CN102781931A - 5-炔基-嘧啶及其作为激酶抑制剂的用途 - Google Patents

5-炔基-嘧啶及其作为激酶抑制剂的用途 Download PDF

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Publication number
CN102781931A
CN102781931A CN2011800114539A CN201180011453A CN102781931A CN 102781931 A CN102781931 A CN 102781931A CN 2011800114539 A CN2011800114539 A CN 2011800114539A CN 201180011453 A CN201180011453 A CN 201180011453A CN 102781931 A CN102781931 A CN 102781931A
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China
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membered
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group
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CN2011800114539A
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English (en)
Chinese (zh)
Inventor
S.施耐德
D.凯斯勒
L.范德维恩
T.温伯格
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of CN102781931A publication Critical patent/CN102781931A/zh
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    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D401/14—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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • 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
    • C07D471/10—Spiro-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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2011800114539A 2010-01-26 2011-01-26 5-炔基-嘧啶及其作为激酶抑制剂的用途 Pending CN102781931A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10151722.5 2010-01-26
EP10151722 2010-01-26
PCT/EP2011/051060 WO2011092197A1 (en) 2010-01-26 2011-01-26 5-alkynyl pyrimidines and their use as kinase inhibitors

Publications (1)

Publication Number Publication Date
CN102781931A true CN102781931A (zh) 2012-11-14

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ID=42140100

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CN2011800114539A Pending CN102781931A (zh) 2010-01-26 2011-01-26 5-炔基-嘧啶及其作为激酶抑制剂的用途

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Country Link
US (1) US8618111B2 (enExample)
EP (1) EP2528910B1 (enExample)
JP (1) JP5670479B2 (enExample)
KR (1) KR20130030742A (enExample)
CN (1) CN102781931A (enExample)
AP (1) AP2012006361A0 (enExample)
AR (1) AR080019A1 (enExample)
AU (1) AU2011209343A1 (enExample)
BR (1) BR112012018454A2 (enExample)
CA (1) CA2787396A1 (enExample)
CL (1) CL2012001926A1 (enExample)
CO (1) CO6592046A2 (enExample)
EA (1) EA201201049A1 (enExample)
EC (1) ECSP12012110A (enExample)
IN (1) IN2012DN06600A (enExample)
MA (1) MA33938B1 (enExample)
MX (1) MX2012008359A (enExample)
PE (1) PE20121527A1 (enExample)
PH (1) PH12012501521A1 (enExample)
SG (1) SG182676A1 (enExample)
TN (1) TN2012000370A1 (enExample)
TW (1) TW201139412A (enExample)
UY (1) UY33198A (enExample)
WO (1) WO2011092197A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8633183B2 (en) * 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
US8466162B2 (en) * 2011-01-26 2013-06-18 Boehringer Ingelheim International Gmbh 5-alkynyl-pyridines

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002008205A1 (en) * 2000-07-24 2002-01-31 Krenitsky Pharmaceuticals, Inc. Substituted 5-alkynyl pyrimidines having neurotrophic activity
WO2006044823A2 (en) * 2004-10-18 2006-04-27 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
CN101558046A (zh) * 2006-08-24 2009-10-14 阿斯利康(瑞典)有限公司 用于治疗增殖病症的吗啉代嘧啶衍生物
WO2010012740A1 (en) * 2008-07-29 2010-02-04 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3832570A1 (de) 1988-09-24 1990-03-29 Hoechst Ag 7-substituierte derivate der 3,5-dihydroxyhept-6-insaeure, verfahren zur ihrer herstellung, ihre verwendung als arzneimittel, sowie zwischenprodukte
JPH08504798A (ja) 1992-12-18 1996-05-21 ザ ウエルカム ファウンデーション リミテッド 酵素阻害薬としての，ピリミジン，ピリジン，プテリジノンおよびインダゾール誘導体
US5622954A (en) 1994-05-11 1997-04-22 Fmc Corporation 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides
EP1608373A4 (en) * 2003-03-19 2010-09-29 Exelixis Inc TIE-2 MODULATORS AND USE METHOD
EP1654251A4 (en) * 2003-08-14 2009-03-11 Smithkline Beecham Corp CHEMICAL COMPOUNDS
DE602004015509D1 (de) * 2003-12-24 2008-09-11 Astrazeneca Ab Pyrimidine mit tie2 (tek) aktivität
EP1863805A1 (en) 2005-02-01 2007-12-12 AstraZeneca AB Pyrimidine compounds having tie2 (tek) inhibitory activity
US20080146599A1 (en) 2005-02-01 2008-06-19 Astrazeneca Ab Pyrimidine Compounds Having Tie-2 (Tek) Inhibitory Activity
GB0502418D0 (en) * 2005-02-05 2005-03-16 Astrazeneca Ab Compounds
US20070135437A1 (en) 2005-03-04 2007-06-14 Alsgen, Inc. Modulation of neurodegenerative diseases
JP4993205B2 (ja) * 2005-03-30 2012-08-08 塩野義製薬株式会社 チロシンキナーゼ阻害作用を有するピリミジン誘導体
JP2008534565A (ja) 2005-03-31 2008-08-28 アストラゼネカ アクチボラグ Ｔｉｅ２阻害活性のあるアミノピリミジン誘導体
BRPI0706395A2 (pt) * 2006-01-11 2011-03-22 Astrazeneca Ab composto, uso do mesmo, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente e para tratar doença, composição farmacêutica, e, processo para preparar um composto
JP2010501537A (ja) 2006-08-24 2010-01-21 アストラゼネカ アクチボラグ 増殖性障害の治療に有用なモルホリノピリミジン誘導体
ES2523863T3 (es) 2006-12-29 2014-12-02 Janssen R&D Ireland Pirimidinas 5,6-sustituidas inhibidoras del VIH
EP2022785A1 (en) 2007-06-20 2009-02-11 Bayer Schering Pharma Aktiengesellschaft Alkynylpyrimidines as Tie2 kinase inhibitors
JP2010018601A (ja) * 2009-02-16 2010-01-28 Tetsuya Nishio 複素環化合物、その製造法および用途
US8633183B2 (en) * 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002008205A1 (en) * 2000-07-24 2002-01-31 Krenitsky Pharmaceuticals, Inc. Substituted 5-alkynyl pyrimidines having neurotrophic activity
WO2006044823A2 (en) * 2004-10-18 2006-04-27 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
CN101558046A (zh) * 2006-08-24 2009-10-14 阿斯利康(瑞典)有限公司 用于治疗增殖病症的吗啉代嘧啶衍生物
WO2010012740A1 (en) * 2008-07-29 2010-02-04 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines

Also Published As

Publication number Publication date
UY33198A (es) 2011-08-31
ECSP12012110A (es) 2012-09-28
AR080019A1 (es) 2012-03-07
EA201201049A1 (ru) 2013-02-28
AP2012006361A0 (en) 2012-08-31
JP5670479B2 (ja) 2015-02-18
MX2012008359A (es) 2012-08-08
US20120028958A1 (en) 2012-02-02
EP2528910B1 (en) 2015-03-18
AU2011209343A1 (en) 2012-08-02
CO6592046A2 (es) 2013-01-02
EP2528910A1 (en) 2012-12-05
TN2012000370A1 (en) 2014-01-30
KR20130030742A (ko) 2013-03-27
WO2011092197A1 (en) 2011-08-04
US8618111B2 (en) 2013-12-31
TW201139412A (en) 2011-11-16
SG182676A1 (en) 2012-08-30
PH12012501521A1 (en) 2012-10-22
BR112012018454A2 (pt) 2016-04-19
JP2013518078A (ja) 2013-05-20
CA2787396A1 (en) 2011-08-04
PE20121527A1 (es) 2012-11-21
MA33938B1 (fr) 2013-01-02
CL2012001926A1 (es) 2012-11-30
IN2012DN06600A (enExample) 2015-10-23

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