JP5913126B2 - キナーゼ阻害剤としての使用のための三環式化合物 - Google Patents

キナーゼ阻害剤としての使用のための三環式化合物 Download PDF

Info

Publication number
JP5913126B2
JP5913126B2 JP2012546501A JP2012546501A JP5913126B2 JP 5913126 B2 JP5913126 B2 JP 5913126B2 JP 2012546501 A JP2012546501 A JP 2012546501A JP 2012546501 A JP2012546501 A JP 2012546501A JP 5913126 B2 JP5913126 B2 JP 5913126B2
Authority
JP
Japan
Prior art keywords
methyl
cyclopenta
phenyl
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.)
Active
Application number
JP2012546501A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013516399A (ja
JP2013516399A5 (https=
Inventor
フェルナンデス， ホアキン パストル
フェルナンデス， ホアキン パストル
リーマ， フランシスコ ハビエル ラモス
リーマ， フランシスコ ハビエル ラモス
イゲラス， アナ イサベル エルナンデス
イゲラス， アナ イサベル エルナンデス
ゴンサレス， ソニア マルティネス
ゴンサレス， ソニア マルティネス
エルナンド， ホセ イグナシオ マルティン
エルナンド， ホセ イグナシオ マルティン
カール−グスタベ ピエーレ サルステ，
カール−グスタベ ピエーレ サルステ，
カンタラピエドラ， エステール ゴンザレス
カンタラピエドラ， エステール ゴンザレス
アパリシオ， カルメン ブランコ
アパリシオ， カルメン ブランコ
エルゲタ， アントニオ ロドリゲス
エルゲタ， アントニオ ロドリゲス
コリャソ， アナ マリア ガルシア
コリャソ， アナ マリア ガルシア
セラーノ， アントニオ サルガド
セラーノ， アントニオ サルガド
マリーニョ， ベアトリス ノーヤ
マリーニョ， ベアトリス ノーヤ
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.)
Centro Nacional de Investigaciones Oncologicas CNIO
Original Assignee
Centro Nacional de Investigaciones Oncologicas CNIO
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 Centro Nacional de Investigaciones Oncologicas CNIO filed Critical Centro Nacional de Investigaciones Oncologicas CNIO
Publication of JP2013516399A publication Critical patent/JP2013516399A/ja
Publication of JP2013516399A5 publication Critical patent/JP2013516399A5/ja
Application granted granted Critical
Publication of JP5913126B2 publication Critical patent/JP5913126B2/ja
Active 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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
JP2012546501A 2009-12-31 2010-12-31 キナーゼ阻害剤としての使用のための三環式化合物 Active JP5913126B2 (ja)

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 (3)

Publication Number Publication Date
JP2013516399A JP2013516399A (ja) 2013-05-13
JP2013516399A5 JP2013516399A5 (https=) 2015-04-23
JP5913126B2 true JP5913126B2 (ja) 2016-04-27

Family

ID=42200029

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012546501A Active JP5913126B2 (ja) 2009-12-31 2010-12-31 キナーゼ阻害剤としての使用のための三環式化合物

