CA2633035C - Kinase inhibitors and their uses - Google Patents

Kinase inhibitors and their uses Download PDF

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Publication number
CA2633035C
CA2633035C CA2633035A CA2633035A CA2633035C CA 2633035 C CA2633035 C CA 2633035C CA 2633035 A CA2633035 A CA 2633035A CA 2633035 A CA2633035 A CA 2633035A CA 2633035 C CA2633035 C CA 2633035C
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group
compound
exo
alkyl
piperidinyl
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French (fr)
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CA2633035A1 (en
Inventor
Pingyu Ding
Ankush Argade
Dane Goff
Rajinder Singh
Esteban Masuda
Vanessa Taylor
Sacha Holland
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Rigel Pharmaceuticals Inc
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Rigel Pharmaceuticals Inc
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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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
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    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
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    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
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    • 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
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—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 three hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA2633035A 2005-12-15 2006-12-15 Kinase inhibitors and their uses Active CA2633035C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US75139305P 2005-12-15 2005-12-15
US60/751,393 2005-12-15
PCT/US2006/062162 WO2007070872A1 (en) 2005-12-15 2006-12-15 Kinase inhibitors and their uses

Publications (2)

Publication Number Publication Date
CA2633035A1 CA2633035A1 (en) 2007-06-21
CA2633035C true CA2633035C (en) 2016-05-10

Family

ID=37891850

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2633035A Active CA2633035C (en) 2005-12-15 2006-12-15 Kinase inhibitors and their uses

Country Status (6)

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US (4) US7601713B2 (enExample)
EP (1) EP1960372B1 (enExample)
JP (1) JP5400388B2 (enExample)
CA (1) CA2633035C (enExample)
ES (1) ES2562428T3 (enExample)
WO (1) WO2007070872A1 (enExample)

