JP5474354B2 - 医薬化合物 - Google Patents

医薬化合物 Download PDF

Info

Publication number
JP5474354B2
JP5474354B2 JP2008548032A JP2008548032A JP5474354B2 JP 5474354 B2 JP5474354 B2 JP 5474354B2 JP 2008548032 A JP2008548032 A JP 2008548032A JP 2008548032 A JP2008548032 A JP 2008548032A JP 5474354 B2 JP5474354 B2 JP 5474354B2
Authority
JP
Japan
Prior art keywords
cancer
group
acid
groups
mutation
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2008548032A
Other languages
English (en)
Japanese (ja)
Other versions
JP2009531276A (ja
JP2009531276A5 (https=
Inventor
バレリオ、ベルディーニ
ジェイン、エリザベス、カリー
ニール、ジェームス、ギャラガー
エイドリアン、リーアム、ギル
ジョン、フランシス、ライアンズ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Astex Therapeutics Ltd
Original Assignee
Astex Therapeutics Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0526607A external-priority patent/GB0526607D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of JP2009531276A publication Critical patent/JP2009531276A/ja
Publication of JP2009531276A5 publication Critical patent/JP2009531276A5/ja
Application granted granted Critical
Publication of JP5474354B2 publication Critical patent/JP5474354B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2008548032A 2005-12-30 2006-12-29 医薬化合物 Expired - Fee Related JP5474354B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US75533905P 2005-12-30 2005-12-30
US60/755,339 2005-12-30
GB0526607.7 2005-12-30
GB0526607A GB0526607D0 (en) 2005-12-30 2005-12-30 Pharmaceutical compounds
US80621806P 2006-06-29 2006-06-29
US60/806,218 2006-06-29
PCT/GB2006/004954 WO2007077435A1 (en) 2005-12-30 2006-12-29 Pharmaceutical compounds

Publications (3)

Publication Number Publication Date
JP2009531276A JP2009531276A (ja) 2009-09-03
JP2009531276A5 JP2009531276A5 (https=) 2010-02-18
JP5474354B2 true JP5474354B2 (ja) 2014-04-16

Family

ID=38006842

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008548032A Expired - Fee Related JP5474354B2 (ja) 2005-12-30 2006-12-29 医薬化合物

Country Status (4)

