CA2909310A1 - Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways - Google Patents

Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways

Info

Publication number
CA2909310A1
CA2909310A1 CA2909310A CA2909310A CA2909310A1 CA 2909310 A1 CA2909310 A1 CA 2909310A1 CA 2909310 A CA2909310 A CA 2909310A CA 2909310 A CA2909310 A CA 2909310A CA 2909310 A1 CA2909310 A1 CA 2909310A1
Authority
CA
Canada
Prior art keywords
sulfonamide
fluoropropane
fluorophenyl
morpholinoquinazolin
methoxy
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2909310A
Other languages
English (en)
French (fr)
Inventor
Scott K. Thompson
Roger A. Smith
Sanjeeva Reddy
Tyler M. John
Vijay Kumar Nyavanandi
Hosahalli Subramanya
Vijay Potluri
Sunil Kumar Panigrahi
Prabhakara Rao Nadipalli
Saumitra Sengupta
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Asana Biosciences LLC
Original Assignee
Asana Biosciences 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 Asana Biosciences LLC filed Critical Asana Biosciences LLC
Publication of CA2909310A1 publication Critical patent/CA2909310A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D401/04—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
    • 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
    • C07D403/04—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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • 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
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57484—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, metabolites
    • G01N33/57496—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, metabolites involving intracellular compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Cell Biology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Toxicology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2909310A 2013-04-12 2014-04-11 Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways Abandoned CA2909310A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361811408P 2013-04-12 2013-04-12
US61/811,408 2013-04-12
PCT/US2014/033727 WO2014169167A1 (en) 2013-04-12 2014-04-11 Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways

Publications (1)

Publication Number Publication Date
CA2909310A1 true CA2909310A1 (en) 2014-10-16

Family

ID=50771612

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2909310A Abandoned CA2909310A1 (en) 2013-04-12 2014-04-11 Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways

Country Status (13)

Country Link
US (5) US9499495B2 (OSRAM)
EP (1) EP2984088B1 (OSRAM)
JP (1) JP6496301B2 (OSRAM)
KR (1) KR20150143672A (OSRAM)
CN (1) CN105283454B (OSRAM)
AU (1) AU2014250836C1 (OSRAM)
BR (1) BR112015025901A8 (OSRAM)
CA (1) CA2909310A1 (OSRAM)
IL (2) IL242020B (OSRAM)
MX (1) MX2015014387A (OSRAM)
RU (1) RU2015148359A (OSRAM)
WO (1) WO2014169167A1 (OSRAM)
ZA (1) ZA201507750B (OSRAM)