Families Citing this family (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5198256B2 (ja) * 2005-05-04 2013-05-15 エボテク エージー 縮合複素環式化合物、並びにそれらの組成物及び使用
EP1960372B1 (en) * 2005-12-15 2015-12-09 Rigel Pharmaceuticals, Inc. Kinase inhibitors and their uses
TW200808360A (en) * 2006-04-13 2008-02-16 Alcon Mfg Ltd RNAi-mediated inhibition of spleen tyrosine kinase-related inflammatory conditions
US8097630B2 (en) 2006-10-10 2012-01-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors
EA019941B1 (ru) 2006-12-08 2014-07-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов протеинкиназы
CN101611035A (zh) 2006-12-28 2009-12-23 大正制药株式会社 吡唑并嘧啶化合物
EP2170395A1 (en) * 2007-07-02 2010-04-07 Wyeth LLC Modulators of axl for use in treating bone disorders
EP2188292B1 (en) * 2007-08-08 2013-05-29 GlaxoSmithKline Intellectual Property Development Limited 2- [ (2-{phenylamino}-1h-pyrrolo [2, 3-d]pyrimidin-4-yl) amino]benzamide derivatives as igf-1r inhibitors for the treatment of cancer
US20090088371A1 (en) * 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
WO2009032703A1 (en) * 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
CA2703519C (en) 2007-11-09 2017-04-18 The Salk Institute For Biological Studies Use of tam receptor inhibitors as immunoenhancers and tam activators as immunosuppressors
SI2215094T1 (sl) 2007-11-15 2016-05-31 Ym Biosciences Australia Pty Ltd N vsebujoče heterociklične spojine
TW200942537A (en) * 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
BRPI0910668A2 (pt) * 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
AU2009259853A1 (en) 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine JAK inhibitor compounds and methods
PE20110063A1 (es) 2008-06-20 2011-02-16 Genentech Inc DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK
BRPI1007046B1 (pt) 2009-01-16 2019-07-16 Rigel Pharmaceuticals, Inc. Inibidores axl para uso em terapia de combinação para evitar, tratar ou controlar o câncer metastático.
SG172857A1 (en) * 2009-02-09 2011-08-29 Supergen Inc Pyrrolopyrimidinyl axl kinase inhibitors
EP2414361A1 (en) * 2009-03-31 2012-02-08 ArQule, Inc. Substituted heterocyclic compounds
CN105037364B (zh) * 2009-04-03 2018-04-27 维拉斯通股份有限公司 作为激酶抑制剂的嘧啶取代的嘌呤化合物
DK2414362T3 (da) 2009-04-03 2014-09-22 Verastem Inc Pyrimidinsubstituerede purinforbindelser som kinaseinhibitorer
TW201105669A (en) * 2009-07-30 2011-02-16 Irm Llc Compounds and compositions as Syk kinase inhibitors
CN102574847A (zh) 2009-07-30 2012-07-11 Irm责任有限公司 作为syk激酶抑制剂的化合物和组合物
ES2654332T3 (es) * 2009-08-07 2018-02-13 Merck Patent Gmbh Nuevos compuestos azaheterocíclicos
KR101094446B1 (ko) * 2009-11-19 2011-12-15 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
EP2516434B1 (en) * 2009-12-23 2015-05-27 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones as syk inhibitors
EP2441755A1 (en) * 2010-09-30 2012-04-18 Almirall, S.A. Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
FR2967854A1 (fr) * 2010-11-19 2012-05-25 France Telecom Procede de communication dans un reseau cooperatif
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
MX343517B (es) 2011-03-10 2016-11-07 Rigel Pharmaceuticals Inc 2,4 pirimidinadiaminas sustituidas para su uso en lupus discoide.
WO2012154518A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
AU2012253885A1 (en) 2011-05-10 2013-10-31 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
WO2012177714A1 (en) * 2011-06-22 2012-12-27 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
US8987456B2 (en) 2011-10-05 2015-03-24 Merck Sharp & Dohme Corp. 3-pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
EP2782579B1 (en) 2011-11-23 2019-01-02 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
SG11201404505PA (en) 2012-01-31 2014-10-30 Daiichi Sankyo Co Ltd Pyridone derivative
WO2013162061A1 (ja) * 2012-04-26 2013-10-31 第一三共株式会社 二環性ピリミジン化合物
WO2013192125A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
EP2863913B1 (en) 2012-06-20 2018-09-12 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
US9376418B2 (en) 2012-06-22 2016-06-28 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (SYK) inhibitors
WO2013192088A1 (en) 2012-06-22 2013-12-27 Merck Sharp & Dohme Corp. SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
WO2014018535A1 (en) 2012-07-25 2014-01-30 Salk Institute For Biological Studies Regulating the interaction between tam ligands and lipid membranes with exposed phosphatidylserine
EP2884982B1 (en) 2012-08-20 2017-09-20 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
JP2015528501A (ja) 2012-09-12 2015-09-28 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 白斑の治療法
WO2014048065A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
EP2931281B1 (en) 2012-12-12 2018-01-17 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase inhibitors
EP2934525B1 (en) 2012-12-21 2019-05-08 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
WO2014176216A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
EP2988744A4 (en) 2013-04-26 2016-11-02 Merck Sharp & Dohme THIAZOLSUBSTITUTED AMINOHETEROARYLE AS MILZTYROSINKINASE INHIBITOR
US9670196B2 (en) 2013-12-20 2017-06-06 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015094997A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine 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
US10611765B2 (en) 2014-11-06 2020-04-07 Ohio State Innovation Foundation Pyrrolopyrimidine derivatives as Mps1/TTK kinase inhibitors
PL3233857T3 (pl) * 2014-12-18 2020-07-27 Takeda Pharmaceutical Company Limited Stałe postacie skondensowanych heteroaromatycznych pirolidynonów
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
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
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
TWI828027B (zh) 2016-03-28 2024-01-01 美商英塞特公司 作為tam抑制劑之吡咯并三嗪化合物
CN107698603B (zh) 2016-08-09 2022-04-08 南京红云生物科技有限公司 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
EP3673907A4 (en) 2017-08-23 2020-08-19 ONO Pharmaceutical Co., Ltd. CANCER TREATMENT PHARMACEUTICAL INCLUDING AX1 INHIBITOR AS AN EFFECTIVE INGREDIENT
US10633387B2 (en) 2017-09-27 2020-04-28 Incyte Corporation Salts of TAM inhibitors
US11826363B2 (en) 2017-10-13 2023-11-28 Ono Pharmaceutical Co., Ltd. Therapeutic agent for solid cancers, which comprises Axl inhibitor as active ingredient
EP3814354B1 (en) * 2018-06-22 2023-11-08 The Royal Institution for the Advancement of Learning / McGill University Purine compounds and method for the treatment of cancer
ES3031110T3 (en) 2018-06-29 2025-07-04 Incyte Corp Formulations of an axl/mer inhibitor
WO2020201362A2 (en) 2019-04-02 2020-10-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
WO2020212395A1 (en) 2019-04-16 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
PH12022552347A1 (en) 2020-03-06 2024-01-29 Incyte Corp Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
US20250283174A1 (en) 2022-05-16 2025-09-11 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation
US20260069610A1 (en) 2022-09-09 2026-03-12 University Of Rochester Inhibition of efferocytosis as a treatment to prevent bone loss and increase bone density and strength
WO2026093435A1 (en) 2024-10-31 2026-05-07 Institut National de la Santé et de la Recherche Médicale Use of jak inhibitors for enhancing the potency of immunotherapy in the treament of cancer

