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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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
Active legal-status Critical Current
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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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • 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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    • A61P25/28Drugs 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]
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    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
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    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (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
GB0625826A GB0625826D0 (en) 2006-12-22 2006-12-22 New compounds
US60/871,543 2006-12-22
US97958707P 2007-10-12 2007-10-12
GB0720000.9 2007-10-12
US60/979,587 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

ID=39260738

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 (https=)
EP (1) EP2114941B1 (https=)
JP (1) JP5442448B2 (https=)
CN (1) CN101679408B (https=)
AR (1) AR064491A1 (https=)
AU (1) AU2007337886C1 (https=)
CA (1) CA2672172C (https=)
HR (1) HRP20150642T1 (https=)
MX (1) MX2009006706A (https=)
NO (1) NO343370B1 (https=)
WO (1) WO2008078091A1 (https=)

Families Citing this family (161)

* 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
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc 1,4-二取代之3-氰基-吡啶酮衍生物及其作為mGluR2-受體之正向異位性調節劑之用途
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
CN101679409B (zh) 2006-12-22 2014-11-26 Astex治疗学有限公司 双环杂环衍生化合物、其医药组合物和其用途
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
PL2203439T3 (pl) 2007-09-14 2011-06-30 Addex Pharmaceuticals Sa 1',3'-dipodstawione-4-fenylo-3,4,5,6-tetrahydro-2H, 1'H-[1, 4']bipirydynylo-2'-ketony
US8252937B2 (en) 2007-09-14 2012-08-28 Janssen Pharmaceuticals, Inc. 1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones
US8722894B2 (en) 2007-09-14 2014-05-13 Janssen Pharmaceuticals, Inc. 1,3-disubstituted-4-phenyl-1H-pyridin-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
BRPI0817434A2 (pt) * 2007-10-17 2015-06-16 Novartis Ag Composto orgânicos
RU2492170C9 (ru) 2007-11-14 2013-12-27 Орто-Макнейл-Янссен Фармасьютикалз, Инк. Имидазо[1,2-а]пиридиновые производные и их применение в качестве положительных аллостерических модуляторов рецепторов mglur2
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
JP5547194B2 (ja) 2008-09-02 2014-07-09 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3−アザビシクロ[3.1.0]ヘキシル誘導体
RU2517181C2 (ru) 2008-10-16 2014-05-27 Орто-Макнейл-Янссен Фармасьютикалз, Инк. Производные индола и бензоморфолина в качестве модулятора метаботропных глутаматных рецепторов
WO2010060589A1 (en) * 2008-11-28 2010-06-03 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
MX2011009796A (es) 2009-03-20 2011-12-14 Amgen Inc Inhibidores de la cinasa pi3.
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
CN102439008B (zh) 2009-05-12 2015-04-29 杨森制药有限公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其用于治疗或预防神经和精神病症的用途
MY153912A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 1, 2, 4,-triazolo[4,3-a[pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
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
PE20121148A1 (es) * 2009-08-17 2012-09-07 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
US20130196986A1 (en) * 2010-09-21 2013-08-01 Marc Labroli Triazolopyrazinones as p2x7 receptor antagonists
CN103261195B (zh) 2010-11-08 2015-09-02 杨森制药公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
EP2661435B1 (en) 2010-11-08 2015-08-19 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
PL2649069T3 (pl) 2010-11-08 2016-01-29 Janssen Pharmaceuticals Inc Pochodne 1,2,4-triazolo[4,3-a]pirydyny i ich zastosowanie jako dodatnich allosterycznych modulatorów receptorów mGluR2
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
KR101901153B1 (ko) * 2011-01-13 2018-09-21 바이엘 인텔렉쳐 프로퍼티 게엠베하 2,2-디플루오로-1-클로로에탄과 암모니아로부터 2,2-디플루오로에틸아민의 제조방법
UA111382C2 (uk) * 2011-10-10 2016-04-25 Оріон Корпорейшн Інгібітори протеїнкінази
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
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
