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WO2009008371A1 - ジ(アリールアミノ)アリール化合物 - Google Patents

ジ(アリールアミノ)アリール化合物 Download PDF

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Publication number
WO2009008371A1
WO2009008371A1 PCT/JP2008/062188 JP2008062188W WO2009008371A1 WO 2009008371 A1 WO2009008371 A1 WO 2009008371A1 JP 2008062188 W JP2008062188 W JP 2008062188W WO 2009008371 A1 WO2009008371 A1 WO 2009008371A1
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WO
WIPO (PCT)
Prior art keywords
eml4
alk fusion
egfr variant
cancer
polynucleotide positive
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP2008/062188
Other languages
English (en)
French (fr)
Inventor
Yutaka Kondoh
Kazuhiko Iikubo
Sadao Kuromitsu
Nobuaki Shindo
Takatoshi Soga
Takashi Furutani
Itsuro Shimada
Takahiro Matsuya
Kazuo Kurosawa
Akio Kamikawa
Hiroyuki Mano
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Astellas Pharma Inc
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Astellas Pharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to CN2008800236055A priority Critical patent/CN101687822B/zh
Priority to MX2009013625A priority patent/MX2009013625A/es
Priority to EP08777903A priority patent/EP2172461A4/en
Priority to US12/448,759 priority patent/US8318702B2/en
Priority to KR1020097026439A priority patent/KR101323566B1/ko
Priority to BRPI0814809-0A2A priority patent/BRPI0814809A2/pt
Priority to CA 2692611 priority patent/CA2692611A1/en
Priority to JP2009522627A priority patent/JP5233996B2/ja
Application filed by Astellas Pharma Inc filed Critical Astellas Pharma Inc
Priority to AU2008273426A priority patent/AU2008273426B2/en
Publication of WO2009008371A1 publication Critical patent/WO2009008371A1/ja
Priority to ZA2009/08305A priority patent/ZA200908305B/en
Anticipated expiration legal-status Critical
Priority to US13/618,732 priority patent/US20130096100A1/en
Ceased legal-status Critical Current

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    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
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    • C07ORGANIC CHEMISTRY
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    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
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    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
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    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40Nitrogen atoms
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    • C07D251/50Two nitrogen atoms with a halogen atom attached to the third ring carbon atom
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
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    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
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    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
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    • C07D251/70Other substituted melamines
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    • 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
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    • 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
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    • 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
    • C07D403/02Heterocyclic 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
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    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

【課題】EML4-ALK融合タンパク及び変異EGFRタンパクのキナーゼ活性の阻害剤として有用な化合物を提供する。 【解決手段】本発明者らは、EML4-ALK融合タンパク及び変異EGFRタンパクのキナーゼ活性を阻害する作用を有する化合物について鋭意検討した結果、本発明のジ(アリールアミノ)アリール化合物が、EML4-ALK融合タンパク及び変異EGFRタンパクのキナーゼ活性の阻害活性を有することを知見し、本発明を完成させた。本発明化合物は、癌、肺癌、非小細胞肺癌、小細胞肺癌、EML4-ALK融合ポリヌクレオチド陽性及び/若しくは変異EGFRポリヌクレオチド陽性の癌、EML4-ALK融合ポリヌクレオチド陽性及び/若しくは変異EGFRポリヌクレオチド陽性の肺癌、又はEML4-ALK融合ポリヌクレオチド陽性及び/若しくは変異EGFRポリヌクレオチド陽性の非小細胞肺癌等の予防及び/若しくは治療用医薬組成物として使用しうる。
PCT/JP2008/062188 2007-07-06 2008-07-04 ジ(アリールアミノ)アリール化合物 Ceased WO2009008371A1 (ja)

Priority Applications (11)

Application Number Priority Date Filing Date Title
CA 2692611 CA2692611A1 (en) 2007-07-06 2008-07-04 Di(arylamino)aryl compounds
EP08777903A EP2172461A4 (en) 2007-07-06 2008-07-04 DI (ARYLAMINO) ARYL COMPOUND
US12/448,759 US8318702B2 (en) 2007-07-06 2008-07-04 Di(arylamino)aryl compounds
KR1020097026439A KR101323566B1 (ko) 2007-07-06 2008-07-04 디(아릴아미노)아릴 화합물
BRPI0814809-0A2A BRPI0814809A2 (pt) 2007-07-06 2008-07-04 Compostos di(arilamino)arílicos
CN2008800236055A CN101687822B (zh) 2007-07-06 2008-07-04 二(芳基氨基)芳基化合物
MX2009013625A MX2009013625A (es) 2007-07-06 2008-07-04 Compuestos de di (arilamino) arilo.
JP2009522627A JP5233996B2 (ja) 2007-07-06 2008-07-04 ジ(アリールアミノ)アリール化合物
AU2008273426A AU2008273426B2 (en) 2007-07-06 2008-07-04 Di(arylamino)aryl compounds
ZA2009/08305A ZA200908305B (en) 2007-07-06 2009-11-24 Di(arylamino)aryl compounds
US13/618,732 US20130096100A1 (en) 2007-07-06 2012-09-14 Di(arylamino)aryl compound

