CA2786002C - Tricyclic compounds for use as kinase inhibitors - Google Patents

Tricyclic compounds for use as kinase inhibitors Download PDF

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Publication number
CA2786002C
CA2786002C CA2786002A CA2786002A CA2786002C CA 2786002 C CA2786002 C CA 2786002C CA 2786002 A CA2786002 A CA 2786002A CA 2786002 A CA2786002 A CA 2786002A CA 2786002 C CA2786002 C CA 2786002C
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optionally substituted
alkyl
substituents selected
groups
ring
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CA2786002A
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English (en)
French (fr)
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CA2786002A1 (en
Inventor
Joaquin Pastor Fernandez
Carmen Blanco Aparicio
Antonio Rodriguez Hergueta
Jose Ignacio Martin Hernando
Francisco Javier Ramos Lima
Ana Isabel Hernandez Higueras
Carl-Gustave Pierre Saluste
Esther Gonzalez Cantalapiedra
Sonia Martinez Gonzalez
Antonio Salgado Serrano
Beatriz Noya Marino
Ana Maria Garcia Collazo
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Fundacion del Sector Publico Estatal Centro Nacional de Investigaciones Oncologicas Carlos III FSP CNIO
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Spanish National Cancer Research Centre
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    • 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
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    • 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
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • AIDS & HIV (AREA)
  • Psychiatry (AREA)
CA2786002A 2009-12-31 2010-12-31 Tricyclic compounds for use as kinase inhibitors Active CA2786002C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09380202.3 2009-12-31
EP09380202 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
CA2786002A1 CA2786002A1 (en) 2011-07-07
CA2786002C true CA2786002C (en) 2018-10-02

Family

ID=42200029

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2786002A Active CA2786002C (en) 2009-12-31 2010-12-31 Tricyclic compounds for use as kinase inhibitors

Country Status (12)

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

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
WO2013005057A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
WO2013005041A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) Tricyclic heterocyclic compounds as kinase inhibitors
WO2013004984A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncologicas (Cnio) Tricyclic compounds for use as kinase inhibitors
MX2015005375A (es) 2012-11-07 2015-07-21 Hoffmann La Roche Compuestos de triazolo.
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

Family Cites Families (65)

