CN102791715B - 用作激酶抑制剂的三环化合物 - Google Patents

用作激酶抑制剂的三环化合物 Download PDF

Info

Publication number
CN102791715B
CN102791715B CN201080064929.0A CN201080064929A CN102791715B CN 102791715 B CN102791715 B CN 102791715B CN 201080064929 A CN201080064929 A CN 201080064929A CN 102791715 B CN102791715 B CN 102791715B
Authority
CN
China
Prior art keywords
methyl
phenyl
base
dihydro
oxa
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.)
Expired - Fee Related
Application number
CN201080064929.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN102791715A (zh
Inventor
华金·帕斯托费尔南德斯
弗朗西斯科·哈维尔·拉莫斯利马
安娜·伊莎贝尔·埃尔南德斯伊格拉斯
索尼娅·马丁内斯冈萨雷斯
何塞·伊格纳西奥·马丁埃纳尔多
卡尔-古斯塔夫·彼雷·萨卢斯特
埃丝特·冈萨雷斯坎塔拉彼德拉
卡门·布兰科阿帕里西奥
安东尼奥·罗德里格斯埃尔格塔
安娜·玛丽亚·加西亚科利亚索
安东尼奥·萨尔加多塞拉诺
比阿特丽斯·诺亚马里尼奥
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.)
National Public Sector Foundation Carlos Iii National Oncology Research Center FSPCnio
Original Assignee
Research Centre Foundation Of Carlos Three Generations National Cancer
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 Research Centre Foundation Of Carlos Three Generations National Cancer filed Critical Research Centre Foundation Of Carlos Three Generations National Cancer
Publication of CN102791715A publication Critical patent/CN102791715A/zh
Application granted granted Critical
Publication of CN102791715B publication Critical patent/CN102791715B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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
    • C07D491/14—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P25/28—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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P37/06—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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
CN201080064929.0A 2009-12-31 2010-12-31 用作激酶抑制剂的三环化合物 Expired - Fee Related CN102791715B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09380202 2009-12-31
EP09380202.3 2009-12-31
PCT/GB2010/002348 WO2011080510A1 (en) 2009-12-31 2010-12-31 Tricyclic compounds for use as kinase inhibitors

Publications (2)

Publication Number Publication Date
CN102791715A CN102791715A (zh) 2012-11-21
CN102791715B true CN102791715B (zh) 2016-04-27

Family

ID=42200029

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080064929.0A Expired - Fee Related CN102791715B (zh) 2009-12-31 2010-12-31 用作激酶抑制剂的三环化合物

Country Status (12)

Country Link
US (1) US9682991B2 (https=)
EP (1) EP2519526B1 (https=)
JP (1) JP5913126B2 (https=)
KR (1) KR20120111739A (https=)
CN (1) CN102791715B (https=)
AU (1) AU2010338038B2 (https=)
CA (1) CA2786002C (https=)
IL (1) IL220701A0 (https=)
NZ (1) NZ601033A (https=)
PH (1) PH12012501361A1 (https=)
SG (1) SG182297A1 (https=)
WO (1) WO2011080510A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
WO2013004984A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncologicas (Cnio) Tricyclic compounds for use as kinase inhibitors
WO2013005041A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) Tricyclic heterocyclic compounds as kinase inhibitors
WO2013005057A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
CN104768554B (zh) 2012-11-07 2018-04-17 霍夫曼-拉罗奇有限公司 三唑并化合物
CN108931633B (zh) * 2018-05-22 2021-08-27 郑州大学第一附属医院 胆囊癌诊断和预后判断标志物pim1
AU2021360636A1 (en) * 2020-10-16 2023-06-15 Shanghai De Novo Pharmatech Co., Ltd. Triheterocyclic derivative, and pharmaceutical composition and application thereof
CN113214255B (zh) * 2021-04-22 2023-09-29 无锡合全药业有限公司 2,6-二氮杂螺[3.5]壬烷-6-甲酸叔丁基酯及其盐的合成方法
US20250042918A1 (en) 2021-12-01 2025-02-06 Fundación Del Sector Públlco Estatal Centro Nacional De Investigaciones Oncológicas Carlos III Compounds
EP4279074A1 (en) * 2022-05-19 2023-11-22 Georg-August-Universität Göttingen Stiftung Öffentlichen Rechts, Universitätsmedizin Azolo compounds for treatment of fibrotic diseases
EP4458358A1 (en) * 2023-05-02 2024-11-06 Tietze Chemical Consulting UG Pyridazine compounds for antifibrotic therapy

