KR20180063339A - 이브루티닙 및 이의 중간체를 제조하는 방법 - Google Patents

이브루티닙 및 이의 중간체를 제조하는 방법 Download PDF

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Publication number
KR20180063339A
KR20180063339A KR1020187014718A KR20187014718A KR20180063339A KR 20180063339 A KR20180063339 A KR 20180063339A KR 1020187014718 A KR1020187014718 A KR 1020187014718A KR 20187014718 A KR20187014718 A KR 20187014718A KR 20180063339 A KR20180063339 A KR 20180063339A
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South Korea
Prior art keywords
ibrutinib
compound
reaction mixture
amorphous
isolated
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KR1020187014718A
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English (en)
Korean (ko)
Inventor
충-유 흐시아오
멩펜 호
흐신창 쳉
웬싱 차오
유안창 후앙
웨이-수오 로
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시노팜 타이완 리미티드
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Publication of KR20180063339A publication Critical patent/KR20180063339A/ko
Withdrawn legal-status Critical Current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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (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)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
KR1020187014718A 2015-10-28 2016-10-28 이브루티닙 및 이의 중간체를 제조하는 방법 Withdrawn KR20180063339A (ko)

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
KR20180063339A true KR20180063339A (ko) 2018-06-11

Family

ID=58630729

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187014718A Withdrawn KR20180063339A (ko) 2015-10-28 2016-10-28 이브루티닙 및 이의 중간체를 제조하는 방법

Country Status (7)

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

Families Citing this family (6)

* 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
WO2019070698A1 (en) * 2017-10-02 2019-04-11 Johnson Matthey Public Limited Company Novel forms of ibrutinib
CN111004239B (zh) * 2018-10-08 2022-09-13 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
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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005272389B2 (en) * 2004-08-11 2011-08-04 Kyorin Pharmaceutical Co., Ltd. Novel cyclic aminobenzoic acid derivative
DK2526933T3 (en) 2006-09-22 2015-05-18 Pharmacyclics Inc Inhibitors of Bruton's tyrosine kinase
KR20210033067A (ko) * 2012-06-04 2021-03-25 파마싸이클릭스 엘엘씨 브루톤 타이로신 키나아제 저해제의 결정 형태
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
US9156847B2 (en) 2013-03-15 2015-10-13 Janssen Pharmaceutica Nv Processes and intermediates for preparing a medicament
MX360498B (es) * 2013-08-12 2018-11-05 Taiho Pharmaceutical Co Ltd Compuesto novedoso de pirimidina fusionada o sal del mismo.
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
WO2015145415A2 (en) 2014-03-27 2015-10-01 Perrigo Api Ltd. Ibrutinib solid forms and production process therefor
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
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
JP6681922B2 (ja) * 2015-02-12 2020-04-15 上▲海▼度▲徳▼医▲藥▼科技有限公司 イブルチニブの製造方法
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

Also Published As

Publication number Publication date
EP3368537A4 (en) 2019-06-19
WO2017074265A1 (en) 2017-05-04
TW201722959A (zh) 2017-07-01
US9834561B2 (en) 2017-12-05
US20170145017A1 (en) 2017-05-25
EP3368537A1 (en) 2018-09-05
CN108349980A (zh) 2018-07-31
JP2018536640A (ja) 2018-12-13
TWI642671B (zh) 2018-12-01

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PA0105 International application

Patent event date: 20180524

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid