JP2014525474A - 光過敏性てんかんの予防または治療における使用のための１ｈ−キナゾリン−２，４−ジオンの使用 - Google Patents
光過敏性てんかんの予防または治療における使用のための１ｈ−キナゾリン−２，４−ジオンの使用 Download PDFInfo
- Publication number
- JP2014525474A JP2014525474A JP2014529647A JP2014529647A JP2014525474A JP 2014525474 A JP2014525474 A JP 2014525474A JP 2014529647 A JP2014529647 A JP 2014529647A JP 2014529647 A JP2014529647 A JP 2014529647A JP 2014525474 A JP2014525474 A JP 2014525474A
- Authority
- JP
- Japan
- Prior art keywords
- dioxo
- dihydro
- quinazolin
- methanesulfonamide
- trifluoromethyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 201000005070 reflex epilepsy Diseases 0.000 title claims abstract description 63
- 201000003040 photosensitive epilepsy Diseases 0.000 title claims abstract description 60
- 238000011282 treatment Methods 0.000 title claims abstract description 60
- 230000002265 prevention Effects 0.000 title claims abstract description 22
- SDQJTWBNWQABLE-UHFFFAOYSA-N 1h-quinazoline-2,4-dione Chemical compound C1=CC=C2C(=O)NC(=O)NC2=C1 SDQJTWBNWQABLE-UHFFFAOYSA-N 0.000 title description 28
- 150000001875 compounds Chemical class 0.000 claims description 134
- 239000001961 anticonvulsive agent Substances 0.000 claims description 45
- 229940002612 prodrug Drugs 0.000 claims description 44
- 239000000651 prodrug Substances 0.000 claims description 44
- 150000003839 salts Chemical class 0.000 claims description 35
- 239000000203 mixture Substances 0.000 claims description 25
- 239000003814 drug Substances 0.000 claims description 18
- 238000000034 method Methods 0.000 claims description 15
- -1 2-isopropyl-2H-pyrazol-3-yl Chemical group 0.000 claims description 14
- 238000009472 formulation Methods 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 125000001424 substituent group Chemical group 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 239000001257 hydrogen Substances 0.000 claims description 5
- HBYOBTHYFIRAOW-UHFFFAOYSA-N n-[2,4-dioxo-6-(oxolan-2-yl)-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound C1=C2C(=O)N(NS(=O)(=O)C)C(=O)NC2=CC(C(F)(F)F)=C1C1CCCO1 HBYOBTHYFIRAOW-UHFFFAOYSA-N 0.000 claims description 4
- LSKJPQVORRUXOV-UHFFFAOYSA-N n-[6-(1-ethoxyethyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(C)OCC)=C2 LSKJPQVORRUXOV-UHFFFAOYSA-N 0.000 claims description 4
- LCFHHNPWFZWYFJ-UHFFFAOYSA-N n-[6-(1-methoxyethyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(C)OC)=C2 LCFHHNPWFZWYFJ-UHFFFAOYSA-N 0.000 claims description 4
- YMFABCOTRXIHFU-UHFFFAOYSA-N n-[7-(difluoromethyl)-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CN1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(F)F YMFABCOTRXIHFU-UHFFFAOYSA-N 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- DSELHYJGEKXXRP-UHFFFAOYSA-N n-[2,4-dioxo-6-(1-propan-2-yloxyethyl)-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(C)OC(C)C)=C2 DSELHYJGEKXXRP-UHFFFAOYSA-N 0.000 claims description 3
- WUTUFPNWYUNDFI-UHFFFAOYSA-N n-[2,4-dioxo-6-(2-propan-2-ylpyrazol-3-yl)-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CC(C)N1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(F)(F)F WUTUFPNWYUNDFI-UHFFFAOYSA-N 0.000 claims description 3
- MIGNZRPDULLXTQ-UHFFFAOYSA-N n-[6-(1-hydroxypropyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(O)CC)=C2 MIGNZRPDULLXTQ-UHFFFAOYSA-N 0.000 claims description 3
- ZWDLCWUDNRHDGU-UHFFFAOYSA-N n-[7-(1,1-difluoroethyl)-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CN1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(C)(F)F ZWDLCWUDNRHDGU-UHFFFAOYSA-N 0.000 claims description 3