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-178795 2007-07-06
JP2007178795 2007-07-06

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US13/618,732 Division US20130096100A1 (en) 2007-07-06 2012-09-14 Di(arylamino)aryl compound

Publications (1)

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WO2009008371A1 true WO2009008371A1 (ja) 2009-01-15

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PCT/JP2008/062188 Ceased WO2009008371A1 (ja) 2007-07-06 2008-07-04 ジ(アリールアミノ)アリール化合物

Country Status (13)

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US (2) US8318702B2 (ja)
EP (1) EP2172461A4 (ja)
JP (1) JP5233996B2 (ja)
KR (1) KR101323566B1 (ja)
CN (1) CN101687822B (ja)
AU (1) AU2008273426B2 (ja)
BR (1) BRPI0814809A2 (ja)
CA (1) CA2692611A1 (ja)
MX (1) MX2009013625A (ja)
RU (1) RU2463299C2 (ja)
TW (1) TWI389893B (ja)
WO (1) WO2009008371A1 (ja)
ZA (1) ZA200908305B (ja)

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010128659A1 (ja) 2009-05-08 2010-11-11 アステラス製薬株式会社 ジアミノへテロ環カルボキサミド化合物
WO2010143664A1 (ja) 2009-06-10 2010-12-16 中外製薬株式会社 4環性化合物
WO2011145548A1 (ja) 2010-05-18 2011-11-24 アステラス製薬株式会社 ジ(アリールアミノ)アリール化合物の結晶
CN102482277A (zh) * 2009-05-05 2012-05-30 达纳-法伯癌症研究所有限公司 表皮生长因子受体抑制剂及治疗障碍的方法
WO2012102393A1 (ja) 2011-01-28 2012-08-02 アステラス製薬株式会社 ジ(アリールアミノ)アリール化合物の製造方法及びその合成中間体
JP2013539795A (ja) * 2010-10-14 2013-10-28 アリアド・ファーマシューティカルズ・インコーポレイテッド Egfr発動性がんの細胞増殖の阻害方法
WO2014071832A1 (en) * 2012-11-06 2014-05-15 Shanghai Fochon Pharmaceutical Co Ltd Alk kinase inhibitors
US9714229B2 (en) 2014-04-25 2017-07-25 Chugai Seiyaku Kabushiki Kaisha Crystal of tetracyclic compound
JP2017521436A (ja) * 2014-07-04 2017-08-03 チル ファーマシューティカル カンパニー リミテッド スピロ環アリールリン酸化物及びアリールリン硫化物(spirocyclic aryl phosphorus oxide and aryl phosphorus sulfide)
US10344014B2 (en) 2014-08-08 2019-07-09 Chugai Seiyaku Kabushiki Kaisha Amorphous form of tetracyclic compound
US10350214B2 (en) 2014-04-25 2019-07-16 Chugai Seiyaku Kabushiki Kaisha Preparation containing tetracyclic compound at high dose
US10646468B2 (en) 2010-08-20 2020-05-12 Chugai Seiyaku Kabushiki Kaisha Composition comprising tetracyclic compound
US10668075B2 (en) 2012-09-25 2020-06-02 Chugai Seiyaku Kabushiki Kaisha RET inhibitor
US11077093B2 (en) 2015-01-16 2021-08-03 Chugai Seiyaku Kabushiki Kaisha Combination drug
JP2021521163A (ja) * 2018-04-09 2021-08-26 上海科技大学Shanghai Tech University 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
RU2526253C9 (ru) * 2009-05-08 2022-08-02 Астеллас Фарма Инк. Диаминогетероциклическое карбоксамидное соединение
US11939322B2 (en) 2018-09-04 2024-03-26 Chugai Seiyaku Kabushiki Kaisha Method for producing tetracyclic compound

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