CY1115188T1 - Πολυκυκλικες ετεροαρυλ-υποκατεστημενες τριαζολες χρησιμες ως αναστολεις του axl - Google Patents

Πολυκυκλικες ετεροαρυλ-υποκατεστημενες τριαζολες χρησιμες ως αναστολεις του axl

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Publication number
CY1115188T1
CY1115188T1 CY20141100312T CY141100312T CY1115188T1 CY 1115188 T1 CY1115188 T1 CY 1115188T1 CY 20141100312 T CY20141100312 T CY 20141100312T CY 141100312 T CY141100312 T CY 141100312T CY 1115188 T1 CY1115188 T1 CY 1115188T1
Authority
CY
Cyprus
Prior art keywords
axl
polycyclic heteroaryl
suspensions
substituted triazoles
triazoles useful
Prior art date
Application number
CY20141100312T
Other languages
English (en)
Inventor
Dane Goff
Jing Zhang
Rajinder Singh
Sacha Holland
Jiaxin Yu
Thilo Heckrodt
Pingyu Ding
Joane Litvak
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 CY1115188T1 publication Critical patent/CY1115188T1/el

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    • A61K31/50Pyridazines; Hydrogenated pyridazines
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Abstract

Αποκαλύπτονται πολυκυκλικές ετεραρυλ-υποκατεστημένες τριαζόλες και φαρμακευτικές συνθέσεις που περιέχουν τις ενώσεις, οι οποίες είναι χρήσιμες στην αναστολή της ενεργότητας του υποδοχέα πρωτεϊνικής κινάσης τυροσίνης Axl. Αποκαλύπτονται επίσης μέθοδοι για χρήση των ενώσεων στη θεραπεία ασθενειών και καταστάσεων που σχετίζονται με την ενεργότητα του Axl.
CY20141100312T 2006-12-29 2014-04-28 Πολυκυκλικες ετεροαρυλ-υποκατεστημενες τριαζολες χρησιμες ως αναστολεις του axl CY1115188T1 (el)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US88285006P 2006-12-29 2006-12-29
US89540007P 2007-03-16 2007-03-16
US97093107P 2007-09-07 2007-09-07
EP07870107.5A EP2078010B1 (en) 2006-12-29 2007-12-29 Polycyclic heteroaryl substituted triazoles useful as axl inhibitors

Publications (1)

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CY1115188T1 true CY1115188T1 (el) 2017-01-04

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CY20141100312T CY1115188T1 (el) 2006-12-29 2014-04-28 Πολυκυκλικες ετεροαρυλ-υποκατεστημενες τριαζολες χρησιμες ως αναστολεις του axl

Country Status (17)