- JVPVBPHLIBMROY-UHFFFAOYSA-N n-[7-(difluoromethyl)-2,4-dioxo-6-(2-propan-2-ylpyrazol-3-yl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CC(C)N1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(F)F JVPVBPHLIBMROY-UHFFFAOYSA-N 0.000 claims description 3
- HSGNDJYOXXCRGB-UHFFFAOYSA-N n-[7-(fluoromethyl)-2,4-dioxo-6-(2-propan-2-ylpyrazol-3-yl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CC(C)N1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1CF HSGNDJYOXXCRGB-UHFFFAOYSA-N 0.000 claims description 3
- 230000002829 reductive effect Effects 0.000 claims description 3
- NXSCFPKPPNHCCN-UHFFFAOYSA-N n-[2,4-dioxo-6-(1-propoxyethyl)-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(C)OCCC)=C2 NXSCFPKPPNHCCN-UHFFFAOYSA-N 0.000 claims description 2
- NZWSWGBRWWTWJP-UHFFFAOYSA-N n-[2,4-dioxo-6-(1-propoxypropyl)-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(CC)OCCC)=C2 NZWSWGBRWWTWJP-UHFFFAOYSA-N 0.000 claims description 2
- KBYZURXFFPMEEI-UHFFFAOYSA-N n-[2,4-dioxo-6-(oxolan-3-yl)-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound C1=C2C(=O)N(NS(=O)(=O)C)C(=O)NC2=CC(C(F)(F)F)=C1C1CCOC1 KBYZURXFFPMEEI-UHFFFAOYSA-N 0.000 claims description 2
- OFJHQRJECRDHRW-UHFFFAOYSA-N n-[6-(1-butoxyethyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(C)OCCCC)=C2 OFJHQRJECRDHRW-UHFFFAOYSA-N 0.000 claims description 2
- RVFCUKBZUNLKHH-UHFFFAOYSA-N n-[6-(1-cyclopentyloxyethyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound C=1C(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C(C(F)(F)F)C=1C(C)OC1CCCC1 RVFCUKBZUNLKHH-UHFFFAOYSA-N 0.000 claims description 2
- MMTLKGVPYZLJTG-UHFFFAOYSA-N n-[6-(1-ethoxypropyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(CC)OCC)=C2 MMTLKGVPYZLJTG-UHFFFAOYSA-N 0.000 claims description 2
- UQTXIYMVGFQNKE-UHFFFAOYSA-N n-[6-(1-hydroxybutyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(O)CCC)=C2 UQTXIYMVGFQNKE-UHFFFAOYSA-N 0.000 claims description 2
- IOMNVPHVACWAQD-UHFFFAOYSA-N n-[6-(1-hydroxyethyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(O)C)=C2 IOMNVPHVACWAQD-UHFFFAOYSA-N 0.000 claims description 2
- QDNJESWDNWORKP-UHFFFAOYSA-N n-[6-(1-methoxybutyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(OC)CCC)=C2 QDNJESWDNWORKP-UHFFFAOYSA-N 0.000 claims description 2
- DKMLPACXXYKYSU-UHFFFAOYSA-N n-[6-(2-hydroxypyrazol-3-yl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound C1=C2C(=O)N(NS(=O)(=O)C)C(=O)NC2=CC(C(F)(F)F)=C1C1=CC=NN1O DKMLPACXXYKYSU-UHFFFAOYSA-N 0.000 claims description 2
- QLUSFZJXGQYNMK-UHFFFAOYSA-N n-[6-(2-methylpyrazol-3-yl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CN1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(F)(F)F QLUSFZJXGQYNMK-UHFFFAOYSA-N 0.000 claims description 2
- CZVNRIDLEZRQFH-UHFFFAOYSA-N n-[6-(3-hydroxypropyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound FC(F)(F)C1=C(CCCO)C=C2C(=O)N(NS(=O)(=O)C)C(=O)NC2=C1 CZVNRIDLEZRQFH-UHFFFAOYSA-N 0.000 claims description 2
- NMIQVXYXYPUJHC-UHFFFAOYSA-N n-[6-(oxan-2-yl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound C1=C2C(=O)N(NS(=O)(=O)C)C(=O)NC2=CC(C(F)(F)F)=C1C1CCCCO1 NMIQVXYXYPUJHC-UHFFFAOYSA-N 0.000 claims description 2
- USURBQLTQADVAD-UHFFFAOYSA-N n-[6-[1-(2-methylpropoxy)ethyl]-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(C)OCC(C)C)=C2 USURBQLTQADVAD-UHFFFAOYSA-N 0.000 claims description 2
- AZAOVWWNNFAHAG-UHFFFAOYSA-N n-[6-[2-(2-methoxyethyl)pyrazol-3-yl]-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound COCCN1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(F)(F)F AZAOVWWNNFAHAG-UHFFFAOYSA-N 0.000 claims description 2
