CA2672521C - Pyrazole derivatives as protein kinase inhibitors - Google Patents

Pyrazole derivatives as protein kinase inhibitors Download PDF

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Publication number
CA2672521C
CA2672521C CA2672521A CA2672521A CA2672521C CA 2672521 C CA2672521 C CA 2672521C CA 2672521 A CA2672521 A CA 2672521A CA 2672521 A CA2672521 A CA 2672521A CA 2672521 C CA2672521 C CA 2672521C
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Prior art keywords
pyrazol
halogen
hydroxyl
optionally substituted
ethyl
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CA2672521A
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English (en)
French (fr)
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CA2672521A1 (en
Inventor
Kevin Michael Foote
Maria-Elena Theoclitou
Andrew Peter Thomas
David Buttar
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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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
CA2672521A 2006-12-21 2007-12-20 Pyrazole derivatives as protein kinase inhibitors Active CA2672521C (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
CA2672521A1 CA2672521A1 (en) 2008-06-26
CA2672521C true CA2672521C (en) 2015-03-17

Family

ID=39536793

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2672521A Active CA2672521C (en) 2006-12-21 2007-12-20 Pyrazole derivatives as protein kinase inhibitors

Country Status (28)

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

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
CA2672213C (en) 2006-12-22 2016-02-16 Astex Therapeutics Limited Bicyclic amine derivatives as protein tyrosine kinase inhibitors
US8131527B1 (en) 2006-12-22 2012-03-06 Astex Therapeutics Ltd. FGFR pharmacophore compounds
US8895745B2 (en) 2006-12-22 2014-11-25 Astex Therapeutics Limited Bicyclic heterocyclic compounds as FGFR inhibitors
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
BRPI0815591B8 (pt) 2007-08-22 2021-05-25 Astrazeneca Ab composto, composição farmacêutica, e, uso de um composto.
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
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
BRPI0914233A2 (pt) * 2008-06-19 2015-11-03 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito inibidor de fgfr e para produzir um efeito anticâncer em um animal de sangue quente, composição farmacêutica, e, método para tratar uma doença
MY160526A (en) 2008-12-22 2017-03-15 Merck Patent Gmbh Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
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
JO2860B1 (en) * 2009-05-07 2015-03-15 ايلي ليلي اند كومباني Phenylendazolyl compounds
AU2011218492B2 (en) * 2010-02-18 2014-11-13 Astrazeneca Ab New crystalline form of a cyclopropyl benzamide derivative
CA2801074A1 (en) 2010-06-04 2011-12-08 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
WO2012088266A2 (en) 2010-12-22 2012-06-28 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
AU2013227139B2 (en) 2012-02-28 2017-02-16 Astellas Pharma Inc. Nitrogen-containing aromatic heterocyclic compound
JP6107812B2 (ja) 2012-03-08 2017-04-05 アステラス製薬株式会社 新規ｆｇｆｒ３融合体
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
HUE042374T2 (hu) 2012-06-13 2019-06-28 Incyte Holdings Corp Szubsztituált triciklusos vegyületek mint FGFR inhibitorok
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
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines 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
RU2015137610A (ru) 2013-03-06 2017-04-10 Дженентек, Инк. Способы лечения и профилактики лекарственной резистентности злокачественных опухолей
PL403149A1 (pl) * 2013-03-14 2014-09-15 Celon Pharma Spółka Akcyjna Nowe związki pochodne pirazolilobenzo[d]imidazolu
AU2014228746B2 (en) 2013-03-15 2018-08-30 Celgene Car Llc Heteroaryl compounds and uses thereof
KR20150129847A (ko) 2013-03-15 2015-11-20 더 트러스티스 오브 컬럼비아 유니버시티 인 더 시티 오브 뉴욕 융합 단백질 및 이들의 방법
NZ711376A (en) 2013-03-15 2020-01-31 Sanofi Sa Heteroaryl compounds and uses thereof
US9321786B2 (en) 2013-03-15 2016-04-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
KR102469849B1 (ko) 2013-04-19 2022-11-23 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
AR096393A1 (es) * 2013-05-23 2015-12-30 Bayer Cropscience Ag Compuestos heterocíclicos pesticidas
ES2768618T3 (es) 2013-10-08 2020-06-23 Daiichi Sankyo Co Ltd Combinación de anticuerpo anti-FGFR2 y otro agente
JP2017517552A (ja) 2014-06-13 2017-06-29 ジェネンテック， インコーポレイテッド 抗癌剤耐性の治療及び防止方法
KR102344105B1 (ko) 2014-08-18 2021-12-29 에자이 알앤드디 매니지먼트 가부시키가이샤 모노시클릭 피리딘 유도체의 염 및 이의 결정
ES2904544T3 (es) * 2014-08-19 2022-04-05 Shanghai Haihe Pharmaceutical Co Ltd Compuestos de indazol como inhibidores de la cinasa FGFR, preparación y uso de los mismos
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3778644A3 (en) 2014-12-23 2021-06-02 The Trustees of Columbia University in the City of New York Fgfr-tacc fusion proteins and methods thereof
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
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
CN114984013A (zh) 2015-03-25 2022-09-02 国立癌症研究中心 胆管癌治疗剂
CN108348486A (zh) 2015-07-17 2018-07-31 巴斯德研究院 用作卫星细胞自我更新和/或分化的启动子的5-羟色胺1b受体激动剂
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
WO2017104739A1 (ja) 2015-12-17 2017-06-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 乳がん治療剤
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
SG11202007591RA (en) 2018-03-28 2020-09-29 Eisai R&D Man Co Ltd Therapeutic agent for hepatocellular carcinoma
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
AU2020282768B2 (en) * 2019-05-31 2023-09-14 Ideaya Biosciences, Inc. Thiadiazolyl derivatives as DNA Polymerase Theta inhibitors
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
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
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
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
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
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
US11957677B2 (en) 2021-10-15 2024-04-16 Cardiff Oncology, Inc. Cancer treatment using FGFR inhibitors and PLK1 inhibitors
WO2023060573A1 (en) * 2021-10-15 2023-04-20 Beijing Danatlas Pharmaceutical Co., Ltd. Novel thiadiazolyl derivatives of dna polymerase theta inhibitors
EP4499628A1 (en) 2022-03-24 2025-02-05 GlaxoSmithKline Intellectual Property Development Limited 2,4-dioxotetrahydropyrimidinyl derivatives 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

