CN109661393A - 帕布昔利布的新晶型及其制备方法及其用途 - Google Patents

帕布昔利布的新晶型及其制备方法及其用途 Download PDF

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Publication number
CN109661393A
CN109661393A CN201780029111.7A CN201780029111A CN109661393A CN 109661393 A CN109661393 A CN 109661393A CN 201780029111 A CN201780029111 A CN 201780029111A CN 109661393 A CN109661393 A CN 109661393A
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cyclopenta
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孟晓明
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Shanghai Begreat Pharmatech
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Shanghai Begreat Pharmatech
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

本发明公开了6‑乙酰基‑8‑环戊基‑5‑甲基‑2‑(5‑哌嗪‑1‑基‑吡啶‑2‑基氨基)‑8H‑吡啶并[2，3‑d]嘧啶‑7‑酮的新多晶型I、II、III、IV、V、VI、VII、VIII、IX、X、XI、XII和XIV及其制备方法和药用用途。晶型VIII为半水合物晶型，与现有晶型相比，新晶型在溶解度、稳定性和制备工艺方面具有明显优势。

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201780029111.7A 2016-05-08 2017-05-08 帕布昔利布的新晶型及其制备方法及其用途 Pending CN109661393A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610300156 2016-05-08
CN2016103001560 2016-05-08
PCT/CN2017/000339 WO2017197904A2 (zh) 2016-05-08 2017-05-08 帕布昔利布的新晶型及其制备方法及其用途

Publications (1)

Publication Number Publication Date
CN109661393A true CN109661393A (zh) 2019-04-19

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CN201780029111.7A Pending CN109661393A (zh) 2016-05-08 2017-05-08 帕布昔利布的新晶型及其制备方法及其用途

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Country Link
US (1) US10544142B2 (zh)
CN (1) CN109661393A (zh)
WO (1) WO2017197904A2 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113845520A (zh) * 2021-09-09 2021-12-28 安徽皓元药业有限公司 一种帕布昔利布乳清酸盐及其制备方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105008357A (zh) * 2013-02-21 2015-10-28 辉瑞大药厂 选择性cdk4/6抑制剂的固态形式
CN105085517A (zh) * 2015-08-06 2015-11-25 天津华洛康生物科技有限公司 一种结晶型帕博西尼游离碱水合物及其制备方法
CN105229004A (zh) * 2013-05-28 2016-01-06 阿斯利康(瑞典)有限公司 化合物
WO2016024232A1 (en) * 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
CN105418603A (zh) * 2015-11-17 2016-03-23 重庆莱美药业股份有限公司 一种高纯度帕布昔利布及其反应中间体的制备方法
WO2016066420A1 (en) * 2014-10-29 2016-05-06 Sandoz Ag Crystalline forms of palbociclib monohydrochloride
CN106831759A (zh) * 2015-12-03 2017-06-13 上海星泰医药科技有限公司 帕布昔利布及其中间体的制备方法

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105008357A (zh) * 2013-02-21 2015-10-28 辉瑞大药厂 选择性cdk4/6抑制剂的固态形式
CN105229004A (zh) * 2013-05-28 2016-01-06 阿斯利康(瑞典)有限公司 化合物
WO2016024232A1 (en) * 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
WO2016066420A1 (en) * 2014-10-29 2016-05-06 Sandoz Ag Crystalline forms of palbociclib monohydrochloride
CN105085517A (zh) * 2015-08-06 2015-11-25 天津华洛康生物科技有限公司 一种结晶型帕博西尼游离碱水合物及其制备方法
CN105418603A (zh) * 2015-11-17 2016-03-23 重庆莱美药业股份有限公司 一种高纯度帕布昔利布及其反应中间体的制备方法
CN106831759A (zh) * 2015-12-03 2017-06-13 上海星泰医药科技有限公司 帕布昔利布及其中间体的制备方法

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Publication number Publication date
US10544142B2 (en) 2020-01-28
US20190071442A1 (en) 2019-03-07
WO2017197904A3 (zh) 2017-12-21
WO2017197904A2 (zh) 2017-11-23

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Application publication date: 20190419