AU2007336011B2 - Acylaminopyrazoles as FGFR inhibitors - Google Patents

Acylaminopyrazoles as FGFR inhibitors Download PDF

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Publication number
AU2007336011B2
AU2007336011B2 AU2007336011A AU2007336011A AU2007336011B2 AU 2007336011 B2 AU2007336011 B2 AU 2007336011B2 AU 2007336011 A AU2007336011 A AU 2007336011A AU 2007336011 A AU2007336011 A AU 2007336011A AU 2007336011 B2 AU2007336011 B2 AU 2007336011B2
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AU
Australia
Prior art keywords
pyrazol
alkyl
ethyl
dimethoxyphenyl
halogen
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Active
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AU2007336011A
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AU2007336011A1 (en
Inventor
David Buttar
Kevin Michael Foote
Maria-Elena Theoclitou
Andrew Peter Thomas
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AstraZeneca AB
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AstraZeneca AB
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 two hetero rings
    • C07D401/06—Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 two hetero rings
    • C07D401/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/06—Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
AU2007336011A 2006-12-21 2007-12-20 Acylaminopyrazoles as FGFR inhibitors Active AU2007336011B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US87119006P 2006-12-21 2006-12-21
US60/871,190 2006-12-21
US98554207P 2007-11-05 2007-11-05
US60/985,542 2007-11-05
PCT/GB2007/004917 WO2008075068A2 (en) 2006-12-21 2007-12-20 Acylaminopyrazoles as fgfr inhibitors

Publications (2)

Publication Number Publication Date
AU2007336011A1 AU2007336011A1 (en) 2008-06-26
AU2007336011B2 true AU2007336011B2 (en) 2011-09-22

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2007336011A Active AU2007336011B2 (en) 2006-12-21 2007-12-20 Acylaminopyrazoles as FGFR inhibitors

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US (6) US7737149B2 (cg-RX-API-DMAC7.html)
EP (1) EP2125748B1 (cg-RX-API-DMAC7.html)
JP (1) JP5000726B2 (cg-RX-API-DMAC7.html)
KR (1) KR101467593B1 (cg-RX-API-DMAC7.html)
AR (1) AR064454A1 (cg-RX-API-DMAC7.html)
AT (1) ATE510825T1 (cg-RX-API-DMAC7.html)
AU (1) AU2007336011B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0720551A2 (cg-RX-API-DMAC7.html)
CA (1) CA2672521C (cg-RX-API-DMAC7.html)
CO (1) CO6210721A2 (cg-RX-API-DMAC7.html)
CY (1) CY1111721T1 (cg-RX-API-DMAC7.html)
DK (1) DK2125748T3 (cg-RX-API-DMAC7.html)
EC (1) ECSP099436A (cg-RX-API-DMAC7.html)
HR (1) HRP20110520T1 (cg-RX-API-DMAC7.html)
IL (1) IL199019A (cg-RX-API-DMAC7.html)
MX (1) MX2009006742A (cg-RX-API-DMAC7.html)
MY (1) MY146111A (cg-RX-API-DMAC7.html)
NO (1) NO342176B1 (cg-RX-API-DMAC7.html)
NZ (1) NZ577209A (cg-RX-API-DMAC7.html)
PE (1) PE20081532A1 (cg-RX-API-DMAC7.html)
PL (1) PL2125748T3 (cg-RX-API-DMAC7.html)
PT (1) PT2125748E (cg-RX-API-DMAC7.html)
RU (1) RU2458920C2 (cg-RX-API-DMAC7.html)
SA (1) SA07280734B1 (cg-RX-API-DMAC7.html)
SI (1) SI2125748T1 (cg-RX-API-DMAC7.html)
