CN101622248B - 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑 - Google Patents

用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑 Download PDF

Info

Publication number
CN101622248B
CN101622248B CN2007800489092A CN200780048909A CN101622248B CN 101622248 B CN101622248 B CN 101622248B CN 2007800489092 A CN2007800489092 A CN 2007800489092A CN 200780048909 A CN200780048909 A CN 200780048909A CN 101622248 B CN101622248 B CN 101622248B
Authority
CN
China
Prior art keywords
optionally substituted
triazole
diamines
pyrimidine
thiotolene
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
CN2007800489092A
Other languages
English (en)
Chinese (zh)
Other versions
CN101622248A (zh
Inventor
戴恩·高夫
张静
拉金德尔·辛格
萨卡·霍兰
余家新
希洛·海克洛特
丁平羽
乔尼·李特瓦克
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.)
Rigel Pharmaceuticals Inc
Original Assignee
Rigel Pharmaceuticals Inc
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 Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of CN101622248A publication Critical patent/CN101622248A/zh
Application granted granted Critical
Publication of CN101622248B publication Critical patent/CN101622248B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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 two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN2007800489092A 2006-12-29 2007-12-28 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑 Expired - Fee Related CN101622248B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US88287506P 2006-12-29 2006-12-29
US60/882,875 2006-12-29
US97544307P 2007-09-26 2007-09-26
US60/975,443 2007-09-26
PCT/US2007/089153 WO2008083354A1 (en) 2006-12-29 2007-12-28 N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors

Publications (2)

Publication Number Publication Date
CN101622248A CN101622248A (zh) 2010-01-06
CN101622248B true CN101622248B (zh) 2013-04-17

Family

ID=39203174

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2007800489092A Expired - Fee Related CN101622248B (zh) 2006-12-29 2007-12-28 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑

Country Status (8)

