CN106822127B - 来那替尼马来酸盐及晶形 - Google Patents

来那替尼马来酸盐及晶形 Download PDF

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CN106822127B
CN106822127B CN201710057547.9A CN201710057547A CN106822127B CN 106822127 B CN106822127 B CN 106822127B CN 201710057547 A CN201710057547 A CN 201710057547A CN 106822127 B CN106822127 B CN 106822127B
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maleate
anilino
chloro
ethoxy
cyano
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CN106822127A (zh
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吕庆红
M·S·库
W·丘
G·K·奇尔
A·F·哈德菲尔德
M·米尔梅拉比
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Wyeth LLC
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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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
CN201710057547.9A 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形 Active CN106822127B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US12479607P 2007-10-17 2007-10-17
US61/124,796 2007-10-17
CN200880118789.3A CN101918390B (zh) 2007-10-17 2008-10-16 (e)-n-{4-[3-氯-4-(2-吡啶基甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基}-4-(二甲基氨基)-2-丁烯酰胺的马来酸盐及其结晶形式
PCT/US2008/080130 WO2009052264A2 (en) 2007-10-17 2008-10-16 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

Related Parent Applications (1)

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CN200880118789.3A Division CN101918390B (zh) 2007-10-17 2008-10-16 (e)-n-{4-[3-氯-4-(2-吡啶基甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基}-4-(二甲基氨基)-2-丁烯酰胺的马来酸盐及其结晶形式

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CN106822127A CN106822127A (zh) 2017-06-13
CN106822127B true CN106822127B (zh) 2022-07-29

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CN201310576791.8A Pending CN103554086A (zh) 2007-10-17 2008-10-16 (e)-n-｛4-[3-氯-4-(2-吡啶甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基｝-4-(二甲氨基)-2-丁烯酰胺马来酸盐及晶形
CN201710057547.9A Active CN106822127B (zh) 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形
CN202310691104.0A Pending CN116715654A (zh) 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形
CN201910667051.2A Pending CN110452221A (zh) 2007-10-17 2008-10-16 (e)-n-{4-[3-氯-4-(2-吡啶甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基}-4-(二甲氨基)-2-丁烯酰胺马来酸盐及晶形
CN200880118789.3A Active CN101918390B (zh) 2007-10-17 2008-10-16 (e)-n-{4-[3-氯-4-(2-吡啶基甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基}-4-(二甲基氨基)-2-丁烯酰胺的马来酸盐及其结晶形式
CN202310690478.0A Pending CN116715653A (zh) 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形
CN202310689097.0A Pending CN117143077A (zh) 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形

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CN201310576791.8A Pending CN103554086A (zh) 2007-10-17 2008-10-16 (e)-n-｛4-[3-氯-4-(2-吡啶甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基｝-4-(二甲氨基)-2-丁烯酰胺马来酸盐及晶形

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Application Number Title Priority Date Filing Date
CN202310691104.0A Pending CN116715654A (zh) 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形
CN201910667051.2A Pending CN110452221A (zh) 2007-10-17 2008-10-16 (e)-n-{4-[3-氯-4-(2-吡啶甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基}-4-(二甲氨基)-2-丁烯酰胺马来酸盐及晶形
CN200880118789.3A Active CN101918390B (zh) 2007-10-17 2008-10-16 (e)-n-{4-[3-氯-4-(2-吡啶基甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基}-4-(二甲基氨基)-2-丁烯酰胺的马来酸盐及其结晶形式
CN202310690478.0A Pending CN116715653A (zh) 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形
CN202310689097.0A Pending CN117143077A (zh) 2007-10-17 2008-10-16 来那替尼马来酸盐及晶形

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US (6) US8022216B2 (enExample)
EP (6) EP2258698A3 (enExample)
JP (11) JP2011500712A (enExample)
KR (5) KR101208301B1 (enExample)
CN (7) CN103554086A (enExample)
AR (2) AR068932A1 (enExample)
AU (1) AU2008312474B2 (enExample)
BR (2) BRPI0818464B8 (enExample)
CA (2) CA2928071C (enExample)
CL (1) CL2008003088A1 (enExample)
ES (3) ES2612273T3 (enExample)
IL (3) IL308687A (enExample)
IN (1) IN2015DN01135A (enExample)
MX (5) MX349332B (enExample)
NZ (3) NZ705641A (enExample)
PA (1) PA8800701A1 (enExample)
RU (2) RU2463300C2 (enExample)
SG (2) SG10201900175TA (enExample)
TW (1) TW200934761A (enExample)
WO (1) WO2009052264A2 (enExample)

