IL242020B - 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
IL242020B
IL242020B IL242020A IL24202015A IL242020B IL 242020 B IL242020 B IL 242020B IL 242020 A IL242020 A IL 242020A IL 24202015 A IL24202015 A IL 24202015A IL 242020 B IL242020 B IL 242020B
Authority
IL
Israel
Prior art keywords
quinzolines
azaquinzolines
pten
erk
suppressors
Prior art date
Application number
IL242020A
Other languages
English (en)
Hebrew (he)
Inventor
Sengupta Saumitra
K Thompson Scott
A Smith Roger
Reddy Sanjeeva
M John Tyler
Kumar NYAVANANDI Vijay
Subramanya Hosahalli
Potluri Vijay
Kumar Panigrahi Sunil
Rao Nadipalli Prabhakara
Original Assignee
Sengupta Saumitra
Asana Biosciences Llc
K Thompson Scott
A Smith Roger
Reddy Sanjeeva
M John Tyler
Kumar NYAVANANDI Vijay
Subramanya Hosahalli
Potluri Vijay
Kumar Panigrahi Sunil
Rao Nadipalli Prabhakara
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 Sengupta Saumitra, Asana Biosciences Llc, K Thompson Scott, A Smith Roger, Reddy Sanjeeva, M John Tyler, Kumar NYAVANANDI Vijay, Subramanya Hosahalli, Potluri Vijay, Kumar Panigrahi Sunil, Rao Nadipalli Prabhakara filed Critical Sengupta Saumitra
Publication of IL242020B publication Critical patent/IL242020B/en

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    • 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
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
    • G01N33/57595—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites involving intracellular compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • Microbiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Toxicology (AREA)
  • Oncology (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)
  • Dermatology (AREA)
IL242020A 2013-04-12 2015-10-11 Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways IL242020B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361811408P 2013-04-12 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
IL242020B true IL242020B (en) 2019-08-29

Family

ID=50771612

Family Applications (2)

Application Number Title Priority Date Filing Date
IL242020A IL242020B (en) 2013-04-12 2015-10-11 Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways
IL262314A IL262314A (en) 2013-04-12 2018-10-11 Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL262314A IL262314A (en) 2013-04-12 2018-10-11 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 (enExample)
EP (1) EP2984088B1 (enExample)
JP (1) JP6496301B2 (enExample)
KR (1) KR20150143672A (enExample)
CN (1) CN105283454B (enExample)
AU (1) AU2014250836C1 (enExample)
BR (1) BR112015025901A8 (enExample)
CA (1) CA2909310A1 (enExample)
IL (2) IL242020B (enExample)
MX (1) MX2015014387A (enExample)
RU (1) RU2015148359A (enExample)
WO (1) WO2014169167A1 (enExample)
ZA (1) ZA201507750B (enExample)

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* Cited by examiner, † Cited by third party
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EP3394056B1 (en) 2015-12-22 2021-04-14 Shy Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
ES3002745T3 (en) * 2016-07-06 2025-03-07 Univ Michigan Regents Multifunctional inhibitors of mek/pi3k and mtor/mek/pi3k biological pathways and therapeutic methods using the same
EP4169918B8 (en) 2016-12-26 2025-09-24 Institute of Materia Medica, Chinese Academy of Medical Sciences Quinazoline derivatives as inhibitors of pi3k for the treatment of cancer
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
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
WO2018212774A1 (en) * 2017-05-17 2018-11-22 Vanderbilt University Quinazoline compounds as modulators of ras signaling
CA3066939A1 (en) * 2017-06-21 2018-12-27 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
US12391705B2 (en) 2018-12-19 2025-08-19 Shy Therapeutics, Llc Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic 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
HUE067805T2 (hu) 2019-11-01 2024-11-28 Fmc Corp Hatékony új eljárás 2-amino-5-klór-N,3-dimetilbenzamid elõállítására
EP4054719B1 (en) 2019-11-04 2026-02-11 Revolution Medicines, Inc. Ras inhibitors
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
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
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
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
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Also Published As

Publication number Publication date
IL262314A (en) 2018-11-29
JP6496301B2 (ja) 2019-04-03
CA2909310A1 (en) 2014-10-16
BR112015025901A8 (pt) 2020-01-14
CN105283454A (zh) 2016-01-27
HK1215810A1 (en) 2016-09-15
BR112015025901A2 (pt) 2017-07-25
US20190151327A1 (en) 2019-05-23
MX2015014387A (es) 2017-04-10
US20160068496A1 (en) 2016-03-10
JP2016519685A (ja) 2016-07-07
US10226468B2 (en) 2019-03-12
US20210113578A1 (en) 2021-04-22
KR20150143672A (ko) 2015-12-23
EP2984088A1 (en) 2016-02-17
WO2014169167A1 (en) 2014-10-16
US9757382B2 (en) 2017-09-12
EP2984088B1 (en) 2019-03-20
AU2014250836A1 (en) 2015-11-26
US9499495B2 (en) 2016-11-22
US20170290838A1 (en) 2017-10-12
RU2015148359A (ru) 2017-05-15
US10912779B2 (en) 2021-02-09
AU2014250836B2 (en) 2018-07-12
ZA201507750B (en) 2017-08-30
CN105283454B (zh) 2019-10-29
US20170027953A1 (en) 2017-02-02
AU2014250836C1 (en) 2019-01-17

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