- JVZQDMCKWPOOIY-UHFFFAOYSA-N n-[6-[2-(2-methoxyethyl)pyrazol-3-yl]-2,4-dioxo-7-propan-2-yl-1h-quinazolin-3-yl]methanesulfonamide Chemical compound COCCN1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(C)C JVZQDMCKWPOOIY-UHFFFAOYSA-N 0.000 claims description 2
- OPYMZVLVOCASOX-UHFFFAOYSA-N n-[7-(1,1-difluoroethyl)-2,4-dioxo-6-(2-propan-2-ylpyrazol-3-yl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CC(C)N1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(C)(F)F OPYMZVLVOCASOX-UHFFFAOYSA-N 0.000 claims description 2
- FDHRJKWFUHLAFO-UHFFFAOYSA-N n-[7-(1-fluoroethyl)-2,4-dioxo-6-(2-propan-2-ylpyrazol-3-yl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CC(C)N1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1C(C)F FDHRJKWFUHLAFO-UHFFFAOYSA-N 0.000 claims description 2
- MMKXICJSNZKSDT-UHFFFAOYSA-N n-[7-(1-fluoroethyl)-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CC(F)C1=CC=2NC(=O)N(NS(C)(=O)=O)C(=O)C=2C=C1C1=CC=NN1C MMKXICJSNZKSDT-UHFFFAOYSA-N 0.000 claims description 2
- ISBCBAUWMPBZMW-UHFFFAOYSA-N n-[7-(difluoromethyl)-6-(1-ethoxyethyl)-2,4-dioxo-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)F)C(C(C)OCC)=C2 ISBCBAUWMPBZMW-UHFFFAOYSA-N 0.000 claims description 2
- XWWOWSFUSLLOTP-UHFFFAOYSA-N n-[7-(fluoromethyl)-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CN1N=CC=C1C1=CC(C(N(NS(C)(=O)=O)C(=O)N2)=O)=C2C=C1CF XWWOWSFUSLLOTP-UHFFFAOYSA-N 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 claims 3
- MCECSFFXUPEPDB-UHFFFAOYSA-N n-[6-(2-methylpyrazol-3-yl)-2,4-dioxo-7-propan-2-yl-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CC(C)C1=CC=2NC(=O)N(NS(C)(=O)=O)C(=O)C=2C=C1C1=CC=NN1C MCECSFFXUPEPDB-UHFFFAOYSA-N 0.000 claims 3
- OEKIBARTEOJEKR-UHFFFAOYSA-N n-[7-ethyl-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CCC1=CC=2NC(=O)N(NS(C)(=O)=O)C(=O)C=2C=C1C1=CC=NN1C OEKIBARTEOJEKR-UHFFFAOYSA-N 0.000 claims 3
- FCGZKGLYOHESAU-UHFFFAOYSA-N n-[2,4-dioxo-6-(1-propan-2-yloxypropyl)-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(OC(C)C)CC)=C2 FCGZKGLYOHESAU-UHFFFAOYSA-N 0.000 claims 1
- MWEPLWMITBXDHS-UHFFFAOYSA-N n-[6-(1-hydroxy-2-methylpropyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(O)C(C)C)=C2 MWEPLWMITBXDHS-UHFFFAOYSA-N 0.000 claims 1
- QDIISXGZVBGRKE-UHFFFAOYSA-N n-[6-(1-hydroxy-3-methoxypropyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(O)CCOC)=C2 QDIISXGZVBGRKE-UHFFFAOYSA-N 0.000 claims 1
- QNOGGNMZYXNFMK-UHFFFAOYSA-N n-[6-(1-methoxy-2-methylpropyl)-2,4-dioxo-7-(trifluoromethyl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound N1C(=O)N(NS(C)(=O)=O)C(=O)C2=C1C=C(C(F)(F)F)C(C(C(C)C)OC)=C2 QNOGGNMZYXNFMK-UHFFFAOYSA-N 0.000 claims 1
- KEEFXFPTFSCWQH-UHFFFAOYSA-N n-[7-ethyl-2,4-dioxo-6-(2-propan-2-ylpyrazol-3-yl)-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CCC1=CC=2NC(=O)N(NS(C)(=O)=O)C(=O)C=2C=C1C1=CC=NN1C(C)C KEEFXFPTFSCWQH-UHFFFAOYSA-N 0.000 claims 1
- KPWVCITWUDVCGS-UHFFFAOYSA-N n-[7-ethyl-6-(2-ethylpyrazol-3-yl)-2,4-dioxo-1h-quinazolin-3-yl]methanesulfonamide Chemical compound CCC1=CC=2NC(=O)N(NS(C)(=O)=O)C(=O)C=2C=C1C1=CC=NN1CC KPWVCITWUDVCGS-UHFFFAOYSA-N 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 230000002860 competitive effect Effects 0.000 abstract description 7
- 229940098747 AMPA receptor antagonist Drugs 0.000 abstract description 3
- 239000000775 AMPA receptor antagonist Substances 0.000 abstract description 3
- 206010010904 Convulsion Diseases 0.000 description 33
- 230000000694 effects Effects 0.000 description 29
- 230000004044 response Effects 0.000 description 24
- 206010015037 epilepsy Diseases 0.000 description 18
