WO2009158431A3 - Pyrimidine derivatives as kinase inhibitors - Google Patents

Pyrimidine derivatives as kinase inhibitors Download PDF

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Publication number
WO2009158431A3
WO2009158431A3 PCT/US2009/048509 US2009048509W WO2009158431A3 WO 2009158431 A3 WO2009158431 A3 WO 2009158431A3 US 2009048509 W US2009048509 W US 2009048509W WO 2009158431 A3 WO2009158431 A3 WO 2009158431A3
Authority
WO
WIPO (PCT)
Prior art keywords
pyrimidine derivatives
kinase inhibitors
analplastic
igf
alk
Prior art date
Application number
PCT/US2009/048509
Other languages
French (fr)
Other versions
WO2009158431A2 (en
Inventor
Thomas H. Marsilje, Iii
Wenshuo Lu
Bei Chen
Xiaohui He
Songchun Jiang
Kunyong Yang
Original Assignee
Irm Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Irm Llc filed Critical Irm Llc
Priority to MX2010014568A priority Critical patent/MX2010014568A/en
Priority to EA201100078A priority patent/EA201100078A1/en
Priority to EP09770964A priority patent/EP2331526A2/en
Priority to JP2011516619A priority patent/JP2011526291A/en
Priority to CA2729546A priority patent/CA2729546A1/en
Priority to US13/000,999 priority patent/US8445505B2/en
Priority to CN200980129584XA priority patent/CN102203083A/en
Priority to AU2009262198A priority patent/AU2009262198B2/en
Publication of WO2009158431A2 publication Critical patent/WO2009158431A2/en
Publication of WO2009158431A3 publication Critical patent/WO2009158431A3/en

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    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

The invention" provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin- like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).
PCT/US2009/048509 2008-06-25 2009-06-24 Compounds and compositions as kinase inhibitors WO2009158431A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
MX2010014568A MX2010014568A (en) 2008-06-25 2009-06-24 Pyrimidine derivatives as kinase inhibitors.
EA201100078A EA201100078A1 (en) 2008-06-25 2009-06-24 DERIVATIVES OF PYRIMIDINE AS KINASE INHIBITORS
EP09770964A EP2331526A2 (en) 2008-06-25 2009-06-24 Pyrimidine derivatives as kinase inhibitors
JP2011516619A JP2011526291A (en) 2008-06-25 2009-06-24 Pyrimidine derivatives as kinase inhibitors
CA2729546A CA2729546A1 (en) 2008-06-25 2009-06-24 Compounds and compositions as kinase inhibitors
US13/000,999 US8445505B2 (en) 2008-06-25 2009-06-24 Pyrimidine derivatives as kinase inhibitors
CN200980129584XA CN102203083A (en) 2008-06-25 2009-06-24 Compounds and compositions as kinase inhibitors
AU2009262198A AU2009262198B2 (en) 2008-06-25 2009-06-24 Pyrimidine derivatives as kinase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US7558308P 2008-06-25 2008-06-25
US61/075,583 2008-06-25

Publications (2)

Publication Number Publication Date
WO2009158431A2 WO2009158431A2 (en) 2009-12-30
WO2009158431A3 true WO2009158431A3 (en) 2010-03-11

Family

ID=41076758

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/048509 WO2009158431A2 (en) 2008-06-25 2009-06-24 Compounds and compositions as kinase inhibitors

Country Status (11)

