CN114630668A - 一种Aprocitentan晶型及其制备方法和用途 - Google Patents

一种Aprocitentan晶型及其制备方法和用途 Download PDF

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CN114630668A
CN114630668A CN202080076776.5A CN202080076776A CN114630668A CN 114630668 A CN114630668 A CN 114630668A CN 202080076776 A CN202080076776 A CN 202080076776A CN 114630668 A CN114630668 A CN 114630668A
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crystal form
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crystal
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CN114630668B (zh
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陈敏华
朱宏艳
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Crystal Pharmaceutical Suzhou Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
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Abstract

Aprocitentan(称为“化合物I”)的新晶型及其制备方法,含有该晶型的药物组合物,以及该晶型在制备双重内皮素受体拮抗剂药物和治疗难治性高血压药物中的用途。提供的Aprocitentan晶型具有一种或多种改进的性质,对未来该药物的优化和开发具有重要价值。
Figure DDA0003626372810000011

Description

PCT国内申请,说明书已公开。

Claims (11)

  1. PCT国内申请,权利要求书已公开。
CN202080076776.5A 2019-11-07 2020-10-21 一种Aprocitentan晶型及其制备方法和用途 Active CN114630668B (zh)

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CN201911073945 2019-11-07
CN2019110739455 2019-11-07
PCT/CN2020/122546 WO2021088645A1 (zh) 2019-11-07 2020-10-21 一种Aprocitentan晶型及其制备方法和用途

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101772494A (zh) * 2007-08-17 2010-07-07 埃科特莱茵药品有限公司 4-嘧啶磺酰胺衍生物
CN105992762A (zh) * 2014-02-14 2016-10-05 埃科特莱茵药品有限公司 制造嘧啶磺酰胺衍生物的方法
WO2018153513A1 (en) * 2017-02-27 2018-08-30 Idorsia Pharmaceuticals Ltd Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
TW201924685A (zh) * 2017-11-30 2019-07-01 瑞士商愛杜西亞製藥有限公司 用於治療內皮素相關疾病之4-嘧啶磺醯胺衍生物與sglt-2抑制劑之組合

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101772494A (zh) * 2007-08-17 2010-07-07 埃科特莱茵药品有限公司 4-嘧啶磺酰胺衍生物
CN105992762A (zh) * 2014-02-14 2016-10-05 埃科特莱茵药品有限公司 制造嘧啶磺酰胺衍生物的方法
WO2018153513A1 (en) * 2017-02-27 2018-08-30 Idorsia Pharmaceuticals Ltd Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
CN110381948A (zh) * 2017-02-27 2019-10-25 爱杜西亚药品有限公司 4-嘧啶磺酰胺衍生物的结晶形式
TW201924685A (zh) * 2017-11-30 2019-07-01 瑞士商愛杜西亞製藥有限公司 用於治療內皮素相關疾病之4-嘧啶磺醯胺衍生物與sglt-2抑制劑之組合

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EP4056182A1 (en) 2022-09-14
CN114630668B (zh) 2024-02-27
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