TW (1) TWI434846B (cg-RX-API-DMAC7.html)
UY (1) UY30819A1 (cg-RX-API-DMAC7.html)
WO (1) WO2008075068A2 (cg-RX-API-DMAC7.html)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
MX2009006706A (es) 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
US8131527B1 (en) 2006-12-22 2012-03-06 Astex Therapeutics Ltd. FGFR pharmacophore compounds
JP5442449B2 (ja) 2006-12-22 2014-03-12 アステックス、セラピューティックス、リミテッド 新規化合物
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
HRP20140047T1 (en) 2007-08-22 2014-02-14 Astrazeneca Ab Cycloptopyl amide derivatives
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
DE102007061963A1 (de) 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
DE102008019907A1 (de) 2008-04-21 2009-10-22 Merck Patent Gmbh Pyridazinonderivate
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
DE102008028905A1 (de) 2008-06-18 2009-12-24 Merck Patent Gmbh 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate
PE20110062A1 (es) * 2008-06-19 2011-03-09 Astrazeneca Ab N-(3-(3,5-dimetoxifenetil)-1h-pirazol-5-il)-4-(3,4-dimetilpiperazin-1-il)benzamida y sales del mismo
HRP20130993T1 (hr) 2008-12-22 2013-11-22 Merck Patent Gmbh Novi polimorfni oblici 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoksi)-pirimidin-2-il]-benzil}-2h-piridazin-3-on dihidrogenfosfata i postupak njihove proizvodnje
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
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
AR078411A1 (es) * 2009-05-07 2011-11-09 Lilly Co Eli Compuesto de vinil imidazolilo y composicion farmaceutica que lo comprende
CA2790040A1 (en) * 2010-02-18 2011-08-25 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith
SG186885A1 (en) 2010-06-04 2013-02-28 Albany Molecular Res Inc Glycine transporter-1 inhibitors, methods of making them, and uses thereof
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9255072B2 (en) 2011-03-04 2016-02-09 National Health Rsearch Institutes Pyrazole compounds and thiazole compounds as protein kinases inhibitors
EP2821402B1 (en) 2012-02-28 2019-08-21 Astellas Pharma Inc. Nitrogen-containing aromatic heterocyclic compound
HK1205528A1 (en) 2012-03-08 2015-12-18 Astellas Pharma Inc. Novel fgfr3 fusion product
WO2013161871A1 (ja) * 2012-04-25 2013-10-31 興和株式会社 Ｔｌｒ阻害作用を有するチオフェン誘導体
EP3495367B1 (en) 2012-06-13 2020-09-30 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
WO2014002922A1 (ja) * 2012-06-26 2014-01-03 アステラス製薬株式会社 抗癌剤の併用による癌治療方法
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US20140179712A1 (en) * 2012-12-21 2014-06-26 Astrazeneca Ab Pharmaceutical formulation of n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
MX2015011428A (es) 2013-03-06 2016-02-03 Genentech Inc Metodos para tratar y prevenir la resistencia a los farmacos para el cancer.
PL403149A1 (pl) * 2013-03-14 2014-09-15 Celon Pharma Spółka Akcyjna Nowe związki pochodne pirazolilobenzo[d]imidazolu
AR095464A1 (es) 2013-03-15 2015-10-21 Celgene Avilomics Res Inc Compuestos de heteroarilo y usos de los mismos
NZ711376A (en) 2013-03-15 2020-01-31 Sanofi Sa Heteroaryl compounds and uses thereof
