CA2649324A1 - Tetrahydropteridines useful as inhibitors of protein kinases - Google Patents

Tetrahydropteridines useful as inhibitors of protein kinases Download PDF

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Publication number
CA2649324A1
CA2649324A1 CA002649324A CA2649324A CA2649324A1 CA 2649324 A1 CA2649324 A1 CA 2649324A1 CA 002649324 A CA002649324 A CA 002649324A CA 2649324 A CA2649324 A CA 2649324A CA 2649324 A1 CA2649324 A1 CA 2649324A1
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CA
Canada
Prior art keywords
compound
aliphatic
optionally substituted
independently
cycloaliphatic
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
CA002649324A
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English (en)
French (fr)
Inventor
Jean-Damien Charrier
David Kay
Ronald Knegtel
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2649324A1 publication Critical patent/CA2649324A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • A61P37/06Immunosuppressants, 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA002649324A 2006-04-12 2007-04-12 Tetrahydropteridines useful as inhibitors of protein kinases Abandoned CA2649324A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US79132706P 2006-04-12 2006-04-12
US60/791,327 2006-04-12
US83872006P 2006-08-18 2006-08-18
US60/838,720 2006-08-18
PCT/US2007/009006 WO2007120752A2 (en) 2006-04-12 2007-04-12 4, 5-dihydro- [1, 2, 4] triazolo [4, 3-f] pteridines as protein kinase plk1 inhibitors for the treatment of proliferative disorders

Publications (1)

Publication Number Publication Date
CA2649324A1 true CA2649324A1 (en) 2007-10-25

Family

ID=38544378

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002649324A Abandoned CA2649324A1 (en) 2006-04-12 2007-04-12 Tetrahydropteridines useful as inhibitors of protein kinases

Country Status (16)

Country Link
US (3) US7763629B2 (enExample)
EP (1) EP2010542B1 (enExample)
JP (1) JP5313875B2 (enExample)
KR (1) KR101432316B1 (enExample)
AR (1) AR060432A1 (enExample)
AT (1) ATE542823T1 (enExample)
AU (1) AU2007238690B2 (enExample)
CA (1) CA2649324A1 (enExample)
ES (1) ES2381212T3 (enExample)
IL (1) IL194699A (enExample)
MX (1) MX2008013110A (enExample)
NO (1) NO20084747L (enExample)
NZ (1) NZ571969A (enExample)
RU (1) RU2441006C2 (enExample)
TW (1) TW200808805A (enExample)
WO (1) WO2007120752A2 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008287339A1 (en) * 2007-08-15 2009-02-19 Vertex Pharmaceuticals Incorporated 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases
AU2008343932B2 (en) 2007-12-19 2013-08-15 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
ATE531372T1 (de) 2008-04-07 2011-11-15 Amgen Inc Gem-disubstituierte und spirocyclische aminopyridine/pyrimidine als zellcyclus- inhibitoren
AU2009271663B2 (en) * 2008-06-23 2014-04-17 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors
JP5869338B2 (ja) * 2008-06-23 2016-02-24 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated タンパク質キナーゼ阻害剤
JP2013505927A (ja) 2009-09-25 2013-02-21 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なピリミジン誘導体の調製方法
JP2013512860A (ja) 2009-09-25 2013-04-18 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なピリミジン誘導体の調製方法
EP2516441B1 (en) 2009-12-23 2015-01-21 Elan Pharmaceuticals Inc. Pteridinones as inhibitors of polo-like kinase
JP5850321B2 (ja) * 2010-02-10 2016-02-03 公立大学法人横浜市立大学 神経選択的転写抑制因子NRSFに特異的に結合するmSin3Bに結合する化合物の利用
US8933070B2 (en) 2010-07-02 2015-01-13 University Health Network Methods of targeting PTEN mutant diseases and compositions therefor
EP2661268A2 (en) * 2010-10-08 2013-11-13 Elan Pharmaceuticals Inc. Inhibitors of polo-like kinase
TW201307347A (zh) 2010-11-01 2013-02-16 Arqule Inc 經取代苯並-咪唑並-吡啶並-二氮呯化合物
WO2012129344A1 (en) 2011-03-23 2012-09-27 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
MD4300C1 (ro) * 2012-12-28 2015-03-31 Государственный Университет Молд0 Inhibitor al proliferării celulelor HepG2 în cancerul hepatic în bază de cloro-[2-fenil(piridin-2-il)metanon-4-(3-metoxifenil)tiosemicarbazono]nichel
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
WO2017027717A1 (en) 2015-08-12 2017-02-16 Incyte Corporation Bicyclic fused pyrimidine compounds as tam inhibitors
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
KR102558066B1 (ko) 2016-03-28 2023-07-25 인사이트 코포레이션 Tam 억제제로서 피롤로트리아진 화합물
IL273579B2 (en) 2017-09-27 2025-10-01 Incyte Corp Salts of pyrrolizidine derivatives used as Tm inhibitors.
HRP20250676T1 (hr) 2018-06-29 2025-08-01 Incyte Corporation Formulacije inhibitora axl/mer
CN109734809A (zh) * 2019-02-27 2019-05-10 南方科技大学 治疗性的人Plk1蛋白单克隆抗体及其制备方法
CN115697343A (zh) 2020-03-06 2023-02-03 因赛特公司 包含axl/mer和pd-1/pd-l1抑制剂的组合疗法
EP4157849A4 (en) * 2021-08-10 2024-12-11 Uppthera, Inc. Novel plk1 degradation inducing compound

