AU2016343517B2 - A salt of EGFR inhibitor, crystalline form and uses thereof - Google Patents

A salt of EGFR inhibitor, crystalline form and uses thereof Download PDF

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Publication number
AU2016343517B2
AU2016343517B2 AU2016343517A AU2016343517A AU2016343517B2 AU 2016343517 B2 AU2016343517 B2 AU 2016343517B2 AU 2016343517 A AU2016343517 A AU 2016343517A AU 2016343517 A AU2016343517 A AU 2016343517A AU 2016343517 B2 AU2016343517 B2 AU 2016343517B2
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cancer
crystalline form
compound
pharmaceutical composition
disclosed
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AU2016343517A1 (en
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Bing Liu
Weihong Zhang
Yingjun Zhang
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Sunshine Lake Pharma Co Ltd
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Sunshine Lake Pharma Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2016343517A 2015-10-19 2016-10-18 A salt of EGFR inhibitor, crystalline form and uses thereof Active AU2016343517B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510677405 2015-10-19
CN201510677405.3 2015-10-19
PCT/CN2016/102453 WO2017067447A1 (en) 2015-10-19 2016-10-18 A salt of egfr inhibitor, crystalline form and uses thereof

Publications (2)

Publication Number Publication Date
AU2016343517A1 AU2016343517A1 (en) 2018-05-24
AU2016343517B2 true AU2016343517B2 (en) 2020-04-30

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AU2016343517A Active AU2016343517B2 (en) 2015-10-19 2016-10-18 A salt of EGFR inhibitor, crystalline form and uses thereof

Country Status (10)

Country Link
US (1) US10308658B2 (OSRAM)
EP (1) EP3365344B1 (OSRAM)
JP (1) JP6812426B2 (OSRAM)
KR (1) KR102627044B1 (OSRAM)
CN (1) CN106588943B (OSRAM)
AU (1) AU2016343517B2 (OSRAM)
CA (1) CA3001655C (OSRAM)
ES (1) ES2841600T3 (OSRAM)
TW (1) TWI693225B (OSRAM)
WO (1) WO2017067447A1 (OSRAM)

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WO2017114735A1 (en) * 2015-12-30 2017-07-06 Synthon B.V. Process for making crystalline form a of gefitinib
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
CN107328871B (zh) * 2017-05-12 2020-04-21 中国医学科学院肿瘤医院 Uplc-ms/ms联用检测人血浆和/或脑脊液中奥希替尼的药物浓度
WO2019165003A1 (en) * 2018-02-20 2019-08-29 Dawei Zhang Substituted quinolines useful as kinase inhibitors
SG11202101712XA (en) 2018-09-14 2021-04-29 Spectrum Pharmaceuticals Inc Kits and methods for treating cancers
CN112969699A (zh) * 2018-10-09 2021-06-15 亚狮康私人有限公司 瓦利替尼的丙二酸盐
BR112021019489A2 (pt) * 2019-03-29 2022-02-08 Univ Texas Compostos com atividade antitumoral contra células cancerosas portando inserções do éxon 20 de egfr ou de her2
JP7350374B2 (ja) * 2019-06-19 2023-09-26 チェンドゥ・ジンルイ・ファウンデーション・バイオテック・カンパニー・リミテッド キナゾリン系化合物の結晶体、塩およびその調製方法
CN115028594A (zh) * 2020-06-03 2022-09-09 吴卫东 恩替他滨药用前体化合物及其制备方法和医学用途
CN113929630B (zh) * 2020-07-13 2024-04-19 山东新时代药业有限公司 一种吉非替尼药物共晶体
UY39342A (es) * 2020-07-27 2022-02-25 Spectrum Pharmaceuticals Inc Tratamiento con poziotinib para el cáncer de pulmón de células no pequeñas
WO2022127807A1 (zh) * 2020-12-18 2022-06-23 江苏豪森药业集团有限公司 一种芳基磷氧化物类衍生物自由碱的晶型及其制备方法和应用
AU2022426699A1 (en) 2021-12-30 2024-07-11 Biomea Fusion, Inc. Pyrazine compounds as inhibitors of flt3

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Publication number Publication date
EP3365344B1 (en) 2020-12-09
CA3001655C (en) 2023-08-01
KR20180064533A (ko) 2018-06-14
US20180298019A1 (en) 2018-10-18
HK1254666A1 (en) 2019-07-26
KR102627044B1 (ko) 2024-01-18
US10308658B2 (en) 2019-06-04
TW201718596A (zh) 2017-06-01
AU2016343517A1 (en) 2018-05-24
JP6812426B2 (ja) 2021-01-13
JP2018534289A (ja) 2018-11-22
TWI693225B (zh) 2020-05-11
WO2017067447A1 (en) 2017-04-27
EP3365344A1 (en) 2018-08-29
ES2841600T3 (es) 2021-07-08
CN106588943B (zh) 2018-10-16
CN106588943A (zh) 2017-04-26
CA3001655A1 (en) 2017-04-27
EP3365344A4 (en) 2019-05-22

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