JP2011500712A - (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態 - Google Patents

(e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態 Download PDF

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JP2011500712A
JP2011500712A JP2010530105A JP2010530105A JP2011500712A JP 2011500712 A JP2011500712 A JP 2011500712A JP 2010530105 A JP2010530105 A JP 2010530105A JP 2010530105 A JP2010530105 A JP 2010530105A JP 2011500712 A JP2011500712 A JP 2011500712A
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anilino
ethoxy
chloro
cyano
quinolinyl
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ル キングホング
シェリー ク マンチング
チェウ ワーレン
ケイ. チェアル グロリア
エフ. ハドフィールド アンソニー
ミルメフラビ マフムード
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ワイス・エルエルシー
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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
    • C07D401/02Heterocyclic 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41Preparation of salts of carboxylic acids
    • C07C51/412Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • 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
    • 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

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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)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
JP2010530105A 2007-10-17 2008-10-16 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態 Pending JP2011500712A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12479607P 2007-10-17 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 Child Applications (1)

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JP2010258729A Division JP2011063610A (ja) 2007-10-17 2010-11-19 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態

Publications (1)

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JP2011500712A true JP2011500712A (ja) 2011-01-06

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Family Applications (11)

Application Number Title Priority Date Filing Date
JP2010530105A Pending JP2011500712A (ja) 2007-10-17 2008-10-16 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2010258729A Withdrawn JP2011063610A (ja) 2007-10-17 2010-11-19 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2011289220A Active JP5965640B2 (ja) 2007-10-17 2011-12-28 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2012279650A Pending JP2013053170A (ja) 2007-10-17 2012-12-21 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2015080748A Pending JP2015127352A (ja) 2007-10-17 2015-04-10 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2016238151A Active JP6412090B2 (ja) 2007-10-17 2016-12-08 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2018079067A Withdrawn JP2018109071A (ja) 2007-10-17 2018-04-17 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2020070281A Withdrawn JP2020111606A (ja) 2007-10-17 2020-04-09 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2021146090A Pending JP2021185200A (ja) 2007-10-17 2021-09-08 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2023160192A Withdrawn JP2023164747A (ja) 2007-10-17 2023-09-25 (e)-n-{4-[3-クロロ-4-(2-ピリジニルメトキシ)アニリノ]-3-シアノ-7-エトキシ-6-キノリニル}-4-(ジメチルアミノ)-2-ブテンアミドのマレイン酸塩およびその結晶形態
JP2025124961A Pending JP2025137789A (ja) 2007-10-17 2025-07-25 (e)-n-{4-[3-クロロ-4-(2-ピリジニルメトキシ)アニリノ]-3-シアノ-7-エトキシ-6-キノリニル}-4-(ジメチルアミノ)-2-ブテンアミドのマレイン酸塩およびその結晶形態

Family Applications After (10)

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JP2010258729A Withdrawn JP2011063610A (ja) 2007-10-17 2010-11-19 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2011289220A Active JP5965640B2 (ja) 2007-10-17 2011-12-28 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2012279650A Pending JP2013053170A (ja) 2007-10-17 2012-12-21 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2015080748A Pending JP2015127352A (ja) 2007-10-17 2015-04-10 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2016238151A Active JP6412090B2 (ja) 2007-10-17 2016-12-08 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2018079067A Withdrawn JP2018109071A (ja) 2007-10-17 2018-04-17 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2020070281A Withdrawn JP2020111606A (ja) 2007-10-17 2020-04-09 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2021146090A Pending JP2021185200A (ja) 2007-10-17 2021-09-08 (e)−n−{4−[3−クロロ−4−(2−ピリジニルメトキシ)アニリノ]−3−シアノ−7−エトキシ−6−キノリニル}−4−(ジメチルアミノ)−2−ブテンアミドのマレイン酸塩およびその結晶形態
JP2023160192A Withdrawn JP2023164747A (ja) 2007-10-17 2023-09-25 (e)-n-{4-[3-クロロ-4-(2-ピリジニルメトキシ)アニリノ]-3-シアノ-7-エトキシ-6-キノリニル}-4-(ジメチルアミノ)-2-ブテンアミドのマレイン酸塩およびその結晶形態
JP2025124961A Pending JP2025137789A (ja) 2007-10-17 2025-07-25 (e)-n-{4-[3-クロロ-4-(2-ピリジニルメトキシ)アニリノ]-3-シアノ-7-エトキシ-6-キノリニル}-4-(ジメチルアミノ)-2-ブテンアミドのマレイン酸塩およびその結晶形態

Country Status (20)

Country Link
US (7) US8022216B2 (https=)
EP (6) EP2537843B1 (https=)
JP (11) JP2011500712A (https=)
KR (5) KR20130025862A (https=)
CN (7) CN110452221A (https=)
AR (2) AR068932A1 (https=)
AU (1) AU2008312474B2 (https=)
BR (2) BRPI0818464B8 (https=)
CA (2) CA2928071C (https=)
CL (1) CL2008003088A1 (https=)
ES (3) ES2602123T3 (https=)
IL (3) IL308687A (https=)
IN (1) IN2015DN01135A (https=)
MX (5) MX387683B (https=)
NZ (3) NZ616136A (https=)
PA (1) PA8800701A1 (https=)
RU (2) RU2463300C2 (https=)
SG (2) SG185312A1 (https=)
TW (1) TW200934761A (https=)
WO (1) WO2009052264A2 (https=)

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JP2015522042A (ja) * 2012-07-12 2015-08-03 ジエンス ヘンルイ メデイシンカンパニー リミテッドJiangsu Hengrui Medicine Co.,Ltd. チロシンキナーゼ阻害剤二マレイン酸塩のi型結晶およびその製造法
JP2018501289A (ja) * 2015-01-09 2018-01-18 クリスタル ファーマテック カンパニー、リミテッドCrystal Pharmatech Co., Ltd. ネラチニブマレイン酸塩の新規な結晶形及びその製造方法

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KR101313702B1 (ko) 2005-02-03 2013-10-04 와이어쓰 제피티니브 및/또는 에를로티니브 내성암 치료용 약제학적 조성물
EP1942937A1 (en) 2005-11-04 2008-07-16 Wyeth 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
BRPI0914790A2 (pt) 2008-06-17 2015-10-20 Wyeth Llc uso de um composto de vinorelbina e um composto de hki-272, composição farmacêutica e produto e kit para o tratamento de neoplasma
US8669273B2 (en) 2008-08-04 2014-03-11 Wyeth Llc Antineoplastic combinations of 4-anilino-3-cyanoquinolines and capecitabine
DK3000467T3 (da) 2009-04-06 2023-03-27 Wyeth Llc Behandling med neratinib mod brystkræft
US8586598B2 (en) * 2009-04-29 2013-11-19 Nerviano Medical Sciences S.R.L. CDK inhibitor salts
CA2780332C (en) 2009-11-09 2018-01-30 Wyeth Llc Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea
CA2783743C (en) 2009-12-11 2022-10-04 Wyeth Llc Phosphatidylinositol-3-kinase pathway biomarkers
US8338456B2 (en) 2010-01-13 2012-12-25 Wyeth Llc Cut-point in PTEN protein expression that accurately identifies tumors and is predictive of drug response to a pan-ErbB inhibitor
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
EP2716633B1 (en) * 2011-05-26 2017-05-17 Xuanzhu Pharma Co., Ltd. Quinazoline derivative as tyrosine-kinase inhibitor, preparation method therefor and application thereof
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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WO2016210345A1 (en) 2015-06-25 2016-12-29 The California Institute For Biomedical Research 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
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