ES2656623T3 - Forma cristalina l de dimaleato inhibidor de tirosina cinasa y métodos de preparación de la misma - Google Patents

Forma cristalina l de dimaleato inhibidor de tirosina cinasa y métodos de preparación de la misma Download PDF

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Publication number
ES2656623T3
ES2656623T3 ES13817593.0T ES13817593T ES2656623T3 ES 2656623 T3 ES2656623 T3 ES 2656623T3 ES 13817593 T ES13817593 T ES 13817593T ES 2656623 T3 ES2656623 T3 ES 2656623T3
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dimaleate
crystalline form
tyrosine kinase
kinase inhibitor
preparation methods
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Piaoyang Sun
Guaili Wu
Bo Yuan
Yongjiang Chen
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Jiangsu Hengrui Medicine Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/08Malonic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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)
  • 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)
  • Epidemiology (AREA)
  • 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

Forma cristalina I de dimaleato de (R,E)-N-(4-(3-cloro-4-(piridin-2-ilmetoxi)-fenilamino)-3-ciano-7-etoxiquinolin-6-il)- 3-(1-metilpirrolidin-2-il)acrilamida, caracterizada por que se usa radiación Kα de Cu para obtener los patrones de difracción de rayos X representados por ángulos 2θ y distancia de cristal interplanar, teniendo el cristal patrones de difracción de rayos X como se muestra en la Figura 1 en la que hay picos característicos en 6,28(14,06), 6,74(13,10), 10,60(8,34), 11,58(7,64), 13,50(6,55), 14,90(5,94), 15,80(5,60), 18,26(4,85), 20,66(4,30), 21,14(4,20), 22,96(3,87), 24,34(3,65), 25,54(3,49) y 26,12(3,41).

Description

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Claims (1)

  1. imagen1
ES13817593.0T 2012-07-12 2013-06-04 Forma cristalina l de dimaleato inhibidor de tirosina cinasa y métodos de preparación de la misma Active ES2656623T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201210240697.0A CN103539783A (zh) 2012-07-12 2012-07-12 一种酪氨酸激酶抑制剂的二马来酸盐的i型结晶及制备方法
CN201210240697 2012-07-12
PCT/CN2013/076717 WO2014008794A1 (zh) 2012-07-12 2013-06-04 一种酪氨酸激酶抑制剂的二马来酸盐的i型结晶及制备方法

Publications (1)

Publication Number Publication Date
ES2656623T3 true ES2656623T3 (es) 2018-02-27

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ES13817593.0T Active ES2656623T3 (es) 2012-07-12 2013-06-04 Forma cristalina l de dimaleato inhibidor de tirosina cinasa y métodos de preparación de la misma

