WO2017197904A3 - 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
WO2017197904A3
WO2017197904A3 PCT/CN2017/000339 CN2017000339W WO2017197904A3 WO 2017197904 A3 WO2017197904 A3 WO 2017197904A3 CN 2017000339 W CN2017000339 W CN 2017000339W WO 2017197904 A3 WO2017197904 A3 WO 2017197904A3
Authority
WO
WIPO (PCT)
Prior art keywords
crystal forms
preparation
new crystal
palbociclib
use therefor
Prior art date
Application number
PCT/CN2017/000339
Other languages
English (en)
French (fr)
Other versions
WO2017197904A2 (zh
Inventor
孟晓明
Original Assignee
上海诚妙医药科技有限公司
孟晓明
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 上海诚妙医药科技有限公司, 孟晓明 filed Critical 上海诚妙医药科技有限公司
Priority to CN201780029111.7A priority Critical patent/CN109661393A/zh
Publication of WO2017197904A2 publication Critical patent/WO2017197904A2/zh
Publication of WO2017197904A3 publication Critical patent/WO2017197904A3/zh
Priority to US16/184,009 priority patent/US10544142B2/en

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Classifications

    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (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。
PCT/CN2017/000339 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 WO2017197904A2 (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN201780029111.7A 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
US16/184,009 US10544142B2 (en) 2016-05-08 2018-11-08 Crystal forms of palbociclib, and preparation method and use therefor

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610300156.0 2016-05-08
CN201610300156 2016-05-08

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US16/184,009 Continuation US10544142B2 (en) 2016-05-08 2018-11-08 Crystal forms of palbociclib, and preparation method and use therefor

Publications (2)

Publication Number Publication Date
WO2017197904A2 WO2017197904A2 (zh) 2017-11-23
WO2017197904A3 true WO2017197904A3 (zh) 2017-12-21

Family

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Family Applications (1)

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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

Country Status (3)

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 (2)

* 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
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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT3004090T (lt) * 2013-05-28 2018-01-10 Astrazeneca Ab Cheminiai junginiai
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
CN105085517B (zh) * 2015-08-06 2016-11-23 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
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 (2)

* 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
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

Also Published As

Publication number Publication date
WO2017197904A2 (zh) 2017-11-23
CN109661393A (zh) 2019-04-19
US20190071442A1 (en) 2019-03-07
US10544142B2 (en) 2020-01-28

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