CN113646313A - 一种a2a受体拮抗剂的盐型、晶型及其制备方法 - Google Patents

一种a2a受体拮抗剂的盐型、晶型及其制备方法 Download PDF

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CN113646313A
CN113646313A CN202080025321.0A CN202080025321A CN113646313A CN 113646313 A CN113646313 A CN 113646313A CN 202080025321 A CN202080025321 A CN 202080025321A CN 113646313 A CN113646313 A CN 113646313A
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CN113646313B (zh
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陈新海
周凯
于衍新
胡伯羽
张丽
陈兆国
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CStone Pharmaceuticals Shanghai Co Ltd
CStone Pharmaceuticals Suzhou Co Ltd
CStone Pharmaceuticals
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CStone Pharmaceuticals Suzhou Co Ltd
CStone Pharmaceuticals
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

提供腺苷A2A受体拮抗剂的盐型、其晶型及其制备方法，还提供包括所述盐型或晶型在制备与A2A受体相关疾病的药物中的应用，所述盐型中马来酸盐具有式(I)结构：

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN202080025321.0A 2019-03-28 2020-03-27 一种a2a受体拮抗剂的盐型、晶型及其制备方法 Active CN113646313B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019102444688 2019-03-28
CN201910244468 2019-03-28
PCT/CN2020/081704 WO2020192762A1 (zh) 2019-03-28 2020-03-27 一种a2a受体拮抗剂的盐型、晶型及其制备方法

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CN113646313A true CN113646313A (zh) 2021-11-12
CN113646313B CN113646313B (zh) 2023-05-30

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US (1) US20220185825A1 (zh)
EP (1) EP3950694A4 (zh)
JP (1) JP2022527910A (zh)
CN (1) CN113646313B (zh)
WO (1) WO2020192762A1 (zh)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1541216A (zh) * 2001-07-20 2004-10-27 - 8-甲氧基-(1,2,4)三唑并(1,5-a)吡啶衍生物及其作为腺苷受体配体的应用
WO2015020565A1 (ru) * 2013-08-05 2015-02-12 Общество С Ограниченной Ответственностью "Ньювак" (Ооо "Ньювак") Замещенные [1,2,4]триазоло[4,3-a]пиридины, проявляющие свойства антогонистов аденозиновых а2а рецепторов, и их применение
CN105025899A (zh) * 2012-12-28 2015-11-04 默沙东公司 具有A2A拮抗剂性质的杂二环取代的-[1,2,4]三唑并[1,5-c]喹唑啉-5-胺化合物
WO2019002606A1 (en) * 2017-06-30 2019-01-03 Selvita S.A. ADENOSINE A2A RECEPTOR 5,6-BICYCLO-IMIDAZO [1,2-A] PYRAZINE MODULATORS
WO2019038214A1 (en) * 2017-08-21 2019-02-28 Merck Patent Gmbh QUINOXALINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS
WO2019062803A1 (zh) * 2017-09-28 2019-04-04 基石药业 作为a2a受体抑制剂的并环类衍生物

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1541216A (zh) * 2001-07-20 2004-10-27 - 8-甲氧基-(1,2,4)三唑并(1,5-a)吡啶衍生物及其作为腺苷受体配体的应用
CN105025899A (zh) * 2012-12-28 2015-11-04 默沙东公司 具有A2A拮抗剂性质的杂二环取代的-[1,2,4]三唑并[1,5-c]喹唑啉-5-胺化合物
WO2015020565A1 (ru) * 2013-08-05 2015-02-12 Общество С Ограниченной Ответственностью "Ньювак" (Ооо "Ньювак") Замещенные [1,2,4]триазоло[4,3-a]пиридины, проявляющие свойства антогонистов аденозиновых а2а рецепторов, и их применение
WO2019002606A1 (en) * 2017-06-30 2019-01-03 Selvita S.A. ADENOSINE A2A RECEPTOR 5,6-BICYCLO-IMIDAZO [1,2-A] PYRAZINE MODULATORS
WO2019038214A1 (en) * 2017-08-21 2019-02-28 Merck Patent Gmbh QUINOXALINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS
WO2019062803A1 (zh) * 2017-09-28 2019-04-04 基石药业 作为a2a受体抑制剂的并环类衍生物

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US20220185825A1 (en) 2022-06-16
CN113646313B (zh) 2023-05-30
EP3950694A4 (en) 2022-12-07
JP2022527910A (ja) 2022-06-07
WO2020192762A1 (zh) 2020-10-01
EP3950694A1 (en) 2022-02-09

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