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
PE20141702A1 (es) 2012-01-06 2014-11-19 Abide Therapeutics Inc Compuestos de carbamato y preparacion y uso de los mismos
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
AU2013250726B2 (en) 2012-04-20 2017-01-05 Advinus Therapeutics Limited Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
ES2704744T3 (es) 2012-06-13 2019-03-19 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
SMT202100451T1 (it) 2012-07-11 2021-09-14 Blueprint Medicines Corp Inibitori del recettore di crescita dei fibroblasti
CN104619709B (zh) * 2012-07-13 2016-11-09 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
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
KR102092988B1 (ko) * 2012-09-28 2020-03-25 벤더르빌트 유니버시티 선택성 bmp 저해제로써 융합된 헤테로 고리 화합물들
CN105164124B (zh) 2012-11-19 2017-03-15 诺华股份有限公司 用于治疗寄生虫疾病的化合物和组合物
US8871754B2 (en) 2012-11-19 2014-10-28 Irm Llc 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
BR112015008200A2 (pt) * 2012-11-29 2017-07-04 Hoffmann La Roche derivados de imidazopiridina
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
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
TWI628176B (zh) * 2013-04-04 2018-07-01 奧利安公司 蛋白質激酶抑制劑
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
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
CA2928042C (en) 2013-10-25 2022-05-10 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2015086642A1 (en) 2013-12-13 2015-06-18 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
HUE053734T2 (hu) 2014-01-21 2021-07-28 Janssen Pharmaceutica Nv 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait tartalmazó kombinációk és alkalmazásuk
KR20220049612A (ko) 2014-01-21 2022-04-21 얀센 파마슈티카 엔.브이. 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도
MA38393B1 (fr) 2014-03-13 2018-11-30 Sanofi Sa Composés hétéroaryle et utilisations associées
MX373150B (es) 2014-03-26 2020-04-21 Astex Therapeutics Ltd Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r).
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JP6752715B2 (ja) 2014-03-26 2020-09-09 アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited 組合せ
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
TWI719960B (zh) 2015-02-10 2021-03-01 英商阿斯迪克治療公司 新穎組成物
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
JP2018513119A (ja) 2015-03-18 2018-05-24 アビデ セラピューティクス,インク. ピペラジンカルバメート、およびピペラジンカルバメートを製造ならびに使用する方法
ES2887148T3 (es) 2015-03-25 2021-12-21 Nat Cancer Ct Agente terapéutico contra el cáncer de vías biliares
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
CN113413387A (zh) 2015-05-11 2021-09-21 H.隆德贝克有限公司 治疗炎症或神经性疼痛的方法
ES2849951T3 (es) 2015-06-18 2021-08-24 89Bio Ltd Derivados de piperidina 4-bencil y 4-benzoil sustituidos
EA201890086A1 (ru) 2015-06-18 2018-06-29 Сефалон, Инк. 1,4-замещенные производные пиперидина
BR112018001438A2 (en) * 2015-07-24 2018-12-04 Debiopharm International S.A. gffr expression and susceptibility to a gffr inhibitor
WO2017024408A1 (en) 2015-08-11 2017-02-16 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
CN108137539B (zh) 2015-08-12 2022-01-11 尼奥迈德研究所 取代的苯并咪唑、它们的制备和它们作为药物的用途
AU2016328693B2 (en) 2015-09-23 2021-03-11 Janssen Pharmaceutica Nv Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
DK3353177T3 (da) 2015-09-23 2020-08-24 Janssen Pharmaceutica Nv Tricykliske heterocykler til behandling af cancer
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
EP3362455A1 (en) 2015-10-16 2018-08-22 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
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
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
US12414945B2 (en) 2015-12-17 2025-09-16 Eisai R&D Management 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
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
US10899737B2 (en) 2016-09-19 2021-01-26 Lundbeck La Jolla Research Center, 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)
CN110869017B (zh) 2017-05-12 2023-05-05 英安塔制药有限公司 细胞凋亡信号调节激酶1抑制剂及其使用方法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019034973A1 (en) 2017-08-14 2019-02-21 Pfizer Inc. PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
EP3746071A4 (en) * 2018-01-29 2021-09-01 Merck Patent GmbH GCN2 INHIBITORS AND THEIR USES
