CY1120325T1 - Τρικυκλικες ετεροκυκλικες ενωσεις ως αναστολεις φωσφοϊνοσιτιδιου 3-κινασης - Google Patents

Τρικυκλικες ετεροκυκλικες ενωσεις ως αναστολεις φωσφοϊνοσιτιδιου 3-κινασης

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Publication number
CY1120325T1
CY1120325T1 CY20181100607T CY181100607T CY1120325T1 CY 1120325 T1 CY1120325 T1 CY 1120325T1 CY 20181100607 T CY20181100607 T CY 20181100607T CY 181100607 T CY181100607 T CY 181100607T CY 1120325 T1 CY1120325 T1 CY 1120325T1
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Cyprus
Prior art keywords
alkyl
phosphoinositide
kinase inhibitors
heterocyclic compounds
membered
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CY20181100607T
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English (en)
Inventor
Stephen Joseph Shuttleworth
Alexander Richard Liam Cecil
Franck Alexandre Silva
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Karus Therapeutics Limited
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Publication date
Application filed by Karus Therapeutics Limited filed Critical Karus Therapeutics Limited
Publication of CY1120325T1 publication Critical patent/CY1120325T1/el

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    • C07ORGANIC CHEMISTRY
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    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems
    • C07D491/147Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical 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)
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  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Μία ένωση του τύπου I: (I) ή φαρμακευτικώς αποδεκτό άλας αυτής, όπου: W είναι Ο, Ν-Η, N-(C1-C10 αλκύλ) ή S· εκάστη Χ ανεξαρτήτως είναι CH ή Ν· R1 είναι 5-μελής έως 7-μελής κορεσμένος ή ακόρεστος, προαιρετικά υποκατεστημένος ετερόκυκλος που περιέχει τουλάχιστον 1 ετεροάτομο επιλεγόμενο από Ν ή Ο· R2 είναι LY· εκάστη L είναι άμεσος δεσμός, C1-C10 αλκυλένο, C2-C10 αλκενυλένο ή C2-C10 αλκυνυλένο, Υ είναι προαιρετικώς υποκατεστημένος συντηγμένος, γεφυρωμένος ή σπειροκυκλικός μη αρωματικός 5-12 μελής ετερόκυκλος που περιέχει μέχρι 4 ετεροάτομα επιλεγόμενα από Ν ή Ο, και εκάστη R3 ανεξαρτήτως είναι Η, C1-C10 αλκύλ, αλογόνο, φθόρο C1-C10 αλκύλ, Ο-C1 -C10 αλκύλ, NH-C1-C10 αλκύλ, S-C1 -C10 αλκύλ, Ο- φθόρο C1 -C10 αλκύλ, ΝΗ-ακύλ, NH-C(Ο)-NH-C1 -C10 αλκύλ, C(Ο)-NH-C1 -C10 αλκύλ, αρύλ ή ετεροαρύλ, είναι χρήσιμα ως αναστολείς του ενζύμου κατηγορίας ΙΑ φωσφοϊνοσιτιδίου 3-κινάση, ΡΙ3Κ-p110δ, και συνεπώς έχουν πιθανή χρησιμότητα στη θεραπεία καρκίνου, άνοσων και φλεγμονωδών ασθενειών.
CY20181100607T 2014-02-12 2018-06-11 Τρικυκλικες ετεροκυκλικες ενωσεις ως αναστολεις φωσφοϊνοσιτιδιου 3-κινασης CY1120325T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1402431.9A GB201402431D0 (en) 2014-02-12 2014-02-12 Compounds
PCT/GB2015/050396 WO2015121657A1 (en) 2014-02-12 2015-02-12 Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors

Publications (1)

Publication Number Publication Date
CY1120325T1 true CY1120325T1 (el) 2019-07-10

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EP (1) EP3105233B1 (el)
JP (1) JP6516371B2 (el)
KR (1) KR102491796B1 (el)
CN (1) CN106103450B (el)
AU (1) AU2015216702B2 (el)
BR (1) BR112016019462B8 (el)
CA (1) CA2939045C (el)
CY (1) CY1120325T1 (el)
DK (1) DK3105233T3 (el)
ES (1) ES2673278T3 (el)
GB (1) GB201402431D0 (el)
HR (1) HRP20180768T1 (el)
HU (1) HUE037210T2 (el)
IL (1) IL247103B (el)
LT (1) LT3105233T (el)
MX (1) MX370151B (el)
NO (1) NO3105233T3 (el)
NZ (1) NZ723502A (el)
PL (1) PL3105233T3 (el)
PT (1) PT3105233T (el)
RS (1) RS57296B1 (el)
SG (1) SG11201606576UA (el)
SI (1) SI3105233T1 (el)
TR (1) TR201807906T4 (el)
WO (1) WO2015121657A1 (el)
ZA (1) ZA201605586B (el)

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LT3105233T (lt) 2018-06-25
TR201807906T4 (tr) 2018-06-21
JP2017505343A (ja) 2017-02-16
BR112016019462A2 (el) 2017-08-15
US11708378B2 (en) 2023-07-25
KR20160127757A (ko) 2016-11-04
MX370151B (es) 2019-12-03
US10513530B2 (en) 2019-12-24
NO3105233T3 (el) 2018-08-25
ES2673278T3 (es) 2018-06-21
CN106103450B (zh) 2018-12-11
IL247103B (en) 2020-03-31
GB201402431D0 (en) 2014-03-26
PL3105233T3 (pl) 2018-09-28
BR112016019462B1 (pt) 2023-02-07
JP6516371B2 (ja) 2019-05-22
US9981987B2 (en) 2018-05-29
US20220041624A1 (en) 2022-02-10
AU2015216702B2 (en) 2018-11-08
PT3105233T (pt) 2018-06-15
SG11201606576UA (en) 2016-09-29
RS57296B1 (sr) 2018-08-31
US20160347771A1 (en) 2016-12-01
US20190092790A1 (en) 2019-03-28
EP3105233B1 (en) 2018-03-28
IL247103A0 (en) 2016-09-29
HRP20180768T1 (hr) 2018-08-10
KR102491796B1 (ko) 2023-01-27
EP3105233A1 (en) 2016-12-21
US20200354378A1 (en) 2020-11-12
DK3105233T3 (en) 2018-06-14
CA2939045A1 (en) 2015-08-20
WO2015121657A1 (en) 2015-08-20
BR112016019462B8 (pt) 2023-02-23
AU2015216702A1 (en) 2016-09-01
CA2939045C (en) 2022-09-13
NZ723502A (en) 2019-05-31
MX2016010404A (es) 2016-11-30
CN106103450A (zh) 2016-11-09
HUE037210T2 (hu) 2018-08-28
SI3105233T1 (sl) 2018-10-30

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