CN113993865A - 一种SGLTs抑制剂的晶型及其应用 - Google Patents

一种SGLTs抑制剂的晶型及其应用 Download PDF

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CN113993865A
CN113993865A CN202080039540.4A CN202080039540A CN113993865A CN 113993865 A CN113993865 A CN 113993865A CN 202080039540 A CN202080039540 A CN 202080039540A CN 113993865 A CN113993865 A CN 113993865A
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degrees
compound
solvent
pentane
formula
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CN113993865B (zh
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毛庆华
于涛
李翼
吴成德
姚婷
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Shandong Danhong Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04—Carbocyclic radicals
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
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    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/06—Separation; Purification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Molecular Biology (AREA)
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  • Medicinal Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)

Abstract

式(Ⅰ)所示化合物的A晶型，及其在制备治疗SGLT1/SGLT2相关疾病的药物的应用。
Figure DDA0003378019410000011

Description

PCT国内申请，说明书已公开。

Claims (18)

  1. PCT国内申请，权利要求书已公开。
CN202080039540.4A 2019-07-05 2020-07-03 一种SGLTs抑制剂的晶型及其应用 Active CN113993865B (zh)

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CN201910604504 2019-07-05
CN2019106045047 2019-07-05
PCT/CN2020/100072 WO2021004388A1 (zh) 2019-07-05 2020-07-03 一种SGLTs抑制剂的晶型及其应用

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EP (1) EP3957634A4 (zh)
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Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006117651A (ja) * 2004-09-27 2006-05-11 Taisho Pharmaceut Co Ltd Ｓｇｌｔ２の活性阻害剤
US20070049537A1 (en) * 2005-08-30 2007-03-01 Matthias Eckhardt Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
US20110077212A1 (en) * 2009-09-25 2011-03-31 Theracos, Inc. Therapeutic uses of sglt2 inhibitors
CN104109154A (zh) * 2013-04-17 2014-10-22 上海阳帆医药科技有限公司 C-芳基葡萄糖苷衍生物及其制备方法和应用
WO2017202351A1 (zh) * 2016-05-25 2017-11-30 苏州科睿思制药有限公司 一种钠-葡萄糖协同转运蛋白抑制剂药物的新晶型及其制备方法和用途
US20180362514A1 (en) * 2015-09-15 2018-12-20 Laurus Labs Ltd. Co-crystals of sglt2 inhibitors, process for their preparation and pharmaceutical compositions thereof
WO2019134667A1 (zh) * 2018-01-05 2019-07-11 南京明德新药研发股份有限公司 一种SGLTs抑制剂及其应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
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CA2557801C (en) * 2004-03-16 2013-06-25 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted benzol derivatives, drugs containing said compounds, the use thereof and method for the production thereof
TWI499414B (zh) * 2006-09-29 2015-09-11 Lexicon Pharmaceuticals Inc 鈉與葡萄糖第２型共同運輸體（ｃｏ-ｔｒａｎｓｐｏｒｔｅｒ ２）的抑制物與其應用方法
TWI472521B (zh) * 2008-07-17 2015-02-11 Lexicon Pharmaceuticals Inc （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）－２－（４－氯－３－（４－乙氧苄基）苯基）－６－（甲硫）四氫－２ｈ－哌喃－３，４，５－三醇的固體形態與其使用方法
CN102234260A (zh) * 2010-04-28 2011-11-09 上海阳帆医药科技有限公司 含二氟亚甲基基团的c-芳基葡糖苷衍生物
TWI631963B (zh) 2011-01-05 2018-08-11 雷西肯製藥股份有限公司 包含鈉－葡萄糖共同輸送體１與２之抑制劑的組合物與應用方法
CN104610208B (zh) * 2013-11-05 2017-08-15 天津药物研究院有限公司 (1s)‑1,6‑二脱氧‑1‑[4‑甲氧基‑3‑(反式‑4‑正丙基环己基)甲基苯基]‑d‑吡喃葡萄糖的晶型a及其制备方法和应用
WO2018153900A1 (de) * 2017-02-22 2018-08-30 Bayer Aktiengesellschaft Selektive partielle adenosin a1 rezeptor-agonisten in kombination mit sglt-2-hemmern
CN109456374A (zh) * 2017-09-06 2019-03-12 上海和誉生物医药科技有限公司 一种SGLTs蛋白抑制剂、其制备方法和药学上的应用

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006117651A (ja) * 2004-09-27 2006-05-11 Taisho Pharmaceut Co Ltd Ｓｇｌｔ２の活性阻害剤
US20070049537A1 (en) * 2005-08-30 2007-03-01 Matthias Eckhardt Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
US20110077212A1 (en) * 2009-09-25 2011-03-31 Theracos, Inc. Therapeutic uses of sglt2 inhibitors
CN104109154A (zh) * 2013-04-17 2014-10-22 上海阳帆医药科技有限公司 C-芳基葡萄糖苷衍生物及其制备方法和应用
US20180362514A1 (en) * 2015-09-15 2018-12-20 Laurus Labs Ltd. Co-crystals of sglt2 inhibitors, process for their preparation and pharmaceutical compositions thereof
WO2017202351A1 (zh) * 2016-05-25 2017-11-30 苏州科睿思制药有限公司 一种钠-葡萄糖协同转运蛋白抑制剂药物的新晶型及其制备方法和用途
CN109195980A (zh) * 2016-05-25 2019-01-11 苏州科睿思制药有限公司 一种钠-葡萄糖协同转运蛋白抑制剂药物的新晶型及其制备方法和用途
WO2019134667A1 (zh) * 2018-01-05 2019-07-11 南京明德新药研发股份有限公司 一种SGLTs抑制剂及其应用

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CN113993865B (zh) 2023-09-22
AU2020310274B2 (en) 2022-09-29
KR20220030930A (ko) 2022-03-11
JP2022533856A (ja) 2022-07-26
WO2021004388A1 (zh) 2021-01-14
EP3957634A1 (en) 2022-02-23
US20220324897A1 (en) 2022-10-13
EP3957634A4 (en) 2022-08-31
JP7273997B2 (ja) 2023-05-15
AU2020310274A1 (en) 2021-12-23

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