CN106166155B - 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
CN106166155B
CN106166155B CN201610591742.5A CN201610591742A CN106166155B CN 106166155 B CN106166155 B CN 106166155B CN 201610591742 A CN201610591742 A CN 201610591742A CN 106166155 B CN106166155 B CN 106166155B
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cancer
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alk
cep
administration
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CN106166155A (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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
CN201610591742.5A 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 CN106166155B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261607305P 2012-03-06 2012-03-06
US61/607,305 2012-03-06
CN201380012764.6A 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

Related Parent Applications (1)

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CN201380012764.6A Division 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

Publications (2)

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CN106166155A CN106166155A (zh) 2016-11-30
CN106166155B true CN106166155B (zh) 2019-01-18

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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) EP3056494B1 (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) EA025859B1 (OSRAM)
ES (2) ES2681487T3 (OSRAM)
HR (1) HRP20160387T1 (OSRAM)
HU (1) HUE027976T2 (OSRAM)
IL (2) IL234239A (OSRAM)
ME (1) ME02460B (OSRAM)
MX (2) MX372740B (OSRAM)
MY (1) MY177290A (OSRAM)
NZ (1) NZ630251A (OSRAM)
PH (1) PH12014501979B1 (OSRAM)
PL (1) PL2822939T3 (OSRAM)
RS (1) RS54689B1 (OSRAM)
SG (2) SG10201507865QA (OSRAM)
SI (1) SI2822939T1 (OSRAM)
SM (1) SMT201600134B (OSRAM)
UA (1) UA115052C2 (OSRAM)
WO (1) WO2013134353A1 (OSRAM)
ZA (1) ZA201406147B (OSRAM)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY177290A (en) * 2012-03-06 2020-09-10 Cephalon Inc Fused bicyclic 2,4-diaminopyrimidine derivative as a dual alk and fak inhibitor
SG11201608303QA (en) 2014-04-04 2016-11-29 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
HK1244789B (en) * 2014-12-23 2019-12-06 Cephalon, Inc. Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives
JP2021534094A (ja) 2018-08-07 2021-12-09 イン3バイオ・リミテッドIn3Bio Ltd. 未分化リンパ腫キナーゼ阻害剤と組み合わせてegf/egfr経路を抑制するための方法および組成物
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
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005080393A1 (en) * 2004-02-14 2005-09-01 Irm Llc Compounds and compositions as protein kinase inhibitors
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
CN104159894B (zh) * 2012-03-06 2016-09-07 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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AU2004259012C1 (en) 2003-07-23 2012-08-02 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
PL2287156T3 (pl) 2003-08-15 2013-11-29 Novartis Ag 2,4-Di(fenyloamino)-pirymidyny stosowane w leczeniu chorób nowotworowych, chorób zapalnych i zaburzeń układu immunologicznego
JP2008502595A (ja) 2004-03-31 2008-01-31 エグゼリクシス, インコーポレイテッド 未分化リンパ腫キナーゼモジュレータおよびその使用方法
CA2642229C (en) * 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN101616895A (zh) * 2006-12-08 2009-12-30 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
JP4782239B2 (ja) * 2007-04-18 2011-09-28 ファイザー・プロダクツ・インク 異常細胞増殖治療のためのスルホニルアミド誘導体
EP3613729A1 (en) * 2009-06-10 2020-02-26 Chugai Seiyaku Kabushiki Kaisha Tetracyclic compounds
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
HK1244789B (en) * 2014-12-23 2019-12-06 Cephalon, Inc. Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005080393A1 (en) * 2004-02-14 2005-09-01 Irm Llc Compounds and compositions as protein kinase inhibitors
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
CN104159894B (zh) * 2012-03-06 2016-09-07 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
MY177290A (en) 2020-09-10
EA201491641A1 (ru) 2015-04-30
UA115052C2 (uk) 2017-09-11
CL2014002353A1 (es) 2015-01-09
CA2865420C (en) 2020-06-02
RS54689B1 (sr) 2016-08-31
US20150011561A1 (en) 2015-01-08
AU2013229995B2 (en) 2017-04-13
WO2013134353A1 (en) 2013-09-12
EA025859B1 (ru) 2017-02-28
US9623026B2 (en) 2017-04-18
MX2014010613A (es) 2014-09-18
EP3056494A1 (en) 2016-08-17
SG11201405371PA (en) 2014-09-26
HRP20160387T1 (hr) 2016-05-20
PL2822939T3 (pl) 2016-08-31
MX372740B (es) 2020-05-04
US10111872B2 (en) 2018-10-30
WO2013134353A8 (en) 2014-06-19
SG10201507865QA (en) 2015-10-29
DK2822939T3 (en) 2016-03-14
HK1226300A1 (zh) 2017-09-29
US9339502B2 (en) 2016-05-17
IL252364B (en) 2018-03-29
ME02460B (me) 2017-02-20
PH12014501979A1 (en) 2014-11-24
KR102068374B1 (ko) 2020-01-20
JP2015509540A (ja) 2015-03-30
CY1117565T1 (el) 2017-04-26
KR20140138247A (ko) 2014-12-03
EA201691574A1 (ru) 2017-03-31
EA033124B1 (ru) 2019-08-30
AU2013229995A1 (en) 2014-09-25
NZ630251A (en) 2016-02-26
CN104159894A (zh) 2014-11-19
CN106166155A (zh) 2016-11-30
JP2017039741A (ja) 2017-02-23
EP3056494B1 (en) 2018-05-02
IL234239A (en) 2017-06-29
SI2822939T1 (sl) 2016-04-29
EP2822939B1 (en) 2016-02-17
ES2681487T3 (es) 2018-09-13
MX347772B (es) 2017-05-12
US20150374693A1 (en) 2015-12-31
HK1205119A1 (zh) 2015-12-11
IL252364A0 (en) 2017-07-31
US9132128B2 (en) 2015-09-15
JP6016953B2 (ja) 2016-10-26
PH12014501979B1 (en) 2014-11-24
HUE027976T2 (en) 2016-11-28
US20190328735A1 (en) 2019-10-31
ZA201406147B (en) 2015-12-23
CN104159894B (zh) 2016-09-07
US20160243119A1 (en) 2016-08-25
US20170173017A1 (en) 2017-06-22
CA2865420A1 (en) 2013-09-12
EP2822939A1 (en) 2015-01-14
ES2570976T3 (es) 2016-05-23
US10632119B2 (en) 2020-04-28
SMT201600134B (it) 2016-07-01

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