KR20200116481A (ko) * 2018-01-29 2020-10-12 메르크 파텐트 게엠베하 Gcn2 억제제 및 이의 용도
WO2019178383A1 (en) * 2018-03-14 2019-09-19 Vanderbilt University Inhibition of bmp signaling, compounds, compositions and uses thereof
SG11202007591RA (en) 2018-03-28 2020-09-29 Eisai R&D Man Co Ltd Therapeutic agent for hepatocellular carcinoma
EP3787621B1 (en) 2018-05-02 2024-12-18 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
GEP20227443B (en) 2018-05-15 2022-11-25 H Lundbeck As Magl inhibitors
CN113194752A (zh) 2018-06-01 2021-07-30 康奈尔大学 Pi3k相关疾病或病症的组合疗法
GB201811695D0 (en) * 2018-07-17 2018-08-29 Salvensis Compounds for use in the treatment of fascioliasis
US10968199B2 (en) 2018-08-22 2021-04-06 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
TW202136261A (zh) 2018-10-31 2021-10-01 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
TWI721623B (zh) 2018-10-31 2021-03-11 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
WO2020106707A1 (en) 2018-11-19 2020-05-28 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
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020131627A1 (en) * 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
US11466033B2 (en) 2019-03-25 2022-10-11 Enanta Pharmaceuticals, Inc. Substituted pyridines as apoptosis signal-regulating kinase 1 inhibitors
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
CA3141424C (en) * 2019-06-14 2023-11-07 Zhengxia CHEN Fused ring compound as fgfr and vegfr dual inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR102753831B1 (ko) * 2019-07-26 2025-01-14 씨젠테크 (쑤저우, 차이나) 컴퍼니 리미티드 Fgfr 및 vegfr 이중 억제제로서의 피리딘 유도체
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為fgfr抑制劑之雙環雜環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
CN111116582B (zh) * 2019-12-18 2022-07-29 大连大学 一种mGluR2拮抗剂
WO2021146424A1 (en) * 2020-01-15 2021-07-22 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
AU2021320860A1 (en) 2020-08-05 2023-02-23 The General Hospital Corporation Salt inducible kinase inhibitors
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
CA3206502A1 (en) * 2021-01-26 2022-08-04 Zhengxia CHEN Crystal form of methylpyrazole-substituted pyridoimidazole compound and preparation method therefor
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20240351996A1 (en) * 2021-07-09 2024-10-24 Cz Biohub Sf, Llc 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
DE69524598T2 (de) 1994-06-20 2002-07-11 Takeda Chemical Industries, Ltd. Kondensierte imidazolderivate, ihre herstellung und verwendung
AU5348396A (en) 1995-05-01 1996-11-21 Fujisawa Pharmaceutical Co., Ltd. Imidazo 1,2-a pyridine and imidazo 1,2-a pyridezine derivati ves and their use as bone resorption inhibitors
WO1998004689A1 (en) 1995-07-31 1998-02-05 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
HU228962B1 (en) 1996-07-24 2013-07-29 Bristol Myers Squibb Pharma Co Azolo triazines, pharmaceutical compositions containing them and use of the compounds
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
WO2000012089A1 (en) 1998-08-31 2000-03-09 Merck & Co., Inc. Novel angiogenesis inhibitors
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
EP1049699B1 (en) 1998-01-28 2004-04-21 Bristol-Myers Squibb Pharma Company Pyrazolotriazines as crf antagonists
US6245759B1 (en) * 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
AU5636900A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
WO2001000214A1 (en) 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor compounds
JP2003503351A (ja) 1999-06-30 2003-01-28 メルク エンド カムパニー インコーポレーテッド Srcキナーゼ阻害化合物
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
WO2001021634A1 (en) 1999-09-21 2001-03-29 Lion Bioscience Ag Benzimidazole derivatives and combinatorial libraries thereof
GB9927687D0 (en) 1999-11-23 2000-01-19 Merck Sharp & Dohme Therapeutic agents
AU2001237401B2 (en) 2000-03-01 2006-11-09 Janssen Pharmaceutica N.V. 2,4-disubstituted thiazolyl derivatives
KR20020081424A (ko) 2000-03-09 2002-10-26 아벤티스 파마 도이칠란트 게엠베하 Ppar 매개인자의 치료학적 용도
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
WO2002034748A1 (fr) 2000-10-24 2002-05-02 Sankyo Company, Limited Derives d'imidazopyridine
GB0027561D0 (en) 2000-11-10 2000-12-27 Merck Sharp & Dohme Therapeutic agents
US20070004713A1 (en) 2000-12-07 2007-01-04 Bernard Barlaam Therapeutic benimidazole 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
