HRP20100324T1 - Derivati hinazolina i njihova upotreba u tretmanu trombocitemije - Google Patents

Derivati hinazolina i njihova upotreba u tretmanu trombocitemije Download PDF

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HRP20100324T1
HRP20100324T1 HR20100324T HRP20100324T HRP20100324T1 HR P20100324 T1 HRP20100324 T1 HR P20100324T1 HR 20100324 T HR20100324 T HR 20100324T HR P20100324 T HRP20100324 T HR P20100324T HR P20100324 T1 HRP20100324 T1 HR P20100324T1
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compound
image
compound according
thrombocythemia
pure
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HR20100324T
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Franklin Richard
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Shire Holdings Ag
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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
    • 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

Spoj formulenjegov uravnoteženi oblik, farmaceutski prihvatljiva sol ovog spoja ili njegovog uravnoteženog oblika, gdje suR1 je H, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi ili C6-10 aril; R2 jeR3 je OH, halogen, SH, O- C1-6 alkil ili NH2; iX i Y neovisno jedan o drugom, su H ili halogen, a pri tome je spoj najmanje 80% čist, kada se čistoća određuje standardnim analitičkim postupcima, a pri tome taj spoj nije Patent sadrži još 15 patentnih zahtjeva.

Claims (16)

1. Spoj formule [image] njegov uravnoteženi oblik, farmaceutski prihvatljiva sol ovog spoja ili njegovog uravnoteženog oblika, gdje su R1 je H, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi ili C6-10 aril; R2 je [image] R3 je OH, halogen, SH, O- C1-6 alkil ili NH2; i X i Y neovisno jedan o drugom, su H ili halogen, a pri tome je spoj najmanje 80% čist, kada se čistoća određuje standardnim analitičkim postupcima, a pri tome taj spoj nije [image]
2. Spoj prema Zahtjevu 1, pri čemu je taj spoj najmanje 85% čist, poželjno najmanje 90% čist, poželjnije najmanje 95% čist, a najpoželjnije 99% čist, kada se čistoća određuje standardnim analitičkim postupcima.
3. Spoj prema Zahtjevu 1 ili Zahtjevu 2, a pri tome taj spoj ima formulu: [image]
4. Spoj prema Zahtjevu 3, pri čemu R2 predstavlja [image]
5. Spoj prema Zahtjevu 3, pri čemu R1 predstavlja H ili C1-6 alkil.
6. Spoj prema Zahtjevu 3, pri čemu R1 predstavlja H.
7. Spoj prema Zahtjevu 3, pri čemu X predstavlja H ili halogen.
8. Spoj prema Zahtjevu 3, pri čemu Y predstavlja H ili Cl.
9. Spoj prema Zahtjevu 3, pri čemu X predstavlja Cl.
10. Spoj prema Zahtjevu 3, pri čemu Y predstavlja Cl.
11. Spoj prema Zahtjevu 1 ili Zahtjevu 2, pri čemu taj spoj predstavlja [image]
12. Spoj prema Zahtjevu 1 ili Zahtjevu 2, ili spoj [image] koji se upotrebljava u tretmanu trombocitemije.
13. Spoj prema Zahtjevu 12, pri čemu se upotreba sastoji od tretmana trombocitemije povezane s esencijalnom trombocitemijom (ET), kroničnom mijelogenom leukemijom (CML), policitemijom verom (PV), agnogenom mijeloidnom metaplazijom (AMM) ili anemijom srpastih stanica (SCA).
14. Spoj definiran u Zahtjevu 11, ili spoj [image] koje se upotrebljava u tretmanu trombocitemije.
15. Spoj prema Zahtjevu 14, pri čemu se upotreba sastoji od tretmana trombocitemije povezane s esencijalnom trombocitemijom (ET), kroničnom mijelogenom leukemijom (CML), policitemijom verom (PV), agnogenom mijeloidnom metaplazijom (AMM) ili anemijom srpastih stanica (SCA).
16. Kompozicija koja sadrži najmanje jednan spoj definiran Zahtjevom 1 ili spoj [image] i najmanje jedan terapeutski agens koji se bira između anagrelida, hidroksiuree, P32, bisulfana, aspirina, klopidogrela, �-interferon tiklopidina i dipiridamola.
HR20100324T 2004-08-04 2010-06-04 Derivati hinazolina i njihova upotreba u tretmanu trombocitemije HRP20100324T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US59843704P 2004-08-04 2004-08-04
PCT/US2005/028086 WO2006017822A2 (en) 2004-08-04 2005-08-04 Quinazoline derivatives and their use in the treatment of thrombocythemia

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HRP20100324T1 true HRP20100324T1 (hr) 2010-07-31

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HR20100324T HRP20100324T1 (hr) 2004-08-04 2010-06-04 Derivati hinazolina i njihova upotreba u tretmanu trombocitemije

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US (2) US7700608B2 (hr)
EP (1) EP1781296B1 (hr)
JP (1) JP4758992B2 (hr)
KR (1) KR100932328B1 (hr)
CN (1) CN101027060A (hr)
AT (1) ATE460166T1 (hr)
AU (1) AU2005271274B2 (hr)
BR (1) BRPI0513944A (hr)
CA (1) CA2574822C (hr)
CY (1) CY1110341T1 (hr)
DE (1) DE602005019890D1 (hr)
DK (1) DK1781296T3 (hr)
EA (1) EA015251B1 (hr)
ES (1) ES2343360T3 (hr)
HR (1) HRP20100324T1 (hr)
NO (1) NO20071019L (hr)
NZ (1) NZ553051A (hr)
PL (1) PL1781296T3 (hr)
PT (1) PT1781296E (hr)
RS (1) RS51376B (hr)
SI (1) SI1781296T1 (hr)
WO (1) WO2006017822A2 (hr)

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EA200700407A1 (ru) 2007-08-31
JP4758992B2 (ja) 2011-08-31
AU2005271274A1 (en) 2006-02-16
WO2006017822A3 (en) 2006-08-24
CN101027060A (zh) 2007-08-29
EP1781296A2 (en) 2007-05-09
US20060052601A1 (en) 2006-03-09
EA015251B1 (ru) 2011-06-30
SI1781296T1 (sl) 2010-09-30
DE602005019890D1 (de) 2010-04-22
EP1781296B1 (en) 2010-03-10
EP1781296A4 (en) 2008-08-20
AU2005271274B2 (en) 2010-03-04
DK1781296T3 (da) 2010-06-21
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ES2343360T3 (es) 2010-07-29
US7700608B2 (en) 2010-04-20
RS51376B (en) 2011-02-28
PL1781296T3 (pl) 2010-08-31
CA2574822A1 (en) 2006-02-16
KR100932328B1 (ko) 2009-12-16
NO20071019L (no) 2007-05-03
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PT1781296E (pt) 2010-06-15
CY1110341T1 (el) 2015-01-14

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