DK2744809T3 - 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazol og anvendelse deraf som bromodomæneinhibitor - Google Patents

4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazol og anvendelse deraf som bromodomæneinhibitor Download PDF

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DK2744809T3
DK2744809T3 DK12748028.3T DK12748028T DK2744809T3 DK 2744809 T3 DK2744809 T3 DK 2744809T3 DK 12748028 T DK12748028 T DK 12748028T DK 2744809 T3 DK2744809 T3 DK 2744809T3
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compound
formula
pharmaceutically acceptable
cancer
methoxy
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DK12748028.3T
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Emmanuel Hubert Demont
Katherine Louise Jones
Robert J Watson
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Glaxosmithkline Llc
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    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (12)

1. Forbindelse ifølge formel (I), som er 4-(8-methoxy-l-(l-methoxypropan-2-yl)-2-(tetrahydro-2H-pyran-4-yl)-lH-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazol
(i) eller et salt deraf.
2. Forbindelse ifølge formel (IA) ifølge krav 1, som er 4-(8-methoxy-l-((R)-l-meth-oxypropan-2-yl)-2-(tetrahydro-2FI-pyran-4-yl)-lFI-imidazo[4,5-c]quinolin-7-yl)-3,5-dime-thylisoxazol
(IA) eller et salt deraf.
3. Forbindelse ifølge formel (IB) ifølge krav 1, som er 4-(8-methoxy-l-((S)-l-meth-oxypropan-2-yl)-2-(tetrahydro-2FI-pyran-4-yl)-lFI-imidazo[4,5-c]quinolin-7-yl)-3,5-dime-thylisoxazol
(IB) eller et salt deraf.
4. Forbindelse ifølge et hvilket som helst af krav 1-3 eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølge krav 4 i form af en fri base.
6. Forbindelse ifølge krav 4 i form af et methansulfonatsalt.
7. Farmaceutisk sammensætning, som omfatter en forbindelse eller et farmaceutisk acceptabelt salt deraf, som defineret i krav 4 og ét eller flere farmaceutisk acceptable bærestoffer, fortyndingsmidler eller excipienser.
8. Kombineret farmaceutisk produkt omfattende en forbindelse eller et farmaceutisk acceptabelt salt deraf som defineret i krav 4, sammen med ét eller flere andre terapeutisk aktive midler.
9. Forbindelse eller et farmaceutisk acceptabelt salt deraf som defineret i krav 4, til anvendelse i terapi.
10. Forbindelse eller et farmaceutisk acceptabelt salt deraf som defineret i krav 4, til anvendelse i behandling afen kronisk autoimmun og/eller inflammatorisk tilstand.
11. Forbindelse eller et farmaceutisk acceptabelt salt deraf som defineret i krav 4, til anvendelse i behandling af cancer.
12. Forbindelse eller et farmaceutisk acceptabelt salt deraf til anvendelse ifølge krav 11, hvor canceren er valgt blandt leukæmi, NUT midtlinje karcinom, knoglemarvskræft, neu-roblastom, Burkitts lymfom, livmoderhalskræft, spiserørskræft, æggestokkræft, brystkræft og kolorektalcancer.
DK12748028.3T 2011-08-17 2012-08-15 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazol og anvendelse deraf som bromodomæneinhibitor DK2744809T3 (da)

Applications Claiming Priority (2)

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GBGB1114103.3A GB201114103D0 (en) 2011-08-17 2011-08-17 Novel compounds
PCT/EP2012/065918 WO2013024104A1 (en) 2011-08-17 2012-08-15 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1 h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor

Publications (1)

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DK2744809T3 true DK2744809T3 (da) 2017-01-23

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EP (2) EP3150601A1 (da)
JP (1) JP6059723B2 (da)
KR (1) KR20140064878A (da)
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CA (1) CA2843537A1 (da)
CL (1) CL2014000365A1 (da)
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CR (1) CR20140076A (da)
CY (1) CY1118370T1 (da)
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DO (1) DOP2014000031A (da)
EA (1) EA023374B1 (da)
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GB (1) GB201114103D0 (da)
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TW (1) TWI558704B (da)
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US9861627B2 (en) 2018-01-09
PE20141406A1 (es) 2014-10-25
US20160317529A1 (en) 2016-11-03
GB201114103D0 (en) 2011-09-28
BR112014003681A8 (pt) 2018-01-23
IL230489A (en) 2016-07-31
HRP20161674T1 (hr) 2017-01-27
HUE030106T2 (en) 2017-04-28
BR112014003681A2 (pt) 2017-03-01
EP3150601A1 (en) 2017-04-05
AU2012296914B2 (en) 2016-03-03
WO2013024104A1 (en) 2013-02-21
MY170729A (en) 2019-08-27
US20170157113A1 (en) 2017-06-08
CY1118370T1 (el) 2017-06-28
KR20140064878A (ko) 2014-05-28
US20140171462A1 (en) 2014-06-19
UY34264A (es) 2013-04-05
CN103889984A (zh) 2014-06-25
SMT201700005B (it) 2017-03-08
JP6059723B2 (ja) 2017-01-11
TW201323424A (zh) 2013-06-16
JO3187B1 (ar) 2018-03-08
US9067936B2 (en) 2015-06-30
MX2014001834A (es) 2014-02-27
CR20140076A (es) 2014-03-19
TWI558704B (zh) 2016-11-21
CO6862151A2 (es) 2014-02-10
US9610284B2 (en) 2017-04-04
PL2744809T3 (pl) 2017-08-31
EP2744809B1 (en) 2016-10-12
CL2014000365A1 (es) 2014-07-11
PT2744809T (pt) 2017-01-06
ES2609857T3 (es) 2017-04-24
US20150315184A1 (en) 2015-11-05
AU2012296914A1 (en) 2014-02-13
SI2744809T1 (sl) 2017-01-31
MX350597B (es) 2017-09-11
AR087545A1 (es) 2014-04-03
EP2744809A1 (en) 2014-06-25
UA110838C2 (uk) 2016-02-25
JP2014521735A (ja) 2014-08-28
CN103889984B (zh) 2016-01-13
NZ620263A (en) 2016-04-29
ME02589B (me) 2017-06-20
RS55560B1 (sr) 2017-05-31
CA2843537A1 (en) 2013-02-21
IN2014CN00568A (da) 2015-04-03
DOP2014000031A (es) 2014-06-01
LT2744809T (lt) 2016-12-27
US9416130B2 (en) 2016-08-16
EA023374B1 (ru) 2016-05-31
EA201490200A1 (ru) 2014-07-30
IL230489A0 (en) 2014-03-31

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