TWI786089B - 4-嘧啶磺醯胺衍生物之結晶形式 - Google Patents

4-嘧啶磺醯胺衍生物之結晶形式 Download PDF

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TWI786089B
TWI786089B TW107106403A TW107106403A TWI786089B TW I786089 B TWI786089 B TW I786089B TW 107106403 A TW107106403 A TW 107106403A TW 107106403 A TW107106403 A TW 107106403A TW I786089 B TWI786089 B TW I786089B
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compound
bromo
pyrimidin
pharmaceutical composition
powder diffraction
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TW107106403A
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Chinese (zh)
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TW201835071A (zh
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馬汀 波利
菲利普 柯勒
艾文 辛德爾霍斯
羅門 馬克思 凡
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瑞士商愛杜西亞製藥有限公司
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • C07—ORGANIC CHEMISTRY
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TW107106403A 2017-02-27 2018-02-26 4-嘧啶磺醯胺衍生物之結晶形式 TWI786089B (zh)

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??PCT/EP2017/054489 2017-02-27
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EP2017054489 2017-02-27
EP2017061487 2017-05-12
WOPCT/EP2017/061487 2017-05-12
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CN114630668B (zh) * 2019-11-07 2024-02-27 苏州科睿思制药有限公司 一种Aprocitentan晶型及其制备方法和用途
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CN114644595A (zh) * 2020-12-19 2022-06-21 普济生物科技(台州)有限公司 阿普昔腾坦的无定型态、其药物组合物和用途
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JP2025519101A (ja) 2022-05-22 2025-06-24 イドルシア・ファーマシューティカルズ・リミテッド 高血圧の治療のための4-ピリミジンスルファミド誘導体の使用
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WO2024140425A1 (zh) * 2022-12-30 2024-07-04 苏州科睿思制药有限公司 一种阿普昔腾坦晶型及其制备方法和用途
KR20250152723A (ko) 2024-04-16 2025-10-24 경북대학교 산학협력단 신규한 피리미딘 유도체 화합물 및 이의 용도

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