蒸除溶剂，加入第二溶剂，出现混浊，收集固体、干燥得白色粉末即为</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
| title | Upatinib-pyroglutamate amorphous substance as well as preparation method and application thereof |
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