CN104159894B - 作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物 - Google Patents

作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物 Download PDF

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Publication number
CN104159894B
CN104159894B CN201380012764.6A CN201380012764A CN104159894B CN 104159894 B CN104159894 B CN 104159894B CN 201380012764 A CN201380012764 A CN 201380012764A CN 104159894 B CN104159894 B CN 104159894B
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alk
fak
day
cep
disorder
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Chinese (zh)
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CN104159894A (zh
Inventor
劳伦特·库瓦西耶
马丁·J·雅各布斯
格雷戈里·R·奥特
肖恩·P·阿尔文
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Cephalon LLC
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Cephalon LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)
CN201380012764.6A 2012-03-06 2013-03-06 作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物 Active CN104159894B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610591742.5A CN106166155B (zh) 2012-03-06 2013-03-06 作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261607305P 2012-03-06 2012-03-06
US61/607,305 2012-03-06
PCT/US2013/029304 WO2013134353A1 (en) 2012-03-06 2013-03-06 Fused bicyclic 2,4-diaminopyrimidine derivative as a dual alk and fak inhibitor

Related Child Applications (1)

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CN201610591742.5A Division CN106166155B (zh) 2012-03-06 2013-03-06 作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物

Publications (2)

Publication Number Publication Date
CN104159894A CN104159894A (zh) 2014-11-19
CN104159894B true CN104159894B (zh) 2016-09-07

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CN201610591742.5A Active CN106166155B (zh) 2012-03-06 2013-03-06 作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物
CN201380012764.6A Active CN104159894B (zh) 2012-03-06 2013-03-06 作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物

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Country Status (28)

Country Link
US (5) US9132128B2 (OSRAM)
EP (2) EP2822939B1 (OSRAM)
JP (2) JP6016953B2 (OSRAM)
KR (1) KR102068374B1 (OSRAM)
CN (2) CN106166155B (OSRAM)
AU (1) AU2013229995B2 (OSRAM)
CA (1) CA2865420C (OSRAM)
CL (1) CL2014002353A1 (OSRAM)
CY (1) CY1117565T1 (OSRAM)
DK (1) DK2822939T3 (OSRAM)
EA (2) EA033124B1 (OSRAM)
ES (2) ES2681487T3 (OSRAM)
HR (1) HRP20160387T1 (OSRAM)
HU (1) HUE027976T2 (OSRAM)
IL (2) IL234239A (OSRAM)
ME (1) ME02460B (OSRAM)
MX (2) MX347772B (OSRAM)
MY (1) MY177290A (OSRAM)
NZ (1) NZ630251A (OSRAM)
PH (1) PH12014501979B1 (OSRAM)
PL (1) PL2822939T3 (OSRAM)
RS (1) RS54689B1 (OSRAM)
SG (2) SG11201405371PA (OSRAM)
SI (1) SI2822939T1 (OSRAM)
SM (1) SMT201600134B (OSRAM)
UA (1) UA115052C2 (OSRAM)
WO (1) WO2013134353A1 (OSRAM)
ZA (1) ZA201406147B (OSRAM)

Cited By (1)

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Publication number Priority date Publication date Assignee Title
CN106166155A (zh) * 2012-03-06 2016-11-30 赛福伦公司 作为alk和fak双重抑制剂的稠合双环2,4‑二氨基嘧啶衍生物

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EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
JP6849594B2 (ja) * 2014-12-23 2021-03-24 セファロン、インク. 縮合二環式2,4−ジアミノピリミジン誘導体を調整する方法
AU2019319109A1 (en) 2018-08-07 2021-02-25 In3Bio Ltd. Methods and compositions for inhibition of EGF/EGFR pathway in cobination with anaplastic lymphoma kinase inhibitors
WO2024178339A2 (en) * 2023-02-23 2024-08-29 The Regents Of The University Of Michigan Methods for treating neuroblastoma with a dual anaplastic lymphoma kinase and focal adhesion kinase inhibitor
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (2)

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CN1918158A (zh) * 2004-02-14 2007-02-21 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
CN101535276A (zh) * 2006-10-23 2009-09-16 赛福伦公司 作为ALK和c-MET抑制剂的2,4-二氨基嘧啶稠合双环衍生物