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
WO2013005057A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) New compounds
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
MX2015005375A (es) 2012-11-07 2015-07-21 Hoffmann La Roche Compuestos de triazolo.
CN113855675A (zh) * 2018-05-22 2021-12-31 郑州大学第一附属医院 基于胆囊癌标志物的试剂盒及药物
EP4230628B1 (en) * 2020-10-16 2025-10-15 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
KR20240110971A (ko) 2021-12-01 2024-07-16 푼다시온 델 섹토르 푸블리코 에스타탈 센트로 나시오날 데 인베스티가시오네스 온콜로지카스 카를로스 3 (에프.에스.피 씨엔아이오) 화합물
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 (https=) 1979-10-29 1982-09-08 Dow Chemical Co
FI81350C (fi) 1982-01-18 1990-10-10 Lepetit Spa Analogfoerfarande foer framstaellning av nya, farmakologiskt aktiva 6-substituerade s-triatsolo/3,4-a/ ftalazinderivat.
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.
DE69411616T2 (de) 1993-04-12 1998-11-19 Takeda Chemical Industries Ltd Triazolopyridazin-Derivate, ihre Herstellung und Verwendung
ES2194205T3 (es) 1996-07-25 2003-11-16 Merck Sharp & Dohme Derivados de triazolo-piridazina sustituidos como ligandos para los receptores gaba.
AU724076B2 (en) 1996-07-25 2000-09-14 Merck Sharp & Dohme Limited Substituted triazolo pyridazine derivatives as inverse agonists of the GABAAalpha5 receptor subtype
ES2137113B1 (es) 1997-07-29 2000-09-16 Almirall Prodesfarma Sa Nuevos derivados de triazolo-piridazinas heterociclicos.
AU1041599A (en) 1997-11-13 1999-06-07 Jose Luis Castro Pineiro 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
ATE377597T1 (de) 1999-07-09 2007-11-15 Glaxo Group Ltd Anilinochinazoline als protein-tyrosin- kinasehemmer
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
PL204958B1 (pl) 2000-06-30 2010-02-26 Glaxo Group Ltd Ditosylany związków chinazolinowych, środek farmaceutyczny i zastosowanie tych związków
DZ3401A1 (fr) 2000-07-19 2002-01-24 Warner Lambert Co Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques
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
US20040102455A1 (en) * 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
WO2002083140A1 (en) 2001-04-10 2002-10-24 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
ES2251677T3 (es) 2002-01-22 2006-05-01 Warner-Lambert Company Llc 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
JP2006508974A (ja) 2002-11-15 2006-03-16 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー 癌を治療するためのｍｅｋ阻害剤およびカペシタビン（ｃａｐｅｃｉｔａｂｉｎｅ）を含む併用化学療法
WO2004058769A2 (en) 2002-12-18 2004-07-15 Vertex Pharmaceuticals Incorporated Triazolopyridazines as protein kinases inhibitors
ATE412650T1 (de) 2003-07-11 2008-11-15 Warner Lambert Co Isethionat salz eines selektiven cdk4 inhibitors
WO2005040098A1 (en) 2003-10-21 2005-05-06 Warner-Lambert Company Llc Polymorphic form of n-[(r)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-benzamide
EP1677799A4 (en) 2003-10-21 2008-09-10 Merck & Co Inc TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF FOR THE TREATMENT OF NEUROPATHIC PAIN
AU2005212096B2 (en) 2004-02-18 2010-12-16 Msd K.K. Nitrogenous fused heteroaromatic ring derivative
CA2561516A1 (en) 2004-03-30 2005-10-13 Pfizer Products Inc. Combinations of signal transduction inhibitors
AU2005279221C9 (en) 2004-09-02 2012-08-23 Takeda Gmbh Triazolophthalazines
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
BRPI0606379A2 (pt) 2005-01-05 2009-06-23 Nycomed Gmbh triazolftalazinas
EP1874775B1 (en) 2005-01-05 2012-10-10 Nycomed GmbH Triazolophthalazines as pde2-inhibitors
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
MX2008013578A (es) 2006-04-26 2009-03-23 Hoffmann La Roche Derivados de tieno [3,2-d]pirimidina utiles como inhibidores de fosfatidilinositol 3-cinasa(p13k).
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
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
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
HRP20151128T1 (hr) 2007-09-27 2015-11-20 Fundación Centro Nacional De Investigaciones Oncológicas Carlos Iii Imidazolotiadiazoli za uporabu kao inhibitori protein kinaze
US20100311736A1 (en) 2007-10-22 2010-12-09 Glaxosmithkline Llc Pyridosulfonamide derivatives as p13 kinase inhibitors
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
EP2217601A1 (en) 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
NZ602675A (en) 2008-03-18 2014-03-28 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
CN102369011A (zh) 2009-03-12 2012-03-07 健泰科生物技术公司 用于治疗造血恶性肿瘤的磷酸肌醇3-激酶抑制剂化合物与化学治疗剂的组合
MX2011009796A (es) 2009-03-20 2011-12-14 Amgen Inc Inhibidores de la cinasa pi3.
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
IN2012DN01403A (https=) 2009-08-24 2015-06-05 Genentech Inc
KR101489045B1 (ko) 2009-10-12 2015-02-02 에프. 호프만-라 로슈 아게 Ｐｉ3ｋ 억제자 및 ｍｅｋ 억제자의 조합
MX2012011887A (es) 2010-04-16 2012-11-30 Genentech Inc Foxo 3a como biomarcador predictivo para la eficacia del inhibidor de la via de quinasa pi3k/akt.

Also Published As

Publication number Publication date
US20130065881A1 (en) 2013-03-14
EP2519526B1 (en) 2014-03-26
WO2011080510A1 (en) 2011-07-07
NZ601033A (en) 2014-02-28
US9682991B2 (en) 2017-06-20
KR20120111739A (ko) 2012-10-10
AU2010338038B2 (en) 2015-07-09
PH12012501361A1 (en) 2012-10-22
CN102791715B (zh) 2016-04-27
JP2013516399A (ja) 2013-05-13
AU2010338038A1 (en) 2012-07-26
CA2786002C (en) 2018-10-02
EP2519526A1 (en) 2012-11-07
CA2786002A1 (en) 2011-07-07
WO2011080510A8 (en) 2011-09-22
IL220701A0 (en) 2012-08-30
CN102791715A (zh) 2012-11-21
SG182297A1 (en) 2012-08-30

Similar Documents

Publication Publication Date Title
JP5913126B2 (ja) キナーゼ阻害剤としての使用のための三環式化合物
RU2598840C2 (ru) Новые соединения
DK2989106T3 (en) CONDENSED HETEROCYCLIC COMPOUNDS AS PROTEINKINASE INHIBITORS
JP5410431B2 (ja) イミダゾロチアジアゾール類のプロテインキナーゼ阻害剤としての使用
ES2627703T3 (es) Inhibidores de PI3·quinasa
KR101792837B1 (ko) 키나아제 억제제로서 사용을 위한 이미다조피라진
WO2013005057A1 (en) New compounds
US20130131057A1 (en) New bicyclic compounds as pi3-k and mtor inhibitors
JP2013519719A (ja) トリアゾロ［４，５−ｂ］ピリジン誘導体
WO2010085597A1 (en) Macrocyclic compounds and their use as kinase inhibitors
JP7462951B2 (ja) Ｊａｋ阻害剤
WO2012020215A1 (en) Amino- imidazolothiadiazoles for use as protein or lipid kinase inhibitors
CA3191362A1 (en) Pyrazolopyridazinone compound, and pharmaceutical composition and use thereof
WO2013004984A1 (en) Tricyclic compounds for use as kinase inhibitors
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
WO2012020217A1 (en) Amino- imidazolothiadiazoles for use as protein or lipid kinase inhibitors

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20131225

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20141125

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20141127

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150225

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20150225

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150317

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150617

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150714

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151014

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20151014

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20160302

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160401

R150 Certificate of patent or registration of utility model

Ref document number: 5913126

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: R3D02

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250