Family Cites Families (57)

* 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 (enExample) 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
CA2119155C (en) 1991-10-18 1999-06-15 Dennis Paul Phillion Fungicides for the control of take-all disease of plants
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 (enExample) 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
JPH10509708A (ja) 1994-11-10 1998-09-22 コア セラピューティクス，インコーポレイティド プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物
CN1246847A (zh) 1996-12-23 2000-03-08 杜邦药品公司 作为Xa因子抑制剂的含氮杂芳族化合物
EP1012150A4 (en) 1997-05-19 2002-05-29 Sugen Inc HETEROARYLCARBOXAMIDE COMPOUNDS THAT ARE EFFECTIVE OF DISEASES CAUSED BY PROTEIN-TYROSIN-KINASE
CA2288787A1 (en) 1997-05-22 1998-11-26 G.D. Searle And Co. Pyrazole derivatives as p38 kinase inhibitors
PL341356A1 (en) * 1997-12-22 2001-04-09 Bayer Ag Raf kinase inhibition employing aryl- and heteroaryl-substituted heterocyclic ureas
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
US7015218B1 (en) 1999-02-10 2006-03-21 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
BR0013143A (pt) 1999-08-12 2002-06-11 Pharmacia Italia Spa Derivados de 3 (5) amino pirazol, processo para sua preparação e uso dos mesmos como agentes antitumorais
AR032130A1 (es) 1999-08-13 2003-10-29 Vertex Pharma Un compuesto inhibidor de quinasas proteicas, una composicion farmaceutica que lo incluye, y un metodo para tratar afecciones con dicho compuesto
WO2001021180A1 (en) 1999-09-24 2001-03-29 Smithkline Beecham Corporation Thrombopoietin mimetics
US20050209297A1 (en) 2000-08-31 2005-09-22 Pfizer Inc Pyrazole derivatives
CN1518543A (zh) * 2000-08-31 2004-08-04 �Ʒ� 吡唑衍生物和它们作为蛋白激酶抑制剂的用途
AU2001290258A1 (en) 2000-09-22 2002-04-02 Nihon Nohyaku Co. Ltd. N-(4-pyrazolyl)amide derivatives, chemicals for agricultural and horticultural use, and usage of the same
US8263657B2 (en) 2000-12-18 2012-09-11 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
CA2445357A1 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Pyrazole derived kinase inhibitors
CA2487900A1 (en) 2002-06-05 2003-12-18 Institute Of Medicinal Molecular Design, Inc. Immunity-related protein kinase inhibitors
EP1510207A4 (en) 2002-06-05 2008-12-31 Inst Med Molecular Design Inc THERAPEUTIC MEDICAMENT AGAINST DIABETES
KR101054562B1 (ko) 2002-06-06 2011-08-04 가부시키가이샤 이야쿠 분지 셋케이 겐쿠쇼 항알레르기약
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
US7176198B2 (en) 2002-08-01 2007-02-13 Pfizer Inc. 1H-pyrazole and 1H-pyrrole-azabicyclic compounds for the treatment of disease
JP4171881B2 (ja) 2002-08-09 2008-10-29 株式会社大塚製薬工場 Ａｃａｔ−１阻害剤
US7169771B2 (en) 2003-02-06 2007-01-30 Bristol-Myers Squibb Company Thiazolyl-based compounds useful as kinase inhibitors
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
ATE522525T1 (de) 2003-05-01 2011-09-15 Bristol Myers Squibb Co Arylsubstituierte pyrazolamidverbindungen, die als kinase-inhibitoren von nutzen sind
US20040220170A1 (en) 2003-05-01 2004-11-04 Atkinson Robert N. Pyrazole-amides and sulfonamides as sodium channel modulators
US7115359B2 (en) 2003-07-25 2006-10-03 Konica Minolta Medical & Graphic, Inc. Photothermographic material
BRPI0413785A (pt) 2003-08-21 2006-11-07 Osi Pharm Inc composto, composição, e, método de tratamento de distúrbio hiperproliferativo
US7432271B2 (en) 2003-09-02 2008-10-07 Bristol-Myers Squibb Company Pyrazolyl inhibitors of 15-lipoxygenase
US20050267182A1 (en) 2003-11-13 2005-12-01 Ambit Biosciences Corporation Urea derivatives as FLT-3 modulators
JP4864719B2 (ja) 2003-11-26 2012-02-01 ファイザー・プロダクツ・インク Ｇｓｋ−３インヒビターとしてのアミノピラゾール誘導体
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
WO2005105780A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
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

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