CN107428686A - 尼达尼布二乙磺酸盐晶体及其制备方法和用途 - Google Patents

尼达尼布二乙磺酸盐晶体及其制备方法和用途 Download PDF

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Publication number
CN107428686A
CN107428686A CN201680014054.0A CN201680014054A CN107428686A CN 107428686 A CN107428686 A CN 107428686A CN 201680014054 A CN201680014054 A CN 201680014054A CN 107428686 A CN107428686 A CN 107428686A
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China
Prior art keywords
nintedanib
esilate
type crystal
preparation
organic solvent
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Pending
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CN201680014054.0A
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English (en)
Inventor
王胡博
朱雪焱
郭猛
胡明通
张家松
孙九德
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Publication of CN107428686A publication Critical patent/CN107428686A/zh
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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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B28/00—Production of homogeneous polycrystalline material with defined structure
    • C30B28/04—Production of homogeneous polycrystalline material with defined structure from liquids
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B29/00—Single crystals or homogeneous polycrystalline material with defined structure characterised by the material or by their shape
    • C30B29/10—Inorganic compounds or compositions
    • C30B29/46—Sulfur-, selenium- or tellurium-containing compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Materials Engineering (AREA)
  • Metallurgy (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

本申请涉及式（）所示的尼达尼布二乙磺酸盐的A型晶体，还涉及包含该晶体的晶体组合物、药物组合物，以及它们的制备方法和用途。本申请的尼达尼布二乙磺酸盐A型晶体的X‑射线粉末衍射光谱用2θ值表示在约14.64、18.79、19.31、20.11、21.20、22.45、26.71º处有衍射峰。本申请的尼达尼布二乙磺酸盐的A型晶体性质稳定，不易降解、不吸潮、特别适合药物生产。

Description

PCT国内申请，说明书已公开。

Claims (14)

  1. PCT国内申请，权利要求书已公开。
CN201680014054.0A 2015-03-13 2016-03-11 尼达尼布二乙磺酸盐晶体及其制备方法和用途 Pending CN107428686A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510112909.0A CN106008308A (zh) 2015-03-13 2015-03-13 尼达尼布乙磺酸盐结晶
CN2015101129090 2015-03-13
PCT/CN2016/076110 WO2016146020A1 (zh) 2015-03-13 2016-03-11 尼达尼布二乙磺酸盐晶体及其制备方法和用途

Publications (1)

Publication Number Publication Date
CN107428686A true CN107428686A (zh) 2017-12-01

Family

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Family Applications (2)

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CN201510112909.0A Withdrawn CN106008308A (zh) 2015-03-13 2015-03-13 尼达尼布乙磺酸盐结晶
CN201680014054.0A Pending CN107428686A (zh) 2015-03-13 2016-03-11 尼达尼布二乙磺酸盐晶体及其制备方法和用途

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CN201510112909.0A Withdrawn CN106008308A (zh) 2015-03-13 2015-03-13 尼达尼布乙磺酸盐结晶

Country Status (6)

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US (1) US10292965B2 (zh)
EP (1) EP3269710B1 (zh)
JP (1) JP2018509421A (zh)
CN (2) CN106008308A (zh)
RU (1) RU2708683C2 (zh)
WO (1) WO2016146020A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110072849A (zh) * 2017-03-14 2019-07-30 新源生物科技股份有限公司 3-z-[1-(4-(n-((4-甲基-哌嗪-1-基)-甲羰基)-n-甲基-氨基)-苯氨基)-1-苯基-亚甲基]-6-甲氧羰基-2-吲哚满酮的晶型
JP7382317B2 (ja) 2017-11-17 2023-11-16 フェルミオン オサケ ユキチュア ニンテダニブを製造するための中間体として公知の２－インドリノン誘導体の合成
CN113024439A (zh) * 2021-03-28 2021-06-25 郑州大学 尼达尼布乙磺酸盐新晶型ⅰ的制备

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1671660A (zh) * 2002-07-24 2005-09-21 贝林格尔英格海姆法玛两合公司 3－z－[1－(4－(n－((4－甲基－哌嗪－1－基)－甲羰基)－n－甲基－氨基)－苯氨基)－1－苯基－亚甲基]－6－甲氧羰基－2－吲哚满酮－单乙烷磺酸盐及其作为药物组合物的用途
WO2012068441A2 (en) * 2010-11-19 2012-05-24 Ratiopharm Gmbh Intedanib salts and solid state forms thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1870400A1 (en) * 2006-06-08 2007-12-26 Boehringer Ingelheim Pharma GmbH & Co. KG Salts and crystalline salt forms of an 2-indolinone derivative
ES2658091T3 (es) * 2007-12-03 2018-03-08 Boehringer Ingelheim International Gmbh Procedimiento para la fabricación de un derivado de indolinona

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1671660A (zh) * 2002-07-24 2005-09-21 贝林格尔英格海姆法玛两合公司 3－z－[1－(4－(n－((4－甲基－哌嗪－1－基)－甲羰基)－n－甲基－氨基)－苯氨基)－1－苯基－亚甲基]－6－甲氧羰基－2－吲哚满酮－单乙烷磺酸盐及其作为药物组合物的用途
WO2012068441A2 (en) * 2010-11-19 2012-05-24 Ratiopharm Gmbh Intedanib salts and solid state forms thereof

Also Published As

Publication number Publication date
RU2017136104A3 (zh) 2019-07-17
US10292965B2 (en) 2019-05-21
WO2016146020A1 (zh) 2016-09-22
RU2017136104A (ru) 2019-04-15
EP3269710A1 (en) 2018-01-17
JP2018509421A (ja) 2018-04-05
US20180064684A1 (en) 2018-03-08
CN106008308A (zh) 2016-10-12
EP3269710B1 (en) 2020-01-01
EP3269710A4 (en) 2018-08-22
RU2708683C2 (ru) 2019-12-11

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