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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    • 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)
  • 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)
  • 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

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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) ES2681487T3 (enExample)
HR (1) HRP20160387T1 (enExample)
HU (1) HUE027976T2 (enExample)
IL (2) IL234239A (enExample)
ME (1) ME02460B (enExample)
MX (2) MX372740B (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

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CA2946538A1 (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
HK1244789B (en) * 2014-12-23 2019-12-06 Cephalon, Inc. Methods for preparing fused bicyclic 2, 4-diaminopyrimidine derivatives
BR112021002145A2 (pt) 2018-08-07 2021-12-14 In3Bio Ltd Métodos e composições para inibição da via egf/egfr em combinação com inibidores da quinase de 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
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
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors

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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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CA2532800C (en) 2003-07-23 2013-06-18 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
BR122019017579B8 (pt) 2003-08-15 2021-07-27 Novartis Ag 2,4-pirimidinadiaminas, seus usos, combinação e composição farmacêutica
CA2559866A1 (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
KR101364277B1 (ko) * 2006-12-08 2014-02-21 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물
DK2146779T3 (en) * 2007-04-18 2016-11-28 Pfizer Prod Inc Sulfonylamid derivatives to treat abnormal cell growth.
PL2975024T3 (pl) * 2009-06-10 2018-09-28 Chugai Seiyaku Kabushiki Kaisha Związki tetracykliczne
PL2822939T3 (pl) * 2012-03-06 2016-08-31 Cephalon Inc Skondensowane bicykliczne pochodne 2,4-diaminopirymidyny jako podwójne inhibitory ALK i FAK
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 (2)

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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

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

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