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HUE032958T2 (hu) 2008-08-04 2017-11-28 Wyeth Llc 4-Anilino-3-ciano-kinolinok és capecitabin antineoplasztikus kombinációi
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CN103539783A (zh) * 2012-07-12 2014-01-29 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i型结晶及制备方法
CN104513200B (zh) * 2013-09-26 2017-05-03 江苏苏中药业集团股份有限公司 取代丁烯酰胺的马来酸盐及其晶型
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CN105949176B (zh) * 2016-06-24 2018-10-26 浙江海正药业股份有限公司 一种来那替尼的纯化方法
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CN109563083B (zh) 2016-08-12 2020-11-10 山东轩竹医药科技有限公司 喹唑啉衍生物类酪氨酸激酶抑制剂的盐及其晶型
CN107721987A (zh) * 2016-08-12 2018-02-23 山东轩竹医药科技有限公司 喹唑啉类酪氨酸激酶抑制剂的晶型
CN107721985A (zh) * 2016-08-12 2018-02-23 山东轩竹医药科技有限公司 喹唑啉类酪氨酸激酶抑制剂的晶型
CN107721986A (zh) * 2016-08-12 2018-02-23 山东轩竹医药科技有限公司 喹唑啉类酪氨酸激酶抑制剂的晶型
WO2018134843A1 (en) * 2017-01-23 2018-07-26 Msn Laboratories Private Limited, R&D Center Polymorphic forms of (e)-n-{4-[3-chloro-4-((pyridin-2-yl methoxy)anilino]-3-cyano-7- ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide, its maleate salt and process for preparation thereof
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WO2019015394A1 (zh) * 2017-07-17 2019-01-24 苏州科睿思制药有限公司 一种来那替尼单马来酸盐的晶型及其制备方法和用途
WO2019096327A1 (en) * 2017-11-20 2019-05-23 Teligene Ltd Maleate salts of (e)-n-(3-cyano-7-ethoxy-4-((4-phenoxyphenyl)amino) quinolin-6-yl)-4-(dimethylamino) but-2-enamide and crystalline forms thereof
CN107698563B (zh) * 2017-11-23 2020-10-30 江苏创诺制药有限公司 制备马来酸来那替尼晶型的方法
CN108299394A (zh) * 2018-02-28 2018-07-20 江苏创诺制药有限公司 来那替尼二马来酸盐晶型及其制备方法
CN110357855A (zh) * 2018-03-26 2019-10-22 江苏创诺制药有限公司 一种来那替尼盐酸盐晶型及其制备方法
CN109053683A (zh) * 2018-07-27 2018-12-21 苏州晶云药物科技股份有限公司 来那替尼马来酸盐晶型c的制备方法以及来那替尼马来酸盐晶型c
CN109053702A (zh) * 2018-08-13 2018-12-21 扬子江药业集团有限公司 一种阿法替尼类似物及其制备方法和用途
CN109503479A (zh) * 2018-12-03 2019-03-22 四川自豪时代药业有限公司 一种磷酸萘酚喹工艺杂质及其合成方法
CN111848581B (zh) * 2020-08-19 2021-08-10 昆明学院 3-氰基-4-苯胺基-6-氨基喹啉衍生物的制备方法
CN111995618B (zh) * 2020-09-02 2021-06-11 重庆医科大学 一种来那替尼杂质g的制备方法
CN111943933B (zh) * 2020-09-02 2021-05-28 重庆医科大学 一种来那替尼杂质d的制备方法
CN114380745A (zh) * 2020-10-19 2022-04-22 江苏苏中药业集团股份有限公司 一种取代丁烯酰胺颗粒混合物及晶型ii制备方法与应用
EP4237421A4 (en) 2020-11-02 2024-11-06 Trethera Corporation CRYSTALLINE FORMS OF A DEOXYCYTIDINE KINASE INHIBITOR AND THEIR USES
CN116723845A (zh) * 2020-11-02 2023-09-08 特雷西拉公司 脱氧胞苷激酶抑制剂的结晶形式及其用途

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