KR102246265B1 - 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도 - Google Patents

5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도 Download PDF

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KR102246265B1
KR102246265B1 KR1020207007411A KR20207007411A KR102246265B1 KR 102246265 B1 KR102246265 B1 KR 102246265B1 KR 1020207007411 A KR1020207007411 A KR 1020207007411A KR 20207007411 A KR20207007411 A KR 20207007411A KR 102246265 B1 KR102246265 B1 KR 102246265B1
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compound
cancer
chk1
treatment
inhibitors
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KR20200038990A (ko
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이안 콜린스
토마스 피터 매튜스
타티아나 파리아 다 폰세카 맥하디
제임스 오스본
마이클 레인치버리
마이클 이안 월턴
미셸 다운 개럿
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캔써 리서치 테크놀로지 리미티드
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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
    • A61K31/435Heterocyclic 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
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
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    • 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
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    • 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
    • C07D403/12Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020207007411A 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도 Active KR102246265B1 (ko)

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KR1020217012299A KR102341637B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도

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US201261647200P 2012-05-15 2012-05-15
US61/647,200 2012-05-15
PCT/GB2013/051233 WO2013171470A1 (en) 2012-05-15 2013-05-14 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof

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KR1020207007411A Active KR102246265B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
KR1020147031572A Active KR102090792B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
KR1020227037439A Active KR102635954B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
KR1020217041302A Ceased KR20210156333A (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
KR1020247004407A Withdrawn KR20240023685A (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴및 그의 치료적 용도
KR1020217012299A Active KR102341637B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도

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KR1020147031572A Active KR102090792B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
KR1020227037439A Active KR102635954B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
KR1020217041302A Ceased KR20210156333A (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
KR1020247004407A Withdrawn KR20240023685A (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴및 그의 치료적 용도
KR1020217012299A Active KR102341637B1 (ko) 2012-05-15 2013-05-14 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도

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US (3) US9663503B2 (enExample)
EP (2) EP2855448B1 (enExample)
JP (2) JP6027230B2 (enExample)
KR (6) KR102246265B1 (enExample)
CN (2) CN106279142B (enExample)
AU (2) AU2013261605B2 (enExample)
BR (1) BR112014026801B1 (enExample)
CA (1) CA2870837C (enExample)
DK (1) DK2855448T3 (enExample)
ES (2) ES2981584T3 (enExample)
IL (1) IL235133A (enExample)
IN (1) IN2014DN09221A (enExample)
MX (1) MX358819B (enExample)
NZ (1) NZ702050A (enExample)
PL (1) PL2855448T3 (enExample)
RU (1) RU2659786C2 (enExample)
SG (1) SG11201407238VA (enExample)
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SG11201407238VA (en) * 2012-05-15 2014-12-30 Cancer Rec Tech Ltd 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof
SMT202000713T1 (it) 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
ES2768678T3 (es) 2013-12-06 2020-06-23 Vertex Pharma Compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de la ATR quinasa, su preparación, diferentes formas sólidas y derivados radiomarcados de las mismas
SG10201902206QA (en) 2014-06-05 2019-04-29 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
AU2015277212B2 (en) * 2014-06-17 2020-07-02 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of Chk1 and ATR inhibitors
RU2768621C1 (ru) 2015-09-30 2022-03-24 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr
WO2018094325A1 (en) * 2016-11-18 2018-05-24 The Trustees Of Columbia University In The City Of New York Therapeutic modulation of oncogenes by pharmacologic top2 targeting for cancer
MX2019011506A (es) * 2017-03-31 2019-11-01 Seattle Genetics Inc Inhibicion de cinasa 1 de punto de control (chk1) para el tratamiento de cancer.
WO2018191299A1 (en) * 2017-04-10 2018-10-18 Sierra Oncology, Inc. Chk1(sra737)wee1 inhibitor combination methods of inhibiting tumor growth
CN116999564A (zh) * 2017-04-10 2023-11-07 塞拉肿瘤学公司 抑制肿瘤生长的CHK1(SRA737)/PARPi组合方法
US20200157638A1 (en) * 2017-06-01 2020-05-21 Sierra Oncology, Inc. Biomarkers and patient selection strategies
CN107266897B (zh) * 2017-08-04 2019-05-14 上海跃贝新材料科技股份有限公司 一种低粘度矿物增强pc/pet合金材料及其制备方法
KR20200126388A (ko) * 2018-02-26 2020-11-06 시에라 온코로지, 인코퍼레이티드 Chk1 저해제를 포함하는 암의 치료 방법
JP2022523028A (ja) * 2019-01-25 2022-04-21 ヌメディー, インコーポレイテッド 特発性肺線維症を処置するための方法
CA3135165A1 (en) * 2019-03-28 2020-10-01 Sierra Oncology, Inc. Methods of treating cancer with chk1 inhibitors
CN114072526A (zh) * 2019-05-14 2022-02-18 塞拉肿瘤学公司 使用chk1抑制剂治疗癌症的方法
CN110872277B (zh) * 2019-11-14 2021-06-04 浙江大学 N-取代芳环-2-氨基嘧啶类化合物及用途
CN110684083B (zh) * 2019-12-06 2020-05-15 北京诺赛启研再生医学研究院有限公司 抑制黑色素合成的偶联物ii及其在药品和化妆品中的应用
CN110680928B (zh) * 2019-12-06 2020-04-28 深圳前海港影生物科技有限公司 抑制黑色素合成的偶联物及其在药品和化妆品中的应用
TW202204348A (zh) * 2020-04-07 2022-02-01 美商西爾拉癌症醫學公司 Chk1抑制劑之合成方法
CN117858870A (zh) * 2021-08-17 2024-04-09 葛兰素史密斯克莱知识产权(第3号)有限公司 P2x3拮抗剂的制备
TW202519226A (zh) 2023-11-08 2025-05-16 美商艾克塞里克斯公司 使用抑制pkmyt1之化合物治療癌症之方法

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