HRP20200666T1 - Derivati piridin-2(1h)-on kinolinona kao inhibitori mutirane izocitrat dehidrogenaze - Google Patents

Derivati piridin-2(1h)-on kinolinona kao inhibitori mutirane izocitrat dehidrogenaze Download PDF

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Publication number
HRP20200666T1
HRP20200666T1 HRP20200666TT HRP20200666T HRP20200666T1 HR P20200666 T1 HRP20200666 T1 HR P20200666T1 HR P20200666T T HRP20200666T T HR P20200666TT HR P20200666 T HRP20200666 T HR P20200666T HR P20200666 T1 HRP20200666 T1 HR P20200666T1
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compound
formula
image
iii
pharmaceutical composition
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HRP20200666TT
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English (en)
Inventor
Susan Ashwell
Ann-Marie Campbell
Justin Andrew CARAVELLA
R. Bruce DIEBOLD
Anna Ericsson
Gary Gustafson
David R. Lancia
Jian Lin
Wei Lu
Zhongguo Wang
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Forma Therapeutics, Inc.
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Publication of HRP20200666T1 publication Critical patent/HRP20200666T1/hr

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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
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (11)

1. Farmaceutski sastav koji sadrži spoj formule I-13 ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljiv nosač: [image] gdje sastav sadrži od oko 0,1% do oko 99% spoja formule I-13 u odnosu na masu ili volumen.
2. Farmaceutski sastav prema zahtjevu 1, gdje sastav sadrži od oko 5% do oko 90% spoja formule I-13 u odnosu na masu ili volumen.
3. Farmaceutski sastav prema zahtjevu 1 ili zahtjevu 2, gdje je postotak spoja formule I-13 prisutan u sastavu mjeren u odnosu na masu.
4. Farmaceutski sastav prema zahtjevu 1, gdje je spoj formule I-13 prisutan u enantiomernoj čistoći (ee%) većoj od 98% što je određeno kiralnom HPLC analizom.
5. Farmaceutski sastav prema zahtjevu 1, gdje je sastav tableta ili želatinska kapsula.
6. Smjesa koja sadrži spoj formule I-13 kako je definirano u zahtjevu 1 i spoj formule II-1 i spoj formule III: [image] Hal=Cl ili F
7. Smjesa prema zahtjevu 6, gdje je spoj formule III spoj formule III-1: [image] III-1
8. Postupak za dobivanje spoja formule I-13 ili njegove farmaceutski prihvatljive soli: [image] gdje spomenuti postupak obuhvaća korak reagiranja spoja formule II-1 sa spojem formule III: [image] Hal = Cl ili F.
9. Postupak prema zahtjevu 8, gdje spoj formule II-1 ima enantiomerni višak (ee%) veći od 98%.
10. Postupak prema zahtjevu 8 ili zahtjevu 9, gdje je spoj formule III spoj formule III-1: [image] III-1
11. Postupak prema bilo kojem od zahtjeva 8-10, gdje je reakcija spoja formule II-1 sa spojem formule III izvedena pod uvjetom pogodnim za nukleofilnu supstituciju.
HRP20200666TT 2014-09-19 2020-04-24 Derivati piridin-2(1h)-on kinolinona kao inhibitori mutirane izocitrat dehidrogenaze HRP20200666T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201462053006P 2014-09-19 2014-09-19
US201562128089P 2015-03-04 2015-03-04
US201562150812P 2015-04-21 2015-04-21
EP18198969.0A EP3447050B1 (en) 2014-09-19 2015-09-18 Pyridin-2(1h)-one quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors

Publications (1)

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HRP20200666T1 true HRP20200666T1 (hr) 2020-07-24

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US (8) US9834539B2 (hr)
EP (4) EP3194376B1 (hr)
JP (1) JP6648115B2 (hr)
KR (1) KR102209667B1 (hr)
CN (3) CN117695280A (hr)
AU (3) AU2015317329B2 (hr)
BR (1) BR112017005238B1 (hr)
CA (1) CA2961817C (hr)
CL (1) CL2017000658A1 (hr)
CO (1) CO2017003241A2 (hr)
CY (2) CY1121149T1 (hr)
DK (2) DK3447050T3 (hr)
EA (1) EA034336B1 (hr)
EC (1) ECSP17022933A (hr)
ES (3) ES2790640T3 (hr)
FI (1) FI3733662T3 (hr)
HR (1) HRP20200666T1 (hr)
HU (2) HUE062424T2 (hr)
IL (3) IL292608A (hr)
LT (2) LT3194376T (hr)
MA (2) MA40481A (hr)
ME (1) ME03776B (hr)
MX (2) MX2017003404A (hr)
MY (2) MY197533A (hr)
NZ (1) NZ730373A (hr)
PE (1) PE20171056A1 (hr)
PH (1) PH12017500517A1 (hr)
PL (3) PL3194376T3 (hr)
PT (3) PT3447050T (hr)
RS (2) RS60140B1 (hr)
SA (1) SA517381129B1 (hr)
SG (1) SG11201702194SA (hr)
SI (2) SI3447050T1 (hr)
TW (1) TWI686390B (hr)
WO (1) WO2016044789A1 (hr)
ZA (2) ZA201702127B (hr)

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EP3447050B1 (en) 2020-02-19
EA034336B1 (ru) 2020-01-29
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IL251163B (en) 2021-05-31
MX2019013203A (es) 2020-01-20
US20200223822A1 (en) 2020-07-16
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US20210078973A1 (en) 2021-03-18
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US10414752B2 (en) 2019-09-17
DK3194376T3 (en) 2019-01-21
ES2953347T3 (es) 2023-11-10
SI3447050T1 (sl) 2020-08-31
PH12017500517A1 (en) 2017-08-07
US10550098B2 (en) 2020-02-04
PL3733662T3 (pl) 2024-01-22
JP6648115B2 (ja) 2020-02-14
KR102209667B1 (ko) 2021-01-29
US11498913B2 (en) 2022-11-15
CN111909130B (zh) 2023-10-31
IL292608A (en) 2022-07-01
CA2961817A1 (en) 2016-03-24
AU2021215141B2 (en) 2023-10-19
ZA201902446B (en) 2023-12-20
MA40481A (fr) 2017-07-26

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