CN109563083A - 喹唑啉衍生物类酪氨酸激酶抑制剂的盐及其晶型 - Google Patents

喹唑啉衍生物类酪氨酸激酶抑制剂的盐及其晶型 Download PDF

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CN109563083A
CN109563083A CN201780048635.0A CN201780048635A CN109563083A CN 109563083 A CN109563083 A CN 109563083A CN 201780048635 A CN201780048635 A CN 201780048635A CN 109563083 A CN109563083 A CN 109563083A
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formula
compound
crystal form
maleate
water
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CN109563083B (zh
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王金远
***
冯玉真
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Shandong Xuanzhu Pharma Co Ltd
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    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41Preparation of salts of carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42Separation; Purification; Stabilisation; Use of additives
    • C07C51/43Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/145Maleic acid
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
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  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

提供了式(I)所示的喹唑啉衍生物类酪氨酸激酶抑制剂的马来酸盐及其晶型和制备方法,含有该马来酸盐及其晶型的药物组合物,以及该马来酸盐及其晶型在制备用于治疗和/或预防过度增生疾病和慢性阻塞性肺病的药物中的应用。

Description

PCT国内申请,说明书已公开。

Claims (11)

  1. PCT国内申请,权利要求书已公开。
CN201780048635.0A 2016-08-12 2017-08-11 喹唑啉衍生物类酪氨酸激酶抑制剂的盐及其晶型 Active CN109563083B (zh)

Applications Claiming Priority (3)

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CN2016106634705 2016-08-12
CN201610663470 2016-08-12
PCT/CN2017/097078 WO2018028673A1 (zh) 2016-08-12 2017-08-11 喹唑啉衍生物类酪氨酸激酶抑制剂的盐及其晶型

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CN109563083A true CN109563083A (zh) 2019-04-02
CN109563083B CN109563083B (zh) 2020-11-10

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Families Citing this family (1)

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Publication number Priority date Publication date Assignee Title
CN112010839B (zh) * 2019-05-31 2022-06-17 轩竹生物科技股份有限公司 靶向丝/苏氨酸激酶抑制剂的晶型

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011098607A1 (de) * 2010-02-15 2011-08-18 Boehringer Ingelheim International Gmbh Salze und hydrate des 4 -[(3-chlor-4-fluor-phenyl)amino]-6-(cis-4-{n-[(morph-1-olin-4-yl)carbonyl]-n-methyl-amino}-cyclohexan-1-yloxy)-7-methoxy-chinazolins, deren verwendung als arzneimittel und deren herstellung
WO2012159457A1 (zh) * 2011-05-26 2012-11-29 山东亨利医药科技有限责任公司 喹唑啉衍生物类酪氨酸激酶抑制剂及其制备方法与应用
CN103965175A (zh) * 2013-02-05 2014-08-06 齐鲁制药有限公司 4-(取代苯氨基)喹唑啉类化合物、其制备方法及应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8022216B2 (en) 2007-10-17 2011-09-20 Wyeth Llc Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
CN102382106A (zh) 2010-08-30 2012-03-21 黄振华 苯胺取代的喹唑啉衍生物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011098607A1 (de) * 2010-02-15 2011-08-18 Boehringer Ingelheim International Gmbh Salze und hydrate des 4 -[(3-chlor-4-fluor-phenyl)amino]-6-(cis-4-{n-[(morph-1-olin-4-yl)carbonyl]-n-methyl-amino}-cyclohexan-1-yloxy)-7-methoxy-chinazolins, deren verwendung als arzneimittel und deren herstellung
WO2012159457A1 (zh) * 2011-05-26 2012-11-29 山东亨利医药科技有限责任公司 喹唑啉衍生物类酪氨酸激酶抑制剂及其制备方法与应用
CN103965175A (zh) * 2013-02-05 2014-08-06 齐鲁制药有限公司 4-(取代苯氨基)喹唑啉类化合物、其制备方法及应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
刘燊: "《EGFR酪氨酸激酶抑制剂的设计、合成及生物活性筛选和类药性化合物库的构建》", 《中国博士学位论文全文数据库(电子期刊)》 *

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US20210053944A1 (en) 2021-02-25
CN109563083B (zh) 2020-11-10
WO2018028673A1 (zh) 2018-02-15
US11111234B2 (en) 2021-09-07

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