WO2010003313A8 - 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 - Google Patents

埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 Download PDF

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Publication number
WO2010003313A8
WO2010003313A8 PCT/CN2009/000773 CN2009000773W WO2010003313A8 WO 2010003313 A8 WO2010003313 A8 WO 2010003313A8 CN 2009000773 W CN2009000773 W CN 2009000773W WO 2010003313 A8 WO2010003313 A8 WO 2010003313A8
Authority
WO
WIPO (PCT)
Prior art keywords
synthesis
crystallographic form
medical combination
icotinib hydrochloride
medical
Prior art date
Application number
PCT/CN2009/000773
Other languages
English (en)
French (fr)
Other versions
WO2010003313A1 (zh
Inventor
王印祥
丁列明
谭芬来
胡云雁
何伟
韩斌
龙伟
刘勇
Original Assignee
浙江贝达药业有限公司
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
Priority to US13/003,216 priority Critical patent/US8822482B2/en
Priority to JP2011516948A priority patent/JP5719770B2/ja
Priority to CN2009801006661A priority patent/CN101878218B/zh
Priority to NZ590334A priority patent/NZ590334A/xx
Priority to CA2730311A priority patent/CA2730311A1/en
Priority to AU2009267683A priority patent/AU2009267683B2/en
Application filed by 浙江贝达药业有限公司 filed Critical 浙江贝达药业有限公司
Priority to EP09793788.2A priority patent/EP2392576B1/en
Publication of WO2010003313A1 publication Critical patent/WO2010003313A1/zh
Publication of WO2010003313A8 publication Critical patent/WO2010003313A8/zh
Priority to HK10111360.7A priority patent/HK1145319A1/xx
Priority to IL210447A priority patent/IL210447A0/en
Priority to US14/448,070 priority patent/US9359370B2/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
PCT/CN2009/000773 2008-07-08 2009-07-07 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途 WO2010003313A1 (zh)

Priority Applications (10)

Application Number Priority Date Filing Date Title
JP2011516948A JP5719770B2 (ja) 2008-07-08 2009-07-07 塩酸イコチニブ、合成物、結晶学的形態、併用薬及びその用途
CN2009801006661A CN101878218B (zh) 2008-07-08 2009-07-07 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途
NZ590334A NZ590334A (en) 2008-07-08 2009-07-07 ICOTINIB HYDROCHLORIDE (4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crownquinazoline hydrochloride), SYNTHESIS, CRYSTALLOGRAPHIC FORM, MEDICAL COMBINATION, AND USES THEREOF
CA2730311A CA2730311A1 (en) 2008-07-08 2009-07-07 Icotinib hydrochloride, synthesis, crystalline forms, drug combinations, and uses thereof
AU2009267683A AU2009267683B2 (en) 2008-07-08 2009-07-07 Icotinib hydrochloride, synthesis, crystallographic form, medical combination, and uses thereof
US13/003,216 US8822482B2 (en) 2008-07-08 2009-07-07 Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof
EP09793788.2A EP2392576B1 (en) 2008-07-08 2009-07-07 Icotinib hydrochloride, synthesis, crystallographic form, medical combination, and uses thereof
HK10111360.7A HK1145319A1 (en) 2008-07-08 2010-12-07 Icotinib hydrochloride, synthesis, crystallographic form, medical combination, and uses thereof
IL210447A IL210447A0 (en) 2008-07-08 2011-01-03 Icotinib hydrochloride, synthesis, crystalline forms, drug combinations, and uses thereof
US14/448,070 US9359370B2 (en) 2008-07-08 2014-07-31 Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CN200810132631 2008-07-08
CN200810132631.3 2008-07-08
CN200810132458 2008-07-17
CN200810132458.7 2008-07-17
CN200810188272 2008-12-23
CN200810188272.3 2008-12-23

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/003,216 A-371-Of-International US8822482B2 (en) 2008-07-08 2009-07-07 Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof
US14/448,070 Continuation US9359370B2 (en) 2008-07-08 2014-07-31 Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof

Publications (2)

Publication Number Publication Date
WO2010003313A1 WO2010003313A1 (zh) 2010-01-14
WO2010003313A8 true WO2010003313A8 (zh) 2010-04-22

Family

ID=41506667

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2009/000773 WO2010003313A1 (zh) 2008-07-08 2009-07-07 埃克替尼盐酸盐及其制备方法、晶型、药物组合物和用途

Country Status (11)

