CN102281875B - 预防、治疗或应对转移癌的使用axl抑制剂的组合疗法 - Google Patents

预防、治疗或应对转移癌的使用axl抑制剂的组合疗法 Download PDF

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Publication number
CN102281875B
CN102281875B CN201080004818.0A CN201080004818A CN102281875B CN 102281875 B CN102281875 B CN 102281875B CN 201080004818 A CN201080004818 A CN 201080004818A CN 102281875 B CN102281875 B CN 102281875B
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optionally substituted
benzo
dihydro
pyridazin
cycloheptatrieno
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Chinese (zh)
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CN102281875A (zh
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等泰道
S·霍兰
D·G·帕扬
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Rigel Pharmaceuticals Inc
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Rigel Pharmaceuticals Inc
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    • 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
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201080004818.0A 2009-01-16 2010-01-15 预防、治疗或应对转移癌的使用axl抑制剂的组合疗法 Active CN102281875B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14544809P 2009-01-16 2009-01-16
US61/145,448 2009-01-16
PCT/US2010/021275 WO2010083465A1 (en) 2009-01-16 2010-01-15 Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer

Publications (2)

Publication Number Publication Date
CN102281875A CN102281875A (zh) 2011-12-14
CN102281875B true CN102281875B (zh) 2017-09-22

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CN201080004818.0A Active CN102281875B (zh) 2009-01-16 2010-01-15 预防、治疗或应对转移癌的使用axl抑制剂的组合疗法

Country Status (13)

Country Link
US (5) US8546433B2 (https=)
EP (1) EP2387395B1 (https=)
JP (2) JP5858789B2 (https=)
CN (1) CN102281875B (https=)
AU (1) AU2010204578B2 (https=)
BR (1) BRPI1007046B1 (https=)
CA (1) CA2749843C (https=)
ES (1) ES2528032T3 (https=)
PL (1) PL2387395T3 (https=)
PT (1) PT2387395E (https=)
RU (1) RU2555326C2 (https=)
SG (1) SG172997A1 (https=)
WO (1) WO2010083465A1 (https=)

Families Citing this family (52)

* 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
ES2672172T3 (es) * 2006-12-29 2018-06-12 Rigel Pharmaceuticals, Inc. Triazoles N3-heteroarilsustituidos y triazoles N5-heteroarilsustituidos útiles como inhibidores de Axl
WO2008083353A1 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2079736B1 (en) 2006-12-29 2017-10-18 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
EP2114955B1 (en) 2006-12-29 2013-02-13 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2078010B1 (en) 2006-12-29 2014-01-29 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
WO2009054864A1 (en) * 2007-10-26 2009-04-30 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
US8309566B2 (en) 2008-02-15 2012-11-13 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases
US8431594B2 (en) 2008-07-09 2013-04-30 Rigel Pharmaceuticals, Inc. Bridged bicyclic heteroaryl substituted triazoles useful as AXL inhibitors
CA2730231C (en) 2008-07-09 2016-10-18 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
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
SG172997A1 (en) 2009-01-16 2011-08-29 Rigel Pharmaceuticals Inc Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer
US8916574B2 (en) 2009-09-28 2014-12-23 Qilu Pharmaceutical Co., Ltd. 4-(substituted anilino)-quinazoline derivatives useful as tyrosine kinase inhibitors
GB201207722D0 (en) 2012-05-02 2012-06-13 Bergenbio As Method
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
JP6527513B2 (ja) 2013-11-20 2019-06-05 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キナゾリン誘導体
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
JP6992960B2 (ja) * 2013-12-02 2022-02-03 ベルゲンビオ アーエスアー キナーゼ阻害剤の用途
US20170027940A1 (en) * 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
US10028958B2 (en) * 2014-04-19 2018-07-24 Massachusetts Institute Of Technology Methods of treating cancer with a combination of selected MEK1/2 and AXL inhibitors
GB201420285D0 (en) 2014-11-14 2014-12-31 Bergenbio As Process
GB201509338D0 (en) * 2015-05-29 2015-07-15 Bergenbio As Combination therapy
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
CN109384774B (zh) * 2017-08-11 2023-02-17 中国科学院上海药物研究所 一类多取代的吡嗪/三嗪酰胺类化合物及其制备方法和应用
US20200289613A1 (en) * 2017-11-04 2020-09-17 Aravive Biologics, Inc. Methods of treating metastatic cancers using axl decoy receptors
US12097194B2 (en) 2018-09-18 2024-09-24 Signalchem Lifesciences Corporation Combination therapy for treating blood cancer
US20220143049A1 (en) 2019-03-21 2022-05-12 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
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
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
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
JPWO2022220227A1 (https=) * 2021-04-14 2022-10-20
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
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008083354A1 (en) * 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors
WO2008083367A2 (en) * 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors

Family Cites Families (43)