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AU2004259012C1 (en) 2003-07-23 2012-08-02 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
RU2395500C2 (ru) 2003-08-15 2010-07-27 Новартис Аг 2,4-пиримидиндиамины, применяемые в лечении неопластических болезней, воспалительных и иммунных расстройств
WO2005097765A1 (en) 2004-03-31 2005-10-20 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
ES2622493T3 (es) * 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
EP3012249A1 (en) * 2006-12-08 2016-04-27 Novartis AG Compounds and composition as protein kinase inhibitors
ES2593486T3 (es) * 2007-04-18 2016-12-09 Pfizer Products Inc. Derivados de sulfonil amida para el tratamiento del crecimiento celular anómalo
WO2010143664A1 (ja) * 2009-06-10 2010-12-16 中外製薬株式会社 4環性化合物
CA2865420C (en) * 2012-03-06 2020-06-02 Cephalon, Inc. Fused bicyclic 2,4-diaminopyrimidine derivative as a dual alk and fak inhibitor
KR101446742B1 (ko) * 2012-08-10 2014-10-01 한국화학연구원 N2,n4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
JP6849594B2 (ja) * 2014-12-23 2021-03-24 セファロン、インク. 縮合二環式2,4−ジアミノピリミジン誘導体を調整する方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1918158A (zh) * 2004-02-14 2007-02-21 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
CN101535276A (zh) * 2006-10-23 2009-09-16 赛福伦公司 作为ALK和c-MET抑制剂的2,4-二氨基嘧啶稠合双环衍生物

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106166155A (zh) * 2012-03-06 2016-11-30 赛福伦公司 作为alk和fak双重抑制剂的稠合双环2,4‑二氨基嘧啶衍生物
CN106166155B (zh) * 2012-03-06 2019-01-18 赛福伦公司 作为alk和fak双重抑制剂的稠合双环2,4-二氨基嘧啶衍生物

Also Published As

Publication number Publication date
EP2822939B1 (en) 2016-02-17
SI2822939T1 (sl) 2016-04-29
IL252364B (en) 2018-03-29
HUE027976T2 (en) 2016-11-28
CA2865420C (en) 2020-06-02
JP2015509540A (ja) 2015-03-30
MX2014010613A (es) 2014-09-18
KR102068374B1 (ko) 2020-01-20
MX347772B (es) 2017-05-12
MX372740B (es) 2020-05-04
CL2014002353A1 (es) 2015-01-09
EA025859B1 (ru) 2017-02-28
US20150011561A1 (en) 2015-01-08
DK2822939T3 (en) 2016-03-14
MY177290A (en) 2020-09-10
ES2681487T3 (es) 2018-09-13
EP3056494A1 (en) 2016-08-17
EA201691574A1 (ru) 2017-03-31
IL234239A (en) 2017-06-29
AU2013229995A1 (en) 2014-09-25
US20170173017A1 (en) 2017-06-22
NZ630251A (en) 2016-02-26
EP3056494B1 (en) 2018-05-02
JP6016953B2 (ja) 2016-10-26
CN104159894A (zh) 2014-11-19
SG10201507865QA (en) 2015-10-29
ES2570976T3 (es) 2016-05-23
SMT201600134B (it) 2016-07-01
CN106166155B (zh) 2019-01-18
HRP20160387T1 (hr) 2016-05-20
RS54689B1 (sr) 2016-08-31
US20190328735A1 (en) 2019-10-31
IL252364A0 (en) 2017-07-31
WO2013134353A8 (en) 2014-06-19
ZA201406147B (en) 2015-12-23
WO2013134353A1 (en) 2013-09-12
AU2013229995B2 (en) 2017-04-13
PH12014501979A1 (en) 2014-11-24
US10111872B2 (en) 2018-10-30
PH12014501979B1 (en) 2014-11-24
EA033124B1 (ru) 2019-08-30
HK1205119A1 (zh) 2015-12-11
US20160243119A1 (en) 2016-08-25
PL2822939T3 (pl) 2016-08-31
US10632119B2 (en) 2020-04-28
EA201491641A1 (ru) 2015-04-30
CN106166155A (zh) 2016-11-30
US9339502B2 (en) 2016-05-17
US9623026B2 (en) 2017-04-18
SG11201405371PA (en) 2014-09-26
UA115052C2 (uk) 2017-09-11
JP2017039741A (ja) 2017-02-23
CA2865420A1 (en) 2013-09-12
EP2822939A1 (en) 2015-01-14
ME02460B (me) 2017-02-20
HK1226300A1 (zh) 2017-09-29
KR20140138247A (ko) 2014-12-03
US9132128B2 (en) 2015-09-15
US20150374693A1 (en) 2015-12-31
CY1117565T1 (el) 2017-04-26

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