- 238000006722 reduction reaction Methods 0.000 description 17
- 229940079593 drug Drugs 0.000 description 16
- 230000009467 reduction Effects 0.000 description 16
- 230000001629 suppression Effects 0.000 description 14
- 238000012360 testing method Methods 0.000 description 13
- 206010034972 Photosensitivity reaction Diseases 0.000 description 10
- 230000036211 photosensitivity Effects 0.000 description 10
- 241000282414 Homo sapiens Species 0.000 description 9
- AEQFSUDEHCCHBT-UHFFFAOYSA-M sodium valproate Chemical compound [Na+].CCCC(C([O-])=O)CCC AEQFSUDEHCCHBT-UHFFFAOYSA-M 0.000 description 9
- 229940102566 valproate Drugs 0.000 description 9
- 150000001408 amides Chemical class 0.000 description 8
- 238000004458 analytical method Methods 0.000 description 8
- 230000008859 change Effects 0.000 description 8
- 229960001848 lamotrigine Drugs 0.000 description 8
- PYZRQGJRPPTADH-UHFFFAOYSA-N lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 description 8
- KJADKKWYZYXHBB-XBWDGYHZSA-N Topiramic acid Chemical compound C1O[C@@]2(COS(N)(=O)=O)OC(C)(C)O[C@H]2[C@@H]2OC(C)(C)O[C@@H]21 KJADKKWYZYXHBB-XBWDGYHZSA-N 0.000 description 7
- 239000004480 active ingredient Substances 0.000 description 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 7
- 238000001727 in vivo Methods 0.000 description 7
- 229960004002 levetiracetam Drugs 0.000 description 7
- HPHUVLMMVZITSG-ZCFIWIBFSA-N levetiracetam Chemical compound CC[C@H](C(N)=O)N1CCCC1=O HPHUVLMMVZITSG-ZCFIWIBFSA-N 0.000 description 7
- 230000000638 stimulation Effects 0.000 description 7
- 229960004394 topiramate Drugs 0.000 description 7
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 description 6
- 230000009471 action Effects 0.000 description 6
- 239000005557 antagonist Substances 0.000 description 6
- 230000005764 inhibitory process Effects 0.000 description 6
- 102000005962 receptors Human genes 0.000 description 6
- 108020003175 receptors Proteins 0.000 description 6
- 239000002904 solvent Substances 0.000 description 6
- 230000008901 benefit Effects 0.000 description 5
- 230000008499 blood brain barrier function Effects 0.000 description 5
- 210000001218 blood-brain barrier Anatomy 0.000 description 5
- 239000002552 dosage form Substances 0.000 description 5
- 230000006698 induction Effects 0.000 description 5
- 230000003285 pharmacodynamic effect Effects 0.000 description 5
- 230000000007 visual effect Effects 0.000 description 5
- 229960002911 zonisamide Drugs 0.000 description 5
- UBQNRHZMVUUOMG-UHFFFAOYSA-N zonisamide Chemical compound C1=CC=C2C(CS(=O)(=O)N)=NOC2=C1 UBQNRHZMVUUOMG-UHFFFAOYSA-N 0.000 description 5
- 102000003678 AMPA Receptors Human genes 0.000 description 4
- 108090000078 AMPA Receptors Proteins 0.000 description 4
- 206010020751 Hypersensitivity Diseases 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- 241000699670 Mus sp. Species 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- CXOXHMZGEKVPMT-UHFFFAOYSA-N clobazam Chemical compound O=C1CC(=O)N(C)C2=CC=C(Cl)C=C2N1C1=CC=CC=C1 CXOXHMZGEKVPMT-UHFFFAOYSA-N 0.000 description 4
- 229960001403 clobazam Drugs 0.000 description 4
- 238000003745 diagnosis Methods 0.000 description 4
- 230000036470 plasma concentration Effects 0.000 description 4
- 238000012216 screening Methods 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- 241000282412 Homo Species 0.000 description 3
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 238000011260 co-administration Methods 0.000 description 3
