HRP20160253T1 - Inhibitor benzodiazepinske bromodomene - Google Patents

Inhibitor benzodiazepinske bromodomene Download PDF

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Publication number
HRP20160253T1
HRP20160253T1 HRP20160253TT HRP20160253T HRP20160253T1 HR P20160253 T1 HRP20160253 T1 HR P20160253T1 HR P20160253T T HRP20160253T T HR P20160253TT HR P20160253 T HRP20160253 T HR P20160253T HR P20160253 T1 HRP20160253 T1 HR P20160253T1
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Croatia
Prior art keywords
compound
pharmaceutically acceptable
alkyl
acceptable salt
alkoxy
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HRP20160253TT
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English (en)
Inventor
James Bailey
Romain Luc Marie Gosmini
Olivier Mirguet
Jason Witherington
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Glaxosmithkline Llc
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Priority claimed from GB0919433A external-priority patent/GB0919433D0/en
Priority claimed from GBGB1010509.6A external-priority patent/GB201010509D0/en
Priority claimed from PCT/EP2010/061518 external-priority patent/WO2011054553A1/en
Priority claimed from GBGB1014231.3A external-priority patent/GB201014231D0/en
Application filed by Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of HRP20160253T1 publication Critical patent/HRP20160253T1/hr

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    • 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (10)

1. Spoj formule (Ic) ili njegova farmaceutski prihvatljiva sol [image] , gdje R1 je C1-3alkil; R2 je -NR2aR2a′ ili -OR2b; gdje je jedan od R2a ili R2′a H, a R2b ili drugog od R2a ili R2′a se bira između C1-6alkila, halogenC1-6alkila, R2cR2′cN-C1-6alkila, karbociklila, karbociklilC1-4alkila, heterociklila i heterociklilC1-4alkila, gdje je bilo koja od karbociklilnih ili heterociklilnih skupina izborno supstituirana s jednom ili više skupina, koje se bira između halogena, C1-6alkila, halogenC1-6alkila, C1-6alkoksi, halogenC1-6alkoksi, karbonila, -CO-karbociklila, azido, nitro i cijano, gdje -CO-karbociklilna skupina može biti dodatano izborno supstituirana s jednom ili više skupina, koje se bira između halogena, C1-6alkila, halogenC1-6alkila, C1-6alkoksi, halogenC1-6alkoksi, azido, nitro i cijano; ili dvije susjedne skupine na bilo kojoj od karbociklilnih ili heterociklilnih skupina zajedno s povezujućim atomima tvore 5- ili 6-eročlani prsten, gdje prsten može sadržavati 1 ili 2 heteroatoma, koje se neovisno bira između O, S i N; ili R2a i R2′a, zajedno s N-atomom na gojeg su vezani, tvore 5-, 6- ili 7-eročlani prsten, koji može izborno sadržavati 1 ili 2 heteroatoma, koje se neovisno bira između O, S i N; gdje 5-, 6- ili 7-eročlani prsten može biti dodatano izborno supstituiran s C1-6alkilom; R2c i R2′csu neovisno H i C1-6alkil; svaki R3 se neovisno bira između H, hidroksi, halogena, C1-6alkila, halogenC1-6alkila, C1-6alkoksi, halogenC1-6alkoksi, nitro, cijano, CF3, -OCF3 i -COOR5; R4 je hidroksi, halogen, C1-6alkil, halogenC1-6alkil, C1-6alkoksi, halogenC1-6alkoksi, nitro, cijano, CF3, -OCF3; -COOR5 ili -OS(O)2C1-4alkil; R5 je C1-3alkil; i n je cijeli broj 1 do 5, naznačen time što je namijenjen upotrebi u liječenju raka.
2. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 1, gdje R4 predstavlja hidroksil ili C1-6alkoksi.
3. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 1, gdje je spoj formule (Ib) [image] , gdje: R1, R2 i R3 i n su u skladu s patentnim zahtjevom 1.
4. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1-3, gdje je R1 metil.
5. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1-4, gdje je n 1.
6. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1-5, gdje je R3 3-fluor, 4-klor, 4-fluor, 4-metoksi ili 4-CF3.
7. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1-6, gdje je S-enantiomer.
8. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1-7, gdje se rak bira između hematološkog, raka epitela, uključujući onog kod pluća, karcinoma dojke i debelog crijeva, te tumora mezenhima, jetre, bubrega i neuroloških tumora.
9. Upotreba spoja, ili njegove farmaceutski prihvatljive soli, u skladu s bilo kojim od patentnih zahtjeva 1-7, naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje raka.
10. Farmaceutski pripravak, koji sadrži spoj formule (Ic), ili njegovu farmaceutski prihvatljivu sol, u skladu s bilo kojim od patentnih zahtjeva 1-7, kao i jednu ili više farmaceutski prihvatljivih podloga, razrjeđivača ili pomoćnih tvari, naznačen time što je namijenjen upotrebi u liječenju raka.
HRP20160253TT 2009-11-05 2016-03-10 Inhibitor benzodiazepinske bromodomene HRP20160253T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0919433A GB0919433D0 (en) 2009-11-05 2009-11-05 Novel compounds
GBGB1010509.6A GB201010509D0 (en) 2010-06-22 2010-06-22 Novel compounds
PCT/EP2010/061518 WO2011054553A1 (en) 2009-11-05 2010-08-06 Benzodiazepine bromodomain inhibitor
GBGB1014231.3A GB201014231D0 (en) 2010-08-25 2010-08-25 Novel compounds
PCT/EP2010/066697 WO2011054845A1 (en) 2009-11-05 2010-11-03 Benzodiazepine bromodomain inhibitor

Publications (1)

Publication Number Publication Date
HRP20160253T1 true HRP20160253T1 (hr) 2016-04-08

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HRP20160253TT HRP20160253T1 (hr) 2009-11-05 2016-03-10 Inhibitor benzodiazepinske bromodomene

Country Status (23)

Country Link
US (3) US9102677B2 (hr)
EP (2) EP2496582B1 (hr)
JP (3) JP5702396B2 (hr)
KR (1) KR20120097508A (hr)
CN (1) CN102781943B (hr)
AU (1) AU2010317096B2 (hr)
BR (1) BR112012010705A2 (hr)
CA (1) CA2779423C (hr)
CY (1) CY1117424T1 (hr)
DK (1) DK2496582T3 (hr)
EA (1) EA023441B1 (hr)
ES (2) ES2654423T3 (hr)
HK (1) HK1221221A1 (hr)
HR (1) HRP20160253T1 (hr)
HU (1) HUE026967T2 (hr)
IL (2) IL219253A (hr)
ME (1) ME02356B (hr)
MX (1) MX341212B (hr)
PL (1) PL2496582T3 (hr)
RS (1) RS54645B1 (hr)
SI (1) SI2496582T1 (hr)
SM (1) SMT201600104B (hr)
WO (1) WO2011054845A1 (hr)

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