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WO2005097137A3 - Advanced quinazoline based protein kinase inhibitors - Google Patents

Advanced quinazoline based protein kinase inhibitors Download PDF

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Publication number
WO2005097137A3
WO2005097137A3 PCT/US2005/010974 US2005010974W WO2005097137A3 WO 2005097137 A3 WO2005097137 A3 WO 2005097137A3 US 2005010974 W US2005010974 W US 2005010974W WO 2005097137 A3 WO2005097137 A3 WO 2005097137A3
Authority
WO
WIPO (PCT)
Prior art keywords
protein kinase
advanced
kinase inhibitors
based protein
quinazoline based
Prior art date
Application number
PCT/US2005/010974
Other languages
French (fr)
Other versions
WO2005097137A2 (en
Inventor
Congxin Liang
Original Assignee
Scripps Research Inst
Congxin Liang
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 Scripps Research Inst, Congxin Liang filed Critical Scripps Research Inst
Publication of WO2005097137A2 publication Critical patent/WO2005097137A2/en
Publication of WO2005097137A3 publication Critical patent/WO2005097137A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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

Landscapes

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

Abstract

Hydroxy containing quinazoline based derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
PCT/US2005/010974 2004-03-31 2005-03-31 Advanced quinazoline based protein kinase inhibitors WO2005097137A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US55802504P 2004-03-31 2004-03-31
US60/558,025 2004-03-31

Publications (2)

Publication Number Publication Date
WO2005097137A2 WO2005097137A2 (en) 2005-10-20
WO2005097137A3 true WO2005097137A3 (en) 2006-02-16

Family

ID=35125608

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2005/010974 WO2005097137A2 (en) 2004-03-31 2005-03-31 Advanced quinazoline based protein kinase inhibitors
PCT/US2005/010968 WO2005097134A2 (en) 2004-03-31 2005-03-31 Quinazoline based protein kinase inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2005/010968 WO2005097134A2 (en) 2004-03-31 2005-03-31 Quinazoline based protein kinase inhibitors

Country Status (1)

Country Link
WO (2) WO2005097137A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9353122B2 (en) 2013-02-15 2016-05-31 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
US9353123B2 (en) 2013-02-20 2016-05-31 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof

Families Citing this family (32)

