AU2012311458B2 - Morpholino substituted urea or carbamate derivatives as mTOR inhibitors - Google Patents

Morpholino substituted urea or carbamate derivatives as mTOR inhibitors Download PDF

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Publication number
AU2012311458B2
AU2012311458B2 AU2012311458A AU2012311458A AU2012311458B2 AU 2012311458 B2 AU2012311458 B2 AU 2012311458B2 AU 2012311458 A AU2012311458 A AU 2012311458A AU 2012311458 A AU2012311458 A AU 2012311458A AU 2012311458 B2 AU2012311458 B2 AU 2012311458B2
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phenyl
alkyl
triazin
compound
different
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AU2012311458A
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AU2012311458A1 (en
Inventor
Rita Adrego
Andrew David Cansfield
Laura CONVERY
Daniel Paul HARDY
Rosemary Lynch
Adeline Morel
Mihiro Sunose
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Cellzome Ltd
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Cellzome Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/22—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring carbon 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2012311458A 2011-09-21 2012-09-21 Morpholino substituted urea or carbamate derivatives as mTOR inhibitors Ceased AU2012311458B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11182221 2011-09-21
EP11182221.9 2011-09-21
PCT/EP2012/068590 WO2013041652A1 (en) 2011-09-21 2012-09-21 Morpholino substituted urea or carbamate derivatives as mtor inhibitors

Publications (2)

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AU2012311458A1 AU2012311458A1 (en) 2014-04-10
AU2012311458B2 true AU2012311458B2 (en) 2016-02-04

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AU2012311458A Ceased AU2012311458B2 (en) 2011-09-21 2012-09-21 Morpholino substituted urea or carbamate derivatives as mTOR inhibitors

Country Status (11)

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US (1) US9175011B2 (enExample)
EP (1) EP2758379B1 (enExample)
JP (1) JP5995975B2 (enExample)
KR (1) KR20140070616A (enExample)
CN (1) CN103917530B (enExample)
AU (1) AU2012311458B2 (enExample)
BR (1) BR112014006743A8 (enExample)
CA (1) CA2849189A1 (enExample)
ES (1) ES2609606T3 (enExample)
RU (1) RU2616619C2 (enExample)
WO (1) WO2013041652A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2542536B1 (en) 2010-03-04 2015-01-21 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors
MX341577B (es) 2011-10-07 2016-08-25 Cellzome Ltd Derivados biciclicos de pirimidin-urea o carbamato sustituidos con morfolino como inhibidores del blanco de rapamicina de mamifero.
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
CN109715163B (zh) 2016-09-19 2022-11-22 诺华股份有限公司 包含raf抑制剂和erk抑制剂的治疗组合
WO2018203219A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
AU2019338207B2 (en) 2018-09-10 2025-01-02 Mirati Therapeutics, Inc. Combination therapies
EP4563150A3 (en) 2019-05-13 2025-07-23 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer
US12576069B2 (en) 2019-09-11 2026-03-17 Yale University Compositions and methods for treating slow-flow vascular malformations
CN115109049B (zh) * 2022-08-12 2023-08-15 江西科技师范大学 含芳基脲结构的三嗪类化合物及其应用
GB202415232D0 (en) 2024-10-16 2024-11-27 Nacamed As Composition
WO2026092678A1 (zh) * 2024-11-01 2026-05-07 上海翰森生物医药科技有限公司 芳香胺类衍生物抑制剂、其制备方法和应用

