CN108349980A - 用于制备依鲁替尼及其中间体的方法 - Google Patents

用于制备依鲁替尼及其中间体的方法 Download PDF

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Publication number
CN108349980A
CN108349980A CN201680063300.1A CN201680063300A CN108349980A CN 108349980 A CN108349980 A CN 108349980A CN 201680063300 A CN201680063300 A CN 201680063300A CN 108349980 A CN108349980 A CN 108349980A
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CN
China
Prior art keywords
ibrutinib
compound
reaction mixture
amorphous
isolated
Prior art date
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Pending
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CN201680063300.1A
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English (en)
Chinese (zh)
Inventor
萧宗育
何孟芬
曾信彰
曹文馨
黄原章
罗伟硕
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Scinopharm Taiwan Ltd
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Scinopharm Taiwan Ltd
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Application filed by Scinopharm Taiwan Ltd filed Critical Scinopharm Taiwan Ltd
Publication of CN108349980A publication Critical patent/CN108349980A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 two hetero rings
    • C07D401/04—Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201680063300.1A 2015-10-28 2016-10-28 用于制备依鲁替尼及其中间体的方法 Pending CN108349980A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562285035P 2015-10-28 2015-10-28
US62/285,035 2015-10-28
PCT/SG2016/050528 WO2017074265A1 (en) 2015-10-28 2016-10-28 Process for preparing ibrutinib and its intermediates

Publications (1)

Publication Number Publication Date
CN108349980A true CN108349980A (zh) 2018-07-31

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680063300.1A Pending CN108349980A (zh) 2015-10-28 2016-10-28 用于制备依鲁替尼及其中间体的方法

Country Status (7)

Country Link
US (1) US9834561B2 (enExample)
EP (1) EP3368537A4 (enExample)
JP (1) JP2018536640A (enExample)
KR (1) KR20180063339A (enExample)
CN (1) CN108349980A (enExample)
TW (1) TWI642671B (enExample)
WO (1) WO2017074265A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106279284A (zh) * 2016-08-08 2017-01-04 上海孚璞生物科技有限公司 三取代膦亚胺类化合物及其制备方法、用途
CN111004239A (zh) * 2018-10-08 2020-04-14 上海柏狮生物科技有限公司 一种依替鲁尼的前体制备方法
CN113135917A (zh) * 2020-01-16 2021-07-20 北京赛思源生物医药技术有限公司 一种依鲁替尼的无定型物及其药用组合物
CN114105991A (zh) * 2020-08-31 2022-03-01 北京四环制药有限公司 一种伊布替尼中间体的制备方法

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019070698A1 (en) * 2017-10-02 2019-04-11 Johnson Matthey Public Limited Company Novel forms of ibrutinib
CN114105990A (zh) * 2020-08-31 2022-03-01 北京四环制药有限公司 一种伊布替尼的合成方法

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CN103965201A (zh) * 2014-04-30 2014-08-06 淮海工学院 一种合成依鲁替尼中间体4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-d]嘧啶的方法
CN104736178A (zh) * 2012-06-04 2015-06-24 药品循环公司 布鲁顿酪氨酸激酶抑制剂的晶形
CN105985343A (zh) * 2015-02-12 2016-10-05 上海昶朗医药科技有限公司 伊布替尼的制备方法
CN106188062A (zh) * 2015-05-08 2016-12-07 苏州鹏旭医药科技有限公司 依鲁替尼的制备方法、依鲁替尼的中间体及中间体的制备方法

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EP2526934B1 (en) 2006-09-22 2015-12-09 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
US9156847B2 (en) 2013-03-15 2015-10-13 Janssen Pharmaceutica Nv Processes and intermediates for preparing a medicament
CN105452257B (zh) * 2013-08-12 2017-09-05 大鹏药品工业株式会社 新型稠合嘧啶化合物或其盐
CN103626774B (zh) 2013-11-20 2015-11-04 苏州明锐医药科技有限公司 伊鲁替尼的制备方法
US9884869B2 (en) 2014-03-27 2018-02-06 Perrigo Api Ltd. Ibrutinib solid forms and production process therefor
US10266535B2 (en) 2015-01-21 2019-04-23 Hefei Institutes Of Physical Science, Chinese Academy Of Sciences Inhibitor of FLT3 kinase and use thereof
CN104557945B (zh) * 2015-01-27 2017-08-04 安润医药科技（苏州）有限公司 依鲁替尼合成方法
WO2016127915A1 (zh) * 2015-02-12 2016-08-18 上海度德医药科技有限公司 伊布替尼的制备方法

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CN104736178A (zh) * 2012-06-04 2015-06-24 药品循环公司 布鲁顿酪氨酸激酶抑制剂的晶形
CN103121999A (zh) * 2012-08-29 2013-05-29 苏州迪飞医药科技有限公司 一种酪氨酸激酶抑制剂pci-32765的合成方法
CN103965201A (zh) * 2014-04-30 2014-08-06 淮海工学院 一种合成依鲁替尼中间体4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-d]嘧啶的方法
CN105985343A (zh) * 2015-02-12 2016-10-05 上海昶朗医药科技有限公司 伊布替尼的制备方法
CN106188062A (zh) * 2015-05-08 2016-12-07 苏州鹏旭医药科技有限公司 依鲁替尼的制备方法、依鲁替尼的中间体及中间体的制备方法

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106279284A (zh) * 2016-08-08 2017-01-04 上海孚璞生物科技有限公司 三取代膦亚胺类化合物及其制备方法、用途
CN111004239A (zh) * 2018-10-08 2020-04-14 上海柏狮生物科技有限公司 一种依替鲁尼的前体制备方法
CN113135917A (zh) * 2020-01-16 2021-07-20 北京赛思源生物医药技术有限公司 一种依鲁替尼的无定型物及其药用组合物
CN114105991A (zh) * 2020-08-31 2022-03-01 北京四环制药有限公司 一种伊布替尼中间体的制备方法

Also Published As

Publication number Publication date
EP3368537A4 (en) 2019-06-19
US9834561B2 (en) 2017-12-05
JP2018536640A (ja) 2018-12-13
WO2017074265A1 (en) 2017-05-04
TWI642671B (zh) 2018-12-01
KR20180063339A (ko) 2018-06-11
TW201722959A (zh) 2017-07-01
US20170145017A1 (en) 2017-05-25
EP3368537A1 (en) 2018-09-05

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Application publication date: 20180731