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Publication number Priority date Publication date Assignee Title
GB0326459D0 (en) 2003-11-13 2003-12-17 Astrazeneca Ab Quinazoline derivatives
GB0509224D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of intracellular enzymatic activity
GB0509227D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Intracellular enzyme inhibitors
EP1940825A1 (en) * 2005-09-20 2008-07-09 Astra Zeneca AB Quinazoline derivatives as anticancer agents
WO2007063291A1 (en) * 2005-12-02 2007-06-07 Astrazeneca Ab 4-anilino-substituted quinazoline derivatives as tyrosine kinase inhibitors
CN101003514A (en) * 2006-01-20 2007-07-25 上海艾力斯医药科技有限公司 Derivative of quinazoline, preparation method and usage
US7547781B2 (en) 2006-09-11 2009-06-16 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
US8604044B2 (en) * 2006-09-11 2013-12-10 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
WO2008033747A2 (en) * 2006-09-11 2008-03-20 Curis, Inc. Multi-functional small molecules as anti-proliferative agents
AU2012216752B2 (en) * 2006-09-11 2014-12-04 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
WO2008033748A2 (en) 2006-09-11 2008-03-20 Curis, Inc. Quinazoline based egfr inhibitors containing a zinc binding moiety
US7851623B2 (en) * 2006-11-02 2010-12-14 Astrazeneca Ab Chemical process
US8148532B2 (en) 2007-03-14 2012-04-03 Guoqing Paul Chen Spiro substituted compounds as angiogenesis inhibitors
JP5474792B2 (en) 2007-09-10 2014-04-16 キュリス，インコーポレイテッド Tartrate salt of a quinazoline-based EGFR inhibitor containing a zinc binding moiety or a complex thereof
US8119616B2 (en) 2007-09-10 2012-02-21 Curis, Inc. Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety
US7829574B2 (en) * 2008-05-09 2010-11-09 Hutchison Medipharma Enterprises Limited Substituted quinazoline compounds and their use in treating angiogenesis-related diseases
US8211911B2 (en) 2008-08-19 2012-07-03 Guoqing Paul Chen Compounds as kinase inhibitors
EP2496237A2 (en) 2009-11-06 2012-09-12 Chelsea Therapeutics, Inc. Enzyme inhibiting compounds
CN101857617A (en) * 2010-04-28 2010-10-13 中国海洋大学 Quinazoline sugar derivatives and their preparation methods and applications
CN102452988B (en) * 2010-10-27 2016-01-27 中国科学院化学研究所 A kind of quinazoline derivant and preparation method thereof
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
PE20152000A1 (en) 2013-03-06 2016-01-22 Astrazeneca Ab QUINAZOLINE INHIBITORS OF MUTATED FORMS ACTIVATING THE RECEPTOR OF THE EPIDERMAL GROWTH FACTOR
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
NZ719185A (en) 2013-11-01 2017-11-24 Kala Pharmaceuticals Inc Crystalline forms of therapeutic compounds and uses thereof
CN104761507B (en) * 2014-01-06 2019-11-12 广东东阳光药业有限公司 Amido quinazoline derivatives and its application in drug
CN105384745A (en) * 2015-07-27 2016-03-09 北京师范大学 Crown ether cyclic quinazoline compound, preparation method therefor and application thereof in preparing tumor therapy and imaging drug
EP3509422A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
US10392399B2 (en) 2016-09-08 2019-08-27 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
AU2017324251A1 (en) 2016-09-08 2019-03-21 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3778589B1 (en) * 2018-04-09 2022-05-11 Weishang (Shanghai) Bio-Pharmaceutical Co., Ltd. 5-substituted difluoropiperidine compound capable of passing through blood-brain barrier
CN110357858B (en) 2018-04-09 2022-02-18 威尚（上海）生物医药有限公司 5-substituted difluoropiperidine compounds having blood-brain barrier crossing capability
CN110590839B (en) * 2018-06-13 2022-04-05 四川海思科制药有限公司 Levatinib derivative and preparation method and application thereof

Citations (5)

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US5362743A (en) * 1993-03-09 1994-11-08 Pfizer Inc. Aminoquinoline derivatives
US5492915A (en) * 1990-07-24 1996-02-20 Rhone-Poulenc Rorer S.A. Substituted quinolyl compounds exhibiting selective leukotriene B4 antagonist activity
WO1996033980A1 (en) * 1995-04-27 1996-10-31 Zeneca Limited Quinazoline derivatives
US6169088B1 (en) * 1996-01-10 2001-01-02 Kyowa Hakko Kogyo Co., Ltd. 1,3 diazines with platelet-derived growth factor receptor inhibitory activity
US20020091130A1 (en) * 2000-11-01 2002-07-11 James Kanter Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5492915A (en) * 1990-07-24 1996-02-20 Rhone-Poulenc Rorer S.A. Substituted quinolyl compounds exhibiting selective leukotriene B4 antagonist activity
US5362743A (en) * 1993-03-09 1994-11-08 Pfizer Inc. Aminoquinoline derivatives
WO1996033980A1 (en) * 1995-04-27 1996-10-31 Zeneca Limited Quinazoline derivatives
US5770599A (en) * 1995-04-27 1998-06-23 Zeneca Limited Quinazoline derivatives
US6169088B1 (en) * 1996-01-10 2001-01-02 Kyowa Hakko Kogyo Co., Ltd. 1,3 diazines with platelet-derived growth factor receptor inhibitory activity
US20020091130A1 (en) * 2000-11-01 2002-07-11 James Kanter Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9353122B2 (en) 2013-02-15 2016-05-31 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
US9353123B2 (en) 2013-02-20 2016-05-31 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof

Also Published As

Publication number Publication date
WO2005097134A3 (en) 2006-01-26
WO2005097134A2 (en) 2005-10-20
WO2005097137A2 (en) 2005-10-20

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