CA2672172C - Bicyclic heterocyclic compounds as fgfr inhibitors - Google Patents

Bicyclic heterocyclic compounds as fgfr inhibitors Download PDF

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Publication number
CA2672172C
CA2672172C CA2672172A CA2672172A CA2672172C CA 2672172 C CA2672172 C CA 2672172C CA 2672172 A CA2672172 A CA 2672172A CA 2672172 A CA2672172 A CA 2672172A CA 2672172 C CA2672172 C CA 2672172C
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CA
Canada
Prior art keywords
compound
phenyl
imidazo
alkyl
pyridin
Prior art date
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Active
Application number
CA2672172A
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English (en)
French (fr)
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CA2672172A1 (en
Inventor
Valerio Berdini
Gilbert Ebai Besong
Owen Callaghan
Maria Grazia Carr
Miles Stuart Congreve
Adrian Liam Gill
Charlotte Mary Griffiths-Jones
Andrew Madin
Christopher William Murray
Rajdeep Kaur Nijjar
Michael Alistair O'brien
Andrew Pike
Gordon Saxty
Richard David Taylor
Emma Vickerstaffe
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Astex Therapeutics Ltd
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Astex Therapeutics Ltd
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Filing date
Publication date
Priority claimed from GB0625826A external-priority patent/GB0625826D0/en
Priority claimed from GB0720000A external-priority patent/GB0720000D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of CA2672172A1 publication Critical patent/CA2672172A1/en
Application granted granted Critical
Publication of CA2672172C publication Critical patent/CA2672172C/en
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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
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    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • 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
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    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
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    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • 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
    • A61P9/06Antiarrhythmics
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Tropical Medicine & Parasitology (AREA)
CA2672172A 2006-12-22 2007-12-21 Bicyclic heterocyclic compounds as fgfr inhibitors Active CA2672172C (en)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US87154306P 2006-12-22 2006-12-22
GB0625826.3 2006-12-22
US60/871,543 2006-12-22
GB0625826A GB0625826D0 (en) 2006-12-22 2006-12-22 New compounds
US97958707P 2007-10-12 2007-10-12
US60/979,587 2007-10-12
GB0720000.9 2007-10-12
GB0720000A GB0720000D0 (en) 2007-10-12 2007-10-12 New compounds
US98103907P 2007-10-18 2007-10-18
US60/981,039 2007-10-18
PCT/GB2007/004934 WO2008078091A1 (en) 2006-12-22 2007-12-21 Bicyclic heterocyclic compounds as fgfr inhibitors

Publications (2)

Publication Number Publication Date
CA2672172A1 CA2672172A1 (en) 2008-07-03
CA2672172C true CA2672172C (en) 2016-05-03

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2672172A Active CA2672172C (en) 2006-12-22 2007-12-21 Bicyclic heterocyclic compounds as fgfr inhibitors

Country Status (11)

Country Link
US (1) US8895745B2 (cg-RX-API-DMAC10.html)
EP (1) EP2114941B1 (cg-RX-API-DMAC10.html)
JP (1) JP5442448B2 (cg-RX-API-DMAC10.html)
CN (1) CN101679408B (cg-RX-API-DMAC10.html)
AR (1) AR064491A1 (cg-RX-API-DMAC10.html)