Country Link
US (5) US7709482B2 (el)
EP (1) EP2078010B1 (el)
JP (2) JP5546250B2 (el)
CN (1) CN101622246B (el)
AU (1) AU2007341937B2 (el)
CA (1) CA2710234C (el)
CY (1) CY1115188T1 (el)
DK (1) DK2078010T3 (el)
ES (1) ES2460894T3 (el)
HK (1) HK1132737A1 (el)
HR (1) HRP20140378T1 (el)
ME (1) ME01832B (el)
PL (1) PL2078010T3 (el)
PT (1) PT2078010E (el)
RS (1) RS53281B (el)
SI (1) SI2078010T1 (el)
WO (1) WO2008083367A2 (el)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2612788A1 (en) * 2005-06-24 2006-12-28 Steven Cesar Alfons De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c
WO2007030680A2 (en) * 2005-09-07 2007-03-15 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as axl inhibitors
US8338435B2 (en) * 2006-07-20 2012-12-25 Gilead Sciences, Inc. Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections
TW200840584A (en) * 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
RS53281B (en) 2006-12-29 2014-08-29 Rigel Pharmaceuticals Inc. POLYCYCLIC HETEROaryl SUBSTITUTED TRIAZOLES USED AS AXL INHIBITORS
PL2114955T3 (pl) * 2006-12-29 2013-06-28 Rigel Pharmaceuticals Inc Triazole podstawione mostkowanym bicyklicznym arylem oraz mostkowanym bicyklicznym heteroarylem użyteczne jako inhibitory Axl
JP5567837B2 (ja) * 2006-12-29 2014-08-06 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インヒビターとして有用なN3−ヘテロアリール置換トリアゾールおよびN5−ヘテロアリール置換トリアゾール
ES2406930T3 (es) * 2006-12-29 2013-06-10 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con arilo bicíclico y heteroarilo bicíclico útiles como inhibidores de AXL
CA2946305C (en) 2006-12-29 2019-09-17 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
US7935693B2 (en) * 2007-10-26 2011-05-03 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as Axl inhibitors
NZ587589A (en) 2008-02-15 2012-10-26 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
ES2537480T3 (es) 2008-07-09 2015-06-08 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con heteroarilo policíclicos útiles como inhibidores de Axl
ES2399319T3 (es) 2008-07-09 2013-03-27 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con heteroarilos bicíclicos que contienen puentes útiles como inhibidores de AXL
JP4644273B2 (ja) * 2008-07-15 2011-03-02 本田技研工業株式会社 車両周辺監視装置
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
AU2011207381B2 (en) 2010-01-22 2016-06-09 The Board Of Trustees Of The Leland Stanford Junior University Inhibition of AXL signaling in anti-metastatic therapy
US9074192B2 (en) 2010-01-22 2015-07-07 The Board Of Trustees Of The Leland Stanford Junior University Inhibition of AXL signaling in anti-metastatic therapy
US9879061B2 (en) 2011-12-15 2018-01-30 The Board Of Trustees Of The Leland Stanford Junior University Inhibition of AXL/GAS6 signaling in the treatment of liver fibrosis
PT2810937T (pt) 2012-01-31 2017-03-03 Daiichi Sankyo Co Ltd Derivado de piridona
EP3184121A3 (en) 2012-07-25 2017-09-27 Salk Institute For Biological Studies Lipid membranes with exposed phosphatidylserine as tam ligands, use for treating autoimmune diseases
TW201534597A (zh) * 2013-06-20 2015-09-16 Ab Science 作為選擇性蛋白質激酶抑制劑之苯并咪唑衍生物
EP3071204B1 (en) 2013-11-20 2019-02-20 SignalChem Lifesciences Corp. Quinazoline derivatives as tam family kinase inhibitors
CN110156770B (zh) 2013-11-27 2022-10-04 圣诺康生命科学公司 作为tam族激酶抑制剂的氨基吡啶衍生物
US9801880B2 (en) 2013-12-02 2017-10-31 Bergenbio As Use of 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
CA2909669C (en) 2014-10-20 2023-12-12 Ruga Corporation Antiviral activity of gas6 inhibitor
GB201420285D0 (en) * 2014-11-14 2014-12-31 Bergenbio As Process
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
GB201509338D0 (en) 2015-05-29 2015-07-15 Bergenbio As Combination therapy
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
ES2896079T3 (es) 2016-02-26 2022-02-23 Ono Pharmaceutical Co Fármaco para la terapia del cáncer, caracterizado por la administración de la combinación entre un inhibidor de Axl y un inhibidor del punto de control inmunitario
PT3436461T (pt) 2016-03-28 2024-01-23 Incyte Corp Compostos de pirrolotriazina como inibidores de tam
CN106083764B (zh) * 2016-07-11 2018-09-18 上海皓元生物医药科技有限公司 一种用于制备axl抑制剂的高纯度中间体的手性拆分方法
JP7156287B2 (ja) 2017-08-23 2022-10-19 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
JP2020535168A (ja) 2017-09-27 2020-12-03 インサイト・コーポレイションIncyte Corporation Tam阻害剤として有用なピロロトリアジン誘導体の塩
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
TWI832871B (zh) 2018-06-29 2024-02-21 美商英塞特公司 Axl/mer 抑制劑之調配物
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
GB201912059D0 (en) 2019-08-22 2019-10-09 Bergenbio As Combaination therapy of a patient subgroup
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) 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
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
TW202304908A (zh) * 2021-04-14 2023-02-01 日商衛材R&D企管股份有限公司 四氫吡啶并嘧啶化合物
CN115504967A (zh) * 2021-06-23 2022-12-23 南京正大天晴制药有限公司 作为axl抑制剂的1,2,4-***化合物
WO2023081923A1 (en) 2021-11-08 2023-05-11 Frequency Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
GB202209285D0 (en) 2022-06-24 2022-08-10 Bergenbio Asa Dosage regimen for AXL inhibitor
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***化合物
WO2024054793A1 (en) * 2022-09-09 2024-03-14 University Of Rochester Inhibition of efferocytosis as a treatment to prevent bone loss and increase bone density and strength