Country Link
US (2) US8822482B2 (zh)
EP (1) EP2392576B1 (zh)
JP (2) JP5719770B2 (zh)
KR (1) KR20110031370A (zh)
CN (5) CN102911179B (zh)
AU (1) AU2009267683B2 (zh)
CA (1) CA2730311A1 (zh)
HK (1) HK1145319A1 (zh)
IL (1) IL210447A0 (zh)
NZ (1) NZ590334A (zh)
WO (1) WO2010003313A1 (zh)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009267683B2 (en) * 2008-07-08 2014-04-03 Beta Pharma, Inc. Icotinib hydrochloride, synthesis, crystallographic form, medical combination, and uses thereof
EP3295796A1 (en) * 2010-03-19 2018-03-21 1Globe Biomedical Co., Ltd. Novel compounds and compositions for targeting cancer stem cells
EP2593462B1 (en) * 2010-07-14 2016-09-07 Betta Pharmaceuticals Co., Ltd. Novel fused heterocyclic derivatives useful as c-met tyrosine kinase inhibitors
JP6112512B2 (ja) * 2010-12-01 2017-04-12 レクシ ファーマ インコーポレイテッド 難治性癌を治療するための方法
TWI505828B (zh) 2010-12-20 2015-11-01 葛蘭素史克智慧財產（第二）有限公司 新穎醫藥組成物
SG11201401953WA (en) 2011-10-31 2014-09-26 Betta Pharmaceuticals Co Ltd Methods of preparing icotinib and icotinib hydrochloride, and intermediates thereof
US9193718B2 (en) * 2012-03-26 2015-11-24 Fujian Institute Of Research On The Structure Of Matter, Chinese Academy Of Sciences Quinazoline derivative and application thereof
WO2014028914A1 (en) * 2012-08-17 2014-02-20 Beta Pharma, Inc. Deuterated icotinib derivatives
WO2014073989A1 (en) * 2012-11-12 2014-05-15 Callaghan Innovation Research Limited Salt and polymorphic forms of (3r,4s)-l-((4-amino-5h-pyrrolo[3,2-d]pyrimidin-7-yl)methyl)-4(methylthiomethyl)pyrodin-3-ol(mtdia)
JP5955396B2 (ja) * 2012-12-28 2016-07-20 ベータ ファーマシューティカルズ カンパニー リミテッド イコチニブ、イコチニブ塩酸塩、及びそれらの中間体の製造方法
CN104470929B (zh) * 2013-06-09 2018-11-30 贝达药业股份有限公司 埃克替尼的晶型及其应用
RU2708079C9 (ru) * 2013-06-09 2020-02-28 Бетта Фармасьютикалз Ко., Лтд Полиморфные формы икотиниба малеата и их применения
KR102270538B1 (ko) * 2013-06-09 2021-06-29 베타 파머수티컬 컴퍼니 리미티드 이코티닙 포스페이트의 신규한 다형체 형태 및 이의 용도
CN104470526B (zh) * 2013-06-09 2016-07-13 贝达药业股份有限公司 埃克替尼磷酸盐的晶型及其用途
KR101804449B1 (ko) * 2013-06-09 2017-12-04 베타 파머수티컬 컴퍼니 리미티드 아이코티닙의 다형체 형태 및 이의 용도
CN104487443B (zh) * 2013-06-09 2016-03-23 贝达药业股份有限公司 埃克替尼马来酸盐的晶型及其用途
CN105101966A (zh) * 2013-10-11 2015-11-25 贝达药业股份有限公司 一种含埃克替尼的皮肤外用药物组合物及其应用
AU2014334222B2 (en) * 2013-10-11 2017-03-09 Betta Pharmaceuticals Co., Ltd Icotinib-containing topical skin pharmaceutical composition and use thereof
CN103784412A (zh) * 2014-01-15 2014-05-14 青岛市肿瘤医院 一种盐酸埃克替尼分散片及其制备方法
CN103860521A (zh) * 2014-03-05 2014-06-18 王栾秋 盐酸埃克替尼胶囊组合物及其制备方法
CN106924739B (zh) * 2017-03-10 2022-07-29 上海交通大学医学院 Egfr抑制剂在制备治疗muc1阳性肿瘤药物中的应用
CN111909163B (zh) * 2020-04-21 2022-02-01 南开大学 具有ido1抑制功能的喹啉胺类化合物及其制备方法
CN111362957B (zh) * 2020-04-21 2022-02-18 上海百利佳生医药科技有限公司 一种埃克替尼关键中间体的制备方法
CN111763214B (zh) * 2020-08-10 2022-03-15 苏州富士莱医药股份有限公司 一种埃克替尼的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002338577A (ja) * 2001-05-15 2002-11-27 Orient Chem Ind Ltd 分子内架橋クラウンエーテル環を有するフタロシアニン誘導体及びその製造方法
US7078409B2 (en) * 2002-03-28 2006-07-18 Beta Pharma, Inc. Fused quinazoline derivatives useful as tyrosine kinase inhibitors
AU2009267683B2 (en) * 2008-07-08 2014-04-03 Beta Pharma, Inc. Icotinib hydrochloride, synthesis, crystallographic form, medical combination, and uses thereof

Also Published As

Publication number Publication date
JP2015110649A (ja) 2015-06-18
CN104530061B (zh) 2017-05-10
CN101878218B (zh) 2013-01-02
CA2730311A1 (en) 2010-01-14
CN103254204B (zh) 2014-10-22
EP2392576A4 (en) 2012-04-11
WO2010003313A1 (zh) 2010-01-14
NZ590334A (en) 2012-12-21
JP2011527291A (ja) 2011-10-27
KR20110031370A (ko) 2011-03-25
US9359370B2 (en) 2016-06-07
EP2392576B1 (en) 2016-02-17
CN104592242B (zh) 2017-01-25
AU2009267683B2 (en) 2014-04-03
US20110182882A1 (en) 2011-07-28
CN101878218A (zh) 2010-11-03
CN102911179B (zh) 2015-04-08
CN102911179A (zh) 2013-02-06
HK1145319A1 (en) 2011-04-15
CN103254204A (zh) 2013-08-21
IL210447A0 (en) 2011-03-31
CN104530061A (zh) 2015-04-22
EP2392576A1 (en) 2011-12-07
JP5719770B2 (ja) 2015-05-20
US8822482B2 (en) 2014-09-02
CN104592242A (zh) 2015-05-06
US20140343082A1 (en) 2014-11-20
AU2009267683A1 (en) 2010-01-14

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