WO2015194764A3 - 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 - Google Patents

피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 Download PDF

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Publication number
WO2015194764A3
WO2015194764A3 PCT/KR2015/005118 KR2015005118W WO2015194764A3 WO 2015194764 A3 WO2015194764 A3 WO 2015194764A3 KR 2015005118 W KR2015005118 W KR 2015005118W WO 2015194764 A3 WO2015194764 A3 WO 2015194764A3
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WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
alk
pyrimidine
effective ingredient
same
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PCT/KR2015/005118
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English (en)
French (fr)
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WO2015194764A2 (ko
Inventor
윤창수
김형래
조성윤
정희정
이광호
채종학
이정옥
박지훈
김필호
황종연
하재두
안선주
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한국화학연구원
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Priority to US15/319,151 priority Critical patent/US10053458B2/en
Priority to EP15809090.2A priority patent/EP3159338A4/en
Priority to CN201580032624.4A priority patent/CN106459007B/zh
Priority to JP2016573780A priority patent/JP6622726B2/ja
Priority to CA2952787A priority patent/CA2952787A1/en
Publication of WO2015194764A2 publication Critical patent/WO2015194764A2/ko
Publication of WO2015194764A3 publication Critical patent/WO2015194764A3/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12—Nitrogen atoms not forming part of a nitro radical
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

본 발명은 피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 의한 화합물은 역형성 림프종 키나아제(ALK) 활성을 억제하는 효과가 우수하므로 이에 따른 EML4-ALK, NPM-ALK 등의 역형성 림프종 키나아제(ALK) 융합 단백질을 가진 암세포에 대한 치료효과가 향상될 수 있으며, 암의 재발을 막는데 효과적일 것으로 예상되므로 암의 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다.
PCT/KR2015/005118 2014-06-17 2015-05-21 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 WO2015194764A2 (ko)

Priority Applications (5)

Application Number Priority Date Filing Date Title
US15/319,151 US10053458B2 (en) 2014-06-17 2015-05-21 Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient
EP15809090.2A EP3159338A4 (en) 2014-06-17 2015-05-21 Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient
CN201580032624.4A CN106459007B (zh) 2014-06-17 2015-05-21 嘧啶-2，4-二胺衍生物及包含其作为有效成分的抗癌用药学组合物
JP2016573780A JP6622726B2 (ja) 2014-06-17 2015-05-21 ピリミジン‐２，４‐ジアミン誘導体及びそれを有効成分として含有する抗癌用医薬組成物
CA2952787A CA2952787A1 (en) 2014-06-17 2015-05-21 Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2014-0073555 2014-06-17
KR20140073555 2014-06-17

Publications (2)

Publication Number Publication Date
WO2015194764A2 WO2015194764A2 (ko) 2015-12-23
WO2015194764A3 true WO2015194764A3 (ko) 2016-04-14

Family

ID=54936206

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PCT/KR2015/005118 WO2015194764A2 (ko) 2014-06-17 2015-05-21 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물

Country Status (7)

Country Link
US (1) US10053458B2 (ko)
EP (1) EP3159338A4 (ko)
JP (1) JP6622726B2 (ko)
KR (2) KR101733733B1 (ko)
CN (1) CN106459007B (ko)
CA (1) CA2952787A1 (ko)
WO (1) WO2015194764A2 (ko)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101937529B1 (ko) * 2016-07-26 2019-01-14 한국화학연구원 신규한 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
JP7025426B2 (ja) * 2016-11-30 2022-02-24 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 造血前駆体キナーゼ１（ｈｐｋ１）阻害剤としてのアニリノピリミジンａｓ
JOP20190281A1 (ar) 2017-06-13 2019-12-02 Korea Res Inst Chemical Tech مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه
KR102063155B1 (ko) 2018-04-11 2020-01-08 한국과학기술연구원 우수한 카이네이즈 저해 활성을 보이는 다양한 치환기를 갖는 피리미딘 유도체
CN111171017B (zh) * 2018-11-09 2021-12-24 天津大学 基于嘧啶的衍生物及其制备方法和应用
CN109593065A (zh) * 2018-12-03 2019-04-09 重庆医科大学 一类hdac/alk双靶点抑制剂及其制备方法与应用
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
BR112022011834A2 (pt) * 2019-12-16 2022-08-30 Korea Res Inst Chemical Tech Derivado de pirimidina e uso do mesmo
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CA3171187A1 (en) * 2020-02-14 2021-08-19 Salk Institute For Biological Studies Inhibitors of ulk1/2 and methods of using same
CN112168773A (zh) * 2020-08-13 2021-01-05 重庆医药高等专科学校 含嘧啶-2,4-二胺衍生物的抗癌用药物的制备方法
KR20220090443A (ko) * 2020-12-21 2022-06-29 주식회사 비투에스바이오 헤테로아릴 유도체 화합물 및 이의 용도
CN116444488A (zh) * 2022-01-14 2023-07-18 上海立森印迹医药技术有限公司 一种嘧啶-2,4-二胺衍生物及其制备方法和用途

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US20170145007A1 (en) 2017-05-25
CA2952787A1 (en) 2015-12-23
JP2017518336A (ja) 2017-07-06
KR101733733B1 (ko) 2017-05-11
EP3159338A4 (en) 2018-01-24
WO2015194764A2 (ko) 2015-12-23
EP3159338A2 (en) 2017-04-26
CN106459007A (zh) 2017-02-22
JP6622726B2 (ja) 2019-12-18
US10053458B2 (en) 2018-08-21
CN106459007B (zh) 2020-02-28
KR20170027757A (ko) 2017-03-10
KR20150145176A (ko) 2015-12-29

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