EP2968551B1 (en) 2013-03-15 2021-05-05 The Trustees of Columbia University in the City of New York Fusion proteins and methods thereof
EA036160B1 (ru) 2013-03-15 2020-10-08 Селджен Кар Ллс Гетероарильные соединения и их применение
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
AR096393A1 (es) * 2013-05-23 2015-12-30 Bayer Cropscience Ag Compuestos heterocíclicos pesticidas
JP6509735B2 (ja) 2013-10-08 2019-05-08 第一三共株式会社 抗ｆｇｆｒ２抗体と他剤の組合せ
CN107073121A (zh) 2014-06-13 2017-08-18 基因泰克公司 治疗及预防癌症药物抗性的方法
RU2658821C1 (ru) 2014-08-18 2018-06-25 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Соль моноциклического производного пиридина и ее кристалл
RU2719428C2 (ru) * 2014-08-19 2020-04-17 Шанхай Хайхэ Фармасьютикал Ко., Лтд. Индазольные соединения в качестве ингибиторов киназы fgfr, их получение и применение
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3925979A3 (en) 2014-12-23 2022-03-23 The Trustees of Columbia University in the City of New York Fgfr-tacc fusion proteins and methods thereof
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
CA2974937C (en) 2015-03-25 2023-09-05 National Cancer Center Therapeutic agent for bile duct cancer
EP3324952B1 (en) 2015-07-17 2020-12-16 Institut Pasteur 5-hydroxytryptamine 1b receptor-stimulating agent for use as a promoter of satellite cells self-renewal and/or differentiation
JP6549311B2 (ja) 2015-08-20 2019-07-24 浙江海正薬業股▲ふん▼有限公司Ｚｈｅｊｉａｎｇ Ｈｉｓｕｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ ＣＯ．，ＬＴＤ． インドール誘導体、その調製方法および医薬におけるその使用
CN115177619A (zh) 2015-12-17 2022-10-14 卫材R&D管理有限公司 用于乳腺癌的治疗剂
CN107459519A (zh) * 2016-06-06 2017-12-12 上海艾力斯医药科技有限公司 稠合嘧啶哌啶环衍生物及其制备方法和应用
US20190290641A1 (en) 2016-07-15 2019-09-26 Institut Pasteur 5-hydroxytryptamine 1b receptor-stimulating agent for skin and/or hair repair
CN107840842A (zh) * 2016-09-19 2018-03-27 北京天诚医药科技有限公司 炔代杂环化合物、其制备方法及其在医药学上的应用
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
KR20200135945A (ko) 2018-03-28 2020-12-04 에자이 알앤드디 매니지먼트 가부시키가이샤 간세포 암종 치료제
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
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
TW202110834A (zh) * 2019-05-31 2021-03-16 美商愛德亞生物科學公司 作為ＤＮＡ聚合酶θ抑制劑之噻二唑基衍生物
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN117083271A (zh) * 2020-12-02 2023-11-17 伊迪亚生物科学有限公司 作为DNA聚合酶θ抑制剂的取代的噻二唑基衍生物
TW202237595A (zh) * 2020-12-02 2022-10-01 美商愛德亞生物科學公司 作為DNA聚合酶θ抑制劑之經取代噻二唑基衍生物
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
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN115819239B (zh) * 2021-09-17 2025-11-18 无锡和誉生物医药科技有限公司 一种成纤维细胞生长因子受体抑制剂的中间体及其制备方法和用途
WO2023060573A1 (en) * 2021-10-15 2023-04-20 Beijing Danatlas Pharmaceutical Co., Ltd. Novel thiadiazolyl derivatives of dna polymerase theta inhibitors
US11957677B2 (en) 2021-10-15 2024-04-16 Cardiff Oncology, Inc. Cancer treatment using FGFR inhibitors and PLK1 inhibitors
US20250205344A1 (en) 2022-03-24 2025-06-26 Glaxosmithkline Intellectual Property Development Limited 2,4-dioxotetrahydropyrimidinyl deratives as degrons in protacs
