AU2017271458B2 - New crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide - Google Patents

New crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide Download PDF

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AU2017271458B2
AU2017271458B2 AU2017271458A AU2017271458A AU2017271458B2 AU 2017271458 B2 AU2017271458 B2 AU 2017271458B2 AU 2017271458 A AU2017271458 A AU 2017271458A AU 2017271458 A AU2017271458 A AU 2017271458A AU 2017271458 B2 AU2017271458 B2 AU 2017271458B2
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crystalline form
cancer
formula
compound
ray powder
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AU2017271458A1 (en
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Ilaria Candiani
Giovanni OTTAIANO
Attilio Tomasi
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Nerviano Medical Sciences SRL
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Nerviano Medical Sciences SRL
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2017271458A 2016-05-24 2017-05-18 New crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide Active AU2017271458B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662340797P 2016-05-24 2016-05-24
US62/340,797 2016-05-24
PCT/EP2017/061919 WO2017202674A1 (en) 2016-05-24 2017-05-18 New crystalline form of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide

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AU2017271458A1 AU2017271458A1 (en) 2019-01-17
AU2017271458B2 true AU2017271458B2 (en) 2020-11-26

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US (2) US10738037B2 (enExample)
EP (2) EP3464276B1 (enExample)
JP (2) JP7094228B2 (enExample)
KR (1) KR102441736B1 (enExample)
CN (1) CN109153669B (enExample)
AU (1) AU2017271458B2 (enExample)
CA (1) CA3024208C (enExample)
ES (1) ES2899953T3 (enExample)
IL (1) IL263004B (enExample)
MX (1) MX379558B (enExample)
PL (1) PL3464276T3 (enExample)
WO (1) WO2017202674A1 (enExample)

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CN109153669B (zh) * 2016-05-24 2021-12-24 内尔维阿诺医学科学有限公司 苯甲酰胺类化合物的新晶型
EP4003309A1 (en) 2019-07-31 2022-06-01 F. Hoffmann-La Roche AG New pharmaceutical formulation
WO2021084260A1 (en) * 2019-11-01 2021-05-06 Johnson Matthey Public Limited Company Crystalline entrectinib anhydrate and monohydrate forms; crystalline entrectinib thf, nitromethane, isopropyl acetate and methanol solvate forms; processes for preparing a crystalline entrectinib anhydrate form
CN113024521B (zh) * 2019-12-09 2023-01-17 武汉九州钰民医药科技有限公司 一种制备恩曲替尼的方法
CN111171009B (zh) * 2020-01-10 2022-07-12 安礼特（上海）医药科技有限公司 恩曲替尼晶型及其制备方法
CN113354626B (zh) * 2020-03-04 2025-06-03 罗欣药业(上海)有限公司 恩曲替尼的晶型及其制备方法
CN113801062B (zh) * 2020-06-15 2023-05-26 沈阳药科大学 3-氨基-5-(3,5-二氟苄基)-1h-吲唑的制备方法
CN112336723B (zh) * 2020-12-11 2023-09-26 江南大学 制备用于降低trpv4与nox2耦联度的药物的方法
US20240308990A1 (en) * 2021-02-03 2024-09-19 Qilu Pharmaceutical Co., Ltd. Crystal form of entrectinib and preparation method therefor

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013174876A1 (en) * 2012-05-23 2013-11-28 Nerviano Medical Sciences S.R.L. Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide

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US8299057B2 (en) * 2007-07-20 2012-10-30 Nerviano Medical Sciences S.R.L. Substituted indazole derivatives active as kinase inhibitors
TWI672141B (zh) 2014-02-20 2019-09-21 美商醫科泰生技 投予ｒｏｓ１突變癌細胞之分子
CN109153669B (zh) 2016-05-24 2021-12-24 内尔维阿诺医学科学有限公司 苯甲酰胺类化合物的新晶型

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013174876A1 (en) * 2012-05-23 2013-11-28 Nerviano Medical Sciences S.R.L. Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide

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US10738037B2 (en) 2020-08-11
EP3464276B1 (en) 2021-09-01
MX2018014298A (es) 2019-03-14
KR20190005236A (ko) 2019-01-15
CA3024208A1 (en) 2017-11-30
IL263004A (en) 2018-12-31
US11091469B2 (en) 2021-08-17
ES2899953T3 (es) 2022-03-15
JP7154271B2 (ja) 2022-10-17
EP3967689A1 (en) 2022-03-16
BR112018073951A2 (pt) 2019-02-26
JP2019516749A (ja) 2019-06-20
AU2017271458A1 (en) 2019-01-17
HK1259405A1 (zh) 2019-11-29
WO2017202674A1 (en) 2017-11-30
PL3464276T3 (pl) 2022-04-04
JP2021042213A (ja) 2021-03-18
KR102441736B1 (ko) 2022-09-13
EP3464276A1 (en) 2019-04-10
MX379558B (es) 2025-03-11
CA3024208C (en) 2022-07-26
JP7094228B2 (ja) 2022-07-01
IL263004B (en) 2022-04-01
CN109153669B (zh) 2021-12-24
US20190169173A1 (en) 2019-06-06
CN109153669A (zh) 2019-01-04
US20200325122A1 (en) 2020-10-15

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