JP2009525292A - ７ｈ−ピリド［３，４−ｄ］ピリミジン−８−オン、それらの製造及びプロテインキナーゼ阻害剤としての使用 - Google Patents

７ｈ−ピリド［３，４−ｄ］ピリミジン−８−オン、それらの製造及びプロテインキナーゼ阻害剤としての使用 Download PDF

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Publication number
JP2009525292A
JP2009525292A JP2008552729A JP2008552729A JP2009525292A JP 2009525292 A JP2009525292 A JP 2009525292A JP 2008552729 A JP2008552729 A JP 2008552729A JP 2008552729 A JP2008552729 A JP 2008552729A JP 2009525292 A JP2009525292 A JP 2009525292A
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Prior art keywords
pyrido
pyrimidin
alkyl
phenyl
tolyl
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Ceased
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JP2008552729A
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Japanese (ja)
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JP2009525292A5 (https=
Inventor
ホノルト，コンラト
ポール，ジェーン
ロッシュローブ，カール
シェーファー，ボルフガンク
シャイブリヒ，ステファン
ヒルシュハイト，トマス フォン
ホイットル，アラン
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of JP2009525292A publication Critical patent/JP2009525292A/ja
Publication of JP2009525292A5 publication Critical patent/JP2009525292A5/ja
Ceased legal-status Critical Current

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    • 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/22—Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of calcitonin
    • 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
    • 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
    • A61P9/10—Drugs 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
JP2008552729A 2006-01-31 2007-01-29 ７ｈ−ピリド［３，４−ｄ］ピリミジン−８−オン、それらの製造及びプロテインキナーゼ阻害剤としての使用 Ceased JP2009525292A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06001915 2006-01-31
PCT/EP2007/000725 WO2007088014A1 (en) 2006-01-31 2007-01-29 7h-pyrido[3,4-d]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
JP2009525292A true JP2009525292A (ja) 2009-07-09
JP2009525292A5 JP2009525292A5 (https=) 2012-01-26

Family

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JP2008552729A Ceased JP2009525292A (ja) 2006-01-31 2007-01-29 ７ｈ−ピリド［３，４−ｄ］ピリミジン−８−オン、それらの製造及びプロテインキナーゼ阻害剤としての使用

Country Status (13)

Country Link
US (1) US8058283B2 (https=)
EP (1) EP1981886B1 (https=)
JP (1) JP2009525292A (https=)
KR (1) KR20080083046A (https=)
CN (1) CN101374840B (https=)
AT (1) ATE439361T1 (https=)
AU (1) AU2007211684A1 (https=)
BR (1) BRPI0706781A2 (https=)
CA (1) CA2636981A1 (https=)
DE (1) DE602007001952D1 (https=)
ES (1) ES2329419T3 (https=)
IL (1) IL191748A0 (https=)
WO (1) WO2007088014A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013519725A (ja) * 2010-02-17 2013-05-30 デバイオファーム エスエイ 二環式化合物および二重ｃ−ＳＲＣ／ＪＡＫ阻害剤としてのそれらの使用
JP2015511245A (ja) * 2012-02-23 2015-04-16 アッヴィ・インコーポレイテッド ピリドピリミジノン系キナーゼ阻害薬
JP2022521901A (ja) * 2019-02-18 2022-04-13 コリア・インスティテュート・オブ・サイエンス・アンド・テクノロジー タンパク質キナーゼ阻害活性を有する新規なピリド［３，４－ｄ］ピリミジン－８－オン誘導体およびこれを含む癌の予防、改善または治療用薬学組成物

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2329419T3 (es) 2006-01-31 2009-11-25 F. Hoffmann-La Roche Ag 7h-pirido(3,4-d)pirimidin-8-onas, su preparacion y uso como inhibidores de proteinas cinasas.
JP6280546B2 (ja) 2012-06-26 2018-02-14 デル マー ファーマシューティカルズ ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法
CN105130986B (zh) * 2015-09-30 2017-07-18 广州科擎新药开发有限公司 嘧啶或吡啶并吡啶酮类化合物及其应用
CN110016026B (zh) * 2018-01-08 2022-11-25 上海凌济生物科技有限公司 一类具有抗肿瘤活性的嘧啶并吡啶酮类化合物、制备方法和用途
KR102329720B1 (ko) 2019-08-30 2021-11-23 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 신규한 피리미도[4,5-d]피리미딘-2-온 유도체

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002500225A (ja) * 1998-01-12 2002-01-08 グラクソ グループ リミテッド プロテインチロシンキナーゼ阻害剤としての二環式ヘテロ芳香族化合物
WO2005034869A2 (en) * 2003-10-08 2005-04-21 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2006012577A2 (en) * 2004-07-22 2006-02-02 Bayer Pharmaceuticals Corporation Quinazolinone derivatives useful for the regulation of glucose homeostasis and food intake

Family Cites Families (15)