EP1423388B1 (en) 2001-02-20 2008-12-03 AstraZeneca AB 2-arylamino-pyrimidines for the treatment of gsk3-related disorders
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
US7074801B1 (en) 2001-04-26 2006-07-11 Eisai Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical 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
EP1505068A4 (en) 2002-04-23 2008-03-19 Shionogi & Co PYRAZOLO (1,5-a) PYRIMIDINE DERIVATIVE AND INHIBITOR OF NAD (P) H OXIDASE CONTAINING SAID DERIVATIVE
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
WO2003092595A2 (en) 2002-05-02 2003-11-13 Merck & Co., Inc Tyrosine kinase inhibitors
NZ537156A (en) 2002-05-23 2007-06-29 Cytopia Pty Ltd Kinase inhibitors
GB0212049D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
GB0212048D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
US7196111B2 (en) 2002-06-04 2007-03-27 Schering Corporation Pyrazolo[1,5a]pyrimidine compounds as antiviral agents
US7196090B2 (en) 2002-07-25 2007-03-27 Warner-Lambert Company Kinase inhibitors
ATE378336T1 (de) 2002-09-19 2007-11-15 Schering Corp Imidazopyridine als hemmstoffe cyclin abhängiger kinasen
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
AU2003298942A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
US7826979B2 (en) 2003-02-14 2010-11-02 Vertex Pharmaceuticals Incorporated Method of modeling complex formation between a query ligan and a target molecule
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
US7893096B2 (en) 2003-03-28 2011-02-22 Novartis Vaccines And Diagnostics, Inc. Use of small molecule compounds for immunopotentiation
AU2004268949A1 (en) 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl C-kit inhibitors
US7442709B2 (en) 2003-08-21 2008-10-28 Osi Pharmaceuticals, Inc. N3-substituted imidazopyridine c-Kit inhibitors
DE602004020073D1 (de) 2003-08-21 2009-04-30 Osi Pharm Inc 3-substituierte imidazopyridinderivate als c-kit-inhibitoren
BRPI0417345A (pt) 2003-12-03 2007-03-13 Cytopia Res Pty Ltd compostos inibidores de quìnase baseados em azola, composições e seus usos
EP1711496A4 (en) 2004-01-28 2009-02-11 Smithkline Beecham Corp THIAZOLE COMPOUNDS
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
CN1950372A (zh) 2004-05-10 2007-04-18 万有制药株式会社 咪唑并吡啶化合物
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
US7718801B2 (en) * 2004-08-31 2010-05-18 Banyu Pharmaceutical Co., Ltd. Substituted imidazole derivative
CN101083985A (zh) 2004-09-21 2007-12-05 幸讬制药公司 用于炎症及免疫相关用途的化合物
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
EP1831206B1 (en) 2004-12-01 2011-08-24 OSI Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library
US20080167314A1 (en) * 2004-12-28 2008-07-10 Osamu Uchikawa Condensed Imidazole Compound And Use Thereof
US20100160324A1 (en) 2004-12-30 2010-06-24 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
DOP2006000051A (es) 2005-02-24 2006-08-31 Lilly Co Eli Inhibidores de vegf-r2 y métodos
AU2006218403A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
NZ562468A (en) 2005-04-05 2009-10-30 Pharmacopeia Inc Purine and imidazopyridine derivatives for immunosuppression
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
WO2007036732A1 (en) 2005-09-30 2007-04-05 Astrazeneca Ab Imidazo [1,2-a] pyridine having anti-cell-proliferation activity
US8119643B2 (en) 2006-03-20 2012-02-21 Synta Pharmaceuticals Corp. Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses
US8163777B2 (en) * 2006-03-23 2012-04-24 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
US8131527B1 (en) 2006-12-22 2012-03-06 Astex Therapeutics Ltd. FGFR pharmacophore compounds
CN101679409B (zh) * 2006-12-22 2014-11-26 Astex治疗学有限公司 双环杂环衍生化合物、其医药组合物和其用途
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
EP2137184B1 (en) 2007-04-03 2013-05-08 Array Biopharma, Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
JP5539864B2 (ja) 2007-06-12 2014-07-02 アカオゲン,インコーポレーテッド 抗菌剤
EP2170882A1 (en) 2007-06-26 2010-04-07 Gilead Colorado, Inc. Imidazopyridinyl thiazolyl histone deacetylase inhibitors
GB0720041D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New Compounds
GB0720038D0 (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
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

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