Country Link
US (2) US9650391B2 (OSRAM)
EP (2) EP2074115B1 (OSRAM)
JP (2) JP5567837B2 (OSRAM)
CN (1) CN101622248B (OSRAM)
AU (1) AU2007342005A1 (OSRAM)
CA (1) CA2710046C (OSRAM)
ES (2) ES2607065T3 (OSRAM)
WO (1) WO2008083354A1 (OSRAM)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007030680A2 (en) * 2005-09-07 2007-03-15 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as axl inhibitors
EP2114954B1 (en) * 2006-12-29 2013-02-13 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
ME01832B (me) * 2006-12-29 2014-12-20 Rigel Pharmaceuticals Inc Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori
US8012965B2 (en) 2006-12-29 2011-09-06 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
US9650391B2 (en) * 2006-12-29 2017-05-16 Rigel Pharmaceuticals Inc. N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors
ES2656496T3 (es) 2006-12-29 2018-02-27 Rigel Pharmaceuticals, Inc. Triazoles sustituidos útiles como inhibidores de AXL
EP2205592B1 (en) * 2007-10-26 2013-05-08 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
MX2010008926A (es) 2008-02-15 2011-02-23 Rigel Pharmaceuticals Inc Compuestos de pirimidin-2-amina y su uso como inhibidores de jak cinasas.
SI2328888T1 (sl) 2008-07-09 2013-03-29 Rigel Pharmaceuticals, Inc. Premoščeni biciklični heteroaril substituirani triazoli, uporabni kot inhibitorji Axl
JP5592884B2 (ja) 2008-07-09 2014-09-17 ライジェル ファーマシューティカルズ, インコーポレイテッド Axl阻害剤として有用な多環式ヘテロアリール置換トリアゾール
WO2010083465A1 (en) * 2009-01-16 2010-07-22 Rigel Pharmaceuticals, Inc. Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer
NZ627586A (en) 2012-01-31 2016-08-26 Daiichi Sankyo Co Ltd Pyridone derivatives
CA2879542A1 (en) 2012-07-25 2014-01-30 Salk Institute For Biological Studies Regulating the interaction between tam ligands and lipid membranes with exposed phosphatidylserine
GB201213556D0 (en) 2012-07-31 2012-09-12 Luminectric Ltd Cases for portable electronic devices
CA2929188C (en) 2013-11-20 2022-08-09 Signalchem Lifesciences Corp. Quinazoline derivatives as tam family kinase inhibitors
US10233176B2 (en) 2013-11-27 2019-03-19 Signalchem Lifesciences Corporation Aminopyridine derivatives as TAM family kinase inhibitors
TWI723572B (zh) 2014-07-07 2021-04-01 日商第一三共股份有限公司 具有四氫吡喃基甲基之吡啶酮衍生物及其用途
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
GB201509338D0 (en) 2015-05-29 2015-07-15 Bergenbio As Combination therapy
WO2017027717A1 (en) 2015-08-12 2017-02-16 Incyte Corporation Bicyclic fused pyrimidine compounds as tam inhibitors
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
US20190099413A1 (en) 2016-02-26 2019-04-04 Ono Pharmaceutical Co., Ltd. Drug for cancer therapy characterized in that axl inhibitor and immune checkpoint inhibitor are administered in combination
EP3436461B1 (en) 2016-03-28 2023-11-01 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
EP3673907A4 (en) 2017-08-23 2020-08-19 ONO Pharmaceutical Co., Ltd. CANCER TREATMENT PHARMACEUTICAL INCLUDING AX1 INHIBITOR AS AN EFFECTIVE INGREDIENT
MY208007A (en) 2017-09-27 2025-04-04 Incyte Corp Salts of pyrrolotriazine derivatives useful as tam inhibitors
JP7223998B2 (ja) 2017-10-13 2023-02-17 小野薬品工業株式会社 Axl阻害剤を有効成分として含む固形がん治療剤
AR117600A1 (es) 2018-06-29 2021-08-18 Incyte Corp Formulaciones de un inhibidor de axl / mer
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
GB201912059D0 (en) 2019-08-22 2019-10-09 Bergenbio As Combaination therapy of a patient subgroup
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4114401A1 (en) 2020-03-06 2023-01-11 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
GB202004189D0 (en) 2020-03-23 2020-05-06 Bergenbio As Combination therapy
EP4132652A1 (en) 2020-04-08 2023-02-15 BerGenBio ASA Axl inhibitors for antiviral therapy
GB202006072D0 (en) 2020-04-24 2020-06-10 Bergenbio Asa Method of selecting patients for treatment with cmbination therapy
GB202104037D0 (en) 2021-03-23 2021-05-05 Bergenbio Asa Combination therapy
GB202209285D0 (en) 2022-06-24 2022-08-10 Bergenbio Asa Dosage regimen for AXL inhibitor
AR129722A1 (es) 2022-06-28 2024-09-18 Arcus Biosciences Inc Compuestos inhibidores de axl
WO2024051667A1 (zh) * 2022-09-05 2024-03-14 南京正大天晴制药有限公司 具有axl抑制活性的取代三唑化合物
WO2024218236A1 (en) * 2023-04-18 2024-10-24 Centre National De La Recherche Scientifique 3,5-diaminotriazole derivatives and uses thereof for treating ocular diseases

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004046120A2 (en) * 2002-11-15 2004-06-03 Vertex Pharmaceuticals Incorporated Diaminotriazoles useful as inhibitors of protein kinases

