KR20130025862A - (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태 - Google Patents

(ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태 Download PDF

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Publication number
KR20130025862A
KR20130025862A KR1020127017202A KR20127017202A KR20130025862A KR 20130025862 A KR20130025862 A KR 20130025862A KR 1020127017202 A KR1020127017202 A KR 1020127017202A KR 20127017202 A KR20127017202 A KR 20127017202A KR 20130025862 A KR20130025862 A KR 20130025862A
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anilino
chloro
cyano
quinolinyl
ethoxy
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Korean (ko)
Inventor
큉홍 루
만칭 셔리 쿠
와렌 츄
글로리아 케이 치일
안쏘니 에프 하드필드
마모우드 미르머라비
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와이어쓰 엘엘씨
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Application filed by 와이어쓰 엘엘씨 filed Critical 와이어쓰 엘엘씨
Publication of KR20130025862A publication Critical patent/KR20130025862A/ko
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    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (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)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
KR1020127017202A 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태 Ceased KR20130025862A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12479607P 2007-10-17 2007-10-17
US61/124,796 2007-10-17
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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KR1020107010637A Division KR101208301B1 (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR20157007530A Division KR20150039872A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태

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KR20130025862A true KR20130025862A (ko) 2013-03-12

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ID=40347915

Family Applications (5)

Application Number Title Priority Date Filing Date
KR1020127017202A Ceased KR20130025862A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태
KR20157007530A Ceased KR20150039872A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태
KR1020187008867A Ceased KR20180041753A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태
KR1020107010637A Active KR101208301B1 (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태
KR1020167032469A Ceased KR20160136474A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태

Family Applications After (4)

Application Number Title Priority Date Filing Date
KR20157007530A Ceased KR20150039872A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태
KR1020187008867A Ceased KR20180041753A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태
KR1020107010637A Active KR101208301B1 (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태
KR1020167032469A Ceased KR20160136474A (ko) 2007-10-17 2008-10-16 (ｅ)-ｎ-｛4-〔3-클로로-4-(2-피리디닐메톡시)아닐리노〕-3-시아노-7-에톡시-6-퀴놀리닐｝-4-(다이메틸아미노)-2-부텐아미드의 말레에이트 염 및 이의 결정질 형태

Country Status (20)

Country Link
US (7) US8022216B2 (enExample)
EP (6) EP2617719B1 (enExample)
JP (11) JP2011500712A (enExample)
KR (5) KR20130025862A (enExample)
CN (7) CN116715654A (enExample)
AR (2) AR068932A1 (enExample)
AU (1) AU2008312474B2 (enExample)
BR (2) BRPI0818464B8 (enExample)
CA (2) CA2702930C (enExample)
CL (1) CL2008003088A1 (enExample)
ES (3) ES2602123T3 (enExample)
IL (4) IL308687A (enExample)
IN (1) IN2015DN01135A (enExample)
MX (5) MX342681B (enExample)
NZ (3) NZ616136A (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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DE10349113A1 (de) 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
NZ556673A (en) 2005-02-03 2010-03-26 Gen Hospital Corp Method for treating gefitinib and/or erlotinib resistant cancer with an EGFR inhibitor
EP3488866A1 (en) 2005-11-04 2019-05-29 Wyeth LLC Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272
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
ES2531322T3 (es) 2008-06-17 2015-03-13 Wyeth Llc Combinaciones antineoplásicas que contienen HKI-272 y vinorelbina
EP3175853B1 (en) 2008-08-04 2023-11-01 Wyeth LLC Antineoplastic combinations of neratinib and capecitabine
PT3000467T (pt) 2009-04-06 2023-03-30 Wyeth Llc Regime de tratamento utilizando neratinib para o cancro de mama
WO2010125004A1 (en) * 2009-04-29 2010-11-04 Nerviano Medical Sciences S.R.L. Cdk inhibitor salts
EP2498751B1 (en) 2009-11-09 2019-04-03 Wyeth LLC Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea
EP2510121A1 (en) 2009-12-11 2012-10-17 Wyeth LLC Phosphatidylinositol-3-kinase pathway biomarkers
JP6126382B2 (ja) * 2010-01-13 2017-05-10 ワイス・エルエルシー 腫瘍を正確に識別し、かつＰＡＮ‐ＥｒｂＢ阻害剤に対する薬物応答を予測するＰＴＥＮタンパク質発現におけるカットポイント
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
HUE033575T2 (hu) 2011-05-26 2017-12-28 Xuanzhu Pharma Co Ltd Tirozin-kináz inhibitor kinazolin származék, elõállítási eljárása és alkalmazása
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
DK3229861T3 (en) * 2014-12-12 2019-04-29 Sanofi Sa PACKAGING FOR MEDICAL DEVICE
JP2017536931A (ja) * 2014-12-12 2017-12-14 サノフイ 医用装置パッケージ
CN105367552A (zh) * 2015-01-09 2016-03-02 苏州晶云药物科技有限公司 来那替尼马来酸盐的新晶型及其制备方法
US10774068B2 (en) * 2015-06-25 2020-09-15 The Scripps Research Institute Composition and methods for inhibiting mammalian sterile 20-like kinase 1
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
US20200308141A1 (en) 2016-06-27 2020-10-01 Pliva Hrvatska D.O.O. Solid state forms of neratinib and salts thereof
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
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
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
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
WO2018189695A1 (en) * 2017-04-11 2018-10-18 Lupin Limited Neratinib crystalline forms and process for preparation thereof
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
CN111344280B (zh) * 2017-11-20 2022-08-12 苏州韬略生物科技股份有限公司 (e)-n-(3-氰基-7-乙氧基-4-((4-苯氧基苯基)氨基)喹啉-6-基)-4-(二甲基氨基) 丁-2-烯酰胺马来酸盐及晶型
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
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