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
WO2009007029A1 (de) * 2007-07-11 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Imidazo-, pyrazolopyrazine und imidazotriazine zur behandlung hämatologischer erkrankungen
WO2009060197A1 (en) * 2007-11-08 2009-05-14 Centro Nacional De Investigaciones Oncologicas (Cnio) Imidazopyridazines for use as protein kinase inhibitors

Family Cites Families (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS603080B2 (ja) 1976-08-10 1985-01-25 三菱化学株式会社 Ｓ―トリアゾロ〔３，４ ―α〕〔５，６，７，８〕テトラヒドロ フタラジン類
GR70309B (https=) 1979-10-29 1982-09-08 Dow Chemical Co
PH21834A (en) 1982-01-18 1988-03-17 Lepetit Spa New 6-substituted-s-triazolo(3,4-a)phthalazine derivatives
US4487930A (en) 1982-09-07 1984-12-11 The Dow Chemical Company 6-[(Cyclic amino)alkylamino]-tetrahydrotriazolo[3,4-a]phthalazines
FR2601675B1 (fr) 1986-07-17 1988-09-23 Rhone Poulenc Sante Derives du taxol, leur preparation et les compositions pharmaceutiques qui les contiennent
US5011835A (en) 1990-02-07 1991-04-30 Merrell Dow Pharmaceuticals Inc. Substituted triazolopyridazines, pharmaceutical compositions and use
US5714512A (en) 1991-07-08 1998-02-03 Rhone-Poulenc Rorer, S.A. Compositions containing taxane derivatives
US5698582A (en) 1991-07-08 1997-12-16 Rhone-Poulenc Rorer S.A. Compositions containing taxane derivatives
US5750561A (en) 1991-07-08 1998-05-12 Rhone-Poulenc Rorer, S.A. Compositions containing taxane derivatives
TW211013B (https=) 1991-12-27 1993-08-11 Takeda Pharm Industry Co Ltd
LT3200B (en) 1992-03-18 1995-03-27 Takeda Chemical Industries Ltd Triazolopyridazine methodfor production thereof and use
FR2698543B1 (fr) 1992-12-02 1994-12-30 Rhone Poulenc Rorer Sa Nouvelles compositions à base de taxoides.
EP0620224B1 (en) 1993-04-12 1998-07-15 Takeda Chemical Industries, Ltd. Triazolopyridazine derivatives, their production and use
WO1998004560A1 (en) 1996-07-25 1998-02-05 Merck Sharp & Dohme Limited SUBSTITUTED TRIAZOLO PYRIDAZINE DERIVATIVES AS INVERSE AGONISTS OF THE GABAAα5 RECEPTOR SUBTYPE
KR20000029548A (ko) 1996-07-25 2000-05-25 더블유. 지. 콜 가바수용체에대한리간드로서의치환된트리아졸로-피리다진유도체
ES2137113B1 (es) 1997-07-29 2000-09-16 Almirall Prodesfarma Sa Nuevos derivados de triazolo-piridazinas heterociclicos.
WO1999025353A1 (en) 1997-11-13 1999-05-27 Merck Sharp & Dohme Limited Therapeutic uses of triazolo-pyridazine derivatives
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9801208D0 (en) 1998-01-21 1998-03-18 Merck Sharp & Dohme Therapeutic agents
GB9813576D0 (en) 1998-06-24 1998-08-19 Merck Sharp & Dohme Therapeutic agents
GB2345443A (en) 1999-01-08 2000-07-12 Merck Sharp & Dohme Use of triazolo-pyridazines for treating premenstrual syndrome
US6933299B1 (en) 1999-07-09 2005-08-23 Smithkline Beecham Corporation Anilinoquinazolines as protein tyrosine kinase inhibitors
JP2003504363A (ja) 1999-07-09 2003-02-04 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アニリノキナゾリン類
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
AU2001273071B2 (en) 2000-06-30 2005-09-08 Glaxo Group Limited Quinazoline ditosylate salt compounds
JP3811775B2 (ja) 2000-07-19 2006-08-23 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー ４−ヨードフェニルアミノベンズヒドロキサム酸の酸素化エステル
DE60203260T2 (de) 2001-01-16 2006-02-02 Glaxo Group Ltd., Greenford Pharmazeutische kombination, die ein 4-chinazolinamin und paclitaxel, carboplatin oder vinorelbin enthält, zur behandlung von krebs
US6958334B2 (en) 2001-04-10 2005-10-25 Merck & Co., Inc. Inhibitors of Akt activity