WO2024031226A1 (zh) * 2022-08-08 2024-02-15 无锡和誉生物医药科技有限公司 Fgfr抑制剂的药物组合物、多晶型物及其在药学上的应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005048948A2 (en) * 2003-11-13 2005-06-02 Ambit Biosciences Corporation Urea derivatives as kinase modulators
WO2005051919A1 (en) * 2003-11-26 2005-06-09 Pfizer Products Inc. Aminopyrazole derivatives as gsk-3 inhibitors
US20050209297A1 (en) * 2000-08-31 2005-09-22 Pfizer Inc Pyrazole derivatives
WO2005105780A2 (en) * 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB843940A (en) 1955-09-27 1960-08-10 Kodak Ltd Method of processing photographic silver halide emulsions containing colour couplers
BE667399A (cg-RX-API-DMAC7.html) 1964-07-30 1965-11-16
JPS57150846A (en) 1981-03-13 1982-09-17 Konishiroku Photo Ind Co Ltd Photographic element
JPS63133152A (ja) 1986-11-26 1988-06-04 Konica Corp 新規なマゼンタカプラ−を含有するハロゲン化銀写真感光材料
JPH0467645A (ja) 1990-07-09 1992-03-03 Nec Kyushu Ltd バーンイン装置
JP2890065B2 (ja) 1990-11-10 1999-05-10 コニカ株式会社 ハロゲン化銀写真感光材料
JPH04184437A (ja) 1990-11-20 1992-07-01 Fuji Photo Film Co Ltd カラー画像形成方法及びハロゲン化銀カラー写真感光材料
JPH04292322A (ja) 1991-03-19 1992-10-16 Fujitsu Ltd ラック給排装置
JPH0511414A (ja) 1991-07-02 1993-01-22 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料
CZ290470B6 (cs) 1991-10-18 2002-07-17 Monsanto Technology Llc 5 či 6 členné aromáty jako fungicidy pro kontrolu stéblolamu rostlin, způsob kontroly a fungicidní směs k provedení tohoto způsobu
WO1993019054A1 (en) 1992-03-26 1993-09-30 Dowelanco N-heterocyclic nitro anilines as fungicides
HRP921338B1 (en) 1992-10-02 2002-04-30 Monsanto Co Fungicides for the control of take-all disease of plants
TW240217B (cg-RX-API-DMAC7.html) 1992-12-30 1995-02-11 Glaxo Group Ltd
JP3156026B2 (ja) 1993-12-27 2001-04-16 株式会社大塚製薬工場 ホスホン酸ジエステル誘導体
ATE262902T1 (de) 1994-11-10 2004-04-15 Millennium Pharm Inc Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose
IL130286A0 (en) 1996-12-23 2000-06-01 Du Pont Pharm Co Nitrogen containing heteroaromatics as factor Xa inhibitors
AU7687998A (en) 1997-05-19 1998-12-11 Sugen, Inc. Heteroarylcarboxamide compounds active against protein tyrosine kinase related disorders
EP1019394A1 (en) 1997-05-22 2000-07-19 G.D. Searle & Co. PYRAZOLE DERIVATIVES AS p38 KINASE INHIBITORS
KR100622138B1 (ko) * 1997-12-22 2006-09-13 바이엘 코포레이션 아릴 및 헤테로아릴 치환 헤테로고리형 우레아를 사용한라프 키나제의 저해
US6271237B1 (en) 1997-12-22 2001-08-07 Dupont Pharmaceuticals Company Nitrogen containing heteromatics with ortho-substituted P1s as factor Xa inhabitors
JP3310226B2 (ja) 1998-10-16 2002-08-05 松下電器産業株式会社 音声合成方法および装置
GB9823103D0 (en) 1998-10-23 1998-12-16 Pfizer Ltd Pharmaceutically active compounds
UA73492C2 (en) * 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
AU2460600A (en) 1999-02-10 2000-08-29 Mitsubishi Pharma Corporation Amide compounds and medicinal use thereof
AU3357700A (en) 1999-02-16 2000-09-04 E.I. Du Pont De Nemours And Company Phenoxypyrimidine insecticides and acaricides
JP2003507329A (ja) 1999-08-12 2003-02-25 フアルマシア・イタリア・エツセ・ピー・アー ３（５）−アミノ−ピラゾール誘導体、それらの製造方法および抗腫瘍薬としてのそれらの使用
CN1222520C (zh) 1999-08-12 2005-10-12 沃泰克斯药物股份有限公司 c－JUN N－末端激酶(JNK)和其它蛋白激酶的抑制剂
ES2279769T3 (es) 1999-09-24 2007-09-01 Smithkline Beecham Corporation Mimeticos de trombopoyetina.
