CA2849189A1 - Morpholino substituted urea or carbamate derivatives as mtor inhibitors - Google Patents

Morpholino substituted urea or carbamate derivatives as mtor inhibitors Download PDF

Info

Publication number
CA2849189A1
CA2849189A1 CA2849189A CA2849189A CA2849189A1 CA 2849189 A1 CA2849189 A1 CA 2849189A1 CA 2849189 A CA2849189 A CA 2849189A CA 2849189 A CA2849189 A CA 2849189A CA 2849189 A1 CA2849189 A1 CA 2849189A1
Authority
CA
Canada
Prior art keywords
phenyl
triazin
methylsulfonyl
urea
methylmorpholino
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
CA2849189A
Other languages
English (en)
French (fr)
Inventor
Rosemary Lynch
Andrew David Cansfield
Daniel Paul HARDY
Mihiro Sunose
Adeline Morel
Laura CONVERY
Rita Adrego
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.)
Cellzome Ltd
Original Assignee
Cellzome Ltd
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 Cellzome Ltd filed Critical Cellzome Ltd
Publication of CA2849189A1 publication Critical patent/CA2849189A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12Heterocyclic 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
    • C07D251/14Heterocyclic 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
    • C07D251/22Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/02Heterocyclic 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
    • C07D407/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/08Bridged systems

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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2849189A 2011-09-21 2012-09-21 Morpholino substituted urea or carbamate derivatives as mtor inhibitors Abandoned CA2849189A1 (en)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
CA2849189A1 true CA2849189A1 (en) 2013-03-28

Family

ID=46881066

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2849189A Abandoned CA2849189A1 (en) 2011-09-21 2012-09-21 Morpholino substituted urea or carbamate derivatives as mtor inhibitors

Country Status (11)

Country Link
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 (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9249129B2 (en) 2010-03-04 2016-02-02 Cellzome Limited Morpholino substituted urea derivatives as mTOR inhibitors
CN103946222B (zh) 2011-10-07 2016-12-28 塞尔佐姆有限公司 作为mtor抑制剂的吗啉代取代的双环嘧啶脲或氨基甲酸衍生物
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
CA3037456A1 (en) 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
IL270224B1 (en) 2017-05-02 2024-04-01 Novartis Ag Combination therapy employing trametinib and a defined raf inhibitor
CA3111980A1 (en) 2018-09-10 2020-03-19 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
US20220378754A1 (en) * 2019-09-11 2022-12-01 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

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69837529T2 (de) 1997-02-12 2007-07-26 Electrophoretics Ltd., Cobham Proteinmarker für lungenkrebs und deren verwendung
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
JP4135318B2 (ja) 1997-12-15 2008-08-20 アステラス製薬株式会社 新規なピリミジン−5−カルボキサミド誘導体
BRPI0017548B8 (pt) 1999-02-10 2023-05-02 Astrazeneca Ab Composto
EE05330B1 (et) 1999-11-05 2010-08-16 Astrazeneca Ab Kinasoliini derivaadid kui VEGF-i inhibiitorid
US6573293B2 (en) 2000-02-15 2003-06-03 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
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
CA2611365C (en) 2005-06-14 2014-02-11 Cellzome Ag Process for the identification of novel enzyme interacting compounds
GB0616747D0 (en) * 2006-08-24 2006-10-04 Astrazeneca Ab Novel compounds
EP1887359B1 (en) 2006-08-03 2008-11-12 Cellzome Ag Methods for the identification of PI3K interacting molecules and for the purification of PI3K
CA2660758A1 (en) 2006-08-24 2008-02-27 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
JP4782239B2 (ja) 2007-04-18 2011-09-28 ファイザー・プロダクツ・インク 異常細胞増殖治療のためのスルホニルアミド誘導体
JP2010532756A (ja) 2007-07-06 2010-10-14 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド mTORC1及びmTORC2の両方の阻害剤を含む組み合わせ抗癌療法
CA2692720A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k
WO2009007749A2 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
CA2692725A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Compound - 946
BRPI0814818A2 (pt) 2007-07-09 2019-09-10 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica
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
CA2713276A1 (en) 2008-02-04 2009-08-13 Cellzome Ag Selectivity profiling of pi3k interacting molecules against multiple targets
EP2300483A1 (en) 2008-05-23 2011-03-30 Wyeth LLC Triazine compounds as p13 kinase and mtor inhibitors
KR20110046514A (ko) 2008-07-31 2011-05-04 제넨테크, 인크. 피리미딘 화합물, 조성물 및 사용 방법
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
US8785457B2 (en) 2009-03-13 2014-07-22 Cellzome Limited Pyrimidine derivatives as mTOR inhibitors
EP2419432B9 (en) 2009-04-17 2016-02-17 Wyeth LLC Pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
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
JP2013500265A (ja) 2009-07-23 2013-01-07 ザ トラスティーズ オブ プリンストン ユニバーシティ 抗ウイルス剤として用いられるmTORキナーゼ阻害剤
US9249129B2 (en) 2010-03-04 2016-02-02 Cellzome Limited Morpholino substituted urea derivatives as mTOR inhibitors
US20140163023A1 (en) 2011-04-04 2014-06-12 Cellzome Limited Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
CN103946222B (zh) 2011-10-07 2016-12-28 塞尔佐姆有限公司 作为mtor抑制剂的吗啉代取代的双环嘧啶脲或氨基甲酸衍生物

Also Published As

Publication number Publication date
BR112014006743A8 (pt) 2018-01-09
EP2758379B1 (en) 2016-10-19
BR112014006743A2 (pt) 2017-04-11
WO2013041652A1 (en) 2013-03-28
US9175011B2 (en) 2015-11-03
CN103917530A (zh) 2014-07-09
AU2012311458B2 (en) 2016-02-04
JP2014530197A (ja) 2014-11-17
RU2616619C2 (ru) 2017-04-18
US20140378438A1 (en) 2014-12-25
KR20140070616A (ko) 2014-06-10
ES2609606T3 (es) 2017-04-21
EP2758379A1 (en) 2014-07-30
JP5995975B2 (ja) 2016-09-21
CN103917530B (zh) 2016-08-24
RU2014109747A (ru) 2015-10-27
AU2012311458A1 (en) 2014-04-10

Similar Documents

Publication Publication Date Title
AU2012311458B2 (en) Morpholino substituted urea or carbamate derivatives as mTOR inhibitors
AU2012320465B2 (en) Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mTOR inhibitors
US9249129B2 (en) Morpholino substituted urea derivatives as mTOR inhibitors
US20140296234A1 (en) Pyrimidine derivatives as mtor inhibitors
US20140163023A1 (en) Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
EP4633735A1 (en) Inhibitory compounds
WO2024243304A2 (en) Bicyclic heteroaryl compounds

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20170913

FZDE Dead

Effective date: 20191217