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 PDFInfo
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- 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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- Prior art keywords
- compound
- formula
- methyl
- pharmaceutically acceptable
- diazaspiro
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- GCZUIPVRHLYYOG-UHFFFAOYSA-N 7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]nonan-6-one Chemical compound O=C1N(C)CCC11NC(C=2N=C(C=C(C)N=2)C=2C=CC(=CC=2)C(F)(F)F)CC1 GCZUIPVRHLYYOG-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 7
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 4
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 2
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 150000002466 imines Chemical class 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- -1 (2R,5S)-7-Methyl-2-[4-methyl-6-[4-(trifluoromethyl)-phenyl]pyrimidin-2-yl] -1,7-diazaspiro[4.4]nonan-6-one hydrate salt Chemical compound 0.000 claims 1
- GCZUIPVRHLYYOG-BEFAXECRSA-N (2r,5s)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]nonan-6-one Chemical class O=C1N(C)CC[C@]11N[C@@H](C=2N=C(C=C(C)N=2)C=2C=CC(=CC=2)C(F)(F)F)CC1 GCZUIPVRHLYYOG-BEFAXECRSA-N 0.000 claims 1
- PWYKAPTWUKNYOC-WSCVZUBPSA-N (2r,5s)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]nonan-6-one;hydrochloride Chemical compound Cl.O=C1N(C)CC[C@]11N[C@@H](C=2N=C(C=C(C)N=2)C=2C=CC(=CC=2)C(F)(F)F)CC1 PWYKAPTWUKNYOC-WSCVZUBPSA-N 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 238000007363 ring formation reaction Methods 0.000 claims 1
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic 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
- A61K31/407—Heterocyclic 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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- A61K31/435—Heterocyclic 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
- A61K31/438—The 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).
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 |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20161349T1 true HRP20161349T1 (hr) | 2017-01-27 |
Family
ID=46546493
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
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 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20200580TT HRP20200580T1 (hr) | 2012-05-22 | 2020-04-06 | Novi spojevi |
Country Status (28)
Country | Link |
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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) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB201122113D0 (en) | 2011-12-22 | 2012-02-01 | Convergence Pharmaceuticals | Novel compounds |
GB201209015D0 (en) | 2012-05-22 | 2012-07-04 | Convergence Pharmaceuticals | Novel compounds |
CA3074923A1 (en) * | 2017-09-28 | 2019-04-04 | Biogen Inc. | Novel salts |
MX2020003821A (es) | 2017-10-10 | 2023-01-12 | Biogen Inc | Proceso de elaboración de espiroderivados. |
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GB0520578D0 (en) * | 2005-10-10 | 2005-11-16 | Glaxo Group Ltd | Novel compounds |
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JP2009511599A (ja) * | 2005-10-12 | 2009-03-19 | バーテックス ファーマシューティカルズ インコーポレイテッド | 電位依存性イオンチャネルの調整剤としてのビフェニル誘導体 |
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CL2007002953A1 (es) | 2006-10-12 | 2008-02-01 | Xenon Pharmaceuticals Inc | Compuestos derivados de espiro-oxindol; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento del dolor, cancer, prurito, hiperplasia prostatica benigna, hipercolesterolemia. |
CN101522685A (zh) * | 2006-10-12 | 2009-09-02 | 泽农医药公司 | 三环螺-吲哚酮衍生物及其作为治疗剂的用途 |
CN101641099A (zh) | 2007-01-24 | 2010-02-03 | 葛兰素集团有限公司 | 包含3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪或r(-)-2,4-二氨基-5-(2,3-二氯苯基)-6-氟甲基嘧啶和nk1的药物组合物 |
GB0701365D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
GB0701366D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
GB0706630D0 (en) | 2007-04-04 | 2007-05-16 | Glaxo Group Ltd | Novel compounds |
AR077252A1 (es) * | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
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GB201122113D0 (en) | 2011-12-22 | 2012-02-01 | Convergence Pharmaceuticals | Novel compounds |
TWI625046B (zh) * | 2012-03-21 | 2018-05-21 | 內數位專利控股公司 | 在無線網路中行動站贊助方法及裝置 |
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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