- 238000013461 design Methods 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 229930195712 glutamate Natural products 0.000 description 3
- 230000003993 interaction Effects 0.000 description 3
- 238000007254 oxidation reaction Methods 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 239000000829 suppository Substances 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 230000036962 time dependent Effects 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 208000012902 Nervous system disease Diseases 0.000 description 2
- 208000025966 Neurological disease Diseases 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 208000026935 allergic disease Diseases 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- 230000004071 biological effect Effects 0.000 description 2
- 230000004397 blinking Effects 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 235000021152 breakfast Nutrition 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 150000001733 carboxylic acid esters Chemical class 0.000 description 2
- 238000011284 combination treatment Methods 0.000 description 2
- 238000002425 crystallisation Methods 0.000 description 2
- 230000008025 crystallization Effects 0.000 description 2
- 125000000000 cycloalkoxy group Chemical group 0.000 description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
- 230000008034 disappearance Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 231100000673 dose–response relationship Toxicity 0.000 description 2
- 230000035622 drinking Effects 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 238000002651 drug therapy Methods 0.000 description 2
- 230000001787 epileptiform Effects 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 125000000524 functional group Chemical group 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 150000004677 hydrates Chemical class 0.000 description 2
- 230000007062 hydrolysis Effects 0.000 description 2
- 238000006460 hydrolysis reaction Methods 0.000 description 2
- 230000009610 hypersensitivity Effects 0.000 description 2
- 150000002466 imines Chemical class 0.000 description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
- 238000012423 maintenance Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
- 230000003287 optical effect Effects 0.000 description 2
- 230000003647 oxidation Effects 0.000 description 2
- 239000000902 placebo Substances 0.000 description 2
- 229940068196 placebo Drugs 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- 230000002441 reversible effect Effects 0.000 description 2
- 230000002269 spontaneous effect Effects 0.000 description 2
- 210000000225 synapse Anatomy 0.000 description 2
- 230000005062 synaptic transmission Effects 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 208000024255 Audiogenic seizures Diseases 0.000 description 1
- 206010009346 Clonus Diseases 0.000 description 1
- 208000032170 Congenital Abnormalities Diseases 0.000 description 1
- 206010010356 Congenital anomaly Diseases 0.000 description 1
- 241000557626 Corvus corax Species 0.000 description 1
- 241001050985 Disco Species 0.000 description 1
- 230000010777 Disulfide Reduction Effects 0.000 description 1
- 208000030453 Drug-Related Side Effects and Adverse reaction Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 208000024658 Epilepsy syndrome Diseases 0.000 description 1
- 208000002877 Epileptic Syndromes Diseases 0.000 description 1
- 208000003078 Generalized Epilepsy Diseases 0.000 description 1
- 208000034308 Grand mal convulsion Diseases 0.000 description 1
- 102000000079 Kainic Acid Receptors Human genes 0.000 description 1
