CN107406430A - 喹唑啉衍生物的盐及其制备方法 - Google Patents

喹唑啉衍生物的盐及其制备方法 Download PDF

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Publication number
CN107406430A
CN107406430A CN201680015924.6A CN201680015924A CN107406430A CN 107406430 A CN107406430 A CN 107406430A CN 201680015924 A CN201680015924 A CN 201680015924A CN 107406430 A CN107406430 A CN 107406430A
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formula
compound
maleate
preparation
maleic acid
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CN201680015924.6A
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CN107406430B (zh
Inventor
张喜全
汤松
丰巍伟
田心
陈智林
顾红梅
徐宏江
刘飞
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Capital Pharmaceutical Holdings Beijing Co ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Shouyao Holdings Beijing Co Ltd
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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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • 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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  • Chemical & Material Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本申请涉及式I化合物的马来酸盐、其制备方法、其药物组合物及其在治疗肿瘤如非小细胞肺癌、乳腺癌等多种恶性肿瘤中的用途。

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。
CN201680015924.6A 2015-03-20 2016-03-18 喹唑啉衍生物的盐及其制备方法 Active CN107406430B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2015101259624 2015-03-20
CN201510125962 2015-03-20
PCT/CN2016/076693 WO2016150340A1 (zh) 2015-03-20 2016-03-18 喹唑啉衍生物的盐及其制备方法

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CN107406430A true CN107406430A (zh) 2017-11-28
CN107406430B CN107406430B (zh) 2019-04-26

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US (1) US10231973B2 (zh)
EP (1) EP3272746B1 (zh)
JP (1) JP6704422B2 (zh)
CN (1) CN107406430B (zh)
ES (1) ES2775614T3 (zh)
HK (1) HK1244278B (zh)
RU (1) RU2720810C2 (zh)
WO (1) WO2016150340A1 (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110627731A (zh) * 2019-10-09 2019-12-31 贵州大学 一类4-氨基喹唑啉接丙烯酰胺类化合物及其制备方法和应用
CN114401957A (zh) * 2019-09-04 2022-04-26 正大天晴药业集团股份有限公司 一种喹唑啉衍生物的制备方法及其结晶
CN114761010A (zh) * 2019-11-25 2022-07-15 正大天晴药业集团股份有限公司 喹唑啉衍生物或其盐的联用药物组合物及其用途

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CN109476634B (zh) * 2016-08-25 2021-04-02 正大天晴药业集团股份有限公司 喹唑啉衍生物的盐的晶体
CN108069946B (zh) * 2016-11-08 2020-06-05 威尚（上海）生物医药有限公司 具有穿过血脑屏障能力的取代的喹唑啉化合物
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
CN114845723B (zh) * 2019-11-01 2024-09-13 正大天晴药业集团股份有限公司 包含喹唑啉衍生物或其盐的药物组合物
WO2021083347A1 (zh) * 2019-11-01 2021-05-06 正大天晴药业集团股份有限公司 喹唑啉衍生物或其盐、或其药物组合物的用途

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CN101878203A (zh) * 2007-10-29 2010-11-03 纳科法尔马有限公司 作为抗癌剂的新的4-(四唑-5-基)喹唑啉衍生物
CN103948689A (zh) * 2014-04-15 2014-07-30 西北农林科技大学 用于治疗非小细胞肺癌的药物组合物及其应用

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Publication number Priority date Publication date Assignee Title
CN114401957A (zh) * 2019-09-04 2022-04-26 正大天晴药业集团股份有限公司 一种喹唑啉衍生物的制备方法及其结晶
CN114401957B (zh) * 2019-09-04 2023-11-21 正大天晴药业集团股份有限公司 一种喹唑啉衍生物的制备方法及其结晶
CN110627731A (zh) * 2019-10-09 2019-12-31 贵州大学 一类4-氨基喹唑啉接丙烯酰胺类化合物及其制备方法和应用
CN114761010A (zh) * 2019-11-25 2022-07-15 正大天晴药业集团股份有限公司 喹唑啉衍生物或其盐的联用药物组合物及其用途
CN114761010B (zh) * 2019-11-25 2024-04-16 正大天晴药业集团股份有限公司 喹唑啉衍生物或其盐的联用药物组合物及其用途

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Publication number Publication date
EP3272746A4 (en) 2018-11-07
EP3272746A1 (en) 2018-01-24
US10231973B2 (en) 2019-03-19
RU2017132330A (ru) 2019-04-22
JP2018508583A (ja) 2018-03-29
RU2017132330A3 (zh) 2019-07-24
CN107406430B (zh) 2019-04-26
US20180085369A1 (en) 2018-03-29
WO2016150340A1 (zh) 2016-09-29
JP6704422B2 (ja) 2020-06-03
EP3272746B1 (en) 2019-12-25
RU2720810C2 (ru) 2020-05-13
ES2775614T3 (es) 2020-07-27
HK1244278B (zh) 2020-04-17

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