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嗎啉衍生物的鹽及其晶型、其製備方法及藥物組成物、用途
专利权人:
SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.;MITSUBISHI TANABE PHARMA CORPORATION
发明人:
XIA, GUANGXIN,夏广新,夏廣新,XIE, JIANSHU,谢建树,謝建樹,JIA, GUOHUI,贾国慧,賈國慧,HAN, JIANSHENG,韩建生,韓建生,UEDA, NAOKO,上田直子,LIJIMA, TORU,饭嶋彻,飯嶋徹
申请号:
TW105143910
公开号:
TW201722950A
申请日:
2016.12.29
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present invention provides a novel pharmaceutically acceptable salt of morpholine derivative including its malate, tartarate, hydrochloride, acetate and naphthyl diphosphate, wherein the tartarate has 3 kinds of crystalline salt forms of A crystal form, B crystal form and dihydrate, each of malate, hydrochloride and acetate has one kind of crystalline salt form, and the naphthyl diphosphate is amorphous. The present invention has one or more improved properties, such as a better crystalline, a great improving of the water solubility, light stability and thermal stability and so on, relative to the known free base of morpholine derivatives. The present invention further provides a method for manufacturing the salt and crystalline of morpholine derivative, pharmaceutical composition and use.本發明提供了新型的可藥用的嗎啉衍生物的鹽,包括其蘋果酸鹽、酒石酸鹽、鹽酸鹽、醋酸鹽和萘二磷酸鹽,其中酒石酸鹽有A晶型、B晶型和二水合物3種晶態鹽型,蘋果酸鹽、鹽酸鹽、醋酸鹽各有1種晶態鹽型,萘二磷酸鹽為無定形。與已知的嗎啉衍生物的游離鹼相比,本發明具有一種或多種的改進性能,如具有較好的晶態,極大程度地提高了水溶解度、光穩定性及熱穩定性等。本發明進一步提供了該嗎啉衍生物的鹽和晶型的製備方法、藥物組成物和用途。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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