CN102695700A - 用作蛋白酪氨酸激酶2抑制剂的嘧啶衍生物 - Google Patents

用作蛋白酪氨酸激酶2抑制剂的嘧啶衍生物 Download PDF

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Publication number
CN102695700A
CN102695700A CN201080054924XA CN201080054924A CN102695700A CN 102695700 A CN102695700 A CN 102695700A CN 201080054924X A CN201080054924X A CN 201080054924XA CN 201080054924 A CN201080054924 A CN 201080054924A CN 102695700 A CN102695700 A CN 102695700A
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Prior art keywords
methyl
group
methoxy
benzamide
ylamino
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Pending
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CN201080054924XA
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English (en)
Chinese (zh)
Inventor
H.斯塔特米勒
I.萨旁特齐斯
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43048878&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102695700(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of CN102695700A publication Critical patent/CN102695700A/zh
Pending legal-status Critical Current

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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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201080054924XA 2009-10-02 2010-10-01 用作蛋白酪氨酸激酶2抑制剂的嘧啶衍生物 Pending CN102695700A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09172026 2009-10-02
EP09172026.8 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 (1)

Publication Number Publication Date
CN102695700A true CN102695700A (zh) 2012-09-26

Family

ID=43048878

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080054924XA Pending CN102695700A (zh) 2009-10-02 2010-10-01 用作蛋白酪氨酸激酶2抑制剂的嘧啶衍生物

Country Status (25)

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

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US20120244141A1 (en) 2010-09-28 2012-09-27 Boehringer Ingelheim International Gmbh Stratification of cancer patients for susceptibility to therapy with PTK2 inhibitors
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9174946B2 (en) 2011-02-17 2015-11-03 Cancer Therapeutics Crc Pty Ltd Selective FAK inhibitors
US20130324532A1 (en) 2011-02-17 2013-12-05 Cancer Therapeutics Crc Pty Limited Fak inhibitors
EP2788378A4 (en) * 2011-12-09 2015-09-09 Oncomed Pharm Inc COMBINATION THERAPY FOR CANCER TREATMENT
WO2013146963A1 (ja) * 2012-03-28 2013-10-03 武田薬品工業株式会社 複素環化合物
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
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
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
AU2019262579B2 (en) 2018-05-04 2024-09-12 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
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (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
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
US12012409B2 (en) 2020-01-15 2024-06-18 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
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1416423A (zh) * 2000-03-01 2003-05-07 阿斯特拉曾尼卡有限公司 用作抗肿瘤剂的2,4-二(杂-)芳基氨基(-氧基)-5-取代的嘧啶
WO2004058144A2 (en) * 2002-12-18 2004-07-15 Glaxo Group Limited Antibacterial agents
CN1633419A (zh) * 2001-05-29 2005-06-29 舍林股份公司 Cdk抑制性嘧啶化合物、其制备方法以及作为药物的应用
WO2008038011A1 (en) * 2006-09-30 2008-04-03 Vernalis (R & D) Limited Pyrimidine derivatives as aurora a and aurora b inhibitors
CN101213179A (zh) * 2005-07-01 2008-07-02 贝林格尔·英格海姆国际有限公司 用作Aurora抑制剂的2,4-二氨基-嘧啶类化合物
WO2008128231A1 (en) * 2007-04-16 2008-10-23 Hutchison Medipharma Enterprises Limited Pyrimidine derivatives
CN101346380A (zh) * 2005-12-21 2009-01-14 辉瑞产品公司 用于治疗异常细胞生长的嘧啶衍生物
CN101511836A (zh) * 2006-07-06 2009-08-19 阿斯利康(瑞典)有限公司 稠合的嘧啶并化合物

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ATE407678T1 (de) 2001-10-17 2008-09-15 Boehringer Ingelheim Pharma Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
EP1483260A1 (de) * 2002-03-11 2004-12-08 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
US7754714B2 (en) * 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP1794134A1 (de) * 2004-09-29 2007-06-13 Bayer Schering Pharma Aktiengesellschaft Substituierte 2-anilinopyrimidine als zellzyklus -kinase oder rezeptortyrosin-kinase inhibitoren, deren herstellung und verwendung als arzneimittel
PE20120006A1 (es) 2006-05-15 2012-02-02 Boehringer Ingelheim Int Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
WO2008077885A2 (en) * 2006-12-22 2008-07-03 Boehringer Ingelheim International Gmbh 2- [(phenylamino) -pyrimidin-4ylamin0] -cyclopentane carboxamide derivatives and related compounds as inhibitors of kinases of the cell cycle for the treatment of cancer
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
TW201024281A (en) * 2008-11-24 2010-07-01 Boehringer Ingelheim Int New compounds
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Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1416423A (zh) * 2000-03-01 2003-05-07 阿斯特拉曾尼卡有限公司 用作抗肿瘤剂的2,4-二(杂-)芳基氨基(-氧基)-5-取代的嘧啶
CN1633419A (zh) * 2001-05-29 2005-06-29 舍林股份公司 Cdk抑制性嘧啶化合物、其制备方法以及作为药物的应用
WO2004058144A2 (en) * 2002-12-18 2004-07-15 Glaxo Group Limited Antibacterial agents
CN101213179A (zh) * 2005-07-01 2008-07-02 贝林格尔·英格海姆国际有限公司 用作Aurora抑制剂的2,4-二氨基-嘧啶类化合物
CN101346380A (zh) * 2005-12-21 2009-01-14 辉瑞产品公司 用于治疗异常细胞生长的嘧啶衍生物
CN101511836A (zh) * 2006-07-06 2009-08-19 阿斯利康(瑞典)有限公司 稠合的嘧啶并化合物
WO2008038011A1 (en) * 2006-09-30 2008-04-03 Vernalis (R & D) Limited Pyrimidine derivatives as aurora a and aurora b inhibitors
WO2008128231A1 (en) * 2007-04-16 2008-10-23 Hutchison Medipharma Enterprises Limited Pyrimidine derivatives

Also Published As

Publication number Publication date
CL2012000825A1 (es) 2012-08-24
AR078513A1 (es) 2011-11-16
EP2483249A1 (en) 2012-08-08
IN2012DN02714A (https=) 2015-09-11
WO2011039344A1 (en) 2011-04-07
ZA201201703B (en) 2014-05-28
KR20120092617A (ko) 2012-08-21
MA33606B1 (fr) 2012-09-01
US20110237598A1 (en) 2011-09-29
PH12012500527A1 (en) 2012-10-22
US8466155B2 (en) 2013-06-18
MX2012003101A (es) 2012-04-11
ECSP12011830A (es) 2012-06-29
JP5702390B2 (ja) 2015-04-15
CA2775418A1 (en) 2011-04-07
PE20121431A1 (es) 2012-11-10
TW201124386A (en) 2011-07-16
JP2013506636A (ja) 2013-02-28
UY32916A (es) 2011-04-29
AU2010302648A1 (en) 2012-04-05
EA201200552A1 (ru) 2013-03-29
TN2012000142A1 (en) 2013-09-19
EP2483249B1 (en) 2015-12-23
BR112012007300A2 (pt) 2017-11-07
AP2012006166A0 (en) 2012-04-30
IL218543A0 (en) 2012-05-31
NZ598614A (en) 2013-08-30

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