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Country Link
US (1) US9309226B2 (es)
EP (1) EP2873664B1 (es)
JP (1) JP6170146B2 (es)
KR (1) KR102078077B1 (es)
CN (2) CN103539783A (es)
AU (1) AU2013289789B2 (es)
BR (1) BR112015000045B1 (es)
CA (1) CA2876884C (es)
DK (1) DK2873664T3 (es)
ES (1) ES2656623T3 (es)
HU (1) HUE037946T2 (es)
MX (1) MX349672B (es)
NO (1) NO2873664T3 (es)
PL (1) PL2873664T3 (es)
PT (1) PT2873664T (es)
RU (1) RU2631321C2 (es)
TW (1) TWI597277B (es)
UA (1) UA113658C2 (es)
WO (1) WO2014008794A1 (es)
ZA (1) ZA201500471B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105985408B (zh) * 2015-02-12 2020-06-26 正大天晴药业集团股份有限公司 一种卡非佐米的纯化方法
CN108026059A (zh) 2015-07-22 2018-05-11 阿纳韦克斯生命科学公司 四氢-n,n-二甲基-2,2-二苯基-3-呋喃甲胺盐酸盐的晶型,制备这样晶型的方法,及其药物组合物
CA3008701A1 (en) 2016-01-27 2017-08-03 Jiangsu Hengrui Medicine Co., Ltd. Method for preparing pharmaceutical composition comprising quinoline derivative or salt thereof
CN108354909B (zh) * 2016-01-27 2021-05-14 江苏恒瑞医药股份有限公司 一种含有喹啉衍生物或其盐的药物组合物
WO2017129094A1 (zh) * 2016-01-28 2017-08-03 江苏恒瑞医药股份有限公司 一种egfr/her2受体酪氨酸激酶抑制剂在制备治疗her2突变癌症药物中的用途
CA3016092C (en) * 2016-03-22 2025-03-11 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. POLYCRYSTALLINE FORM OF FREE BASIC OR SALT EGFR INHIBITOR ACID, PROCESS FOR ITS PREPARATION AND APPLICATION
CN113769097A (zh) 2017-01-22 2021-12-10 江苏恒瑞医药股份有限公司 Egfr/her2抑制剂联合嘧啶类抗代谢药物的用途
WO2019029477A1 (zh) * 2017-08-07 2019-02-14 江苏恒瑞医药股份有限公司 一种酪氨酸激酶抑制剂的二马来酸盐的晶型及其制备方法
CN109516976B (zh) * 2017-09-19 2022-05-27 南京圣和药业股份有限公司 取代嘧啶类pi3k抑制剂甲磺酸盐的晶型及其制备方法
CA3079916A1 (en) 2017-10-24 2019-05-02 Jiangsu Hengrui Medicine Co., Ltd. Pharmaceutical composition containing quinoline derivative
CN110960529A (zh) * 2018-09-30 2020-04-07 江苏恒瑞医药股份有限公司 一种降低了毒性杂质含量的酪氨酸激酶抑制剂的原料药
MX2021004600A (es) 2018-10-22 2021-06-15 Jiangsu Hengrui Medicine Co Forma cristalina del inhibidor de maleato de tirosina quinasa y metodo de preparacion para el mismo.
CN111138414A (zh) * 2018-11-05 2020-05-12 江苏恒瑞医药股份有限公司 一种酪氨酸激酶抑制剂的晶型及其制备方法
WO2021037185A1 (zh) * 2019-08-30 2021-03-04 江苏恒瑞医药股份有限公司 一种低杂质含量的酪氨酸激酶抑制剂
CN114674937B (zh) * 2020-12-24 2024-07-05 沈阳药科大学 一种马来酸长链脂肪酰胺中长链脂肪胺的测定方法

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UA73073C2 (uk) * 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
WO2001051919A2 (en) * 2000-01-07 2001-07-19 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
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
CN101824029A (zh) * 2009-03-05 2010-09-08 厦门艾德生物医药科技有限公司 酪氨酸激酶不可逆抑制剂、其药物组合物及其用途
CN102020639A (zh) * 2009-09-14 2011-04-20 上海恒瑞医药有限公司 6-氨基喹唑啉或3-氰基喹啉类衍生物、其制备方法及其在医药上的应用
CN102675287A (zh) * 2011-03-11 2012-09-19 江苏恒瑞医药股份有限公司 (e)-n-[4-[[3-氯-4-(2-吡啶基甲氧基)苯基]氨基]-3-氰基-7-乙氧基-6-喹啉基]-3-[(2r)-1-甲基吡咯烷-2-基]丙-2-烯酰胺的可药用的盐、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
UA113658C2 (xx) 2017-02-27
EP2873664A1 (en) 2015-05-20
CA2876884C (en) 2019-12-10
JP2015522042A (ja) 2015-08-03
HK1199027A1 (zh) 2015-06-19
AU2013289789A1 (en) 2015-01-22
EP2873664B1 (en) 2017-11-01
CN103974949B (zh) 2015-11-25
CN103539783A (zh) 2014-01-29
US9309226B2 (en) 2016-04-12
KR20150036336A (ko) 2015-04-07
KR102078077B1 (ko) 2020-02-17
MX349672B (es) 2017-08-08
RU2631321C2 (ru) 2017-09-21
MX2014015623A (es) 2015-06-23
US20150166511A1 (en) 2015-06-18
TWI597277B (zh) 2017-09-01
JP6170146B2 (ja) 2017-07-26
ZA201500471B (en) 2016-10-26
BR112015000045B1 (pt) 2021-10-26
NO2873664T3 (es) 2018-03-31
PT2873664T (pt) 2018-01-24
CA2876884A1 (en) 2014-01-16
CN103974949A (zh) 2014-08-06
BR112015000045A2 (pt) 2017-06-27
EP2873664A4 (en) 2015-12-30
TW201402563A (zh) 2014-01-16
RU2015103065A (ru) 2016-08-27
AU2013289789B2 (en) 2017-06-29
DK2873664T3 (en) 2018-01-08
PL2873664T3 (pl) 2018-06-29
HUE037946T2 (hu) 2018-09-28
WO2014008794A1 (zh) 2014-01-16

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