- 108010069902 Kainic Acid Receptors Proteins 0.000 description 1
- 206010067125 Liver injury Diseases 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 description 1
- 238000011795 OF1 mouse Methods 0.000 description 1
- WYNCHZVNFNFDNH-UHFFFAOYSA-N Oxazolidine Chemical compound C1COCN1 WYNCHZVNFNFDNH-UHFFFAOYSA-N 0.000 description 1
- 206010061334 Partial seizures Diseases 0.000 description 1
- 206010071141 Rasmussen encephalitis Diseases 0.000 description 1
- 208000004160 Rasmussen subacute encephalitis Diseases 0.000 description 1
- 206010039897 Sedation Diseases 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 description 1
- 125000002777 acetyl group Chemical class [H]C([H])([H])C(*)=O 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 210000001056 activated astrocyte Anatomy 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 150000001299 aldehydes Chemical class 0.000 description 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 description 1
- 125000005907 alkyl ester group Chemical group 0.000 description 1
- 208000030961 allergic reaction Diseases 0.000 description 1
- 230000003281 allosteric effect Effects 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 229940049706 benzodiazepine Drugs 0.000 description 1
- 150000001557 benzodiazepines Chemical class 0.000 description 1
- 230000007698 birth defect Effects 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 description 1
- 229960000623 carbamazepine Drugs 0.000 description 1
- 150000004657 carbamic acid derivatives Chemical class 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 238000004891 communication Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
- 230000002254 contraceptive effect Effects 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000036461 convulsion Effects 0.000 description 1
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 238000006900 dealkylation reaction Methods 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 238000009510 drug design Methods 0.000 description 1
- 230000008406 drug-drug interaction Effects 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 238000000537 electroencephalography Methods 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 206010014599 encephalitis Diseases 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 230000001037 epileptic effect Effects 0.000 description 1
- 208000028329 epileptic seizure Diseases 0.000 description 1
- 238000006735 epoxidation reaction Methods 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000000763 evoking effect Effects 0.000 description 1
- 230000004399 eye closure Effects 0.000 description 1
- 201000003373 familial cold autoinflammatory syndrome 3 Diseases 0.000 description 1
- 125000003709 fluoroalkyl group Chemical group 0.000 description 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 229960002870 gabapentin Drugs 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 231100000234 hepatic damage Toxicity 0.000 description 1
- 201000001993 idiopathic generalized epilepsy Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 230000002427 irreversible effect Effects 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000008818 liver damage Effects 0.000 description 1
- 210000003141 lower extremity Anatomy 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 201000001119 neuropathy Diseases 0.000 description 1
- 230000007823 neuropathy Effects 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 238000007833 oxidative deamination reaction Methods 0.000 description 1