Family Cites Families (32)

* 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 (fr) 1993-07-23 1995-02-02 The Green Cross Corporation Derive de triazole et son utilisation pharmaceutique
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
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
WO2004017997A1 (ja) 2002-08-06 2004-03-04 Toray Industries, Inc. 腎疾患治療又は予防剤及び腎疾患の診断方法
EP1563094A4 (en) * 2002-10-29 2007-04-25 Rigel Pharmaceuticals Inc MODULATORS OF ANGIOGENESIS AND TUMORIGENESIS
CN1738615A (zh) * 2002-11-15 2006-02-22 沃泰克斯药物股份有限公司 用作蛋白质激酶的抑制剂的二氨基***类
CL2003002353A1 (es) * 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
JP4889489B2 (ja) 2003-08-06 2012-03-07 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼのインヒビターとして有用なアミノトリアゾール化合物
JP2007522213A (ja) 2004-02-11 2007-08-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 置換されたトリアゾール化合物の製造方法
GB2415863A (en) 2004-07-01 2006-01-04 British Sky Broadcasting Ltd Wireless network system and devices with redundancy between orthogonally polarised beams
KR20070049655A (ko) * 2004-08-13 2007-05-11 제넨테크, 인크. Atp-이용 효소 억제 활성을 나타내는2-아미도-티아졸-기재 화합물과 조성물 및 이들의 용도
ZA200702645B (en) * 2004-09-17 2008-08-27 Vertex Pharma Diaminotriazole compounds useful as protein kinase inhibitors
US9265731B2 (en) * 2005-01-28 2016-02-23 Bend Research, Inc. Drying of drug-containing particles
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
FR2908131B1 (fr) 2006-11-03 2009-01-09 Univ Haute Alsace Etablissemen Derives d'aminobenzocycloheptene,leurs procedes de preparation et leur utilisation en therapeutique
US7879856B2 (en) 2006-12-22 2011-02-01 Rigel Pharmaceuticals, Inc. Diaminothiazoles useful as Axl inhibitors
JP5567837B2 (ja) 2006-12-29 2014-08-06 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インヒビターとして有用なN3−ヘテロアリール置換トリアゾールおよびN5−ヘテロアリール置換トリアゾール
ES2406930T3 (es) 2006-12-29 2013-06-10 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con arilo bicíclico y heteroarilo bicíclico útiles como inhibidores de AXL
CA2946305C (en) 2006-12-29 2019-09-17 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
RS53281B (en) * 2006-12-29 2014-08-29 Rigel Pharmaceuticals Inc. POLYCYCLIC HETEROaryl SUBSTITUTED TRIAZOLES USED AS AXL INHIBITORS
PL2114955T3 (pl) * 2006-12-29 2013-06-28 Rigel Pharmaceuticals Inc Triazole podstawione mostkowanym bicyklicznym arylem oraz mostkowanym bicyklicznym heteroarylem użyteczne jako inhibitory Axl
EP2170867A1 (en) 2007-06-15 2010-04-07 Irm Llc Protein kinase inhibitors and methods for using thereof
US7935693B2 (en) 2007-10-26 2011-05-03 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as Axl inhibitors
NZ587589A (en) 2008-02-15 2012-10-26 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
ES2537480T3 (es) 2008-07-09 2015-06-08 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con heteroarilo policíclicos útiles como inhibidores de Axl
ES2399319T3 (es) 2008-07-09 2013-03-27 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con heteroarilos bicíclicos que contienen puentes útiles como inhibidores de AXL
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
CA2766735C (en) 2011-02-07 2020-06-02 Ortho-Clinical Diagnostics, Inc. Determining conditions in centrifuged blood using measured pressure

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