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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Priority to CN201610591742.5A priority Critical patent/CN106166155B/zh
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    • 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
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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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)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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

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Country Status (28)

Country Link
US (5) US9132128B2 (enExample)
EP (2) EP3056494B1 (enExample)
JP (2) JP6016953B2 (enExample)
KR (1) KR102068374B1 (enExample)
CN (2) CN104159894B (enExample)
AU (1) AU2013229995B2 (enExample)
CA (1) CA2865420C (enExample)
CL (1) CL2014002353A1 (enExample)
CY (1) CY1117565T1 (enExample)
DK (1) DK2822939T3 (enExample)
EA (2) EA025859B1 (enExample)
ES (2) ES2570976T3 (enExample)
HR (1) HRP20160387T1 (enExample)
HU (1) HUE027976T2 (enExample)
IL (2) IL234239A (enExample)
ME (1) ME02460B (enExample)
MX (2) MX347772B (enExample)
MY (1) MY177290A (enExample)
NZ (1) NZ630251A (enExample)
PH (1) PH12014501979A1 (enExample)
PL (1) PL2822939T3 (enExample)
RS (1) RS54689B1 (enExample)
SG (2) SG10201507865QA (enExample)
SI (1) SI2822939T1 (enExample)
SM (1) SMT201600134B (enExample)
UA (1) UA115052C2 (enExample)
WO (1) WO2013134353A1 (enExample)
ZA (1) ZA201406147B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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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

Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
WO2015154064A2 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
WO2016105529A1 (en) 2014-12-23 2016-06-30 Cephalon, Inc. Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives
MX2021001398A (es) 2018-08-07 2021-08-16 In3Bio Ltd Métodos y composiciones para la inhibición de la vía egf/egfr en combinación con inhibidores de la cinasa del linfoma anaplásico.
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
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
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

Citations (2)

* Cited by examiner, † Cited by third party
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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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US7872014B2 (en) 2003-07-23 2011-01-18 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
JP4607879B2 (ja) 2003-08-15 2011-01-05 ノバルティス アーゲー 新生物疾患、炎症および免疫障害の処置に有用な２，４−ピリミジンジアミン
AU2005230847B2 (en) 2004-03-31 2012-11-08 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
US8962643B2 (en) * 2006-02-24 2015-02-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
RS53588B1 (sr) * 2006-12-08 2015-02-27 Irm Llc Jedinjenja i kompozicije kao inhibitori protein kinaza
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
HUE046402T2 (hu) * 2009-06-10 2020-03-30 Chugai Pharmaceutical Co Ltd Tetraciklusos vegyületek
UA115052C2 (uk) * 2012-03-06 2017-09-11 Сефалон, Інк. Конденсоване біциклічне 2,4-діамінопіримідинове похідне як подвійний alk- i fak-інгібітор
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
WO2016105529A1 (en) * 2014-12-23 2016-06-30 Cephalon, Inc. Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives

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

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

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