Country Link
US (1) US8399442B2 (https=)
EP (1) EP1968579A1 (https=)
JP (1) JP5474354B2 (https=)
WO (1) WO2007077435A1 (https=)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
EP1833819A1 (en) 2004-12-30 2007-09-19 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
WO2007087246A2 (en) * 2006-01-24 2007-08-02 Merck & Co., Inc. Jak2 tyrosine kinase inhibition
EP2049119A2 (en) 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea
WO2008001101A2 (en) * 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
JP5528807B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
GB0720113D0 (en) * 2007-10-15 2007-11-28 Cambridge Cancer Diagnostics L Diagnostic, prognostic and predictive testing for cancer
JP2011522212A (ja) * 2007-10-19 2011-07-28 セル・シグナリング・テクノロジー・インコーポレイテツド 癌の分類および使用法
WO2009138799A1 (en) * 2008-05-14 2009-11-19 Astex Therapeutics Limited Therapeutic uses of 1-cycl0pr0pyl-3 - [3- ( 5 -morpholin- 4 -ylmethyl- 1h-benz0imidaz0l- 2 -yl) -lh-pyrazol-4-yl] -urea
PT2350075E (pt) 2008-09-22 2014-06-09 Array Biopharma Inc Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
PH12012500252A1 (en) 2009-08-07 2015-06-26 Chugai Pharmaceutical Co Ltd Aminopyrazole derivative
JP6161537B2 (ja) 2010-04-07 2017-07-12 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ピラゾール−4−イル−ヘテロシクリル−カルボキサミド化合物及び使用の方法
EP2568980B1 (en) * 2010-05-12 2015-11-11 Merial, Inc. Injectable parasiticidal formulations of levamisole and macrocyclic lactones
WO2012119091A1 (en) * 2011-03-02 2012-09-07 Beth Israel Deaconess Medical Center, Inc. Mcl-1 as a therapeutic target in scffbw7 deficient neoplasm
AR088061A1 (es) 2011-09-27 2014-05-07 Hoffmann La Roche Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso
US9241920B2 (en) 2011-10-27 2016-01-26 New York University Inhibition of c-Myc ubiquitination to prevent cancer initiation and progression
JP6180425B2 (ja) 2011-11-23 2017-08-23 メディミューン,エルエルシー Her3に特異的な結合分子及びそれらの使用
EP2636752A1 (en) * 2012-03-06 2013-09-11 Universiteit Maastricht In vitro method for determining disease outcome in pulmonary carcinoids.
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
RU2015117950A (ru) * 2012-10-26 2016-12-20 Ф. Хоффманн-Ля Рош Аг 3,4-дизамещенный 1н-пиразол и 4,5-дизамещенный тиазол в качестве ингибиторов тирозинкиназы syk
PL403149A1 (pl) * 2013-03-14 2014-09-15 Celon Pharma Spółka Akcyjna Nowe związki pochodne pirazolilobenzo[d]imidazolu
JP6799201B2 (ja) 2013-07-31 2020-12-16 アヴァリン ファーマ インク. エアロゾルチロシンキナーゼ阻害剤の化合物、及びその使用
US11305012B2 (en) 2013-09-24 2022-04-19 Medimmune, Llc Binding molecules specific for HER3 and uses thereof
US10391081B2 (en) 2013-12-27 2019-08-27 Chugai Seiyaku Kabushiki Kaisha FGFR gatekeeper mutant gene and drug targeting same
ES2913339T3 (es) * 2014-01-31 2022-06-01 Draka Elevator Products Inc Dispositivo sensor de detección sísmica para equipo de transporte vertical
US10745490B2 (en) 2014-04-11 2020-08-18 Celldex Therapeutics, Inc. Anti-ErbB antibodies and methods of use thereof
EA201692549A1 (ru) * 2014-06-20 2017-08-31 Эвайраджен Терепьютикс, Инк. Безводная кристаллическая форма свободного основания 6-{2-[1-(6-метил-3-пиридазинил)-4-пиперидинил]этокси}-3-этокси-1,2-бензизоксазола
MA40596B1 (fr) 2014-08-11 2021-12-31 Acerta Pharma Bv Combinaisons thérapeutiques d'un inhibiteur de btk et d'un inhibiteur de bcl-2
TW201618773A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Btk抑制劑、pi3k抑制劑、jak-2抑制劑、及/或cdk4/6抑制劑的治療組合物
US20170239351A1 (en) 2014-08-11 2017-08-24 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, a PD-1 Inhibitor, and/or a PD-L1 Inhibitor
HUE061448T2 (hu) 2014-11-16 2023-07-28 Array Biopharma Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid-hidrogénszulfát kristályos formája
EP3312172B1 (en) 2015-06-17 2020-05-06 Chugai Seiyaku Kabushiki Kaisha Aminopyrazole derivatives useful as src kinase inhibitors
BR112018000808A2 (pt) 2015-07-16 2018-09-04 Array Biopharma Inc compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase
CN108697708A (zh) 2015-10-26 2018-10-23 洛克索肿瘤学股份有限公司 Trk抑制剂抗性癌症中的点突变以及与此相关的方法
BR112018009252A2 (pt) 2015-11-06 2018-11-06 Samumed Llc tratamento da osteoartrite
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
ES2987474T3 (es) 2016-04-04 2024-11-15 Loxo Oncology Inc Formulaciones líquidas de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-IL)-pirazolo[1,5-A]pirimidin-3-IL)-3-hidroxipirrolidina-1-carboxamida
ES2836222T3 (es) 2016-05-18 2021-06-24 Loxo Oncology Inc Preparación de (S)-N-(5-((R)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
LT3464285T (lt) 2016-06-01 2022-12-27 Biosplice Therapeutics, Inc. N-(5-(3-(7-(3-fluorfenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)- 3-metilbutanamido gamybos būdas
TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CN110494434B (zh) * 2017-03-14 2022-05-24 豪夫迈·罗氏有限公司 吡唑并氯苯基化合物、其组合物及其使用方法
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
CN111615514B (zh) 2018-01-18 2022-10-11 奥瑞生物药品公司 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物
EP3752161A4 (en) * 2018-02-15 2021-12-22 Children's Hospital Medical Center METHOD OF TREATMENT OF FIBROSE
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
WO2019178239A1 (en) * 2018-03-13 2019-09-19 Board Of Regents, The University Of Texas System Methods for treatment of cancers with egfr activating mutations
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
EP3849986B1 (en) 2018-09-10 2022-06-08 Array Biopharma, Inc. Fused heterocyclic compounds as ret kinase inhibitors
US20230000842A1 (en) * 2019-01-17 2023-01-05 Samumed, Llc Methods of treating cartilage disorders through inhibition of clk and dyrk
CN113631179A (zh) * 2019-01-25 2021-11-09 努梅迪公司 用于治疗特发性肺纤维化的方法
WO2025040140A1 (en) * 2023-08-22 2025-02-27 National Institute Of Biological Sciences, Beijing Substituted pyrazol-4-yl urea as kinase inhibitors
WO2025111251A1 (en) * 2023-11-20 2025-05-30 Exelixis, Inc. Compounds that inhibit polo-like kinase 4