- 150000002923 oximes Chemical class 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000032696 parturition Effects 0.000 description 1
- 239000013610 patient sample Substances 0.000 description 1
- 230000008447 perception Effects 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
- 210000001428 peripheral nervous system Anatomy 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 239000008024 pharmaceutical diluent Substances 0.000 description 1
- 239000002831 pharmacologic agent Substances 0.000 description 1
- 150000003014 phosphoric acid esters Chemical class 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 230000001242 postsynaptic effect Effects 0.000 description 1
- 229960001233 pregabalin Drugs 0.000 description 1
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000002203 pretreatment Methods 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 238000012797 qualification Methods 0.000 description 1
- 108091006082 receptor inhibitors Proteins 0.000 description 1
- 238000005932 reductive alkylation reaction Methods 0.000 description 1
- 230000011514 reflex Effects 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 230000004043 responsiveness Effects 0.000 description 1
- 230000000630 rising effect Effects 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 150000003462 sulfoxides Chemical class 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
- C07D239/96—Two oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2011/050687 WO2013036224A1 (en) | 2011-09-07 | 2011-09-07 | Use of 1h-quinazoline- 2, 4 -diones for use in the prevention or treatment photosensitive epilepsy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2014525474A true JP2014525474A (ja) | 2014-09-29 |
Family
ID=44652020
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014529647A Withdrawn JP2014525474A (ja) | 2011-09-07 | 2011-09-07 | 光過敏性てんかんの予防または治療における使用のための１ｈ−キナゾリン−２，４−ジオンの使用 |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP2753331A1 (https=) |
| JP (1) | JP2014525474A (https=) |
| KR (1) | KR20140071405A (https=) |
| CN (1) | CN103889427A (https=) |
| AU (1) | AU2011376333A1 (https=) |
| BR (1) | BR112014005210A2 (https=) |
| CA (1) | CA2846503A1 (https=) |
| IN (1) | IN2014DN01791A (https=) |
| MX (1) | MX2014002693A (https=) |
| WO (1) | WO2013036224A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201609719A (zh) | 2014-05-28 | 2016-03-16 | 美國禮來大藥廠 | 作為ＴＡＲＰ－γ８依賴性ＡＭＰＡ受體拮抗劑之６－經取代－３Ｈ－１，３－苯并噻唑－２－酮化合物 |
| MA43532A (fr) | 2015-12-30 | 2018-11-07 | Adamas Pharmaceuticals Inc | Méthodes et compositions destinés au traitement de troubles liés à des crises épileptiques |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0128996D0 (en) | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
| SE0201943D0 (sv) | 2002-06-20 | 2002-06-20 | Astrazeneca Ab | New use |
| CA2549965A1 (en) | 2003-10-31 | 2005-05-19 | Astrazeneca Ab | Alkynes iii |
| CA2549967A1 (en) | 2003-10-31 | 2005-05-19 | Astrazeneca Ab | Alkynes i |
| EP1677790A1 (en) | 2003-10-31 | 2006-07-12 | AstraZeneca AB | Alkynes ii |
| EP1715867A4 (en) | 2004-02-12 | 2009-04-15 | Merck & Co Inc | BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5 |
| GB0507298D0 (en) | 2005-04-11 | 2005-05-18 | Novartis Ag | Organic compounds |
| GB0508319D0 (en) | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
| AU2006329007A1 (en) | 2005-12-20 | 2007-06-28 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutamate receptors |
| US10786464B2 (en) * | 2009-11-03 | 2020-09-29 | Lupin Limited | Modified release formulation of lacosamide |
-
2011
- 2011-09-07 CN CN201180073318.7A patent/CN103889427A/zh active Pending
