WO2014160177A3 - Quinazoline inhibitors of pi3k - Google Patents

Quinazoline inhibitors of pi3k Download PDF

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Publication number
WO2014160177A3
WO2014160177A3 PCT/US2014/025980 US2014025980W WO2014160177A3 WO 2014160177 A3 WO2014160177 A3 WO 2014160177A3 US 2014025980 W US2014025980 W US 2014025980W WO 2014160177 A3 WO2014160177 A3 WO 2014160177A3
Authority
WO
WIPO (PCT)
Prior art keywords
pi3k
quinazoline inhibitors
quinazoline
inhibitors
compounds
Prior art date
Application number
PCT/US2014/025980
Other languages
French (fr)
Other versions
WO2014160177A2 (en
Inventor
Kenneth D. Rice
Paul Foster
Original Assignee
Exelixis, Inc.
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 Exelixis, Inc. filed Critical Exelixis, Inc.
Publication of WO2014160177A2 publication Critical patent/WO2014160177A2/en
Publication of WO2014160177A3 publication Critical patent/WO2014160177A3/en

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/04—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 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
    • C07D403/04—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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

Abstract

The invention is directed to compounds of formula (I): and pharmaceutically acceptable salts as well as methods of making and using the compounds to inhibit PI3K.
PCT/US2014/025980 2013-03-13 2014-03-13 Quinazoline inhibitors of pi3k WO2014160177A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361779679P 2013-03-13 2013-03-13
US61/779,679 2013-03-13

Publications (2)

Publication Number Publication Date
WO2014160177A2 WO2014160177A2 (en) 2014-10-02
WO2014160177A3 true WO2014160177A3 (en) 2015-05-14

Family

ID=50625117

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2014/025980 WO2014160177A2 (en) 2013-03-13 2014-03-13 Quinazoline inhibitors of pi3k

Country Status (1)

Country Link
WO (1) WO2014160177A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111315723A (en) * 2017-08-31 2020-06-19 艾伯维公司 Extramembranous nucleotide pyrophosphatase-phosphodiesterase 1(ENPP-1) inhibitor and application thereof
TW202128686A (en) * 2019-10-25 2021-08-01 大陸商江蘇恆瑞醫藥股份有限公司 A fused heteroaryl derivative, a preparation method and medical use thereof
WO2023045960A1 (en) * 2021-09-22 2023-03-30 四川汇宇制药股份有限公司 Pyridine derivative and use thereof
WO2023165581A1 (en) * 2022-03-03 2023-09-07 四川汇宇制药股份有限公司 Pyridine derivative and use thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2585909A (en) * 1948-11-05 1952-02-19 Muriel Ruth Curd Quaternary salts of pyrimidylaminoquinolines
WO2008009078A2 (en) * 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
WO2010151737A2 (en) * 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
WO2011022439A1 (en) * 2009-08-17 2011-02-24 Intellikine, Inc. Heterocyclic compounds and uses thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4107288A (en) 1974-09-18 1978-08-15 Pharmaceutical Society Of Victoria Injectable compositions, nanoparticles useful therein, and process of manufacturing same
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2585909A (en) * 1948-11-05 1952-02-19 Muriel Ruth Curd Quaternary salts of pyrimidylaminoquinolines
WO2008009078A2 (en) * 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
WO2010151737A2 (en) * 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
WO2011022439A1 (en) * 2009-08-17 2011-02-24 Intellikine, Inc. Heterocyclic compounds and uses thereof

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
ANDREAS SCHMIDT ET AL: "Functionalized 4-Aminoquinolines by Rearrangement of Pyrazole N-Heterocyclic Carbenes", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, vol. 49, no. 15, 12 March 2010 (2010-03-12), pages 2790 - 2793, XP055119383, ISSN: 1433-7851, DOI: 10.1002/anie.200905436 *
ANDREW S ROSENTHAL ET AL: "Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk)", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 21, no. 10, 28 February 2011 (2011-02-28), pages 3152 - 3158, XP028208799, ISSN: 0960-894X, [retrieved on 20110304], DOI: 10.1016/J.BMCL.2011.02.114 *
DAVIS S E ET AL: "2,4-DIAMINO-5-BENZYLPYRIMIDINES AND ANALOGUES AS ANTIBACTERIAL AGENTS. 11. QUINOLYLMETHYL ANALOGUES WITH BASIC SUBSTITUENTS CONVEYING SPECIFICITY", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 32, 1 January 1989 (1989-01-01), pages 1936 - 1942, XP002273433, ISSN: 0022-2623, DOI: 10.1021/JM00128A041 *
GEMMA ET AL: "Microwave-assisted synthesis of 4-quinolylhydrazines followed by nickel boride reduction: a convenient approach to 4-aminoquinolines and derivatives", TETRAHEDRON LETTERS, PERGAMON, GB, vol. 49, no. 13, 2 February 2008 (2008-02-02), pages 2074 - 2077, XP022502902, ISSN: 0040-4039, DOI: 10.1016/J.TETLET.2008.01.128 *
SIVARAMAKRISHNAN K P ET AL: "Biquinoline Series: Part III - Synthesis of Substituted 6,6'-Biuinolines", JOURNAL OF SCIENTIFIC AND INDUSTRIAL RESEARCH. SERIE B: PHYSICALSCIENCES, COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH, NEW DEHLI, IN, vol. 20, 1 January 1961 (1961-01-01), pages 223 - 227, XP009178121, ISSN: 0368-4210 *
TOBE M ET AL: "A novel structural class of potent inhibitors of NF-kappaB activation: structure-activity relationship and biological effects of 6-aminoquinazoline derivatives", BIOORGANIC & MEDICINAL CHEMISTRY, PERGAMON, GB, vol. 11, no. 18, 1 January 2003 (2003-01-01), pages 3869 - 3878, XP003024664, ISSN: 0968-0896, DOI: 10.1016/S0968-0896(03)00438-3 *
YVONNICK LOIDREAU ET AL: "Microwave-assisted thermal decomposition of formamide: a tool for coupling a pyrimidine ring with an aromatic partner", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 67, no. 26, 3 May 2011 (2011-05-03), pages 4852 - 4857, XP028227650, ISSN: 0040-4020, [retrieved on 20110517], DOI: 10.1016/J.TET.2011.05.010 *

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