* 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 (enExample) 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 (enExample) 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
EP0915877A1 (en) 1996-07-25 1999-05-19 MERCK SHARP & DOHME LTD. SUBSTITUTED TRIAZOLO PYRIDAZINE DERIVATIVES AS INVERSE AGONISTS OF THE GABA A?$g(a)5 RECEPTOR SUBTYPE
EP0915875B1 (en) 1996-07-25 2003-04-09 MERCK SHARP & DOHME LTD. Substituted triazolo-pyridazine derivatives as ligands for gaba receptors
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
CA2413134C (en) 2000-06-30 2010-05-11 Glaxo Group Limited Quinazoline ditosylate salt compounds
AU7349801A (en) 2000-07-19 2002-01-30 Warner Lambert Co Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids
US7141576B2 (en) 2001-01-16 2006-11-28 Smithkline Beecham (Cork) Limited Cancer treatment method
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
JP2004527531A (ja) 2001-04-10 2004-09-09 メルク　エンド　カムパニー　インコーポレーテッド 癌を治療する方法
WO2002083140A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
IL149462A0 (en) 2001-05-09 2002-11-10 Warner Lambert Co Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor
NZ534069A (en) 2002-01-22 2007-03-30 Warner Lambert Co 2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones to be used to treat neurodegenerative disorders, viruses and cancer
AU2003226301A1 (en) 2002-04-08 2003-10-20 Merck And 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
EP1562601A1 (en) 2002-11-15 2005-08-17 Warner-Lambert Company LLC Combination chemotherapy comprising a mek inhibitor and capecitabine for treating cancer
AU2003297161B8 (en) 2002-12-18 2011-03-31 Vertex Pharmaceuticals Incorporated Triazolopyridazines as protein kinases inhibitors
DE602004017474D1 (de) 2003-07-11 2008-12-11 Warner Lambert Co Isethionat salz eines selektiven cdk4 inhibitors
KR101013932B1 (ko) 2003-10-21 2011-02-14 워너-램버트 캄파니 엘엘씨 Ｎ-[(ｒ)-2,3-디히드록시-프로폭시]-3,4-디플루오로-2-(2-플루오로-4-요오도페닐아미노)-벤자미드 다형체 형태
US20070213338A1 (en) 2003-10-21 2007-09-13 Lebsack Alec D Triazolo-Pyridazine Compounds and Derivatives Thereof Useful in the Treatment of Neuropathic Pain
WO2005077953A1 (ja) 2004-02-18 2005-08-25 Banyu Pharmaceutical Co., Ltd. 含窒素縮合へテロ芳香環誘導体
BRPI0509580A (pt) 2004-03-30 2007-11-27 Pfizer Prod Inc combinações de inibidores de transdução de sinal
WO2006024640A2 (en) 2004-09-02 2006-03-09 Altana Pharma Ag Triazolophthalazines
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
MX2007008137A (es) 2005-01-05 2007-07-19 Altana Pharma Ag Triazoloftalazinas como inhibidores de pde2.
JP5130053B2 (ja) 2005-01-05 2013-01-30 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング トリアゾロフタラジン
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
KR101533461B1 (ko) 2006-04-26 2015-07-02 에프. 호프만-라 로슈 아게 Ｐｉ３ｋ저해제로 유용한 티에노［3,2-ｄ］피리미딘 유도체
KR20090052385A (ko) 2006-09-08 2009-05-25 화이자 프로덕츠 인크. 2-（피리딘-2-일아미노）-피리도［2,3-ｄ］피리미딘-7-온의합성
WO2008109104A1 (en) 2007-03-07 2008-09-12 The Regents Of The University Of California Bivalent inhibitors of akt protein kinase
US8546394B2 (en) * 2007-04-17 2013-10-01 Bristol-Myers Squibb Company Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors
DE102007032349A1 (de) * 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung
BRPI0816769A2 (pt) 2007-09-12 2016-11-29 Hoffmann La Roche combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso
DK2193133T3 (en) 2007-09-27 2015-10-05 Fundacion Ct Nac Investigaciones Oncologicas Carlos Iii IMIDAZOLOTHIADIAZOLES USED AS PROTEINKINASE INHIBITORS
JP2011500823A (ja) 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体
WO2009055730A1 (en) 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds
US20110046127A1 (en) 2007-11-08 2011-02-24 Paolo Pevarello Imidazopyridazines for Use as Protein Kinase Inhibitors
NZ587706A (en) 2008-03-18 2012-12-21 Genentech Inc Combinations of an anti-her2 antibody-drug conjugate and chemotherapeutic agents, and methods of use
US8765727B2 (en) 2009-01-23 2014-07-01 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
CA2755285C (en) 2009-03-20 2014-02-11 Yunxin Y. Bo Inhibitors of pi3 kinase
SG172951A1 (en) 2009-03-24 2011-08-29 Sumitomo Chemical Co Method for manufacturing a boronic acid ester compound
CN102859355B (zh) 2009-08-24 2015-10-07 基因泰克公司 通过检测kras突变和rtk表达水平来测定细胞对b-raf抑制剂治疗的敏感性
AU2010314287A1 (en) 2009-10-12 2012-05-03 F. Hoffmann-La Roche Ag Combinations of a PI3K inhibitor and a MEK inhibitor
KR20130058672A (ko) 2010-04-16 2013-06-04 제넨테크, 인크. ＰＩ3Ｋ/ＡＫＴ 키나제 경로 억제제 효능에 대한 예측 바이오마커로서의 ＦＯＸＯ３ａ

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WO2011080510A1 (en) 2011-07-07
IL220701A0 (en) 2012-08-30
JP2013516399A (ja) 2013-05-13
SG182297A1 (en) 2012-08-30
CN102791715B (zh) 2016-04-27
US9682991B2 (en) 2017-06-20
EP2519526B1 (en) 2014-03-26
CA2786002A1 (en) 2011-07-07
AU2010338038A1 (en) 2012-07-26
CN102791715A (zh) 2012-11-21
US20130065881A1 (en) 2013-03-14
WO2011080510A8 (en) 2011-09-22
JP5913126B2 (ja) 2016-04-27
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