WO2014139447A1 - Forme cristalline a de (1s)-1-[4-chloro-3-(4-éthoxybenzyl)phényl]-1,6-didésoxy-d-glucose et procédé de préparation et utilisation de celle-ci - Google Patents

Forme cristalline a de (1s)-1-[4-chloro-3-(4-éthoxybenzyl)phényl]-1,6-didésoxy-d-glucose et procédé de préparation et utilisation de celle-ci Download PDF

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Publication number
WO2014139447A1
WO2014139447A1 PCT/CN2014/073365 CN2014073365W WO2014139447A1 WO 2014139447 A1 WO2014139447 A1 WO 2014139447A1 CN 2014073365 W CN2014073365 W CN 2014073365W WO 2014139447 A1 WO2014139447 A1 WO 2014139447A1
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WO
WIPO (PCT)
Prior art keywords
crystal form
glucose
preparation
ethoxybenzyl
chloro
Prior art date
Application number
PCT/CN2014/073365
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English (en)
Chinese (zh)
Inventor
赵桂龙
刘冰妮
谢亚非
刘钰强
魏群超
刘鹏
王玉丽
吴疆
徐为人
汤立达
邹美香
Original Assignee
天津药物研究院
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Filing date
Publication date
Application filed by 天津药物研究院 filed Critical 天津药物研究院
Publication of WO2014139447A1 publication Critical patent/WO2014139447A1/fr

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    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D309/10—Oxygen atoms
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A61K31/708—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
    • 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

Abstract

La présente invention concerne une forme cristalline A de (1S)-1-[4-chloro-3-(4-éthoxybenzyl)phényl]-1,6-didésoxy-D-glucose, caractérisée en ce que la diffraction des rayons X sur poudre telle que décrite par l'angle 2θ a des pics de diffraction autour de 3,56, 5,42, 10,84, 13,58, 16,28, 17,00, 18,48, 19,74, 21,72, 22,52, 22,96, 28,32 et 29,58. La présente invention concerne en outre le procédé de préparation de la forme cristalline A, l'utilisation de celle-ci dans la préparation de compositions pharmaceutiques pour traiter le diabète, et des compositions pharmaceutiques contenant cette forme cristalline.
PCT/CN2014/073365 2013-03-15 2014-03-13 Forme cristalline a de (1s)-1-[4-chloro-3-(4-éthoxybenzyl)phényl]-1,6-didésoxy-d-glucose et procédé de préparation et utilisation de celle-ci WO2014139447A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201310084842 2013-03-15
CN2013100848425 2013-03-15
CN2013102395241 2013-06-17
CN201310239524.1A CN104045615B (zh) 2013-03-15 2013-06-17 (1s)-1-[4-氯-3-(4-乙氧基苄基)苯基]-1,6-二脱氧-d-葡萄糖的晶型a及其制备方法和应用

Publications (1)

Publication Number Publication Date
WO2014139447A1 true WO2014139447A1 (fr) 2014-09-18

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PCT/CN2014/073365 WO2014139447A1 (fr) 2013-03-15 2014-03-13 Forme cristalline a de (1s)-1-[4-chloro-3-(4-éthoxybenzyl)phényl]-1,6-didésoxy-d-glucose et procédé de préparation et utilisation de celle-ci

Country Status (2)

Country Link
CN (1) CN104045615B (fr)
WO (1) WO2014139447A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111559997A (zh) * 2019-02-13 2020-08-21 罗欣药业(上海)有限公司 一种达格列净新晶型及其制备方法
WO2021176096A1 (fr) 2020-03-05 2021-09-10 Krka, D.D., Novo Mesto Composition pharmaceutique comprenant un inhibiteur du sglt2

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016155578A1 (fr) * 2015-03-27 2016-10-06 苏州晶云药物科技有限公司 Nouvelle forme cristalline de dapagliflozine et son procédé de préparation
CN108675976B (zh) * 2018-05-14 2020-07-14 浙江宏元药业股份有限公司 一种6-卤代葡萄糖碳苷及其制备方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101065391A (zh) * 2004-09-23 2007-10-31 布里斯托尔-迈尔斯斯奎布公司 C－芳基葡糖苷sglt2抑制剂和方法
CN102408459A (zh) * 2011-09-29 2012-04-11 天津药物研究院 一类含异头位烷基的苯基c-葡萄糖苷衍生物、其制备方法和用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101065391A (zh) * 2004-09-23 2007-10-31 布里斯托尔-迈尔斯斯奎布公司 C－芳基葡糖苷sglt2抑制剂和方法
CN102408459A (zh) * 2011-09-29 2012-04-11 天津药物研究院 一类含异头位烷基的苯基c-葡萄糖苷衍生物、其制备方法和用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SHI, Y. ET AL.: "A facile synthesis of 6-deoxydapagliflozin", MONATSH CHEM, vol. 144, no. 12, 1 October 2013 (2013-10-01), pages 1903 - 1910, XP035303911, DOI: doi:10.1007/s00706-013-1053-0 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111559997A (zh) * 2019-02-13 2020-08-21 罗欣药业(上海)有限公司 一种达格列净新晶型及其制备方法
WO2021176096A1 (fr) 2020-03-05 2021-09-10 Krka, D.D., Novo Mesto Composition pharmaceutique comprenant un inhibiteur du sglt2

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Publication number Publication date
CN104045615A (zh) 2014-09-17
CN104045615B (zh) 2015-11-18

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