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1066147C (zh) * 1995-11-01 2001-05-23 诺瓦提斯公司 嘌呤衍生物及其制备方法
WO1997020821A1 (en) * 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
WO1997020822A1 (en) * 1995-12-01 1997-06-12 Novartis Ag Quinazolin-2,4-diazirines as npy receptor antagonist
GB9903762D0 (en) 1999-02-18 1999-04-14 Novartis Ag Organic compounds
GB9918035D0 (en) * 1999-07-30 1999-09-29 Novartis Ag Organic compounds
SV2002000205A (es) 1999-11-01 2002-06-07 Lilly Co Eli Compuestos farmaceuticos ref. x-01095
FR2818642B1 (fr) * 2000-12-26 2005-07-15 Hoechst Marion Roussel Inc Nouveaux derives de la purine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilistion
PE20030008A1 (es) * 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
AU2002334992B2 (en) * 2001-10-12 2009-07-02 Irm Llc Methods for the synthesis of substituted purines
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US6897307B2 (en) * 2002-03-28 2005-05-24 Novartis Ag Process for preparing 2,6-diaminopurine derivatives
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
US7384937B2 (en) * 2002-11-06 2008-06-10 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
JP2007530089A (ja) 2003-07-14 2007-11-01 ユニバーシティ・オブ・リムリック 血管グラフト
JP2007502776A (ja) * 2003-08-15 2007-02-15 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｒｔｋ阻害剤としての６−置換アニリノプリン類
WO2005047524A2 (en) * 2003-11-10 2005-05-26 The Scripps Research Institute Compositions and methods for inducing cell dedifferentiation
GB0327319D0 (en) 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
CA2549510A1 (en) * 2003-12-16 2005-07-07 Pfizer Products Inc. Pyrido[2,3-d]pyrimidine-2,4-diamines as pde 2 inhibitors
GB0407723D0 (en) 2004-04-05 2004-05-12 Novartis Ag Organic compounds
JP4812763B2 (ja) * 2004-05-18 2011-11-09 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 シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
WO2006014420A1 (en) 2004-07-06 2006-02-09 Angion Biomedica Corporation Quinazoline modulators of hepatocyte growth factor / c-met activity for the treatment of cancer
DE602005012597D1 (de) 2004-11-15 2009-03-19 Rigel Pharmaceuticals Inc Verfahren zur herstellung optisch aktiver n-carbamat-geschützter beta-lactame durch optische auflösung unter verwendung einer candida antarctica lipase
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
WO2006105056A2 (en) * 2005-03-28 2006-10-05 Fmc Corporation Insecticidal 2,4-diaminoquinazolines and related derivatives
CN100526315C (zh) * 2005-06-16 2009-08-12 浙江医药股份有限公司新昌制药厂 N2-喹啉或异喹啉取代的嘌呤衍生物及其制备方法和其用途
JP2009511527A (ja) * 2005-10-13 2009-03-19 グラクソ グループ リミテッド Ｓｙｋ阻害物質としてのピロロピリミジン誘導体
EP1960372B1 (en) * 2005-12-15 2015-12-09 Rigel Pharmaceuticals, Inc. Kinase inhibitors and their uses

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