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PL181893B1 (pl) 1994-11-14 2001-10-31 Warner Lambert Co Zwiazki bedace pochodnymi pirymidyny i naftyrydyny oraz preparat farmaceutyczny zawierajacy je PL PL PL
IL117923A (en) 1995-05-03 2000-06-01 Warner Lambert Co Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds
TR200003429T2 (tr) 1998-05-26 2001-07-23 Warner-Lambert Company Hücresel çoğalma inhibitörleri olarak bisiklik pirimidinler ve bisiklik 3,4-dihidropirimidinler.
HK1041483B (zh) 1998-10-23 2004-12-24 霍夫曼-拉罗奇有限公司 雙環氮雜環
AU776250B2 (en) 1999-10-21 2004-09-02 F. Hoffmann-La Roche Ag Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of P38 protein kinase
CZ20021743A3 (cs) 1999-10-21 2002-08-14 F. Hoffmann-La Roche Ag Bicyklické dusíkové heterocykly substituované alkylaminoskupinou jako inhibitory P38 proteinkinázy
CA2420122A1 (en) 2000-08-31 2002-03-07 F. Hoffmann-La Roche Ag 7-oxo pyridopyrimidines
CA2420286A1 (en) 2000-08-31 2002-03-07 F. Hoffmann-La Roche Ag 7-oxo pyridopyrimidines as inhibitors of a cellular proliferation
US7196090B2 (en) 2002-07-25 2007-03-27 Warner-Lambert Company Kinase inhibitors
US7112676B2 (en) 2002-11-04 2006-09-26 Hoffmann-La Roche Inc. Pyrimido compounds having antiproliferative activity
TW200413381A (en) 2002-11-04 2004-08-01 Hoffmann La Roche Novel amino-substituted dihydropyrimido [4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents
CL2004000366A1 (es) 2003-02-26 2005-01-07 Pharmacia Corp Sa Organizada B USO DE UNA COMBINACION DE UN COMPUESTO DERIVADO DE PIRAZOL INHIBIDOR DE QUINASA p38, Y UN INHIBIDOR DE ACE PARA TRATAR DISFUNCION RENAL, ENFERMEDAD CARDIOVASCULAR Y VASCULAR, RETINOPATIA, NEUROPATIA, EDEMA, DISFUNCION ENDOTELIAL O INSULINOPATIA.
WO2004089955A1 (en) 2003-04-10 2004-10-21 F.Hoffmann-La Roche Ag Pyrimido compounds
WO2005011597A2 (en) 2003-07-29 2005-02-10 Irm Llc Compounds and compositions as protein kinase inhibitors
ES2329419T3 (es) 2006-01-31 2009-11-25 F. Hoffmann-La Roche Ag 7h-pirido(3,4-d)pirimidin-8-onas, su preparacion y uso como inhibidores de proteinas cinasas.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002500225A (ja) * 1998-01-12 2002-01-08 グラクソ グループ リミテッド プロテインチロシンキナーゼ阻害剤としての二環式ヘテロ芳香族化合物
WO2005034869A2 (en) * 2003-10-08 2005-04-21 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2006012577A2 (en) * 2004-07-22 2006-02-02 Bayer Pharmaceuticals Corporation Quinazolinone derivatives useful for the regulation of glucose homeostasis and food intake

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013519725A (ja) * 2010-02-17 2013-05-30 デバイオファーム エスエイ 二環式化合物および二重ｃ−ＳＲＣ／ＪＡＫ阻害剤としてのそれらの使用
JP2015511245A (ja) * 2012-02-23 2015-04-16 アッヴィ・インコーポレイテッド ピリドピリミジノン系キナーゼ阻害薬
JP2022521901A (ja) * 2019-02-18 2022-04-13 コリア・インスティテュート・オブ・サイエンス・アンド・テクノロジー タンパク質キナーゼ阻害活性を有する新規なピリド［３，４－ｄ］ピリミジン－８－オン誘導体およびこれを含む癌の予防、改善または治療用薬学組成物
JP7262599B2 (ja) 2019-02-18 2023-04-21 コリア・インスティテュート・オブ・サイエンス・アンド・テクノロジー タンパク質キナーゼ阻害活性を有する新規なピリド［３，４－ｄ］ピリミジン－８－オン誘導体およびこれを含む癌の予防、改善または治療用薬学組成物

Also Published As

Publication number Publication date
IL191748A0 (en) 2008-12-29
US20090030020A1 (en) 2009-01-29
CN101374840A (zh) 2009-02-25
EP1981886A1 (en) 2008-10-22
CA2636981A1 (en) 2007-08-09
EP1981886B1 (en) 2009-08-12
KR20080083046A (ko) 2008-09-12
WO2007088014A1 (en) 2007-08-09
CN101374840B (zh) 2011-09-28
ES2329419T3 (es) 2009-11-25
AU2007211684A1 (en) 2007-08-09
BRPI0706781A2 (pt) 2011-04-05
DE602007001952D1 (de) 2009-09-24
ATE439361T1 (de) 2009-08-15
US8058283B2 (en) 2011-11-15

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