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4619686A (en) 1984-07-17 1986-10-28 Eli Lilly And Company Pyridazinylurea compounds and methods of use as herbicides
US5451596A (en) 1992-12-29 1995-09-19 Rhone Poulenc Rorer Pharmaceuticals Inc. Cycloalkyl amine bis-aryl squalene synthase inhibitors
FR2707295A1 (fr) 1993-06-07 1995-01-13 Rhone Poulenc Agrochimie Fongicides pyrazoles substitués en position 3 par un hétérocycle.
US5852011A (en) 1994-05-31 1998-12-22 Mitsui Chemicals, Inc. Benzimidazole derivatives
EP0766676B1 (en) 1994-06-24 2002-05-22 Euroceltique S.A. Compounds for inhibiting phosphodiesterase iv
ATE251141T1 (de) * 1995-03-10 2003-10-15 Berlex Lab Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
AU706497B2 (en) 1996-04-03 1999-06-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DK0906279T3 (da) * 1996-05-30 2003-02-03 Hoffmann La Roche Pyrrolderivater
AU2713799A (en) 1998-03-12 1999-09-27 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
NZ525108A (en) 1998-03-31 2005-02-25 Acadia Pharm Inc Compounds with activity on muscarinic receptors
ATE316961T1 (de) 1998-05-22 2006-02-15 Scios Inc Heterozyclische derivate für die behandlung von herzversagen und andere erkrankungen
WO2000038683A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
WO2000059902A2 (en) 1999-04-02 2000-10-12 Du Pont Pharmaceuticals Company Aryl sulfonyls as factor xa inhibitors
NZ515086A (en) 1999-04-28 2003-10-31 Aventis Pharma Gmbh Di-aryl acid derivatives as PPAR receptor ligands
DE19920936A1 (de) * 1999-05-07 2000-11-09 Basf Ag Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung
SI1194425T1 (sl) * 1999-06-23 2005-12-31 Sanofi Aventis Deutschland Substituirani benzimidazoli
FR2795726A1 (fr) 1999-06-30 2001-01-05 Aventis Cropscience Sa Nouveaux pyrazoles fongicides
DE60040676D1 (de) 1999-09-17 2008-12-11 Millennium Pharm Inc BENZAMIDE UND ÄHNLICHE INHIBITOREN VON FAKTOR Xa
JP2003509412A (ja) 1999-09-17 2003-03-11 シーオーアール セラピューティクス インコーポレイテッド Xa因子阻害剤
HUP0202332A2 (en) 2000-02-05 2002-10-28 Vertex Pharma Pyrazole compositions useful as inhibitors of erk
AU2001250783A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
US20040087798A1 (en) 2000-03-14 2004-05-06 Akira Yamada Novel amide compounds
JP2004501083A (ja) 2000-04-18 2004-01-15 アゴーロン・ファーマシューティカルズ・インコーポレイテッド プロテインキナーゼを阻害するためのピラゾール
EP1296982B1 (en) 2000-06-23 2007-09-19 Bristol-Myers Squibb Pharma Company 1-(heteroaryl-phenyl)-condensed pyrazol derivatives as factor xa inhibitors
AU2001268711A1 (en) 2000-06-23 2002-01-08 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
NZ526472A (en) 2000-12-21 2004-04-30 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
DE10108480A1 (de) * 2001-02-22 2002-09-05 Bayer Ag Pyrazolylpyrimidine
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
US6951848B2 (en) 2001-03-12 2005-10-04 Millennium Pharmaceuticals, Inc., Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
US6890915B2 (en) 2001-05-25 2005-05-10 Bristol-Myers Squibb Pharma Company Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
DE60206756T2 (de) 2001-06-29 2006-07-13 CV Therapeutics, Inc., Palo Alto Purin derivate als a2b adenosin rezeptor antagonisten
US7064215B2 (en) 2001-07-03 2006-06-20 Chiron Corporation Indazole benzimidazole compounds
WO2003006465A1 (en) 2001-07-13 2003-01-23 Cv Therapeutics, Inc. Partial and full agonist of a adenosine receptors
US6897208B2 (en) * 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
FR2831536A1 (fr) 2001-10-26 2003-05-02 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr
JP5039268B2 (ja) * 2001-10-26 2012-10-03 アベンティス・ファーマスーティカルズ・インコーポレイテツド ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
AU2002349477A1 (en) 2001-11-26 2003-06-10 Takeda Chemical Industries, Ltd. Bicyclic derivative, process for producing the same, and use
AU2002357312A1 (en) 2001-12-20 2003-07-09 Bristol-Myers Squibb Company Barbituric acid derivatives as inhibitors of tnf-alpha converting enzyme (tace) and/or matrix metalloproteinases
EP1472245A2 (en) 2002-02-06 2004-11-03 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
TWI324597B (en) * 2002-03-28 2010-05-11 Astrazeneca Ab Quinazoline derivatives
EP1581217A4 (en) 2002-11-01 2007-07-11 Merck & Co Inc CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF ANDROGENIC RECEPTORS
AU2003285336B2 (en) 2002-12-04 2009-11-26 Sanofi-Aventis Deutschland Gmbh Imidazole-derivatives as factor Xa inhibitors
WO2004052371A2 (en) 2002-12-11 2004-06-24 7Tm Pharma A/S Cyclic quinoline compounds for use in mch receptor related disorders
EP1581527A4 (en) 2002-12-13 2006-11-22 Smithkline Beecham Corp MIMETICS OF THROMBOPOIETINE
JP4585448B2 (ja) 2002-12-23 2010-11-24 サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 第Xa因子阻害剤としてのピラゾール−誘導体
US20040242559A1 (en) * 2003-04-25 2004-12-02 Aventis Pharma S.A. Novel indole derivatives, preparation thereof as medicinal products and pharmaceutical compositions, and especially as KDR inhibitors
FR2854159B1 (fr) * 2003-04-25 2008-01-11 Aventis Pharma Sa Nouveaux derives de l'indole, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de kdr
GB0315657D0 (en) * 2003-07-03 2003-08-13 Astex Technology Ltd Pharmaceutical compounds
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
US20050032869A1 (en) * 2003-07-08 2005-02-10 Pharmacia Italia S.P.A. Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
US8969372B2 (en) 2003-11-14 2015-03-03 Aptose Boisciences Inc. Aryl imidazoles and their use as anti-cancer agents
US7932281B2 (en) 2004-03-10 2011-04-26 Kureha Corporation Amine-based compound and use thereof
WO2006071940A2 (en) 2004-12-23 2006-07-06 Deciphera Pharmaceuticals, Llc Enzyme modulators and treatments
EP1833819A1 (en) * 2004-12-30 2007-09-19 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
WO2006070192A1 (en) * 2004-12-30 2006-07-06 Astex Therapeutics Limited Thiazole and isothiazole derivatives that modulate the acivity of cdk, gsk and aurora kynases
WO2006092430A1 (de) 2005-03-03 2006-09-08 Universität des Saarlandes Selektive hemmstoffe humaner corticoidsynthasen
AU2006218403A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
WO2006094209A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N-benzimidazolylalkyl-substituted amide sirtuin modulators
WO2006124780A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Ih-benzo [d] imidazole compounds as inhibitors of b-raf kinase
EP1899299B1 (en) 2005-06-27 2010-10-20 Bristol-Myers Squibb Company C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
EP1910385B1 (en) 2005-08-04 2013-07-24 Sirtris Pharmaceuticals, Inc. Benzothiazoles and thiazolopyridines as sirtuin modulators
JP2007045752A (ja) 2005-08-10 2007-02-22 Takeda Chem Ind Ltd 5員芳香族複素環誘導体、その製造法および用途
DE102005057894A1 (de) 2005-12-02 2007-06-06 Basf Ag Stabilisierte polymerisierbare Mischungen
EP2049119A2 (en) * 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea
WO2008001101A2 (en) 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
FR2903406B1 (fr) 2006-07-04 2012-08-10 Aventis Pharma Sa Derives de pyrazolylbenzimidazole,compositions les contenant et utilisation
JP5528807B2 (ja) * 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤

Also Published As

Publication number Publication date
JP2009531276A (ja) 2009-09-03
US8399442B2 (en) 2013-03-19
WO2007077435A1 (en) 2007-07-12
EP1968579A1 (en) 2008-09-17
US20100004232A1 (en) 2010-01-07

Similar Documents

Publication Publication Date Title
JP5474354B2 (ja) 医薬化合物
KR101334511B1 (ko) Cdk, gsk 및 오로라 키나아제의 활성을 조절하는피라졸 화합물
CA2531050C (en) Pharmaceutical compounds
US9856236B2 (en) Substituted quinoxalines as FGFR kinase inhibitors
JP5639261B2 (ja) ピラゾリルキノキサリンキナーゼ阻害剤
JP5596023B2 (ja) レセプターチロシンキナーゼのインヒビターとしてのイミダゾピリジン誘導体
JP6169583B2 (ja) Fgfrキナーゼの阻害を介した抗癌ピリドピラジン
JP2008505167A (ja) 医薬組成物
US20100160324A1 (en) Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
BR112014010183B1 (pt) Composto, composição farmacêutica, produto, e, uso de um composto
BR112014029706B1 (pt) Composto, composição farmacêutica, e, uso de um composto
JP2008526721A (ja) Cdk、gsk及びオーロラキナーゼの活性を調節するチアゾールおよびイソチアゾール誘導体
CN101379058A (zh) 调节cdk、gsk极光激酶活性的吡唑类化合物
KR101190964B1 (ko) 벤즈이미다졸 유도체 및 단백질 키나제로서의 그의 용도
HK1087925B (en) Benzimidazole derivatives and their use as protein kinases inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20091225

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20100104

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20101213

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20121012

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130111

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130121

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20130611

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131010

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20131203

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140107

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140205

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees