CN101511798B - 作为蛋白激酶抑制剂的[4,5']联嘧啶-6,4'-二胺衍生物 - Google Patents

作为蛋白激酶抑制剂的[4,5']联嘧啶-6,4'-二胺衍生物 Download PDF

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Publication number
CN101511798B
CN101511798B CN2007800337140A CN200780033714A CN101511798B CN 101511798 B CN101511798 B CN 101511798B CN 2007800337140 A CN2007800337140 A CN 2007800337140A CN 200780033714 A CN200780033714 A CN 200780033714A CN 101511798 B CN101511798 B CN 101511798B
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CN
China
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bases
pyrimidine
chloro
amino
dimethoxy
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Expired - Fee Related
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CN2007800337140A
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English (en)
Chinese (zh)
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CN101511798A (zh
Inventor
P·A·阿尔博格
贺耘
S·江
任平达
王霞
王兴
谢永平
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IRM LLC
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IRM LLC
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    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2007800337140A 2006-07-12 2007-07-10 作为蛋白激酶抑制剂的[4,5']联嘧啶-6,4'-二胺衍生物 Expired - Fee Related CN101511798B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US83049206P 2006-07-12 2006-07-12
US60/830,492 2006-07-12
PCT/US2007/073111 WO2008008747A1 (en) 2006-07-12 2007-07-10 [4,5']bipyrimidinyl-6,4'-diamine derivatives as protein kinase inhbitors

Publications (2)

Publication Number Publication Date
CN101511798A CN101511798A (zh) 2009-08-19
CN101511798B true CN101511798B (zh) 2011-11-02

Family

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Family Applications (1)

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CN2007800337140A Expired - Fee Related CN101511798B (zh) 2006-07-12 2007-07-10 作为蛋白激酶抑制剂的[4,5']联嘧啶-6,4'-二胺衍生物

Country Status (21)

Country Link
US (1) US8026243B2 (enExample)
EP (1) EP2044036B1 (enExample)
JP (1) JP2009543798A (enExample)
KR (1) KR20090029832A (enExample)
CN (1) CN101511798B (enExample)
AR (1) AR061867A1 (enExample)
AT (1) ATE508119T1 (enExample)
AU (1) AU2007272646A1 (enExample)
BR (1) BRPI0714291A2 (enExample)
CA (1) CA2657381A1 (enExample)
CL (1) CL2007002017A1 (enExample)
DE (1) DE602007014374D1 (enExample)
ES (1) ES2367666T3 (enExample)
MX (1) MX2009000429A (enExample)
PE (1) PE20080548A1 (enExample)
PL (1) PL2044036T3 (enExample)
PT (1) PT2044036E (enExample)
RU (1) RU2009104340A (enExample)
TW (1) TW200811134A (enExample)
UY (1) UY30477A1 (enExample)
WO (1) WO2008008747A1 (enExample)

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US8131527B1 (en) 2006-12-22 2012-03-06 Astex Therapeutics Ltd. FGFR pharmacophore compounds
HRP20150642T1 (hr) 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
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
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
EP2308866A1 (de) 2009-10-09 2011-04-13 Bayer CropScience AG Phenylpyri(mi)dinylpyrazole und ihre Verwendung als Fungizide
AR079545A1 (es) 2009-12-21 2012-02-01 Bayer Cropscience Ag Tienilpiri(mi)dinilazol
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2012175513A1 (en) 2011-06-20 2012-12-27 Bayer Intellectual Property Gmbh Thienylpyri(mi)dinylpyrazole
UA114410C2 (uk) 2011-10-06 2017-06-12 Байєр Інтеллектуал Проперті Гмбх Гетероциклілпіри(mi)динілпіразол
EP2763987B1 (en) 2011-10-06 2018-07-18 Bayer CropScience AG Heterocyclylpyri(mi)dinylpyrazole as fungicidals
RS61664B1 (sr) 2012-04-24 2021-04-29 Vertex Pharma Inhibitori dna-pk
ES2984771T3 (es) 2012-06-13 2024-10-31 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
HK1210500A1 (en) * 2012-09-27 2016-04-22 中外制药株式会社 Fgfr3 fusion gene and pharmaceutical drug targeting same
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
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
SI3424920T1 (sl) 2013-10-17 2020-08-31 Vertex Pharmaceuticals Incorporated Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk
US9951047B2 (en) 2014-08-18 2018-04-24 Eisai R&D Management Co., Ltd. Salt of monocyclic pyridine derivative and crystal thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
US9580423B2 (en) 2015-02-20 2017-02-28 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
EP3275442B1 (en) 2015-03-25 2021-07-28 National Cancer Center Therapeutic agent for bile duct cancer
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
KR20190062485A (ko) 2016-09-27 2019-06-05 버텍스 파마슈티칼스 인코포레이티드 Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
KR102613433B1 (ko) * 2017-10-11 2023-12-13 주식회사 대웅제약 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물
BR112020017922A2 (pt) 2018-03-28 2020-12-22 Eisai R&D Management Co., Ltd. Agente terapêutico para carcinoma hepatocelular
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
KR102133595B1 (ko) 2019-05-31 2020-07-13 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR102112336B1 (ko) 2019-08-12 2020-05-18 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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Also Published As

Publication number Publication date
EP2044036A1 (en) 2009-04-08
DE602007014374D1 (de) 2011-06-16
EP2044036B1 (en) 2011-05-04
US20100234376A1 (en) 2010-09-16
ATE508119T1 (de) 2011-05-15
US8026243B2 (en) 2011-09-27
ES2367666T3 (es) 2011-11-07
KR20090029832A (ko) 2009-03-23
UY30477A1 (es) 2009-04-30
PE20080548A1 (es) 2008-06-24
CN101511798A (zh) 2009-08-19
PT2044036E (pt) 2011-08-23
MX2009000429A (es) 2009-01-29
WO2008008747A1 (en) 2008-01-17
PL2044036T3 (pl) 2011-09-30
BRPI0714291A2 (pt) 2014-10-21
AU2007272646A1 (en) 2008-01-17
CA2657381A1 (en) 2008-01-17
TW200811134A (en) 2008-03-01
RU2009104340A (ru) 2010-08-20
AR061867A1 (es) 2008-09-24
CL2007002017A1 (es) 2008-06-13
JP2009543798A (ja) 2009-12-10

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Granted publication date: 20111102

Termination date: 20120710