AU (1) AU2007337886C1 (cg-RX-API-DMAC10.html)
CA (1) CA2672172C (cg-RX-API-DMAC10.html)
HR (1) HRP20150642T1 (cg-RX-API-DMAC10.html)
MX (1) MX2009006706A (cg-RX-API-DMAC10.html)
NO (1) NO343370B1 (cg-RX-API-DMAC10.html)
WO (1) WO2008078091A1 (cg-RX-API-DMAC10.html)

Families Citing this family (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
US8513276B2 (en) 2006-12-22 2013-08-20 Astex Therapeutics Limited Imidazo[1,2-a]pyridine compounds for use in treating cancer
CN101679408B (zh) 2006-12-22 2016-04-27 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
EP2200985B1 (en) 2007-09-14 2011-07-13 Ortho-McNeil-Janssen Pharmaceuticals, Inc. 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones
NZ584148A (en) 2007-09-14 2011-05-27 Ortho Mcneil Janssen Pharm 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones
CA2696948C (en) 2007-09-14 2013-04-30 Jose Maria Cid-Nunez 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
GB0720041D0 (en) * 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
CN101827844B (zh) * 2007-10-17 2013-08-14 诺瓦提斯公司 可用作ALK抑制剂的咪唑并[1,2-a]吡啶衍生物
CN101861316B (zh) 2007-11-14 2013-08-21 奥梅-杨森制药有限公司 咪唑并[1,2-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
GB0810902D0 (en) * 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
US8518911B2 (en) 2008-08-05 2013-08-27 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyridines as MARK inhibitors
CN102143955B (zh) 2008-09-02 2013-08-14 Omj制药公司 作为代谢型谷氨酸受体调节剂的3-氮杂二环[3.1.0]己烷衍生物
WO2010043396A1 (en) 2008-10-16 2010-04-22 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
JP5690277B2 (ja) * 2008-11-28 2015-03-25 ジャンセン ファーマシューティカルズ, インコーポレイテッド. 代謝型グルタミン酸受容体の調節因子としてのインドールおよびベンゾオキサジン誘導体
EP2408773A2 (en) 2009-03-20 2012-01-25 Amgen, Inc Inhibitors of pi3 kinase
GB0906470D0 (en) * 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906472D0 (en) * 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
CN102439015B (zh) 2009-05-12 2015-05-13 杨森制药有限公司 1,2,4-三唑并[4,3-a]吡啶衍生物和其作为mGluR2受体的正向变构调节剂的用途
ES2440001T3 (es) 2009-05-12 2014-01-27 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-A]piridina y su uso para el tratamiento o prevención de trastornos neurológicos y psiquiátricos
PE20170003A1 (es) 2009-08-17 2017-03-15 Intellikine Llc Compuestos heterociclicos y usos de los mismos
FR2950345B1 (fr) * 2009-09-18 2011-09-23 Sanofi Aventis Derives acetyleniques de 5-phenyl-pyrazolopyridine, leur preparation et leur application en therapeutique
FR2950344B1 (fr) * 2009-09-18 2011-11-25 Sanofi Aventis Derives de 5-phenyl-pyrazolopyridine, leur preparation et leur aplication en therapeutique.
GB201007286D0 (en) * 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
WO2012040048A2 (en) * 2010-09-21 2012-03-29 Schering Corporation Triazolopyrazinones as p2x7 receptor antagonists
ES2552879T3 (es) 2010-11-08 2015-12-02 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
CA2814998C (en) 2010-11-08 2019-10-29 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
US9271967B2 (en) 2010-11-08 2016-03-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
GB201020179D0 (en) * 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
DK2663539T3 (en) * 2011-01-13 2016-11-07 Bayer Ip Gmbh PROCESS FOR THE PREPARATION OF 2,2-difluoroethylamine of 2,2-difluoro-1-chloroethane and ammonia
UA111382C2 (uk) * 2011-10-10 2016-04-25 Оріон Корпорейшн Інгібітори протеїнкінази
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
CN102432472A (zh) * 2011-11-03 2012-05-02 浙江工业大学 一种2,2-二氟丙烷-1,3-二胺的制备方法