- 2011-09-07 IN IN1791DEN2014 patent/IN2014DN01791A/en unknown
- 2011-09-07 JP JP2014529647A patent/JP2014525474A/ja not_active Withdrawn
- 2011-09-07 WO PCT/US2011/050687 patent/WO2013036224A1/en not_active Ceased
- 2011-09-07 EP EP11757513.4A patent/EP2753331A1/en not_active Withdrawn
- 2011-09-07 KR KR1020147008752A patent/KR20140071405A/ko not_active Withdrawn
- 2011-09-07 MX MX2014002693A patent/MX2014002693A/es not_active Application Discontinuation
- 2011-09-07 BR BR112014005210A patent/BR112014005210A2/pt not_active IP Right Cessation
- 2011-09-07 CA CA2846503A patent/CA2846503A1/en not_active Abandoned
- 2011-09-07 AU AU2011376333A patent/AU2011376333A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2753331A1 (en) | 2014-07-16 |
| MX2014002693A (es) | 2014-06-04 |
| KR20140071405A (ko) | 2014-06-11 |
| AU2011376333A1 (en) | 2014-03-13 |
| WO2013036224A1 (en) | 2013-03-14 |
| CA2846503A1 (en) | 2013-03-14 |
| BR112014005210A2 (pt) | 2017-03-21 |
| IN2014DN01791A (https=) | 2015-05-15 |
| CN103889427A (zh) | 2014-06-25 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10111889B2 (en) | Uses of ganaxolone | |
| DE602004007225T2 (de) | Methode zur behandlung von erkrankungen der unteren harnwege | |
| US20140163050A1 (en) | Use of 1H-quinazoline-2,4-diones | |
| JP2003510273A (ja) | 神経障害性の疼痛の治療のためのレチガビンの使用 | |
| EA017443B1 (ru) | Производные тетрагидрохинолина для лечения посттравматических стрессовых расстройств | |
| JP6137833B2 (ja) | 脱髄性および他の神経系疾患を患っている患者における神経認知的および／または神経精神医学的障害を改善するための４−アミノピリジンの使用 | |
| ES2936833T3 (es) | Tasimelteón para tratar síndrome de Smith-Magenis | |
| US20040266737A1 (en) | Compounds of use in the treatment of epilepsy, seizure, and electroconvulsive disorders | |
| JP2003520193A (ja) | Ｒ（−）−ケトプロフェンを用いる神経障害性疼痛、耳鳴り、およびその他の障害治療のための方法および組成物 | |
| EP3258930A1 (en) | Oxabicycloheptanes and oxabicycloheptenes for the treatment of depressive and stress disorders | |
| US20220273662A1 (en) | Use of sildenafil and rock inhibitors for treating stroke or sequelae following stroke | |
| JP2014525474A (ja) | 光過敏性てんかんの予防または治療における使用のための１ｈ−キナゾリン−２，４−ジオンの使用 | |
| EA023728B1 (ru) | Терапевтическое средство от тревожных расстройств | |
| EA038087B1 (ru) | Трехкомпонентная фармацевтическая комбинация чистых антагонистов 5-ht6 рецепторов, ингибиторов ацетилхолинэстеразы и антагониста nmda рецептора, применение указанной комбинации и содержащей ее фармацевтической композиции в лечении когнитивных расстройств и способ такого лечения | |
| KR20180101322A (ko) | 뇌졸중으로부터의 회복을 위한 방법 및 조성물 | |
| JP2019516699A (ja) | 純粋な５−ｈｔ６受容体アンタゴニストとアセチルコリンエステラーゼ阻害剤の組合せ | |
| CA2814828C (en) | Method of treatment for mental disorders | |
| JP6606298B2 (ja) | 純粋な５−ｈｔ６受容体アンタゴニストのｎｍｄａ受容体アンタゴニストとの組合せ | |
| Herrling et al. | D-CPPene (SDZ EAA-494)—a competitive NMDA antagonist: pharmacology and results in humans | |
| KR20200132858A (ko) | 간질 치료제 | |
| KR102336701B1 (ko) | 실데나필 및 rock 저해제를 포함하는 뇌졸중으로 인한 인지 기능 저하의 치료용 약학적 조성물 | |
| JP5830983B2 (ja) | 抗癌剤の副作用軽減剤 | |
| CA3176643A1 (en) | Use of dopamine d3 partial agonists for treating central nervous system disorders | |
| BR112021004938A2 (pt) | métodos e composições para tratamento de danos associados com o envelhecimento usando inibidores de ccr3 | |
| JP2012533605A (ja) | 神経セロイドリポフスチン症の治療における使用のための１ｈ−キナゾリン−２，４−ジオン |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A300 | Application deemed to be withdrawn because no request for examination was validly filed |
Free format text: JAPANESE INTERMEDIATE CODE: A300 Effective date: 20141202 |