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 PDFInfo
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- 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
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- Prior art keywords
- optionally substituted
- triazole
- diamines
- pyrimidine
- thiotolene
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- 0 *N(*)C(N1)NNC1N(*)* Chemical compound *N(*)C(N1)NNC1N(*)* 0.000 description 1
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- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic 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
- C07D495/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/12—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic 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
- C07D407/14—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- C07D487/02—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 two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic 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
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Pregnancy & Childbirth (AREA)
- Gynecology & Obstetrics (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Immunology (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)
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 (enExample) |
| EP (2) | EP2074115B1 (enExample) |
| JP (2) | JP5567837B2 (enExample) |
| CN (1) | CN101622248B (enExample) |
| AU (1) | AU2007342005A1 (enExample) |
| CA (1) | CA2710046C (enExample) |
| ES (2) | ES2672172T3 (enExample) |
| WO (1) | WO2008083354A1 (enExample) |
Families Citing this family (40)
| 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 |
| CA2710230C (en) | 2006-12-29 | 2016-02-23 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| ES2406930T3 (es) | 2006-12-29 | 2013-06-10 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos con arilo bicíclico y heteroarilo bicíclico útiles como inhibidores de AXL |
| ES2558477T3 (es) | 2006-12-29 | 2016-02-04 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos útiles como inhibidores de AXL |
| PL2078010T3 (pl) | 2006-12-29 | 2014-07-31 | Rigel Pharmaceuticals Inc | Triazole podstawione policyklicznym heteroarylem użyteczne jako inhibitory Axl |
| US9650391B2 (en) * | 2006-12-29 | 2017-05-16 | Rigel Pharmaceuticals Inc. | N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors |
| SI2205592T1 (sl) * | 2007-10-26 | 2013-09-30 | Rigel Pharmaceuticals, Inc. | Triazoli substituirani s policikličnim arilom in triazoli substituirani s policikličnim heteroarilom uporabni kot Axl inhibitorji |
| MX2010008926A (es) | 2008-02-15 | 2011-02-23 | Rigel Pharmaceuticals Inc | Compuestos de pirimidin-2-amina y su uso como inhibidores de jak cinasas. |
| EP2326641B1 (en) | 2008-07-09 | 2014-09-03 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2730251C (en) | 2008-07-09 | 2016-08-09 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| US8546433B2 (en) * | 2009-01-16 | 2013-10-01 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
| HUE031624T2 (en) | 2012-01-31 | 2017-07-28 | Daiichi Sankyo Co Ltd | Pyridone derivative |
| US20150164800A1 (en) | 2012-07-25 | 2015-06-18 | Xetrios Therapeutics, Inc. | Regulating the interaction between tam ligands and lipid membranes with exposed phosphatidyl serine |
| GB201213556D0 (en) | 2012-07-31 | 2012-09-12 | Luminectric Ltd | Cases for portable electronic devices |
| AU2014353006B2 (en) | 2013-11-20 | 2019-04-04 | Signalchem Life Sciences Corp. | Quinazoline derivatives as TAM family kinase inhibitors |
| JP6496731B2 (ja) | 2013-11-27 | 2019-04-03 | シグナルケム・ライフサイエンシーズ・コーポレイションSignalchem Lifesciences Corporation | Tamファミリーキナーゼ阻害剤としてのアミノピリジン誘導体 |
| TWI690525B (zh) | 2014-07-07 | 2020-04-11 | 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 |
| US10053465B2 (en) | 2015-08-26 | 2018-08-21 | Incyte Corporation | Pyrrolopyrimidine derivatives as TAM inhibitors |
| JP6885390B2 (ja) | 2016-02-26 | 2021-06-16 | 小野薬品工業株式会社 | Axl阻害剤と免疫チェックポイント阻害剤とを組み合わせて投与することを特徴とする癌治療のための医薬 |
| HRP20231614T1 (hr) | 2016-03-28 | 2024-03-15 | Incyte Corporation | Spojevi pirolotriazina kao tam inhibitori |
| WO2019039525A1 (ja) | 2017-08-23 | 2019-02-28 | 小野薬品工業株式会社 | Axl阻害剤を有効成分として含むがん治療剤 |
| WO2019067594A1 (en) | 2017-09-27 | 2019-04-04 | Incyte Corporation | SALTS OF PYRROLOTRIAZINE DERIVATIVES USEFUL AS TAM INHIBITORS |
| WO2019074116A1 (ja) | 2017-10-13 | 2019-04-18 | 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 |
| MX2021000127A (es) | 2018-06-29 | 2021-03-29 | Incyte Corp | Formulaciones de un inhibidor de axl/mer. |
| MX2021009863A (es) | 2019-03-21 | 2021-11-12 | Onxeo | Una molecula dbait en combinacion con inhibidor de quinasa para el tratamiento del cancer. |
