HRP20161349T1 - 7-metil-2-[4-metil-6-[4-(trifluorometil)-fenil]piramidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on - Google Patents

7-metil-2-[4-metil-6-[4-(trifluorometil)-fenil]piramidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on Download PDF

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Publication number
HRP20161349T1
HRP20161349T1 HRP20161349TT HRP20161349T HRP20161349T1 HR P20161349 T1 HRP20161349 T1 HR P20161349T1 HR P20161349T T HRP20161349T T HR P20161349TT HR P20161349 T HRP20161349 T HR P20161349T HR P20161349 T1 HRP20161349 T1 HR P20161349T1
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compound
formula
methyl
pharmaceutically acceptable
diazaspiro
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HRP20161349TT
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English (en)
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Gerard MP Giblin
David T Macpherson
David R Witty
Steven J STANWAY
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Convergence Pharmaceuticals Limited
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Publication of HRP20161349T1 publication Critical patent/HRP20161349T1/hr

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    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/407Heterocyclic 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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
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    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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Claims (10)

1. Spoj formule (I) koji je 7-metil-2-[4-metil-6-[4-(trifluorometil)-fenil]pirimidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on: [image] ili njegova farmaceutski prikladna sol.
2. Spoj prema zahtjevu 1 ili njegova farmaceutski prikladna sol, gdje spoj formule (I) jest spoj formule (Ia): [image]
3. Spoj formule (I) prema zahtjevu 1 ili zahtjevu 2, koji je (2R,5S)-7-Metil-2-[4-metil-6-[4-(trifluorometil)-fenil]pirimidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on hidroklorid (E1).
4. Spoj formule (I) prema zahtjevu 1 ili zahtjevu 2, koji je (2R,5S)-7-Metil-2-[4-metil-6-[4-(trifluorometil)-fenil]pirimidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on sol sumporne kiseline (E2).
5. Spoj formule (I) prema zahtjevu 1 ili zahtjevu 2, koji je (2R,5S)-7-Metil-2-[4-metil-6-[4-(trifluorometil)-fenil]pirimidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on hidrat soli sumporne kiseline (E3).
6. Farmaceutski pripravak koji sadrži spoj formule (I) prema bilo kojem od zahtjeva 1 do 5 ili njegovu farmaceutski prikladnu sol s jednim ili više farmaceutski prikladnih nosača, punila i/ili pomoćnih tvari.
7. Spoj formule (I) prema bilo kojem od zahtjeva 1 do 5 ili njegova farmaceutski prikladna sol za uporabu u liječenju.
8. Spoj formule (I) prema bilo kojem od zahtjeva 1 do 5 ili njegova farmaceutski prikladna sol za uporabu u liječenju bolesti ili stanja posredovanih modulacijom natrijskih kanala reguliranih naponom.
9. Uporaba spoja formule (I) prema bilo kojem od zahtjeva 1 do 5 ili njegove farmaceutski prikladne soli u proizvodnji lijeka za liječenje bolesti ili stanja posredovanih modulacijom natrijskih kanala reguliranih naponom.
10. Postupak pripreme spoja formule (I) prema zahtjevu 1, koji obuhvaća: (a) formiranje spoja formule (I) provođenjem reakcije zatvaranja prstena spoja formule (II) nakon čega slijedi redukcija dobivenog imina (IIA): [image] (b) uklanjanje zaštite sa zaštićenog derivata spoja formule (I); (c) izborno formiranje farmaceutski prikladne soli spoja formule (I).
HRP20161349TT 2012-05-22 2016-10-17 7-metil-2-[4-metil-6-[4-(trifluorometil)-fenil]piramidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on HRP20161349T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261650325P 2012-05-22 2012-05-22
GB201209015A GB201209015D0 (en) 2012-05-22 2012-05-22 Novel compounds
US201361773710P 2013-03-06 2013-03-06
EP13725438.9A EP2861602B1 (en) 2012-05-22 2013-05-22 7-Methyl-2-[4-methyl-6-[4-(trifluoromethyl)-phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]nonan-6-one
PCT/GB2013/051335 WO2013175205A1 (en) 2012-05-22 2013-05-22 Novel Compounds

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HRP20161349T1 true HRP20161349T1 (hr) 2017-01-27

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HRP20161349TT HRP20161349T1 (hr) 2012-05-22 2016-10-17 7-metil-2-[4-metil-6-[4-(trifluorometil)-fenil]piramidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on
HRP20200580TT HRP20200580T1 (hr) 2012-05-22 2020-04-06 Novi spojevi

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US (7) US9309254B2 (hr)
EP (3) EP2861602B1 (hr)
JP (3) JP2015517562A (hr)
KR (2) KR102161101B1 (hr)
CN (2) CN107344942B (hr)
AU (3) AU2013265001B2 (hr)
BR (1) BR112014029280B1 (hr)
CA (1) CA2873956C (hr)
CY (2) CY1118274T1 (hr)
DK (2) DK3106464T3 (hr)
EA (1) EA025579B1 (hr)
ES (3) ES2602193T3 (hr)
GB (1) GB201209015D0 (hr)
HK (1) HK1209423A1 (hr)
HR (2) HRP20161349T1 (hr)
HU (2) HUE031664T2 (hr)
IL (4) IL235805A (hr)
IN (1) IN2014MN02393A (hr)
LT (2) LT3106464T (hr)
MX (1) MX355303B (hr)
PL (2) PL2861602T3 (hr)
PT (2) PT2861602T (hr)
RS (2) RS60368B1 (hr)
SG (2) SG11201407755UA (hr)
SI (2) SI2861602T1 (hr)
SM (1) SMT201600421B (hr)
WO (2) WO2013175205A1 (hr)
ZA (1) ZA201408253B (hr)

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GB201209015D0 (en) 2012-05-22 2012-07-04 Convergence Pharmaceuticals Novel compounds
GB201209670D0 (en) 2012-05-31 2012-07-18 Convergence Pharmaceuticals Novel compounds

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