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011107585A1 (en) * 2010-03-04 2011-09-09 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2284200T3 (es) 1997-02-12 2007-11-01 Electrophoretics Limited Marcadores proteicos para cancer de pulmon y uso de los mismos.
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
ATE401312T1 (de) 1997-12-15 2008-08-15 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
EE05345B1 (et) 1999-02-10 2010-10-15 Astrazeneca Ab Kinasoliini derivaadid angiogeneesi inhibiitoritena
PT1244647E (pt) 1999-11-05 2006-10-31 Astrazeneca Ab Derivados de quinazolina como inibidores de vegf
HRP20020751B1 (hr) 2000-02-15 2011-01-31 Sugen Pirolom supstituirani 2-indolinoni kao inhibitori protein kinaze
US7135298B2 (en) 2003-03-26 2006-11-14 The Burnham Institute For Medical Research Screening assay for agents that alter target of Rapamycin activity
JP2008540391A (ja) 2005-05-05 2008-11-20 アストラゼネカ アクチボラグ ピラゾリルアミノ置換ピリミジン、および癌の処置におけるそれらの使用
PL1891446T3 (pl) 2005-06-14 2013-08-30 Cellzome Gmbh Sposób identyfikacji nowych związków oddziałujących z enzymami
GB0616747D0 (en) * 2006-08-24 2006-10-04 Astrazeneca Ab Novel compounds
ES2317382T3 (es) 2006-08-03 2009-04-16 Cellzome Ag Metodos para la identificacion de moleculas que interactuan con p13k y para la purificacion p13k.
WO2008023159A1 (en) 2006-08-24 2008-02-28 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
US20080233127A1 (en) 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
US8012986B2 (en) * 2007-04-02 2011-09-06 Hoffmann-La Roche Inc. Pyridine and pyrimidine derivatives as MGLUR2 antagonists
DK2146779T3 (en) 2007-04-18 2016-11-28 Pfizer Prod Inc Sulfonylamid derivatives to treat abnormal cell growth.
WO2009008992A2 (en) 2007-07-06 2009-01-15 Osi Pharmaceuticals Inc. Combination anti-cancer therapy comprising an inhibitor of both mtorc1 and mt0rc2
JP2010533159A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物９４７
JP2010533158A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物類−９４５
JP2010533161A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物−９４６
WO2009007750A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k
CN101224207A (zh) 2007-10-12 2008-07-23 中国科学院上海有机化学研究所 具有诱导自吞噬治疗错误折叠蛋白聚集所致疾病的药物及其筛选方法
WO2009093981A1 (en) * 2008-01-23 2009-07-30 S Bio Pte Ltd Triazine compounds as kinase inhibitors
EP2410062A1 (en) 2008-02-04 2012-01-25 Cellzome Ag Selectivity profiling of PI3K interacting molecules against multiple targets
MY155653A (en) * 2008-05-23 2015-11-13 Wyeth Llc Triazine compounds as p13 kinase and mtor inhibitors
US8163763B2 (en) 2008-07-31 2012-04-24 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
WO2010096619A1 (en) 2009-02-23 2010-08-26 Wyeth Llc Process, purification and crystallization of 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea
WO2010103094A1 (en) 2009-03-13 2010-09-16 Cellzome Limited PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2010120994A2 (en) 2009-04-17 2010-10-21 Wyeth Llc Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis
ES2439793T3 (es) 2009-04-17 2014-01-24 Wyeth Llc Compuestos de pirimidina, su uso como inhibidores de la mTOR quinasa y de la PI3 quinasa, y su síntesis
WO2011011716A1 (en) 2009-07-23 2011-01-27 The Trustees Of Princeton University Inhibitors of mtor kinase as anti-viral agents
US20140163023A1 (en) 2011-04-04 2014-06-12 Cellzome Limited Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
MX341577B (es) 2011-10-07 2016-08-25 Cellzome Ltd Derivados biciclicos de pirimidin-urea o carbamato sustituidos con morfolino como inhibidores del blanco de rapamicina de mamifero.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011107585A1 (en) * 2010-03-04 2011-09-09 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors

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Publication number Publication date
BR112014006743A8 (pt) 2018-01-09
EP2758379A1 (en) 2014-07-30
BR112014006743A2 (pt) 2017-04-11
CA2849189A1 (en) 2013-03-28
US9175011B2 (en) 2015-11-03
AU2012311458A1 (en) 2014-04-10
JP2014530197A (ja) 2014-11-17
US20140378438A1 (en) 2014-12-25
WO2013041652A1 (en) 2013-03-28
ES2609606T3 (es) 2017-04-21
JP5995975B2 (ja) 2016-09-21
RU2014109747A (ru) 2015-10-27
EP2758379B1 (en) 2016-10-19
CN103917530B (zh) 2016-08-24
RU2616619C2 (ru) 2017-04-18
CN103917530A (zh) 2014-07-09
KR20140070616A (ko) 2014-06-10

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