CN112566904A - 一种酪氨酸激酶抑制剂的一马来酸盐的晶型及其制备方法 - Google Patents

一种酪氨酸激酶抑制剂的一马来酸盐的晶型及其制备方法 Download PDF

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Publication number
CN112566904A
CN112566904A CN201980052673.2A CN201980052673A CN112566904A CN 112566904 A CN112566904 A CN 112566904A CN 201980052673 A CN201980052673 A CN 201980052673A CN 112566904 A CN112566904 A CN 112566904A
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formula
compound
crystal form
solvent
diffraction pattern
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CN201980052673.2A
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Inventor
邱振均
张全良
韦艳丽
曹永兴
杨俊然
马亚辉
杜振兴
王捷
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Jiangsu Hengrui Medicine Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/145Maleic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

提供一种酪氨酸激酶抑制剂的一马来酸盐的晶型及其制备方法。具体而言,提供一种式(I)所示化合物的I晶型、II晶型、III晶型、IV晶型、V晶型及其制备方法。新晶型具备良好的稳定性,可更好地用于临床治疗。

Description

PCT国内申请,说明书已公开。

Claims (19)

  1. PCT国内申请,权利要求书已公开。
CN201980052673.2A 2018-10-22 2019-10-21 一种酪氨酸激酶抑制剂的一马来酸盐的晶型及其制备方法 Pending CN112566904A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201811231321 2018-10-22
CN2018112313217 2018-10-22
PCT/CN2019/112216 WO2020083188A1 (zh) 2018-10-22 2019-10-21 一种酪氨酸激酶抑制剂的一马来酸盐的晶型及其制备方法

Publications (1)

Publication Number Publication Date
CN112566904A true CN112566904A (zh) 2021-03-26

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CN201980052673.2A Pending CN112566904A (zh) 2018-10-22 2019-10-21 一种酪氨酸激酶抑制剂的一马来酸盐的晶型及其制备方法

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US (1) US20210355109A1 (zh)
EP (1) EP3872072A4 (zh)
JP (1) JP2022508864A (zh)
KR (1) KR20210081367A (zh)
CN (1) CN112566904A (zh)
AU (1) AU2019365166A1 (zh)
BR (1) BR112021007477A2 (zh)
CA (1) CA3115872A1 (zh)
MX (1) MX2021004600A (zh)
TW (2) TWI770934B (zh)
WO (1) WO2020083188A1 (zh)
ZA (1) ZA202103278B (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202115027A (zh) * 2019-08-30 2021-04-16 大陸商江蘇恒瑞醫藥股份有限公司 低雜質含量的酪胺酸激酶抑制劑

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102675287A (zh) * 2011-03-11 2012-09-19 江苏恒瑞医药股份有限公司 (e)-n-[4-[[3-氯-4-(2-吡啶基甲氧基)苯基]氨基]-3-氰基-7-乙氧基-6-喹啉基]-3-[(2r)-1-甲基吡咯烷-2-基]丙-2-烯酰胺的可药用的盐、其制备方法及其在医药上的应用
CN107793399A (zh) * 2016-09-07 2018-03-13 上海翰森生物医药科技有限公司 Cdk4/6抑制剂及其制备方法和应用

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102020639A (zh) 2009-09-14 2011-04-20 上海恒瑞医药有限公司 6-氨基喹唑啉或3-氰基喹啉类衍生物、其制备方法及其在医药上的应用
CN103539783A (zh) 2012-07-12 2014-01-29 江苏恒瑞医药股份有限公司 一种酪氨酸激酶抑制剂的二马来酸盐的i型结晶及制备方法
CN105367552A (zh) * 2015-01-09 2016-03-02 苏州晶云药物科技有限公司 来那替尼马来酸盐的新晶型及其制备方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102675287A (zh) * 2011-03-11 2012-09-19 江苏恒瑞医药股份有限公司 (e)-n-[4-[[3-氯-4-(2-吡啶基甲氧基)苯基]氨基]-3-氰基-7-乙氧基-6-喹啉基]-3-[(2r)-1-甲基吡咯烷-2-基]丙-2-烯酰胺的可药用的盐、其制备方法及其在医药上的应用
CN107793399A (zh) * 2016-09-07 2018-03-13 上海翰森生物医药科技有限公司 Cdk4/6抑制剂及其制备方法和应用

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Publication number Publication date
TWI770934B (zh) 2022-07-11
TW202030186A (zh) 2020-08-16
BR112021007477A2 (pt) 2021-07-27
EP3872072A4 (en) 2022-07-13
MX2021004600A (es) 2021-06-15
KR20210081367A (ko) 2021-07-01
TWI762825B (zh) 2022-05-01
TW202130629A (zh) 2021-08-16
CA3115872A1 (en) 2020-04-30
WO2020083188A1 (zh) 2020-04-30
US20210355109A1 (en) 2021-11-18
EP3872072A1 (en) 2021-09-01
ZA202103278B (en) 2022-08-31
AU2019365166A1 (en) 2021-06-03
JP2022508864A (ja) 2022-01-19

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