JP5702390B2 - タンパク質チロシンキナーゼ2阻害剤としてのピリミジン誘導体 - Google Patents

タンパク質チロシンキナーゼ2阻害剤としてのピリミジン誘導体 Download PDF

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JP5702390B2
JP5702390B2 JP2012531442A JP2012531442A JP5702390B2 JP 5702390 B2 JP5702390 B2 JP 5702390B2 JP 2012531442 A JP2012531442 A JP 2012531442A JP 2012531442 A JP2012531442 A JP 2012531442A JP 5702390 B2 JP5702390 B2 JP 5702390B2
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JP2013506636A (ja
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ハインツ シュタットミューラー
ハインツ シュタットミューラー
イオアニス サポウンツィス
イオアニス サポウンツィス
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2012531442A 2009-10-02 2010-10-01 タンパク質チロシンキナーゼ2阻害剤としてのピリミジン誘導体 Active JP5702390B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09172026.8 2009-10-02
EP09172026 2009-10-02
EP10172460.7 2010-08-11
EP10172460 2010-08-11
PCT/EP2010/064628 WO2011039344A1 (en) 2009-10-02 2010-10-01 Pyrimidine derivatives as protein tyrosine kinase 2 inhibitors

Publications (2)

Publication Number Publication Date
JP2013506636A JP2013506636A (ja) 2013-02-28
JP5702390B2 true JP5702390B2 (ja) 2015-04-15

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JP2012531442A Active JP5702390B2 (ja) 2009-10-02 2010-10-01 タンパク質チロシンキナーゼ2阻害剤としてのピリミジン誘導体

Country Status (25)

Country Link
US (1) US8466155B2 (enExample)
EP (1) EP2483249B1 (enExample)
JP (1) JP5702390B2 (enExample)
KR (1) KR20120092617A (enExample)
CN (1) CN102695700A (enExample)
AP (1) AP2012006166A0 (enExample)
AR (1) AR078513A1 (enExample)
AU (1) AU2010302648A1 (enExample)
BR (1) BR112012007300A2 (enExample)
CA (1) CA2775418A1 (enExample)
CL (1) CL2012000825A1 (enExample)
EA (1) EA201200552A1 (enExample)
EC (1) ECSP12011830A (enExample)
IL (1) IL218543A0 (enExample)
IN (1) IN2012DN02714A (enExample)
MA (1) MA33606B1 (enExample)
MX (1) MX2012003101A (enExample)
NZ (1) NZ598614A (enExample)
PE (1) PE20121431A1 (enExample)
PH (1) PH12012500527A1 (enExample)
TN (1) TN2012000142A1 (enExample)
TW (1) TW201124386A (enExample)
UY (1) UY32916A (enExample)
WO (1) WO2011039344A1 (enExample)
ZA (1) ZA201201703B (enExample)

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WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
CA2827172C (en) 2011-02-17 2019-02-26 Cancer Therapeutics Crc Pty Limited Selective fak inhibitors
CN103534241B (zh) 2011-02-17 2015-11-25 癌症疗法Crc私人有限公司 Fak抑制剂
US20150132301A1 (en) * 2011-12-09 2015-05-14 Oncomed Pharmaceuticals, Inc. Combination Therapy for Treatment of Cancer
US9187453B2 (en) 2012-03-28 2015-11-17 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP3495367B1 (en) 2012-06-13 2020-09-30 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
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
JP6449244B2 (ja) 2013-04-19 2019-01-09 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Fgfr抑制剤としての二環式複素環
EP2999472B1 (en) 2013-05-22 2020-07-22 The Regents of The University of California Aurora kinase inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3259269B9 (en) 2015-02-20 2020-03-04 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JP7568512B2 (ja) 2018-05-04 2024-10-16 インサイト・コーポレイション Fgfr阻害剤の塩
SMT202400507T1 (it) 2018-05-04 2025-01-14 Incyte Corp Forme solide di un inibitore di fgfr e procedimenti per preparare le stesse
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
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
KR20220100879A (ko) 2019-10-14 2022-07-18 인사이트 코포레이션 Fgfr 저해제로서의 이환식 헤테로사이클
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
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
EP4069695A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Derivatives of an fgfr inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
US12428420B2 (en) 2021-06-09 2025-09-30 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors

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Also Published As

Publication number Publication date
CL2012000825A1 (es) 2012-08-24
KR20120092617A (ko) 2012-08-21
TW201124386A (en) 2011-07-16
EP2483249A1 (en) 2012-08-08
WO2011039344A1 (en) 2011-04-07
CA2775418A1 (en) 2011-04-07
MX2012003101A (es) 2012-04-11
US8466155B2 (en) 2013-06-18
PH12012500527A1 (en) 2012-10-22
IL218543A0 (en) 2012-05-31
EP2483249B1 (en) 2015-12-23
AR078513A1 (es) 2011-11-16
BR112012007300A2 (pt) 2017-11-07
UY32916A (es) 2011-04-29
ZA201201703B (en) 2014-05-28
AU2010302648A1 (en) 2012-04-05
ECSP12011830A (es) 2012-06-29
AP2012006166A0 (en) 2012-04-30
PE20121431A1 (es) 2012-11-10
EA201200552A1 (ru) 2013-03-29
MA33606B1 (fr) 2012-09-01
US20110237598A1 (en) 2011-09-29
CN102695700A (zh) 2012-09-26
TN2012000142A1 (en) 2013-09-19
JP2013506636A (ja) 2013-02-28
NZ598614A (en) 2013-08-30
IN2012DN02714A (enExample) 2015-09-11

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