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA973884B (en) * 1996-05-23 1998-11-06 Du Pont Merck Pharma Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
JP2003509425A (ja) * 1999-09-15 2003-03-11 ワーナー−ランバート・カンパニー キナーゼ阻害剤としてのプテリジノン
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
RU2351586C2 (ru) * 2002-10-03 2009-04-10 Таргеджен, Инк. Васкулостатические агенты и способы их применения
BR0315053A (pt) 2002-10-03 2005-08-09 Targegen Inc Agentes vasculostáticos , composição, artigo e processo de preparação dos mesmos
MXPA05013478A (es) 2003-06-10 2006-03-09 Pfizer Combinaciones terapeuticas.
GB0315966D0 (en) * 2003-07-08 2003-08-13 Cyclacel Ltd Compounds
GB0400700D0 (en) 2004-01-13 2004-02-18 Pfizer Ltd Compounds useful in therapy
GB0412874D0 (en) 2004-06-09 2004-07-14 Pfizer Ltd Novel pharmaceuticals
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel

Also Published As

Publication number Publication date
WO2007120752A3 (en) 2008-05-08
NO20084747L (no) 2008-11-25
IL194699A0 (en) 2009-08-03
JP2009536155A (ja) 2009-10-08
MX2008013110A (es) 2009-03-06
KR101432316B1 (ko) 2014-08-29
ATE542823T1 (de) 2012-02-15
RU2441006C2 (ru) 2012-01-27
US20110021519A1 (en) 2011-01-27
HK1134486A1 (en) 2010-04-30
US7763629B2 (en) 2010-07-27
NZ571969A (en) 2011-10-28
WO2007120752A2 (en) 2007-10-25
AU2007238690B2 (en) 2013-05-02
RU2008144584A (ru) 2010-05-20
EP2010542A2 (en) 2009-01-07
AU2007238690A1 (en) 2007-10-25
TW200808805A (en) 2008-02-16
US8524902B2 (en) 2013-09-03
JP5313875B2 (ja) 2013-10-09
KR20080109919A (ko) 2008-12-17
IL194699A (en) 2014-07-31
ES2381212T3 (es) 2012-05-24
EP2010542B1 (en) 2012-01-25
US20090062292A1 (en) 2009-03-05
US20120277425A1 (en) 2012-11-01
AR060432A1 (es) 2008-06-18
US8067417B2 (en) 2011-11-29

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued

Effective date: 20160324