CA2599212A1 - 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors - Google Patents

2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors Download PDF

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Publication number
CA2599212A1
CA2599212A1 CA002599212A CA2599212A CA2599212A1 CA 2599212 A1 CA2599212 A1 CA 2599212A1 CA 002599212 A CA002599212 A CA 002599212A CA 2599212 A CA2599212 A CA 2599212A CA 2599212 A1 CA2599212 A1 CA 2599212A1
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CA
Canada
Prior art keywords
compound
nitrogen atom
nitrogen
optionally substituted
group
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
CA002599212A
Other languages
English (en)
French (fr)
Inventor
Marc Geoffrey Hummersone
Sylvie Gomez
Keith Allan Menear
Xiao-Ling Fan Cockcroft
Peter Edwards
Vincent Junior Ming Lai Loh
Graeme Cameron Murray Smith
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.)
Kudos Pharmaceuticals Ltd
Original Assignee
Kudos Pharmaceuticals Limited
Marc Geoffrey Hummersone
Sylvie Gomez
Keith Allan Menear
Xiao-Ling Fan Cockcroft
Peter Edwards
Vincent Junior Ming Lai Loh
Graeme Cameron Murray Smith
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
Priority claimed from GBGB0503961.5A external-priority patent/GB0503961D0/en
Application filed by Kudos Pharmaceuticals Limited, Marc Geoffrey Hummersone, Sylvie Gomez, Keith Allan Menear, Xiao-Ling Fan Cockcroft, Peter Edwards, Vincent Junior Ming Lai Loh, Graeme Cameron Murray Smith filed Critical Kudos Pharmaceuticals Limited
Publication of CA2599212A1 publication Critical patent/CA2599212A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • 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
    • 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
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (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)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA002599212A 2005-02-25 2006-02-24 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors Abandoned CA2599212A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US65617805P 2005-02-25 2005-02-25
US60/656,178 2005-02-25
GBGB0503961.5A GB0503961D0 (en) 2005-02-25 2005-02-25 Compounds
GB0503961.5 2005-02-25
US74240305P 2005-12-05 2005-12-05
US60/742,403 2005-12-05
PCT/GB2006/000671 WO2006090169A1 (en) 2005-02-25 2006-02-24 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors

Publications (1)

Publication Number Publication Date
CA2599212A1 true CA2599212A1 (en) 2006-08-31

Family

ID=36282842

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002599212A Abandoned CA2599212A1 (en) 2005-02-25 2006-02-24 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors

Country Status (9)

Country Link
EP (1) EP1871377A1 (ja)
JP (1) JP2008531538A (ja)
KR (1) KR20070113252A (ja)
AU (1) AU2006217744A1 (ja)
CA (1) CA2599212A1 (ja)
IL (1) IL184901A0 (ja)
MX (1) MX2007010401A (ja)
NO (1) NO20074057L (ja)
WO (1) WO2006090169A1 (ja)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
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US8338435B2 (en) 2006-07-20 2012-12-25 Gilead Sciences, Inc. Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections
MX2009001946A (es) * 2006-08-23 2009-03-05 Kudos Pharm Ltd Derivados de 2-metilmorfolin-pirido-, pirazo- y pirimido- pirimidina como inhibidores de mtor.
TW200840584A (en) 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
RU2473549C2 (ru) 2008-07-31 2013-01-27 Дженентек, Инк. Пиримидиновые соединения, композиции и способы применения
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
MX2011001872A (es) * 2008-08-18 2011-05-23 Univ Yale Moduladores de mif.
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
US8110578B2 (en) * 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
CA2751501C (en) * 2009-02-12 2018-01-16 Merck Serono S.A. 2-morpholino-pyrido[3,2-d]pyrimidines
WO2010118207A1 (en) * 2009-04-09 2010-10-14 Schering Corporation Pyrazolo [1, 5-a] pyrimidine derivatives as mtor inhibitors
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
US8658651B2 (en) 2009-09-30 2014-02-25 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
EP2493460A4 (en) 2009-10-30 2013-04-24 Ariad Pharma Inc METHOD AND COMPOSITIONS FOR THE TREATMENT OF CANCER
BR112012011147A2 (pt) 2009-11-12 2021-09-08 F.Hoffmann-La Roche Ag Composto, composição farmacêutica e uso de um composto.
KR101469334B1 (ko) 2009-11-12 2014-12-04 에프. 호프만-라 로슈 아게 N-9-치환된 퓨린 화합물, 조성물 및 사용 방법
WO2011067348A2 (en) 2009-12-03 2011-06-09 Novartis Ag Mek inhibitor salts and solvates thereof
WO2011067356A2 (en) 2009-12-03 2011-06-09 Novartis Ag Polymorphs of a mek inhibitor
CN102821767A (zh) 2010-02-03 2012-12-12 西格诺药品有限公司 Lkb1突变作为对tor激酶抑制剂的敏感性的预测生物标记的鉴定
EP2552428A1 (en) 2010-03-30 2013-02-06 Novartis AG Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling
AU2011240735B2 (en) 2010-04-13 2015-01-29 Novartis Ag Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (CDK4/6) inhibitor and an mTOR inhibitor for treating cancer
CA2803055A1 (en) 2010-06-25 2011-12-29 Novartis Ag Heteroaryl compounds and compositions as protein kinase inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
CN105039520A (zh) 2011-08-03 2015-11-11 西格诺药品有限公司 作为lkb1状态的预测性生物标志物的基因表达谱的鉴定
TWI663165B (zh) * 2012-09-28 2019-06-21 美商伊格尼塔公司 非典型蛋白質激酶c之氮雜喹唑啉抑制劑
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
CN103588792B (zh) * 2013-03-04 2016-03-23 中国科学院上海药物研究所 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途
EP2986321A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
TW201521725A (zh) 2013-04-17 2015-06-16 Signal Pharm Llc 使用tor激酶抑制劑組合療法以治療癌症之方法
CA2908957C (en) 2013-04-17 2021-05-18 Signal Pharmaceuticals, Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
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Also Published As

Publication number Publication date
AU2006217744A1 (en) 2006-08-31
JP2008531538A (ja) 2008-08-14
KR20070113252A (ko) 2007-11-28
MX2007010401A (es) 2008-02-19
NO20074057L (no) 2007-09-17
IL184901A0 (en) 2007-12-03
WO2006090169A1 (en) 2006-08-31
EP1871377A1 (en) 2008-01-02

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Legal Events

Date Code Title Description
FZDE Discontinued