AU2013207252B2 (en) * 2012-01-06 2016-06-09 H.Lundbeck A/S Carbamate compounds and pharmaceutical compositions thereof
GB201205669D0 (en) * 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
US10280168B2 (en) 2012-03-30 2019-05-07 Agency For Science, Technology And Research Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
CN104662018B (zh) 2012-04-20 2017-10-24 阿迪维纳斯治疗有限公司 取代的杂双环化合物、组合物及其医疗应用
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
ES2916220T3 (es) 2012-07-11 2022-06-29 Blueprint Medicines Corp Inhibidores del receptor de factor de crecimiento de fibroblasto
ES2689429T3 (es) * 2012-07-13 2018-11-14 Ucb Biopharma Sprl Derivados de imidazopiridina como moduladores de actividad de TNF
CN102786543B (zh) * 2012-07-24 2016-04-27 上海瑞博化学有限公司 咪唑并[1,2-a]吡啶-6-硼酸频哪醇酯及其衍生物的制备方法
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
JP6430383B2 (ja) 2012-09-28 2018-11-28 ヴァンダービルト ユニバーシティーVanderbilt University 選択的bmp阻害剤としての縮合複素環化合物
US8871754B2 (en) 2012-11-19 2014-10-28 Irm Llc Compounds and compositions for the treatment of parasitic diseases
SI2925757T1 (en) 2012-11-19 2018-01-31 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
WO2014080241A1 (en) * 2012-11-21 2014-05-30 Piramal Enterprises Limited Imidazopyridine compounds and uses thereof
JP6007339B2 (ja) * 2012-11-29 2016-10-12 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft イミダゾピリジン誘導体
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
AU2014228746B2 (en) 2013-03-15 2018-08-30 Celgene Car Llc Heteroaryl compounds and uses thereof
US9321786B2 (en) 2013-03-15 2016-04-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
ES2892423T3 (es) 2013-03-15 2022-02-04 Celgene Car Llc Compuestos de heteroarilo y usos de los mismos
TWI628176B (zh) * 2013-04-04 2018-07-01 奧利安公司 蛋白質激酶抑制劑
JP6449244B2 (ja) * 2013-04-19 2019-01-09 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Fgfr抑制剤としての二環式複素環
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
SMT202200292T1 (it) 2013-10-25 2022-09-14 Blueprint Medicines Corp Inibitori del recettore del fattore di crescita dei fibroblasti
US9556150B2 (en) 2013-12-13 2017-01-31 Hoffmann-La Roche Inc. Inhibitors of bruton's tyrosine kinase
LT3431106T (lt) 2014-01-21 2021-02-10 Janssen Pharmaceutica Nv Deriniai, apimantys 2 potipio metabotropinio glutamaterginio receptoriaus teigiamus alosterinius moduliatorius arba ortosterinius agonistus, ir jų panaudojimas
EA033889B1 (ru) 2014-01-21 2019-12-05 Янссен Фармацевтика Нв Комбинация на основе лиганда sv2a и положительного аллостерического модулятора метаботропного глутаматергического рецептора 2 подтипа
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
CA2943687C (en) 2014-03-26 2024-02-13 Astex Therapeutics Ltd Combinations of an fgfr inhibitor and an igf1r inhibitor
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
KR102344105B1 (ko) 2014-08-18 2021-12-29 에자이 알앤드디 매니지먼트 가부시키가이샤 모노시클릭 피리딘 유도체의 염 및 이의 결정
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
WO2016149401A2 (en) 2015-03-18 2016-09-22 Abide Therapeutics, Inc. Piperazine carbamates and methods of making and using same
JP6503450B2 (ja) 2015-03-25 2019-04-17 国立研究開発法人国立がん研究センター 胆管癌治療剤
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
EA201792496A1 (ru) 2015-05-11 2018-04-30 Абиде Терапеутикс, Инк. Способы лечения воспаления или нейропатической боли
KR20180026459A (ko) 2015-06-18 2018-03-12 세파론, 인코포레이티드 1,4-치환된 피페리딘 유도체
CA3014432C (en) 2015-06-18 2024-05-07 Cephalon, Inc. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
