CN103958510B - 用于治疗癌症的吡咯并嘧啶化合物 - Google Patents

用于治疗癌症的吡咯并嘧啶化合物 Download PDF

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CN103958510B
CN103958510B CN201280056825.4A CN201280056825A CN103958510B CN 103958510 B CN103958510 B CN 103958510B CN 201280056825 A CN201280056825 A CN 201280056825A CN 103958510 B CN103958510 B CN 103958510B
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alkyl
compound
pyrrolo
aryl
group
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CN103958510A (zh
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王晓东
刘京
张维河
S·弗赖依
D·基里弗
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University of North Carolina at Chapel Hill
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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280056825.4A 2011-10-03 2012-10-01 用于治疗癌症的吡咯并嘧啶化合物 Active CN103958510B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161542392P 2011-10-03 2011-10-03
US61/542,392 2011-10-03
US201161547183P 2011-10-14 2011-10-14
US61/547,183 2011-10-14
PCT/US2012/058298 WO2013052417A1 (en) 2011-10-03 2012-10-01 Pyrrolopyrimidine compounds for the treatment of cancer

Publications (2)

Publication Number Publication Date
CN103958510A CN103958510A (zh) 2014-07-30
CN103958510B true CN103958510B (zh) 2016-10-19

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CN201280056825.4A Active CN103958510B (zh) 2011-10-03 2012-10-01 用于治疗癌症的吡咯并嘧啶化合物

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Country Link
US (3) US9273056B2 (https=)
EP (1) EP2763988B1 (https=)
JP (2) JP2014532060A (https=)
KR (1) KR102063098B1 (https=)
CN (1) CN103958510B (https=)
AU (1) AU2012318896B2 (https=)
BR (1) BR112014007788A2 (https=)
CA (1) CA2850617A1 (https=)
ES (1) ES2650630T3 (https=)
IL (1) IL231835A0 (https=)
MX (1) MX2014004086A (https=)
RU (1) RU2631655C2 (https=)
WO (1) WO2013052417A1 (https=)

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US9290499B2 (en) 2010-05-19 2016-03-22 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
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AU2013266438B2 (en) 2012-05-22 2017-09-07 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
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EP2925752A4 (en) 2012-11-27 2016-06-01 Univ North Carolina PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
US9555031B2 (en) * 2014-04-11 2017-01-31 The University Of North Carolina At Chapel Hill Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity
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US20180296561A1 (en) * 2015-10-07 2018-10-18 The University Of North Carolina At Chapel Hill The Methods For Treatment Of Tumors
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
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KR102163494B1 (ko) * 2018-10-26 2020-10-08 한국과학기술연구원 단백질 키나아제 저해제인 헤테로방향족 매크로시클릭 유도체
TWI843838B (zh) * 2019-04-02 2024-06-01 美商Ｍｅｒｙｘ股份有限公司 激酶抑制劑之多晶型、含有該化合物之醫藥組成物、製備方法、及應用
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CN112043710A (zh) * 2020-09-28 2020-12-08 广州智睿医药科技有限公司 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物
CN115073469B (zh) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物作为激酶抑制剂的制备及其应用
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AU2012318896A1 (en) 2014-05-22
JP2014532060A (ja) 2014-12-04
KR102063098B1 (ko) 2020-01-08
JP2017101043A (ja) 2017-06-08
CA2850617A1 (en) 2013-04-11
IL231835A0 (en) 2014-05-28
AU2012318896B2 (en) 2017-03-02
US9273056B2 (en) 2016-03-01
ES2650630T3 (es) 2018-01-19
US9795606B2 (en) 2017-10-24
BR112014007788A2 (pt) 2017-04-18
EP2763988A4 (en) 2015-06-03
US20140243315A1 (en) 2014-08-28
WO2013052417A1 (en) 2013-04-11
KR20140095471A (ko) 2014-08-01
EP2763988A1 (en) 2014-08-13
MX2014004086A (es) 2014-09-22
US20180104247A1 (en) 2018-04-19
US10179133B2 (en) 2019-01-15
CN103958510A (zh) 2014-07-30
JP6316925B2 (ja) 2018-04-25
RU2631655C2 (ru) 2017-09-26
RU2014115847A (ru) 2015-11-10
HK1201256A1 (en) 2015-08-28
EP2763988B1 (en) 2017-09-20
US20160151372A1 (en) 2016-06-02

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