US20040106540A1 (en) 2001-04-10 2004-06-03 Barnett Stanley F Method of treating cancer
IL149462A0 (en) 2001-05-09 2002-11-10 Warner Lambert Co Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor
MXPA04005939A (es) 2002-01-22 2005-01-25 Warner Lambert Co 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-onas.
EP1496981A2 (en) 2002-04-08 2005-01-19 Merck & Co., Inc. Method of treating cancer
DE10239042A1 (de) 2002-08-21 2004-03-04 Schering Ag Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
US20040102360A1 (en) 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
MXPA05003431A (es) 2002-11-15 2005-07-05 Warner Lambert Co Quimioterapia de combinacion.
WO2004058769A2 (en) 2002-12-18 2004-07-15 Vertex Pharmaceuticals Incorporated Triazolopyridazines as protein kinases inhibitors
AU2004255934B2 (en) 2003-07-11 2010-02-25 Warner-Lambert Company Llc Isethionate salt of a selective CDK4 inhibitor
CN1871008A (zh) 2003-10-21 2006-11-29 默克公司 用于治疗神经病变性疼痛的三唑并－哒嗪化合物和它们的衍生物
NZ546011A (en) 2003-10-21 2009-09-25 Warner Lambert Co Polymorphic form of N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-benzamide
AU2005212096B2 (en) 2004-02-18 2010-12-16 Msd K.K. Nitrogenous fused heteroaromatic ring derivative
WO2005094830A1 (en) 2004-03-30 2005-10-13 Pfizer Products Inc. Combinations of signal transduction inhibitors
KR101368093B1 (ko) 2004-09-02 2014-03-14 다케다 게엠베하 트리아졸로프탈라진
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
CN101103033B (zh) 2005-01-05 2010-08-04 尼科梅德有限责任公司 作为pde2抑制剂的三唑并酞嗪
CA2591991C (en) 2005-01-05 2013-11-19 Altana Pharma Ag Triazolophthalazines
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
WO2007129161A2 (en) 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
BRPI0716880A2 (pt) 2006-09-08 2013-10-15 Pfizer Prod Inc Síntese de 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-onas
WO2008109104A1 (en) 2007-03-07 2008-09-12 The Regents Of The University Of California Bivalent inhibitors of akt protein kinase
EP2142551B1 (en) 2007-04-17 2015-10-14 Bristol-Myers Squibb Company Fused heterocyclic 11-beta-hydroxysteroid dehydrogenase type i inhibitors
EP2205242B1 (en) 2007-09-12 2015-04-15 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
HUE025976T2 (en) 2007-09-27 2016-05-30 Fund Centro Nac De Investig Oncologicas Carlos Iii Imidazolothiadiazoles for use as protein kinase inhibitors
EP2211615A4 (en) 2007-10-22 2010-10-13 Glaxosmithkline Llc PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック， インコーポレイテッド チエノピリミジン化合物の製造方法
DK2644194T3 (en) 2008-03-18 2017-07-03 Genentech Inc Combinations of an anti-HER2 antibody-drug conjugate and docetaxel
WO2010085597A1 (en) 2009-01-23 2010-07-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
JP5709766B2 (ja) 2009-03-12 2015-04-30 ジェネンテック， インコーポレイテッド 造血器腫瘍の治療のためのホスホイノシチド３キナーゼ阻害剤化合物と化学療法剤の併用
JP2012521354A (ja) 2009-03-20 2012-09-13 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
CN102361878A (zh) 2009-03-24 2012-02-22 住友化学株式会社 用于制备硼酸酯化合物的方法
US20120214828A1 (en) 2009-08-24 2012-08-23 Georgia Hatzivassiliou Determining sensitivity of cells to b-raf inhibitor treatment by detecting kras mutation and rtk expression levels
CA2776944A1 (en) 2009-10-12 2011-05-12 F. Hoffmann-La Roche Ag Combinations of a pi3k inhibitor and a mek inhibitor
WO2011130654A1 (en) 2010-04-16 2011-10-20 Genentech, Inc. Fox03a as predictive biomarker for pi3k/akt kinase pathway inhibitor efficacy