CA2991846A1 (en) * 2015-07-24 2017-02-02 Anne VASLIN-CHESSEX Fgfr expression and susceptibility to an fgfr inhibitor
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
CN108290856A (zh) 2015-08-11 2018-07-17 尼奥迈德研究所 芳基-取代的二氢喹诺酮、它们的制备和它们作为药物的用途
KR102784592B1 (ko) 2015-08-12 2025-03-19 에피제네틱스, 인크. 치환된 벤즈이미다졸, 그의 제조법 및 제약으로서의 그의 용도
US11542247B2 (en) 2015-09-23 2023-01-03 Janssen Pharmaceutica Nv Bi-heteroaryl substitute 1,4-benzodiazepines and uses thereof for the treatment of cancer
ES2811845T3 (es) 2015-09-23 2021-03-15 Janssen Pharmaceutica Nv Heterociclos tricíclicos para el tratamiento del cáncer
CA3257291C (en) 2015-10-16 2026-01-06 Abbvie Inc. Processes for the preparation of (3s,4r)-3-ethyl-4-(3h-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11780848B2 (en) 2015-10-16 2023-10-10 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof
US12365689B2 (en) 2015-10-16 2025-07-22 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
SG10201913213WA (en) 2015-12-17 2020-03-30 Eisai R&D Man Co Ltd Therapeutic agent for breast cancer
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
US10463753B2 (en) 2016-02-19 2019-11-05 Lundbeck La Jolla Research Center, Inc. Radiolabeled monoacylglycerol lipase occupancy probe
CR20180372A (es) 2016-02-24 2018-09-19 Pfizer Derivados de pirazolo [1,5-a] pirazin-4-ilo
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
WO2018053447A1 (en) 2016-09-19 2018-03-22 Abide Therapeutics, Inc. Piperazine carbamates and methods of making and using same
JOP20190106A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
JOP20190105A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
AU2018266911C1 (en) 2017-05-12 2022-10-20 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US11254668B2 (en) 2017-08-14 2022-02-22 Pfizer Inc. Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
MX2020007797A (es) * 2018-01-29 2020-09-18 Merck Patent Gmbh Inhibidores de la cinasa 2 de control general no desrepresible (gcn2) y usos de los mismos.
US10988477B2 (en) 2018-01-29 2021-04-27 Merck Patent Gmbh GCN2 inhibitors and uses thereof
WO2019178383A1 (en) * 2018-03-14 2019-09-19 Vanderbilt University Inhibition of bmp signaling, compounds, compositions and uses thereof
CN111712245A (zh) 2018-03-28 2020-09-25 卫材R&D管理有限公司 用于肝细胞癌的治疗剂
WO2019213244A1 (en) * 2018-05-02 2019-11-07 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
PE20210919A1 (es) 2018-05-04 2021-05-19 Incyte Corp Sales de un inhibidor de fgfr
CN119241541A (zh) 2018-05-04 2025-01-03 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
EP3793547A4 (en) 2018-05-15 2021-11-17 H. Lundbeck A/S MAGL INHIBITORS
CA3102279A1 (en) 2018-06-01 2019-12-05 Cornell University Combination therapy for pi3k-associated disease or disorder
GB201811695D0 (en) * 2018-07-17 2018-08-29 Salvensis Compounds for use in the treatment of fascioliasis
WO2020041417A1 (en) 2018-08-22 2020-02-27 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
TWI803696B (zh) 2018-09-14 2023-06-01 日商橘生藥品工業股份有限公司 次黃嘌呤化合物
CN117105933A (zh) 2018-10-31 2023-11-24 吉利德科学公司 具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物
CR20210215A (es) 2018-10-31 2021-06-17 Gilead Sciences Inc Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
US11345699B2 (en) 2018-11-19 2022-05-31 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CN111217816B (zh) * 2018-11-27 2022-08-16 中国科学院上海药物研究所 一类flt3激酶抑制剂及其制备和应用
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
WO2020198214A1 (en) 2019-03-25 2020-10-01 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