* 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
US4512992A (en) * 1980-06-13 1985-04-23 Burroughs Wellcome Co. Treatment with dialkoxy pyridopyrimidine compounds
MX19185A (es) 1989-01-20 1993-12-01 Pfizer Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas.
US6258360B1 (en) 1989-05-04 2001-07-10 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
WO1995003286A1 (en) 1993-07-23 1995-02-02 The Green Cross Corporation Triazole derivative and pharmaceutical use thereof
UA71971C2 (en) * 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
GB9918180D0 (en) 1999-08-02 1999-10-06 Smithkline Beecham Plc Novel compositions
DE60120494T2 (de) 2000-12-22 2006-12-21 Ortho-Mcneil Pharmaceutical, Inc. Substituieten triazoldiamin derivaten und ihre verwendung als kinase inhibitoren
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
AU2003217961B2 (en) 2002-03-08 2008-02-28 Signal Pharmaceuticals, Llc Combination therapy for treating, preventing or managing proliferative disorders and cancers
CN1290893C (zh) 2002-05-03 2006-12-20 詹森药业有限公司 聚合物微乳状液
US20060293256A1 (en) * 2002-08-06 2006-12-28 Masateru Yamada Remedy or preventive for kidney disease and method of diagnosing kidney disease
AU2003286746A1 (en) 2002-10-29 2004-05-25 Rigel Pharmaceuticals, Inc. Modulators of angiogenesis and tumorigenesis
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
AU2004220176A1 (en) 2003-03-14 2004-09-23 Astrazeneca Ab Novel fused triazolones and the uses thereof
MXPA05013434A (es) 2003-06-12 2006-03-17 Astellas Pharma Inc Derivados de benzamida o sal del mismo.
WO2005013982A1 (en) 2003-08-06 2005-02-17 Vertex Pharmaceuticals Incorporated Aminotriazole compounds useful as inhibitors of protein kinases
CA2554925A1 (en) 2004-01-30 2005-08-11 Ab Science 2-(3-substituted-aryl)amino-4-aryl-thiazoles as tyrosine kinase inhibitors
EP1720843A2 (en) 2004-02-11 2006-11-15 Janssen Pharmaceutica N.V. Process for the preparation of substituted triazole compounds
EP1763514A2 (en) 2004-05-18 2007-03-21 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
SG155222A1 (en) 2004-08-13 2009-09-30 Genentech Inc Thiazole based inhibitors of atp-utilizing enzymes
KR20070057955A (ko) 2004-09-17 2007-06-07 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 디아미노트리아졸 화합물
SI1811998T1 (sl) 2004-10-21 2011-01-31 Vertex Pharma Triazoli uporabni kot inhibitorji proteinskih kinaz
US20060166936A1 (en) 2004-10-29 2006-07-27 Hayley Binch Diaminotriazole compounds useful as inhibitors of protein kinases
RU2007123675A (ru) 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
US20070166388A1 (en) * 2005-02-18 2007-07-19 Desai Neil P Combinations and modes of administration of therapeutic agents and combination therapy
WO2007030680A2 (en) 2005-09-07 2007-03-15 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as axl inhibitors
JP5400388B2 (ja) 2005-12-15 2014-01-29 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 キナーゼインヒビターおよびその利用
WO2007118149A2 (en) 2006-04-07 2007-10-18 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical Lollege Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers
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
JP2008130120A (ja) 2006-11-17 2008-06-05 Sharp Corp 光ピックアップ装置
WO2008080134A2 (en) 2006-12-22 2008-07-03 Rigel Pharmaceuticals, Inc. 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors
EP2114955B1 (en) 2006-12-29 2013-02-13 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2079736B1 (en) * 2006-12-29 2017-10-18 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
WO2008083353A1 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
AU2008266290A1 (en) 2007-06-15 2008-12-24 Irm Llc Protein kinase inhibitors and methods for using thereof
WO2009054864A1 (en) 2007-10-26 2009-04-30 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
US8309566B2 (en) * 2008-02-15 2012-11-13 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases
CA2730231C (en) 2008-07-09 2016-10-18 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
US8431594B2 (en) 2008-07-09 2013-04-30 Rigel Pharmaceuticals, Inc. Bridged bicyclic heteroaryl substituted triazoles useful as AXL inhibitors
SG172997A1 (en) * 2009-01-16 2011-08-29 Rigel Pharmaceuticals Inc Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008083354A1 (en) * 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors
WO2008083367A2 (en) * 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors

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BRPI1007046A2 (pt) 2015-07-21
US8546433B2 (en) 2013-10-01
WO2010083465A1 (en) 2010-07-22
AU2010204578B2 (en) 2016-05-12
CN102281875A (zh) 2011-12-14
EP2387395A1 (en) 2011-11-23
US20100196511A1 (en) 2010-08-05
SG172997A1 (en) 2011-08-29
HK1164146A1 (en) 2012-09-21
ES2528032T3 (es) 2015-02-03
US20130338161A1 (en) 2013-12-19
CA2749843C (en) 2017-09-05
RU2555326C2 (ru) 2015-07-10
JP2015007135A (ja) 2015-01-15
JP5858789B2 (ja) 2016-02-10
US20190336500A1 (en) 2019-11-07
CA2749843A1 (en) 2011-07-22
EP2387395B1 (en) 2014-10-15
PT2387395E (pt) 2015-02-04
US20170042891A1 (en) 2017-02-16
AU2010204578A1 (en) 2011-07-28
US20210379064A1 (en) 2021-12-09
RU2011132118A (ru) 2013-02-27
JP2012515225A (ja) 2012-07-05
BRPI1007046B1 (pt) 2019-07-16
PL2387395T3 (pl) 2015-03-31

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