RU2015148359A - Хиназолины и азахиназолины - двойные ингибиторы путей ras/raf/mek/erk и pi3k/akt/pten/mtor - Google Patents

Хиназолины и азахиназолины - двойные ингибиторы путей ras/raf/mek/erk и pi3k/akt/pten/mtor Download PDF

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Publication number
RU2015148359A
RU2015148359A RU2015148359A RU2015148359A RU2015148359A RU 2015148359 A RU2015148359 A RU 2015148359A RU 2015148359 A RU2015148359 A RU 2015148359A RU 2015148359 A RU2015148359 A RU 2015148359A RU 2015148359 A RU2015148359 A RU 2015148359A
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Prior art keywords
sulfonamide
fluorophenyl
morpholinoquinazolin
methoxy
pyrimidin
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RU2015148359A
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English (en)
Russian (ru)
Inventor
Скотт К. Томпсон
Роджер А. СМИТ
Санджива РЕДДИ
Тайлер М. ДЖОН
Виджай Кумар НАЙАВАНАНДИ
Хосахалли СУБРАМАНЬЯ
Виджай ПОТЛУРИ
Сунил Кумар Паниграхи
Прабхакара Рао НАДИПАЛЛИ
Саумитра Сенгупта
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Асана Биосайенсис, Ллк
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Application filed by Асана Биосайенсис, Ллк filed Critical Асана Биосайенсис, Ллк
Publication of RU2015148359A publication Critical patent/RU2015148359A/ru

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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
    • G01N33/574—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

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  • 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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Cell Biology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
RU2015148359A 2013-04-12 2014-04-11 Хиназолины и азахиназолины - двойные ингибиторы путей ras/raf/mek/erk и pi3k/akt/pten/mtor RU2015148359A (ru)

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
RU2015148359A true RU2015148359A (ru) 2017-05-15

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RU2015148359A RU2015148359A (ru) 2013-04-12 2014-04-11 Хиназолины и азахиназолины - двойные ингибиторы путей ras/raf/mek/erk и pi3k/akt/pten/mtor

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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WO2017112777A1 (en) 2015-12-22 2017-06-29 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
WO2018009638A1 (en) * 2016-07-06 2018-01-11 The Regents Of The University Of Michigan MULTIFUNCTIONAL INHIBITORS OF MEK/PI3K AND mTOR/MEK/PI3K BIOLOGICAL PATHWAYS AND THERAPEUTIC METHODS USING THE SAME
CA3174865A1 (en) * 2016-12-26 2018-07-05 Institute Of Materia Medica, Chinese Academy Of Medical Sciences Quinazoline compound and preparation method, application, and pharmaceutical composition thereof
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
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
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
US11318137B2 (en) 2017-05-17 2022-05-03 Vanderbilt University Quinazoline compounds as modulators of Ras signaling
BR112019027640A2 (pt) 2017-06-21 2020-07-07 SHY Therapeutics LLC composto, método para testar a capacidade de um ou mais compostos, método para inibir a função de ras, método para inibir a função de rho, método para inibir a função de rac, composição farmacêutica
US10695296B2 (en) * 2017-07-14 2020-06-30 Asana Biosciences, Llc Formulations, methods, kit, and dosage forms for improved stability of an 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
IL294707B2 (en) 2019-11-01 2024-12-01 Fmc Corp An efficient process for synthesis of 2-amino-5-chloro-n-,3-dimethylbenzamide
CN114786777A (zh) 2019-11-04 2022-07-22 锐新医药公司 Ras抑制剂
EP4214209A1 (en) 2020-09-15 2023-07-26 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
US11912668B2 (en) * 2020-11-18 2024-02-27 Deciphera Pharmaceuticals, Llc GCN2 and perk kinase inhibitors and methods of use thereof
EP4334325A1 (en) 2021-05-05 2024-03-13 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
CN118488947A (zh) * 2022-01-04 2024-08-13 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
MX2008013583A (es) * 2006-04-26 2008-10-31 Genentech Inc Compuestos del inhibidor de fosfoinositido 3-cinasa y composiciones farmaceuticas que los contienen.
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US9499495B2 (en) 2016-11-22
US10226468B2 (en) 2019-03-12
AU2014250836A1 (en) 2015-11-26
AU2014250836B2 (en) 2018-07-12
BR112015025901A2 (pt) 2017-07-25
MX2015014387A (es) 2017-04-10
US20190151327A1 (en) 2019-05-23
AU2014250836C1 (en) 2019-01-17
CN105283454B (zh) 2019-10-29
CN105283454A (zh) 2016-01-27
IL242020B (en) 2019-08-29
WO2014169167A1 (en) 2014-10-16
CA2909310A1 (en) 2014-10-16
JP6496301B2 (ja) 2019-04-03
EP2984088A1 (en) 2016-02-17
US20210113578A1 (en) 2021-04-22
EP2984088B1 (en) 2019-03-20
US20160068496A1 (en) 2016-03-10
JP2016519685A (ja) 2016-07-07
KR20150143672A (ko) 2015-12-23
ZA201507750B (en) 2017-08-30
US20170290838A1 (en) 2017-10-12
US9757382B2 (en) 2017-09-12
HK1215810A1 (en) 2016-09-15
US20170027953A1 (en) 2017-02-02
BR112015025901A8 (pt) 2020-01-14
US10912779B2 (en) 2021-02-09
IL262314A (en) 2018-11-29

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