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HRP20160246T4 - Dimaleat od aminokrotonilskog spoja i postupak njegove proizvodnje - Google Patents

Dimaleat od aminokrotonilskog spoja i postupak njegove proizvodnje Download PDF

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Publication number
HRP20160246T4
HRP20160246T4 HRP20160246TT HRP20160246T HRP20160246T4 HR P20160246 T4 HRP20160246 T4 HR P20160246T4 HR P20160246T T HRP20160246T T HR P20160246TT HR P20160246 T HRP20160246 T HR P20160246T HR P20160246 T4 HRP20160246 T4 HR P20160246T4
Authority
HR
Croatia
Prior art keywords
amino
chloro
fluorophenyl
buten
quinazoline
Prior art date
Application number
HRP20160246TT
Other languages
English (en)
Inventor
Werner Rall
Christian Kulinna
Juergen Schnaubelt
Peter Sieger
Rainer Soyka
Original Assignee
Boehringer Ingelheim International Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34428508&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20160246(T4) "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 HRP20160246T1 publication Critical patent/HRP20160246T1/hr
Publication of HRP20160246T4 publication Critical patent/HRP20160246T4/hr

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Classifications

    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (6)

1. Postupak za proizvodnju dimaleata od 4-[(3-kloro-4-fluorofenil)amino]-6-{[4-(N,N-dimetilamino)-1-okso-2-buten-1-il]amino}-7-((S)-tetrahidrofuran-3-iloksi)-kinazolina, naznačen time, da obuhvaća sljedeće korake a) i b): a) reakcija spoja opće formule (V) [image] gdje X predstavlja atom dušika i Rapredstavlja atom 3-kloro-4-fluorofenilnu skupinu, u prikladnim otapalima slijedom nakon odgovarajućeg aktiviranja s di-(C1-4-alkil)-fosfono-octenom kiselinom, i b) reakcija tako dobivenog spoja opće formule (VI) [image] gdje X predstavlja atom dušika, Ra predstavlja 3-kloro-4-fluorofenilnu skupinu i R1 predstavlja ravnolančanu ili razgranatu C1-4alkil skupinu, s aldehidom formule [image] gdje R3 i R4 u svakom slučaju predstavljaju metilnu skupinu, ili odgovarajući ekvivalent aldehida pri uporabi prikladnih organskih ili anorganskih baza, kao i sljedeći korak c): c) pretvaranje tako dobivenog 4-[(3-kloro-4-fluorofenil)amino]-6-{[4-(N,N-dimetilamino)-1-okso-2-buten-1-il]amino}-7-((S)-tetrahidrofuran-3-iloksi)-kinazolina u dimaleat putem reakcije, uz zagrijavanje, s maleinskom kiselinom u prikladnom otapalu.
2. Postupak prema patentnom zahtjevu 1, naznačen time, da se kao otapala mogu upotrebljavati etanol ili izopropanol, opcionalno s dodavanjem vode.
3. Postupak prema patentnom zahtjevu 1 ili 2, naznačen time, da se upotrebljavaju najmanje dva ekvivalenta maleinske kiseline.
4. Kristalni 4-[(3-kloro-4-fluorofenil)amino]-6-{[4-(N,N-dimetilamino)-1-okso-2-buten-1-il]amino}-7-((S)-tetrahidrofuran-3-iloksi)-kinazolin-dimaleat, naznačen time, da ima karakterističan kut difrakcije određen pomoću CuKα radijacije s valnom duljinom od λ = 1,5418 Å, kako slijedi: [image]
5. Medicinski proizvod, naznačen time, da sadrži kristalni 4-[(3-kloro-4-fluorofenil)amino]-6-{[4-(N,N-dimetilamino)-1-okso-2-buten-1-il]amino}-7-((S)-tetrahidrofuran-3-iloksi)-kinazolin-dimaleat prema patentnom zahtjevu 4 te osim toga, opcijski, jedan ili više inertnih nosača i/ili razrjeđivača.
6. Uporaba kristalnog 4-[(3-kloro-4-fluorofenil)amino]-6-{[4-(N,N-dimetilamino)-1-okso-2-buten-1-il]amino}-7-((S)-tetrahidrofuran-3-iloksi)-kinazolin-dimaleata prema patentnom zahtjevu 4, naznačena time, da je za proizvodnju medicinskog proizvoda koji je prikladan za liječenje benignih ili malignih tumora, za prevenciju i liječenje bolesti respiratornog trakta i pluća, kao i za liječenje bolesti gastrointestinalnog trakta te žučnih vodova i žučnog mjehura.
HRP20160246TT 2003-10-17 2004-10-12 Dimaleat od aminokrotonilskog spoja i postupak njegove proizvodnje HRP20160246T4 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10349113A DE10349113A1 (de) 2003-10-17 2003-10-17 Verfahren zur Herstellung von Aminocrotonylverbindungen
EP12155662.5A EP2508521B2 (de) 2003-10-17 2004-10-12 Dimaleat einer Aminocrotonylverbindung und Verfahren zu ihrer Herstellung

Publications (2)

Publication Number Publication Date
HRP20160246T1 HRP20160246T1 (hr) 2016-04-08
HRP20160246T4 true HRP20160246T4 (hr) 2022-11-11

Family

ID=34428508

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20160246TT HRP20160246T4 (hr) 2003-10-17 2004-10-12 Dimaleat od aminokrotonilskog spoja i postupak njegove proizvodnje
HRP20131214TT HRP20131214T1 (hr) 2003-10-17 2013-12-20 Postupak za proizvodnju aminokrotonilskih spojeva

Family Applications After (1)

Application Number Title Priority Date Filing Date
HRP20131214TT HRP20131214T1 (hr) 2003-10-17 2013-12-20 Postupak za proizvodnju aminokrotonilskih spojeva

Country Status (35)

Country Link
US (2) US20050085495A1 (hr)
EP (2) EP1678165B1 (hr)
JP (2) JP4594317B2 (hr)
KR (2) KR101180752B1 (hr)
CN (2) CN101402631A (hr)
AR (1) AR046118A1 (hr)
AU (2) AU2004281938B2 (hr)
BR (2) BRPI0415424B8 (hr)
CA (2) CA2759063C (hr)
CY (2) CY1114866T1 (hr)
DE (1) DE10349113A1 (hr)
DK (2) DK1678165T3 (hr)
EA (1) EA016624B1 (hr)
EC (1) ECSP066509A (hr)
ES (2) ES2563211T5 (hr)
HK (1) HK1095817A1 (hr)
HR (2) HRP20160246T4 (hr)
HU (1) HUE028254T2 (hr)
IL (2) IL174951A (hr)
ME (1) ME00341B (hr)
MX (2) MXPA06004076A (hr)
MY (2) MY155425A (hr)
NO (2) NO333971B1 (hr)
NZ (2) NZ547154A (hr)
PE (2) PE20100267A1 (hr)
PL (2) PL1678165T3 (hr)
PT (2) PT1678165E (hr)
RS (3) RS60563B1 (hr)
SG (1) SG139743A1 (hr)
SI (2) SI2508521T2 (hr)
TW (2) TWI373470B (hr)
UA (2) UA91006C2 (hr)
UY (2) UY28559A1 (hr)
WO (1) WO2005037824A2 (hr)
ZA (1) ZA200602234B (hr)

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