| GB201912059D0 (en) | 2019-08-22 | 2019-10-09 | Bergenbio As | Combaination therapy of a patient subgroup |
| WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| MX2022010860A (es) | 2020-03-06 | 2022-12-02 | Incyte Corp | Terapia combinada que comprende inhibidores de axl/mer y pd-1/pd-l1. |
| GB202004189D0 (en) | 2020-03-23 | 2020-05-06 | Bergenbio As | Combination therapy |
| KR20230013241A (ko) | 2020-04-08 | 2023-01-26 | 베르겐바이오 에이에스에이 | 항바이러스 요법을 위한 axl 억제제 |
| 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 |
| CN121039109A (zh) * | 2023-04-18 | 2025-11-28 | 国家科学研究中心 | 3,5-二氨基三唑衍生物及其用于治疗眼部疾病的用途 |
Citations (1)
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|---|---|---|---|---|
| WO2004046120A2 (en) * | 2002-11-15 | 2004-06-03 | Vertex Pharmaceuticals Incorporated | Diaminotriazoles useful as inhibitors of protein kinases |
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| GB1403866A (en) | 1971-12-06 | 1975-08-28 | Wyeth John & Brother Ltd | Derivatives of 3-amino-1,2,4-triazoles |
| EP0710654A4 (en) | 1993-07-23 | 1996-08-28 | Green Cross Corp | TRIAZOLE DERIVATIVE AND ITS PHARMACEUTICAL USE |
| 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 |
| PL363316A1 (en) * | 2000-12-22 | 2004-11-15 | Ortho Mc Neil Pharmaceutical, Inc. | 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 |
| BR0309688A (pt) | 2002-05-03 | 2005-02-22 | Janssen Pharmaceutica Nv | Microemulsões poliméricas |
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| CA2555825A1 (en) | 2004-02-11 | 2005-08-25 | Janssen Pharmaceutica N.V. | Process for the preparation of substituted triazole compounds |
| CA2580610C (en) * | 2004-09-17 | 2013-07-09 | Vertex Pharmaceuticals Incorporated | Diaminotriazole compounds useful as protein kinase inhibitors |
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| WO2007030680A2 (en) * | 2005-09-07 | 2007-03-15 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| US8097630B2 (en) * | 2006-10-10 | 2012-01-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors |
| PL2078010T3 (pl) * | 2006-12-29 | 2014-07-31 | Rigel Pharmaceuticals Inc | Triazole podstawione policyklicznym heteroarylem użyteczne jako inhibitory Axl |
| US9650391B2 (en) | 2006-12-29 | 2017-05-16 | Rigel Pharmaceuticals Inc. | N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors |
| CA2710230C (en) * | 2006-12-29 | 2016-02-23 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| ES2558477T3 (es) * | 2006-12-29 | 2016-02-04 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos útiles como inhibidores de AXL |
| ES2406930T3 (es) * | 2006-12-29 | 2013-06-10 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos con arilo bicíclico y heteroarilo bicíclico útiles como inhibidores de AXL |
| CA2681516A1 (en) * | 2007-03-22 | 2008-09-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of janus kinases |
| EA200901654A1 (ru) | 2007-06-15 | 2010-06-30 | Айрм Ллк | Ингибиторы и способы с их использованием |
| SI2205592T1 (sl) * | 2007-10-26 | 2013-09-30 | Rigel Pharmaceuticals, Inc. | Triazoli substituirani s policikličnim arilom in triazoli substituirani s policikličnim heteroarilom uporabni kot Axl inhibitorji |
| MX2010008926A (es) * | 2008-02-15 | 2011-02-23 | Rigel Pharmaceuticals Inc | Compuestos de pirimidin-2-amina y su uso como inhibidores de jak cinasas. |
| EP2326641B1 (en) * | 2008-07-09 | 2014-09-03 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2730251C (en) * | 2008-07-09 | 2016-08-09 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| US8546433B2 (en) * | 2009-01-16 | 2013-10-01 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
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2007
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- 2007-12-28 EP EP07866122.0A patent/EP2074115B1/en active Active
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Patent Citations (1)
| 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 |
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| AU2007342005A1 (en) | 2008-07-10 |
| US8796259B2 (en) | 2014-08-05 |
| ES2607065T3 (es) | 2017-03-29 |
| US20130090330A1 (en) | 2013-04-11 |
| EP2074115B1 (en) | 2018-03-07 |
| CA2710046A1 (en) | 2008-07-10 |
| CN101622248A (zh) | 2010-01-06 |
| EP2484679B1 (en) | 2016-09-28 |
| CA2710046C (en) | 2016-02-09 |
| HK1174631A1 (en) | 2013-06-14 |
| JP2010514809A (ja) | 2010-05-06 |
| EP2074115A1 (en) | 2009-07-01 |
| US9650391B2 (en) | 2017-05-16 |
| EP2484679A2 (en) | 2012-08-08 |
| JP5890445B2 (ja) | 2016-03-22 |
| JP5567837B2 (ja) | 2014-08-06 |
| JP2014111641A (ja) | 2014-06-19 |
| WO2008083354A1 (en) | 2008-07-10 |
| US20080182862A1 (en) | 2008-07-31 |
| ES2672172T3 (es) | 2018-06-12 |
| EP2484679A3 (en) | 2012-10-10 |
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