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1403866A (en) 1971-12-06 1975-08-28 Wyeth John & Brother Ltd Derivatives of 3-amino-1,2,4-triazoles
WO1995003286A1 (en) 1993-07-23 1995-02-02 The Green Cross Corporation Triazole derivative and pharmaceutical use thereof
JP2002241368A (ja) 1997-02-18 2002-08-28 Shionogi & Co Ltd 新規ベンゾラクタム誘導体およびそれを含有する医薬組成物
GB9918180D0 (en) 1999-08-02 1999-10-06 Smithkline Beecham Plc Novel compositions
CA2432870A1 (en) 2000-12-22 2002-07-25 Ronghui Lin Substituted triazole diamine derivatives as kinase inhibitors
DE10123586A1 (de) * 2001-05-08 2002-11-28 Schering Ag 3,5-Diamino-1,2,4-triazole als Kinase Inhibitoren
TW201041580A (en) 2001-09-27 2010-12-01 Alcon Inc Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma
EP1504047B1 (en) 2002-05-03 2007-12-12 Janssen Pharmaceutica N.V. Polymeric microemulsions
CA2501719C (en) 2002-08-06 2013-02-05 Toray Industries, Inc. Remedy or preventive for kidney disease and method of diagnosing kidney disease
WO2004039955A2 (en) 2002-10-29 2004-05-13 Rigel Pharmaceuticals, Inc. Modulators of angiogenesis and tumorigenesis
AR045731A1 (es) 2003-08-06 2005-11-09 Vertex Pharma Compuestos de aminotriazol utiles como inhibidores de quinasas de proteinas
US20060100259A1 (en) 2004-02-11 2006-05-11 Palmer David C Process for the preparation of substituted triazole compounds
NZ580450A (en) * 2004-09-17 2011-06-30 Vertex Pharma Diaminotriazole Compounds Useful as Protein Kinase Inhibitors
CA2584752A1 (en) 2004-10-21 2006-05-04 Vertex Pharmaceuticals Incorporated Triazoles useful as inhibitors of protein kinases
WO2007030680A2 (en) 2005-09-07 2007-03-15 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as axl inhibitors
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
US8012965B2 (en) 2006-12-29 2011-09-06 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
ES2656496T3 (es) 2006-12-29 2018-02-27 Rigel Pharmaceuticals, Inc. Triazoles sustituidos útiles como inhibidores de AXL
ME01832B (me) * 2006-12-29 2014-12-20 Rigel Pharmaceuticals Inc Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori
US9650391B2 (en) 2006-12-29 2017-05-16 Rigel Pharmaceuticals Inc. N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors
EP2114954B1 (en) 2006-12-29 2013-02-13 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
MX2009010127A (es) * 2007-03-22 2009-11-05 Vertex Pharma Compuestos utiles como inhibidores de janus cinasas.
JP2010529990A (ja) 2007-06-15 2010-09-02 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤およびそれを使用するための方法
EP2205592B1 (en) 2007-10-26 2013-05-08 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
MX2010008926A (es) 2008-02-15 2011-02-23 Rigel Pharmaceuticals Inc Compuestos de pirimidin-2-amina y su uso como inhibidores de jak cinasas.
JP5592884B2 (ja) 2008-07-09 2014-09-17 ライジェル ファーマシューティカルズ, インコーポレイテッド Axl阻害剤として有用な多環式ヘテロアリール置換トリアゾール
SI2328888T1 (sl) 2008-07-09 2013-03-29 Rigel Pharmaceuticals, Inc. Premoščeni biciklični heteroaril substituirani triazoli, uporabni kot inhibitorji Axl
WO2010083465A1 (en) 2009-01-16 2010-07-22 Rigel Pharmaceuticals, Inc. Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004046120A2 (en) * 2002-11-15 2004-06-03 Vertex Pharmaceuticals Incorporated Diaminotriazoles useful as inhibitors of protein kinases

Also Published As

Publication number Publication date
CA2710046C (en) 2016-02-09
HK1174631A1 (en) 2013-06-14
JP2010514809A (ja) 2010-05-06
WO2008083354A1 (en) 2008-07-10
CA2710046A1 (en) 2008-07-10
JP5890445B2 (ja) 2016-03-22
EP2484679A3 (en) 2012-10-10
ES2607065T3 (es) 2017-03-29
EP2074115B1 (en) 2018-03-07
EP2074115A1 (en) 2009-07-01
US8796259B2 (en) 2014-08-05
US20080182862A1 (en) 2008-07-31
ES2672172T3 (es) 2018-06-12
AU2007342005A1 (en) 2008-07-10
CN101622248A (zh) 2010-01-06
JP5567837B2 (ja) 2014-08-06
EP2484679A2 (en) 2012-08-08
US20130090330A1 (en) 2013-04-11
EP2484679B1 (en) 2016-09-28
JP2014111641A (ja) 2014-06-19
US9650391B2 (en) 2017-05-16

Similar Documents

Publication Publication Date Title
CN101622248B (zh) 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑
CN101622246B (zh) 可用作axl抑制剂的多环杂芳基取代的三唑
CN101622252B (zh) 用作axl抑制剂的取代三唑
CA2704052C (en) Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
JP2010514809A5 (OSRAM)
WO2008045978A1 (en) Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
CA2710043A1 (en) Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
AU2014200825B2 (en) N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors
AU2014200824B2 (en) Substituted triazoles useful as Axl inhibitors
HK1174631B (en) N3-heteroaryl substituted triazoles and n5-heteroaryl substitued triazoles useful as axl inhibitors
HK1132737B (en) Polycyclic heteroaryl substituted triazoles useful as axl inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20130417

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