[go: up one dir, main page]

WO2003035615A3 - Tyrosine kinase inhibitors - Google Patents

Tyrosine kinase inhibitors Download PDF

Info

Publication number
WO2003035615A3
WO2003035615A3 PCT/US2002/033920 US0233920W WO03035615A3 WO 2003035615 A3 WO2003035615 A3 WO 2003035615A3 US 0233920 W US0233920 W US 0233920W WO 03035615 A3 WO03035615 A3 WO 03035615A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
tyrosine kinase
kinase inhibitors
present
receptor
Prior art date
Application number
PCT/US2002/033920
Other languages
French (fr)
Other versions
WO2003035615A2 (en
Inventor
B Wesley Trotter
Ian M Bell
C Blair Zartman
Craig Lindsley
Zhijian Zhao
Original Assignee
Merck & Co Inc
B Wesley Trotter
Ian M Bell
C Blair Zartman
Craig Lindsley
Zhijian Zhao
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 Merck & Co Inc, B Wesley Trotter, Ian M Bell, C Blair Zartman, Craig Lindsley, Zhijian Zhao filed Critical Merck & Co Inc
Priority to AU2002348394A priority Critical patent/AU2002348394A1/en
Publication of WO2003035615A2 publication Critical patent/WO2003035615A2/en
Publication of WO2003035615A3 publication Critical patent/WO2003035615A3/en

Links

Classifications

    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a 2-carboxy pyrrole. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
PCT/US2002/033920 2001-10-25 2002-10-21 Tyrosine kinase inhibitors WO2003035615A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002348394A AU2002348394A1 (en) 2001-10-25 2002-10-21 Tyrosine kinase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34311901P 2001-10-25 2001-10-25
US60/343,119 2001-10-25

Publications (2)

Publication Number Publication Date
WO2003035615A2 WO2003035615A2 (en) 2003-05-01
WO2003035615A3 true WO2003035615A3 (en) 2004-03-18

Family

ID=23344789

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/033920 WO2003035615A2 (en) 2001-10-25 2002-10-21 Tyrosine kinase inhibitors

Country Status (2)

Country Link
AU (1) AU2002348394A1 (en)
WO (1) WO2003035615A2 (en)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004258963A1 (en) * 2003-07-24 2005-02-03 Merck & Co., Inc. Tyrosine kinase inhibitors
CN100457728C (en) * 2003-07-24 2009-02-04 麦克公司 Tyrosine kinase inhibitors
EP1747206A1 (en) 2004-04-29 2007-01-31 Abbott Laboratories Amino-tetrazoles analogues and methods of use
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
AU2005292317B2 (en) * 2004-09-30 2011-09-08 Janssen Pharmaceutica N.V. Novel benzimidazole derivatives useful as selective androgen receptor modulators (sarms)
DK1926996T3 (en) 2005-09-20 2012-01-23 Osi Pharmaceuticals Llc Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
WO2010099139A2 (en) 2009-02-25 2010-09-02 Osi Pharmaceuticals, Inc. Combination anti-cancer therapy
US20110171124A1 (en) 2009-02-26 2011-07-14 Osi Pharmaceuticals, Inc. In situ methods for monitoring the EMT status of tumor cells in vivo
WO2010099363A1 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
US8465912B2 (en) 2009-02-27 2013-06-18 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
US20100316639A1 (en) 2009-06-16 2010-12-16 Genentech, Inc. Biomarkers for igf-1r inhibitor therapy
EP2519826A2 (en) 2010-03-03 2012-11-07 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
WO2011109584A2 (en) 2010-03-03 2011-09-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
EP2544672A1 (en) 2010-03-09 2013-01-16 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
WO2012116040A1 (en) 2011-02-22 2012-08-30 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma
US9896730B2 (en) 2011-04-25 2018-02-20 OSI Pharmaceuticals, LLC Use of EMT gene signatures in cancer drug discovery, diagnostics, and treatment
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
EP2961412A4 (en) 2013-02-26 2016-11-09 Triact Therapeutics Inc Cancer therapy
SG11201601679TA (en) 2013-09-06 2016-04-28 Aurigene Discovery Tech Ltd 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives as immunomodulators
US9381246B2 (en) 2013-09-09 2016-07-05 Triact Therapeutics, Inc. Cancer therapy
US11161823B2 (en) 2019-03-11 2021-11-02 National Guard Health Affairs Anticancer 1,3-dioxane-4,6-dione derivatives and method of combinatorial synthesis thereof
WO2024101337A1 (en) * 2022-11-07 2024-05-16 国立大学法人京都大学 Quinazoline derivatives

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JACKSON ET AL.: "Pyrroles and related compounds. Part V. Syntheses of some pyrromethanes, tripyrranes and porphyrins", J. CHEM. SOC., February 1965 (1965-02-01), pages 1328 - 1337, XP002965506 *

Also Published As

Publication number Publication date
AU2002348394A1 (en) 2003-05-06
WO2003035615A2 (en) 2003-05-01

Similar Documents

Publication Publication Date Title
WO2003035615A3 (en) Tyrosine kinase inhibitors
WO2004014300A3 (en) Tyrosine kinase inhibitors
WO2004014851A3 (en) Tyrosine kinase inhibitors
WO2003035616A3 (en) Tyrosine kinase inhibitors
WO2003035614A3 (en) Tyrosine kinase inhibitors
WO2003035619A8 (en) Tyrosine kinase inhibitors
WO2002046183A3 (en) Indazolyl-substituted pyrroline compounds as kinase inhibitors
WO2001060814A3 (en) Pyrrole substituted 2-indolinone protein kinase inhibitors
AU2001241798A1 (en) 3-(pyrolyllactone)-2-indolinone compounds as kinase inhibitors
AU2002303892A1 (en) 5-aralkylsulfonyl-3- (pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors
AU2001288374A1 (en) Substituted oxindole derivatives as tyrosine kinase inhibitors
WO2001019828A3 (en) Kinase inhibitors as therapeutic agents
AU9158498A (en) Benzylidene-1,3-dihydro-indol-2-one derivatives as receptor tyrosine kinase inhibitors, particularly of raf kinases
AP1718A (en) 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
WO2004009597A3 (en) Pyrazolopyrimidines as protein kinase inhibitors
AU8760798A (en) Irreversible inhibitors of tyrosine kinases
EP0766676A4 (en) Compounds for and method of inhibiting phosphodiesterase iv
EP1247803A3 (en) Indolinone compounds suitable for modulation of protein kinases
UA74370C2 (en) Pyrrole(2,3-d)pyrimidine compounds as immunosuppressors
WO2000002576A3 (en) Egf-genistein for prevention of restenosis
AU2002231139A1 (en) Thiazolyl inhibitors of tec family tyrosine kinases
PL331221A1 (en) Heteroaromatic bicyclic compounds as inhibitors of propteinous tyrosine kinase
WO2006047479A3 (en) C-fms kinase inhibitors
WO2003076398A3 (en) Pyrrole-2, 5-dione derivatives and their use as gsk-3 inhibitors
AU5215700A (en) Substituted indolinone as tyrosine kinase inhibitors

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LU MC NL PT SE SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP