AU2011315552B2 - Process for manufacturing dihydropteridinones and intermediates thereof - Google Patents

Process for manufacturing dihydropteridinones and intermediates thereof Download PDF

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Publication number
AU2011315552B2
AU2011315552B2 AU2011315552A AU2011315552A AU2011315552B2 AU 2011315552 B2 AU2011315552 B2 AU 2011315552B2 AU 2011315552 A AU2011315552 A AU 2011315552A AU 2011315552 A AU2011315552 A AU 2011315552A AU 2011315552 B2 AU2011315552 B2 AU 2011315552B2
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AU
Australia
Prior art keywords
compound
formula
hereinbefore defined
manufacturing
toluene
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Ceased
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AU2011315552A
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English (en)
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AU2011315552A1 (en
Inventor
Rolf Herter
Juergen Schnaubelt
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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 AU2011315552A1 publication Critical patent/AU2011315552A1/en
Application granted granted Critical
Publication of AU2011315552B2 publication Critical patent/AU2011315552B2/en
Ceased legal-status Critical Current
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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/06Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/033Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Hydrogenated Pyridines (AREA)
AU2011315552A 2010-10-12 2011-10-11 Process for manufacturing dihydropteridinones and intermediates thereof Ceased AU2011315552B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10187194.5 2010-10-12
EP10187194 2010-10-12
PCT/EP2011/067696 WO2012049153A1 (en) 2010-10-12 2011-10-11 Process for manufacturing dihydropteridinones and intermediates thereof

Publications (2)

Publication Number Publication Date
AU2011315552A1 AU2011315552A1 (en) 2013-02-21
AU2011315552B2 true AU2011315552B2 (en) 2015-05-21

Family

ID=43902841

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2011315552A Ceased AU2011315552B2 (en) 2010-10-12 2011-10-11 Process for manufacturing dihydropteridinones and intermediates thereof

Country Status (18)

Country Link
US (1) US8546566B2 (enExample)
EP (1) EP2627656B1 (enExample)
JP (1) JP5937087B2 (enExample)
KR (1) KR20140005877A (enExample)
CN (1) CN103168040A (enExample)
AU (1) AU2011315552B2 (enExample)
BR (1) BR112013008883A2 (enExample)
CA (1) CA2813838A1 (enExample)
CL (1) CL2013000730A1 (enExample)
DK (1) DK2627656T3 (enExample)
EA (1) EA024256B1 (enExample)
ES (1) ES2509741T3 (enExample)
IL (1) IL224602A (enExample)
MX (1) MX2013003994A (enExample)
NZ (1) NZ606700A (enExample)
PH (1) PH12013500694A1 (enExample)
PL (1) PL2627656T3 (enExample)
WO (1) WO2012049153A1 (enExample)

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US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US20060035903A1 (en) * 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US7439358B2 (en) 2006-02-08 2008-10-21 Boehringer Ingelheim International Gmbh Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
US8546566B2 (en) 2010-10-12 2013-10-01 Boehringer Ingelheim International Gmbh Process for manufacturing dihydropteridinones and intermediates thereof
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
US9370535B2 (en) 2011-05-17 2016-06-21 Boehringer Ingelheim International Gmbh Method for treatment of advanced solid tumors
WO2015011236A1 (en) 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Treatment of myelodysplastic syndrome
CN104003989B (zh) * 2014-05-26 2015-11-11 苏州明锐医药科技有限公司 伏拉塞替及其中间体的制备方法
US9867831B2 (en) 2014-10-01 2018-01-16 Boehringer Ingelheim International Gmbh Combination treatment of acute myeloid leukemia and myelodysplastic syndrome
CN105646398B (zh) * 2014-12-05 2018-09-07 上海医药工业研究院 N-((1r,4r)-4-(4-(环丙基甲基)哌嗪-1-基)环己基)乙酰胺的制备方法
CN108610343A (zh) * 2018-06-12 2018-10-02 杨文思 一种用于治疗癌症的表皮生长因子受体抑制剂及其合成方法
CA3124330A1 (en) 2018-12-21 2020-06-25 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor

Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2007090844A1 (en) * 2006-02-08 2007-08-16 Boehringer Ingelheim International Gmbh Trihydrochloride forms of a dihydropteridinone derivative and processes for preparation

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Also Published As

Publication number Publication date
DK2627656T3 (da) 2014-09-08
EA024256B1 (ru) 2016-08-31
AU2011315552A1 (en) 2013-02-21
ES2509741T3 (es) 2014-10-17
JP5937087B2 (ja) 2016-06-22
EP2627656B1 (en) 2014-08-20
US20120238754A1 (en) 2012-09-20
WO2012049153A1 (en) 2012-04-19
BR112013008883A2 (pt) 2017-10-10
CA2813838A1 (en) 2012-04-19
EP2627656A1 (en) 2013-08-21
MX2013003994A (es) 2013-06-05
CL2013000730A1 (es) 2013-08-09
KR20140005877A (ko) 2014-01-15
CN103168040A (zh) 2013-06-19
US8546566B2 (en) 2013-10-01
IL224602A (en) 2016-04-21
JP2013539771A (ja) 2013-10-28
NZ606700A (en) 2015-06-26
EA201300443A1 (ru) 2013-11-29
PL2627656T3 (pl) 2015-02-27
PH12013500694A1 (en) 2015-06-19

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