KR102441736B1 - N-[5-(3,5-디플루오로-벤질)-1h-인다졸-3-일]-4-(4-메틸-피페라진-1-일)-2-(테트라하이드로-피란-4-일아미노)-벤즈아미드의 신규 결정형 - Google Patents

N-[5-(3,5-디플루오로-벤질)-1h-인다졸-3-일]-4-(4-메틸-피페라진-1-일)-2-(테트라하이드로-피란-4-일아미노)-벤즈아미드의 신규 결정형 Download PDF

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KR102441736B1
KR102441736B1 KR1020187037182A KR20187037182A KR102441736B1 KR 102441736 B1 KR102441736 B1 KR 102441736B1 KR 1020187037182 A KR1020187037182 A KR 1020187037182A KR 20187037182 A KR20187037182 A KR 20187037182A KR 102441736 B1 KR102441736 B1 KR 102441736B1
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cancer
formula
crystalline form
compound
degrees
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KR20190005236A (ko
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일라리아 칸디아니
지오반니 오타이아노
아틸리오 토마시
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네르비아노 메디칼 사이언시스 에스.알.엘.
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    • 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
    • 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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
KR1020187037182A 2016-05-24 2017-05-18 N-[5-(3,5-디플루오로-벤질)-1h-인다졸-3-일]-4-(4-메틸-피페라진-1-일)-2-(테트라하이드로-피란-4-일아미노)-벤즈아미드의 신규 결정형 Active KR102441736B1 (ko)

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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KR20190005236A KR20190005236A (ko) 2019-01-15
KR102441736B1 true KR102441736B1 (ko) 2022-09-13

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US (2) US10738037B2 (https=)
EP (2) EP3967689A1 (https=)
JP (2) JP7094228B2 (https=)
KR (1) KR102441736B1 (https=)
CN (1) CN109153669B (https=)
AU (1) AU2017271458B2 (https=)
CA (1) CA3024208C (https=)
ES (1) ES2899953T3 (https=)
IL (1) IL263004B (https=)
MX (1) MX379558B (https=)
PL (1) PL3464276T3 (https=)
WO (1) WO2017202674A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3967689A1 (en) 2016-05-24 2022-03-16 Nerviano Medical Sciences S.r.l. New crystalline form of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydropyran-4-ylamino)-benzamide
CN119909073A (zh) 2019-07-31 2025-05-02 豪夫迈·罗氏有限公司 新型药物制剂
US20220372024A1 (en) * 2019-11-01 2022-11-24 Johnson Matthey Public Limited Company Crystalline forms of entrectinib
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
EP4273144B1 (en) * 2021-02-03 2026-05-06 Qilu Pharmaceutical Co., Ltd. Crystal form of entrectinib and preparation method therefor

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2176231T (pt) 2007-07-20 2016-12-09 Nerviano Medical Sciences Srl Derivados de indazol substituídos activos como inibidores de quinases
ES2751944T3 (es) * 2012-05-23 2020-04-02 Nerviano Medical Sciences Srl Proceso para la preparación de N-[5-(3,5-difluoro-bencil)-1H-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetrahidro-piran-4-ilamino)-benzamida
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
EP3967689A1 (en) 2016-05-24 2022-03-16 Nerviano Medical Sciences S.r.l. New crystalline form of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydropyran-4-ylamino)-benzamide

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AU2017271458A1 (en) 2019-01-17
JP7154271B2 (ja) 2022-10-17
JP7094228B2 (ja) 2022-07-01
BR112018073951A2 (pt) 2019-02-26
HK1259405A1 (zh) 2019-11-29
AU2017271458B2 (en) 2020-11-26
PL3464276T3 (pl) 2022-04-04
EP3464276B1 (en) 2021-09-01
CN109153669B (zh) 2021-12-24
MX2018014298A (es) 2019-03-14
WO2017202674A1 (en) 2017-11-30
US11091469B2 (en) 2021-08-17
EP3464276A1 (en) 2019-04-10
CN109153669A (zh) 2019-01-04
US20190169173A1 (en) 2019-06-06
CA3024208C (en) 2022-07-26
ES2899953T3 (es) 2022-03-15
IL263004A (en) 2018-12-31
MX379558B (es) 2025-03-11
KR20190005236A (ko) 2019-01-15
US10738037B2 (en) 2020-08-11
JP2021042213A (ja) 2021-03-18
US20200325122A1 (en) 2020-10-15
CA3024208A1 (en) 2017-11-30
IL263004B (en) 2022-04-01
JP2019516749A (ja) 2019-06-20
EP3967689A1 (en) 2022-03-16

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