EP1313710A1 (en) * 2000-08-31 2003-05-28 Pfizer Products Inc. Pyrazole derivatives and their use as protein kinase inhibitors
KR20030030029A (ko) 2000-09-22 2003-04-16 니혼노야쿠가부시키가이샤 Ｎ-(4-피라졸릴)아미드 유도체 및 농원예용 약제 그리고그 사용방법
EP1352650B1 (en) 2000-12-18 2012-03-07 Institute of Medicinal Molecular Design, Inc. Inhibitors against the production and release of inflammatory cytokines
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
MXPA03009847A (es) 2001-04-27 2004-02-12 Vertex Pharma Inhibidores de cinasa derivados de pirazol.
EA008622B1 (ru) 2002-06-05 2007-06-29 Инститьют Оф Медисинал Молекьюлар Дизайн. Инк. Ингибиторы ассоциированной с иммунитетом протеинкиназы
EP1510207A4 (en) 2002-06-05 2008-12-31 Inst Med Molecular Design Inc THERAPEUTIC MEDICAMENT AGAINST DIABETES
US20060122243A1 (en) 2002-06-06 2006-06-08 Susumu Muto Antiallergic
ES2246603B1 (es) 2002-07-03 2007-06-16 Consejo Sup. De Investig. Cientificas Procedimiento para la preparacion de esteres de hidroxitirosol, esteres obtenidos y utilizacion.
JPWO2004007472A1 (ja) 2002-07-10 2005-11-17 小野薬品工業株式会社 Ｃｃｒ４アンタゴニストおよびその医薬用途
EP1542999A1 (en) 2002-08-01 2005-06-22 Pharmacia & Upjohn Company LLC 1h-pyrazole and 1h-pyrrole-azabicyclic compounds with alfa-7 nachr activity
JP4171881B2 (ja) 2002-08-09 2008-10-29 株式会社大塚製薬工場 Ａｃａｔ−１阻害剤
ATE479667T1 (de) 2003-02-06 2010-09-15 Bristol Myers Squibb Co Als kinaseinhibitoren geeignete verbindungen auf thiazolylbasis
JP2004292322A (ja) 2003-03-25 2004-10-21 Fuji Photo Film Co Ltd 水溶性アミド連結体の製造方法
US20040220170A1 (en) 2003-05-01 2004-11-04 Atkinson Robert N. Pyrazole-amides and sulfonamides as sodium channel modulators
PL1618092T3 (pl) 2003-05-01 2011-02-28 Bristol Myers Squibb Co Związki amidopirazolowe z podstawnikami arylowymi jako inhibitory kinazy
US7115359B2 (en) 2003-07-25 2006-10-03 Konica Minolta Medical & Graphic, Inc. Photothermographic material
AU2004268948A1 (en) 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. N-substituted pyrazolyl-amidyl-benzimidazolyl c-kit inhibitors
US7432271B2 (en) 2003-09-02 2008-10-07 Bristol-Myers Squibb Company Pyrazolyl inhibitors of 15-lipoxygenase
US7652146B2 (en) 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
US7253204B2 (en) 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
JP2009503073A (ja) 2005-08-02 2009-01-29 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての５−置換チアゾール−２−イルアミノ化合物および組成物
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050209297A1 (en) * 2000-08-31 2005-09-22 Pfizer Inc Pyrazole derivatives
WO2005048948A2 (en) * 2003-11-13 2005-06-02 Ambit Biosciences Corporation Urea derivatives as kinase modulators
WO2005051919A1 (en) * 2003-11-26 2005-06-09 Pfizer Products Inc. Aminopyrazole derivatives as gsk-3 inhibitors
WO2005105780A2 (en) * 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CAVASOTTO C. N. et al: "In silico identification of novel EGFR inhibitors with antiproliferative activity against cancer cells", Bioorganic & Medicinal Chem. Letters, 2006, 16, 1969-1974. *
PEVARELLO P. et al: J. Med. Chem., 2004, 47(13), 3367-3380. *

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