EP3985005A4 (en) * 2019-06-14 2023-07-19 CGeneTech (Suzhou, China) Co., Ltd. FUSED RING COMPOUND AS DUAL FGFR AND VEGFR INHIBITOR
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP7300057B2 (ja) * 2019-07-26 2023-06-28 シージーンテック (スーチョウ, チャイナ) カンパニー リミテッド Fgfrとvegfr二重阻害剤としてのピリジン誘導体
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
IL293001A (en) 2019-12-04 2022-07-01 Incyte Corp Derivatives of fgfr repressors
CN111116582B (zh) * 2019-12-18 2022-07-29 大连大学 一种mGluR2拮抗剂
US12012409B2 (en) * 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021147699A1 (zh) * 2020-01-21 2021-07-29 四川科伦博泰生物医药股份有限公司 吡啶并杂环类化合物、其制备方法及用途
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR102537615B1 (ko) 2020-02-25 2023-05-30 주식회사 종근당 히스톤 탈아세틸화효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이를 포함하는 약제학적 조성물
KR102537616B1 (ko) * 2020-02-25 2023-05-26 주식회사 종근당 히스톤 탈아세틸화 효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이를 포함하는 약제학적 조성물
WO2021214550A1 (en) 2020-04-21 2021-10-28 H. Lundbeck A/S Synthesis of a monoacylglycerol lipase inhibitor
CN112641782B (zh) * 2020-12-29 2022-02-11 北京鑫开元医药科技有限公司 一种fgfr4抑制剂的制剂组合物、制备方法及其用途
CN112279834B (zh) * 2020-12-29 2021-04-09 北京鑫开元医药科技有限公司 一种fgfr4抑制剂、制备方法、药物组合物及其应用
CN116783192B (zh) * 2021-01-26 2025-10-31 盛世泰科生物医药技术(苏州)股份有限公司 甲基吡唑取代的吡啶并咪唑类化合物的晶型及其制备方法
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
WO2023283488A2 (en) * 2021-07-09 2023-01-12 Chan Zuckerberg Biohub, Inc. Cdk19-selective inhibitors, and methods of use thereof
EP4469035A4 (en) * 2022-01-28 2026-01-07 Bridgene Biosciences Inc IMIDAZOPYRIDINE TYROSINE KINASE INHIBITORS
CN115368351B (zh) * 2022-07-28 2025-03-25 广东工业大学 一种多取代噁唑化合物的制备方法及其应用

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4503050A (en) 1983-06-02 1985-03-05 Riker Laboratories, Inc. Substituted imidazo[1,2-c]pyrimidines
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
EP0308020A3 (en) 1987-09-18 1990-12-05 Merck & Co. Inc. 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo 3-pyridinecarboxylic acids and derivatives thereof
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
US5554630A (en) * 1993-03-24 1996-09-10 Neurosearch A/S Benzimidazole compounds
CN1046725C (zh) 1994-06-20 1999-11-24 武田药品工业株式会社 稠合的咪唑化合物,它们的制备和应用
WO1996034866A1 (en) 1995-05-01 1996-11-07 Fujisawa Pharmaceutical Co., Ltd. Imidazo 1,2-a pyridine and imidazo 1,2-a pyridezine derivatives and their use as bone resorption inhibitors
US5882864A (en) 1995-07-31 1999-03-16 Urocor Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
PT915880E (pt) 1996-07-24 2007-12-31 Bristol Myers Squibb Pharma Co Azol triazinas e pirimidinas
CA2291709A1 (en) 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
US5990146A (en) * 1997-08-20 1999-11-23 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
US6465484B1 (en) * 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
ATE301657T1 (de) 1998-01-28 2005-08-15 Bristol Myers Squibb Pharma Co Azolo-pyrimidine
AU760020B2 (en) 1998-08-31 2003-05-08 Merck & Co., Inc. Novel angiogenesis inhibitors
US6245759B1 (en) 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2001000213A1 (en) 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor compounds
AU6605200A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
EP1194152A4 (en) 1999-06-30 2002-11-06 Merck & Co Inc Links to SRC kinase inhibition
JP2001057292A (ja) 1999-08-20 2001-02-27 Toray Ind Inc 発光素子
GB9919778D0 (en) * 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
GB9921150D0 (en) 1999-09-07 1999-11-10 Merck Sharp & Dohme Therapeutic agents
EP1214330A1 (en) 1999-09-21 2002-06-19 LION Bioscience AG Benzimidazole derivatives and combinatorial libraries thereof
GB9927687D0 (en) 1999-11-23 2000-01-19 Merck Sharp & Dohme Therapeutic agents
JP2003525291A (ja) * 2000-03-01 2003-08-26 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 2,4−二置換チアゾリル誘導体
CA2402315A1 (en) 2000-03-09 2001-09-13 Michael Jaye Therapeutic uses of ppar mediators
US20020041880A1 (en) * 2000-07-05 2002-04-11 Defeo-Jones Deborah Method of treating cancer
CA2417942C (en) 2000-08-04 2010-06-29 Warner-Lambert Company 2-(4-pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
AU2001295992A1 (en) 2000-10-24 2002-05-06 Sankyo Company Limited Imidazopyridine derivatives
GB0027561D0 (en) 2000-11-10 2000-12-27 Merck Sharp & Dohme Therapeutic agents
WO2002046168A1 (en) 2000-12-07 2002-06-13 Astrazeneca Ab Therapeutic benzimidazole compounds
US20020107262A1 (en) 2000-12-08 2002-08-08 3M Innovative Properties Company Substituted imidazopyridines
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
SE0100567D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
SE0100568D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
ATE416175T1 (de) 2001-02-20 2008-12-15 Astrazeneca Ab 2-arylaminopyrimidine zur behandlung von mit gsk3 in zusammenhang stehenden erkrankungen
TWI248936B (en) 2001-03-21 2006-02-11 Merck Sharp & Dohme Imidazo-pyrimidine derivatives as ligands for GABA receptors
DE10117183A1 (de) 2001-04-05 2002-10-10 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]-pyridinverbindungen als Arzneimittel
EP1382603B1 (en) * 2001-04-26 2008-07-23 Eisai R&D Management Co., Ltd. Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof
WO2003007955A2 (en) 2001-07-20 2003-01-30 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
GB0128499D0 (en) 2001-11-28 2002-01-23 Merck Sharp & Dohme Therapeutic agents
US6900208B2 (en) * 2002-03-28 2005-05-31 Bristol Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
US7662826B2 (en) * 2002-04-23 2010-02-16 Shionogi & Co., Ltd. Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same
JP2004002826A (ja) 2002-04-24 2004-01-08 Sankyo Co Ltd 高分子イミダゾピリジン誘導体
DE60318198T2 (de) 2002-05-02 2008-12-04 Merck & Co., Inc. Tyrosinkinase-hemmer
CN1671696B (zh) 2002-05-23 2010-12-08 Ym生物科学澳大利亚私人有限公司 激酶抑制剂
GB0212048D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
GB0212049D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
EP1511751B1 (en) 2002-06-04 2008-03-19 Neogenesis Pharmaceuticals, Inc. Pyrazolo[1,5-a]pyrimidine compounds as antiviral agents
PA8577501A1 (es) * 2002-07-25 2004-02-07 Warner Lambert Co Inhibidores de quinasas
CN100549011C (zh) 2002-09-19 2009-10-14 先灵公司 用作细胞周期蛋白依赖性激酶抑制剂的新颖咪唑并吡啶
GB0223349D0 (en) * 2002-10-08 2002-11-13 Merck Sharp & Dohme Therapeutic agents
WO2004035579A1 (ja) 2002-10-15 2004-04-29 Takeda Pharmaceutical Company Limited イミダゾピリジン誘導体、その製造法および用途
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
AU2003298942A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
WO2004075021A2 (en) * 2003-02-14 2004-09-02 Vertex Pharmaceuticals, Inc. Molecular modeling methods
US7476670B2 (en) * 2003-02-18 2009-01-13 Aventis Pharma S.A. Purine derivatives, method for preparing, pharmaceutical compositions and novel use
US7157460B2 (en) * 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
CA2520124A1 (en) 2003-03-28 2004-10-14 Chiron Corporation Use of benzazole compounds for immunopotentiation
MXPA06002019A (es) 2003-08-21 2006-05-31 Osi Pharm Inc Imidazopiridinas n3 sustituidas inhibidoras de c_kit.
US7442709B2 (en) * 2003-08-21 2008-10-28 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine c-Kit inhibitors
KR20060121818A (ko) 2003-08-21 2006-11-29 오에스아이 파마슈티컬스, 인코포레이티드 N-치환된 벤즈이미다졸릴 c-kit 억제제
ES2578254T3 (es) 2003-12-03 2016-07-22 Ym Biosciences Australia Pty Ltd Inhibidores de cinasas basados en azol
US7560568B2 (en) 2004-01-28 2009-07-14 Smithkline Beecham Corporation Thiazole compounds
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
CA2566184A1 (en) 2004-05-10 2005-11-17 Banyu Pharmaceutical Co., Ltd. Imidazopyridine compound
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
AU2005278292B2 (en) 2004-08-31 2011-09-08 Msd K.K. Novel substituted imidazole derivatives
JP2008513508A (ja) 2004-09-21 2008-05-01 シンタ ファーマシューティカルズ コーポレーション 炎症及び免疫に関連する用途に用いる化合物
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
CA2589770A1 (en) * 2004-12-01 2006-06-08 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library
JPWO2006070943A1 (ja) * 2004-12-28 2008-06-12 武田薬品工業株式会社 縮合イミダゾール化合物およびその用途
JP2008526723A (ja) 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Cdk、gsk及びオーロラキナーゼの活性を調節するピラゾール誘導体
DOP2006000051A (es) * 2005-02-24 2006-08-31 Lilly Co Eli Inhibidores de vegf-r2 y métodos
US7998974B2 (en) 2005-03-03 2011-08-16 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
RU2007140903A (ru) 2005-04-05 2009-05-20 Фармакопия, Инк. (Us) Производные пурина и имидазопиридина для иммуносупрессии
FR2884821B1 (fr) * 2005-04-26 2007-07-06 Aventis Pharma Sa Pyrrolopyridines substitues, compositions les contenant, procede de fabrication et utilisation
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
US7745428B2 (en) 2005-09-30 2010-06-29 Astrazeneca Ab Imidazo[1,2-A]pyridine having anti-cell-proliferation activity
TW200812587A (en) 2006-03-20 2008-03-16 Synta Pharmaceuticals Corp Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses
CA2646886A1 (en) * 2006-03-23 2007-10-04 Synta Pharmaceuticals Corp. Benzimidazolyl-pyridine compounds for inflammation and immune-related uses
ITVA20060041A1 (it) 2006-07-05 2008-01-06 Dialectica Srl Uso di composti derivati amminotiazolici, di loro composizioni farmaceutiche, nel trattamento di malattie caratterizzate dalla anormale repressione della trascrizione genica, particolarmente il morbo di huntington
TW200811134A (en) 2006-07-12 2008-03-01 Irm Llc Compounds and compositions as protein kinase inhibitors
EP1882475A1 (en) 2006-07-26 2008-01-30 Novartis AG Method of treating disorders mediated by the fibroblast growth factor receptor
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
US8513276B2 (en) * 2006-12-22 2013-08-20 Astex Therapeutics Limited Imidazo[1,2-a]pyridine compounds for use in treating cancer
CN101679408B (zh) 2006-12-22 2016-04-27 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
US8131527B1 (en) * 2006-12-22 2012-03-06 Astex Therapeutics Ltd. FGFR pharmacophore compounds
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
US8138181B2 (en) 2007-04-03 2012-03-20 Array Biopharma Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
CA2691987C (en) 2007-06-12 2016-08-16 Achaogen, Inc. Antibacterial agents
US20090005374A1 (en) 2007-06-26 2009-01-01 Melvin Jr Lawrence S Imidazopyridinyl thiazolyl histone deacetylase inhibitors
GB0720038D0 (en) * 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds

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AU2007337886C1 (en) 2014-10-16
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