Country Link
EP (1) EP2331526A2 (en)
JP (1) JP2011526291A (en)
KR (1) KR20110020940A (en)
CN (1) CN102203083A (en)
AU (1) AU2009262198B2 (en)
BR (1) BRPI0914545A2 (en)
CA (1) CA2729546A1 (en)
EA (1) EA201100078A1 (en)
MX (1) MX2010014568A (en)
UA (1) UA101057C2 (en)
WO (1) WO2009158431A2 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
WO2011018517A1 (en) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
US20130005733A1 (en) 2010-03-09 2013-01-03 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
US8987307B2 (en) 2011-03-03 2015-03-24 Hoffmann-La Roche Inc. 3-amino-pyridines as GPBAR1 agonists
KR102012057B1 (en) * 2011-11-29 2019-08-19 제넨테크, 인크. Aminopyrimidine derivatives as lrrk2 modulators
AU2013344049B2 (en) 2012-11-06 2017-12-21 Fochon Pharmaceuticals, Ltd. ALK kinase inhibitors
EP2970205B1 (en) * 2013-03-14 2019-05-08 Tolero Pharmaceuticals, Inc. Jak2 and alk2 inhibitors and methods for their use
EP3150592B1 (en) * 2014-05-30 2023-08-30 Shanghai Emerald Wellcares Pharmaceutical Co., LTD Alk kinase inhibitor, and preparation method and use thereof
US10377743B2 (en) * 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
CN107488148A (en) * 2017-06-26 2017-12-19 安徽省黄淮兽药有限公司 A kind of hydrocinnamamide insecticides and preparation method thereof
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
TW202045008A (en) * 2019-02-01 2020-12-16 印度商皮埃企業有限公司 4-substituted isoxazole/isoxazoline (hetero) arylamidine compounds, preparation and use thereof

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001064655A1 (en) * 2000-03-01 2001-09-07 Astrazeneca Ab 2, 4-di(hetero-)arylamino (-oxy)-5-substituted pyrimidines as antineoplastic agents
WO2003026666A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4- (5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, as src kinase inhibitors
WO2005016893A2 (en) * 2003-07-30 2005-02-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
WO2005026130A1 (en) * 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
WO2005026158A1 (en) * 2003-09-16 2005-03-24 Novartis Ag 2,4 di (hetero) -arylamino-pyrimidine derivatives as zap-70 and/or syk inhibitors
WO2006074057A2 (en) * 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
WO2007027238A2 (en) * 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
WO2008005538A2 (en) * 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
US20080176881A1 (en) * 2006-12-08 2008-07-24 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
WO2009103652A1 (en) * 2008-02-22 2009-08-27 F. Hoffmann-La Roche Ag Modulators for amyloid beta

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2365223T3 (en) * 2003-08-07 2011-09-26 Rigel Pharmaceuticals, Inc. 2,4-PYRIMIDINDIAMINE COMPOUNDS AND USES AS ANTIPROLIFERATIVE AGENTS.
CA2671744C (en) * 2006-12-08 2012-08-28 Irm Llc Compounds and compositions as protein kinase inhibitors

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001064655A1 (en) * 2000-03-01 2001-09-07 Astrazeneca Ab 2, 4-di(hetero-)arylamino (-oxy)-5-substituted pyrimidines as antineoplastic agents
WO2003026666A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4- (5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, as src kinase inhibitors
WO2003026664A1 (en) * 2001-09-26 2003-04-03 Bayer Corporation 2-phenylamino-4- (5-pyrazolylamino) -pyramidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
WO2005016893A2 (en) * 2003-07-30 2005-02-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
WO2005026158A1 (en) * 2003-09-16 2005-03-24 Novartis Ag 2,4 di (hetero) -arylamino-pyrimidine derivatives as zap-70 and/or syk inhibitors
WO2005026130A1 (en) * 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
WO2006074057A2 (en) * 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
WO2007027238A2 (en) * 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
WO2008005538A2 (en) * 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
US20080176881A1 (en) * 2006-12-08 2008-07-24 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
WO2009103652A1 (en) * 2008-02-22 2009-08-27 F. Hoffmann-La Roche Ag Modulators for amyloid beta

Also Published As

Publication number Publication date
CA2729546A1 (en) 2009-12-30
JP2011526291A (en) 2011-10-06
MX2010014568A (en) 2011-03-29
WO2009158431A2 (en) 2009-12-30
EP2331526A2 (en) 2011-06-15
CN102203083A (en) 2011-09-28
KR20110020940A (en) 2011-03-03
AU2009262198A1 (en) 2009-12-30
BRPI0914545A2 (en) 2017-05-23
UA101057C2 (en) 2013-02-25
AU2009262198B2 (en) 2012-09-27
EA201100078A1 (en) 2011-08-30

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