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US10221191B2 (en) 2015-12-22 2019-03-05 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
EP4086250B1 (en) * 2016-07-06 2024-12-11 The Regents Of The University Of Michigan Multifunctional inhibitors of mek/pi3k and mtor/mek/pi3k biological pathways and therapeutic methods using the same
EP3560921B1 (en) * 2016-12-26 2024-08-14 Institute Of Materia Medica, Chinese Academy Of Medical Sciences Quinazoline compound, preparation method, application as pi3k inhibitor for the treatment of cancer, and pharmaceutical compostion thereof
CN108239074B (zh) * 2016-12-26 2021-07-06 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
CN108239076B (zh) * 2016-12-26 2021-07-06 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
CN108239075B (zh) * 2016-12-26 2021-07-02 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
WO2018212774A1 (en) * 2017-05-17 2018-11-22 Vanderbilt University Quinazoline compounds as modulators of ras signaling
SG11201911929XA (en) 2017-06-21 2020-01-30 SHY Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
WO2019014668A1 (en) * 2017-07-14 2019-01-17 Asana Biosciences, Llc FORMULATIONS, METHODS, KIT AND DOSAGE FORMS FOR ENHANCED STABILITY OF ACTIVE PHARMACEUTICAL INGREDIENT
CN108623582A (zh) * 2017-10-10 2018-10-09 河南省锐达医药科技有限公司 一类新型含取代基吡啶并嘧啶化合物的制备方法
WO2020132071A1 (en) 2018-12-19 2020-06-25 Shy Therapeutics. Llc Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and f1brotic disease
CN111499634B (zh) * 2019-01-31 2023-05-12 贝达药业股份有限公司 一种喹唑啉化合物及其在医药上的应用
CN112341434B (zh) * 2019-08-08 2021-11-26 恩瑞生物医药科技（上海）有限公司 PI3K/mTOR蛋白降解靶向嵌合体类化合物及其制备方法和医药用途
BR112022008061A2 (pt) 2019-11-01 2022-07-12 Fmc Corp Processo eficaz para síntese de 2-amino-5-cloro-n,3-dimetilbenzamida
CA3159561A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
IL301298A (en) 2020-09-15 2023-05-01 Revolution Medicines Inc Indole derivatives as RAS inhibitors in cancer therapy
JP2023549540A (ja) * 2020-11-18 2023-11-27 デシフェラ・ファーマシューティカルズ，エルエルシー Ｇｃｎ２およびｐｅｒｋキナーゼ阻害剤およびその使用方法
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
CN113416181B (zh) * 2021-08-02 2022-05-03 四川大学 喹唑啉类衍生物及其用途
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023131122A1 (zh) * 2022-01-04 2023-07-13 劲方医药科技(上海)有限公司 稠环取代的六元杂环化合物及其制法和用途
CN115894211A (zh) * 2022-11-10 2023-04-04 山东龙立恒医药有限公司 一种3-羟基-4-甲基苯甲酸的制备方法

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GB0428475D0 (en) 2004-12-30 2005-02-02 4 Aza Bioscience Nv Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
GB0503506D0 (en) 2005-02-21 2005-03-30 4 Aza Bioscience Nv Substituted pyrido(2,3-d) pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
KR101402474B1 (ko) 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
UY31137A1 (es) * 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
EP2217590A4 (en) * 2007-09-17 2011-12-14 Glaxosmithkline Llc Pyridopyrimidine derivatives as PI3-kinase inhibitors
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WO2010037765A2 (en) * 2008-10-03 2010-04-08 Merck Serono S.A. 4-morpholino-pyrido[3,2-d]pyrimidines
US9181238B2 (en) * 2010-02-05 2015-11-10 Novartis Ag N-(pyridin-2-yl)sulfonamides and compositions thereof as protein kinase inhibitors
MX2012009059A (es) 2010-02-22 2012-09-07 Hoffmann La Roche Compuestos inhibidores de fosfoinositida 3-cinasa delta (pi3k) pirido [3,2-d]pirimidina y metodos de uso.
WO2012118492A1 (en) * 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors

Also Published As

Publication number Publication date
JP6496301B2 (ja) 2019-04-03
EP2984088B1 (en) 2019-03-20
AU2014250836C1 (en) 2019-01-17
IL262314A (en) 2018-11-29
BR112015025901A8 (pt) 2020-01-14
US20210113578A1 (en) 2021-04-22
CN105283454A (zh) 2016-01-27
US20170027953A1 (en) 2017-02-02
BR112015025901A2 (pt) 2017-07-25
AU2014250836B2 (en) 2018-07-12
ZA201507750B (en) 2017-08-30
WO2014169167A1 (en) 2014-10-16
US10912779B2 (en) 2021-02-09
EP2984088A1 (en) 2016-02-17
AU2014250836A1 (en) 2015-11-26
US20170290838A1 (en) 2017-10-12
MX2015014387A (es) 2017-04-10
US20160068496A1 (en) 2016-03-10
KR20150143672A (ko) 2015-12-23
RU2015148359A (ru) 2017-05-15
US9757382B2 (en) 2017-09-12
IL242020B (en) 2019-08-29
CN105283454B (zh) 2019-10-29
US9499495B2 (en) 2016-11-22
HK1215810A1 (en) 2016-09-15
US20190151327A1 (en) 2019-05-23
JP2016519685A (ja) 2016-07-07
US10226468B2 (en) 2019-03-12

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Effective date: 20151009

FZDE Discontinued

Effective date: 20210831