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
WO2009007029A1 (de) * 2007-07-11 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Imidazo-, pyrazolopyrazine und imidazotriazine zur behandlung hämatologischer erkrankungen
WO2009060197A1 (en) * 2007-11-08 2009-05-14 Centro Nacional De Investigaciones Oncologicas (Cnio) Imidazopyridazines for use as protein kinase inhibitors

Also Published As

Publication number Publication date
IL220701A0 (en) 2012-08-30
US20130065881A1 (en) 2013-03-14
CN102791715A (zh) 2012-11-21
AU2010338038A1 (en) 2012-07-26
AU2010338038B2 (en) 2015-07-09
KR20120111739A (ko) 2012-10-10
JP5913126B2 (ja) 2016-04-27
NZ601033A (en) 2014-02-28
PH12012501361A1 (en) 2012-10-22
SG182297A1 (en) 2012-08-30
CA2786002C (en) 2018-10-02
WO2011080510A1 (en) 2011-07-07
JP2013516399A (ja) 2013-05-13
EP2519526B1 (en) 2014-03-26
EP2519526A1 (en) 2012-11-07
US9682991B2 (en) 2017-06-20
CA2786002A1 (en) 2011-07-07
WO2011080510A8 (en) 2011-09-22

Similar Documents

Publication Publication Date Title
CN102791715B (zh) 用作激酶抑制剂的三环化合物
CN113527299B (zh) 一类含氮稠环类化合物、制备方法和用途
KR100710402B1 (ko) 3환식 축합 이항환 화합물, 그 제조법 및 그것을 함유하는의약
RU2598840C2 (ru) Новые соединения
AU2019222026A1 (en) Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
WO2013005057A1 (en) New compounds
PT2651951E (pt) Compostos tricíclicos do inibidor pi3k e processos para a sua utilização
AU2014249192A1 (en) BET bromodomain inhibitors and therapeutic methods using the same
CN102947302A (zh) 三唑并[4，5-b]吡啶衍生物
JP2020515571A (ja) 共有結合性メニン阻害剤としてのピペリジン
WO2010085597A1 (en) Macrocyclic compounds and their use as kinase inhibitors
JP2020519667A (ja) ＬＳＤ−１インヒビターとしてのピロロ〔２，３−ｃ〕ピリジン及び関連類似体
EP4223759B1 (en) Pyrazolopyridazinone compound, and pharmaceutical composition and use thereof
CN113939518A (zh) 作为激酶抑制剂的稠合三环化合物
WO2013004984A1 (en) Tricyclic compounds for use as kinase inhibitors
WO2022143576A1 (zh) 一种吡唑并喹唑啉类化合物、其制备方法及应用
CA3231988A1 (en) Azaindazole macrocycle compound and use thereof
WO2012098387A1 (en) 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors
WO2013005041A1 (en) Tricyclic heterocyclic compounds as kinase inhibitors
TWI894448B (zh) Ctla-4小分子降解劑及其應用
JP2001233876A (ja) 三環式縮合異項環化合物、その製造法およびその医薬
WO2012020217A1 (en) Amino- imidazolothiadiazoles for use as protein or lipid kinase inhibitors
EA041973B1 (ru) Замещенные бициклические гетероциклические соединения в качестве ингибиторов prmt5

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C53 Correction of patent of invention or patent application
CB02 Change of applicant information

Address after: Madrid

Applicant after: FUNDACIoN CENTRO NACIONAL DE INVESTIGACIONES ONCOLoGICAS CARLOS III

Address before: Madrid

Applicant before: CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO)

COR Change of bibliographic data

Free format text: CORRECT: APPLICANT; FROM: CT NAC DE INVESTIGACIONES ONCO TO: CARLOS III NATIONAL CANCER RESEARCH CENTER FOUNDATION

Free format text: CORRECT: ADDRESS; FROM:

C14 Grant of patent or utility model
GR01 Patent grant
CP01 Change in the name or title of a patent holder
CP01 Change in the name or title of a patent holder

Address after: Madrid

Patentee after: National public sector foundation Carlos III National Oncology Research Center (f.s.p.cnio)

Address before: Madrid

Patentee before: FUNDACIoN CENTRO NACIONAL DE INVESTIGACIONES ONCOLoGICAS CARLOS III

CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160427