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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D401/12—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
    • 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
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (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)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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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ID=43048878

Family Applications (1)

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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
WO2012110773A1 (en) 2011-02-17 2012-08-23 Cancer Therapeutics Crc Pty Limited Fak inhibitors
DK2675794T3 (da) 2011-02-17 2019-05-06 Cancer Therapeutics Crc Pty Ltd Selektive fak-inhibitorer
WO2013086260A2 (en) * 2011-12-09 2013-06-13 Oncomed Pharmaceuticals, Inc. Combination therapy for treatment of cancer
EP2832734A4 (en) 2012-03-28 2015-08-26 Takeda Pharmaceutical HETEROCYCLIC COMPOUND
CA2876689C (en) 2012-06-13 2022-04-26 Incyte 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
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
CA2949048A1 (en) * 2013-05-22 2014-11-27 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
CA2976790C (en) 2015-02-20 2024-02-27 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
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
KR102956194B1 (ko) 2018-05-04 2026-04-23 인사이트 코포레이션 Fgfr 억제제의 염
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
TW202329937A (zh) 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ck12抑制劑
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

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Also Published As

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

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