JP2010526102A5 - - Google Patents
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- Publication number
- JP2010526102A5 JP2010526102A5 JP2010506692A JP2010506692A JP2010526102A5 JP 2010526102 A5 JP2010526102 A5 JP 2010526102A5 JP 2010506692 A JP2010506692 A JP 2010506692A JP 2010506692 A JP2010506692 A JP 2010506692A JP 2010526102 A5 JP2010526102 A5 JP 2010526102A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- hydrochloride
- bernakalant
- mammal
- item
- 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.)
- Pending
Links
- 238000000034 method Methods 0.000 claims description 75
- 241000124008 Mammalia Species 0.000 claims description 63
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 61
- 239000000203 mixture Substances 0.000 claims description 56
- 102000002004 Cytochrome P-450 Enzyme System Human genes 0.000 claims description 42
- 108010015742 Cytochrome P-450 Enzyme System Proteins 0.000 claims description 42
- 206010003119 arrhythmia Diseases 0.000 claims description 40
- 230000006793 arrhythmia Effects 0.000 claims description 40
- 150000001875 compounds Chemical class 0.000 claims description 31
- 102000004310 Ion Channels Human genes 0.000 claims description 27
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 26
- 238000013270 controlled release Methods 0.000 claims description 20
- 239000007916 tablet composition Substances 0.000 claims description 17
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 15
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 15
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 15
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 15
- 235000021355 Stearic acid Nutrition 0.000 claims description 14
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 14
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 14
- 239000008117 stearic acid Substances 0.000 claims description 14
- 235000019359 magnesium stearate Nutrition 0.000 claims description 13
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 12
- 229960001021 lactose monohydrate Drugs 0.000 claims description 12
- 230000002503 metabolic effect Effects 0.000 claims description 12
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 11
- 238000009472 formulation Methods 0.000 claims description 10
- 229920000881 Modified starch Polymers 0.000 claims description 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 9
- 239000012453 solvate Substances 0.000 claims description 9
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 239000002552 dosage form Substances 0.000 claims description 7
- 208000003663 ventricular fibrillation Diseases 0.000 claims description 6
- 230000002980 postoperative effect Effects 0.000 claims description 5
- 230000000306 recurrent effect Effects 0.000 claims description 5
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 4
- 206010003130 Arrhythmia supraventricular Diseases 0.000 claims description 4
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 4
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 4
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 4
- 229920002125 Sokalan® Polymers 0.000 claims description 4
- 206010047281 Ventricular arrhythmia Diseases 0.000 claims description 4
- 229960001631 carbomer Drugs 0.000 claims description 4
- 229940082500 cetostearyl alcohol Drugs 0.000 claims description 4
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 4
- 239000011159 matrix material Substances 0.000 claims description 4
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 229920000642 polymer Polymers 0.000 claims description 4
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 claims description 4
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 3
- 239000005913 Maltodextrin Substances 0.000 claims description 3
- 229920002774 Maltodextrin Polymers 0.000 claims description 3
- 239000002253 acid Substances 0.000 claims description 3
- 230000001154 acute effect Effects 0.000 claims description 3
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims description 3
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims description 3
- 208000028867 ischemia Diseases 0.000 claims description 3
- 229940035034 maltodextrin Drugs 0.000 claims description 3
- 208000003311 Cytochrome P-450 Enzyme Inhibitors Diseases 0.000 claims description 2
- 229940122280 Cytochrome P450 inhibitor Drugs 0.000 claims description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- 229910052749 magnesium Inorganic materials 0.000 claims description 2
- 239000011777 magnesium Substances 0.000 claims description 2
- VBHQKCBVWWUUKN-KZNAEPCWSA-N vernakalant Chemical compound C1=C(OC)C(OC)=CC=C1CCO[C@H]1[C@H](N2C[C@H](O)CC2)CCCC1 VBHQKCBVWWUUKN-KZNAEPCWSA-N 0.000 claims 4
- 229960000527 vernakalant Drugs 0.000 claims 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000007935 oral tablet Substances 0.000 description 4
- 229940096978 oral tablet Drugs 0.000 description 4
- 239000003826 tablet Substances 0.000 description 4
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 0 *c1c(*)cc(CCOC(CCCC2)C2N(CC2)CC2O)cc1 Chemical compound *c1c(*)cc(CCOC(CCCC2)C2N(CC2)CC2O)cc1 0.000 description 1
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 1
- DCXXMTOCNZCJGO-UHFFFAOYSA-N Glycerol trioctadecanoate Natural products CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 235000015218 chewing gum Nutrition 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 230000003166 hypermetabolic effect Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91612907P | 2007-05-04 | 2007-05-04 | |
| US6615607P | 2007-08-01 | 2007-08-01 | |
| US3411908P | 2008-03-05 | 2008-03-05 | |
| US3719808P | 2008-03-17 | 2008-03-17 | |
| PCT/US2008/062551 WO2008137778A2 (en) | 2007-05-04 | 2008-05-02 | Controlled release oral formulations of ion channel modulating compounds and related methods for preventing arrhythmia |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010526102A JP2010526102A (ja) | 2010-07-29 |
| JP2010526102A5 true JP2010526102A5 (OSRAM) | 2011-06-23 |
Family
ID=39691347
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010506692A Pending JP2010526102A (ja) | 2007-05-04 | 2008-05-02 | イオンチャネル調節化合物の制御放出経口製剤および不整脈を予防するための関連する方法 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US20080312309A1 (OSRAM) |
| EP (3) | EP2155334A2 (OSRAM) |
| JP (1) | JP2010526102A (OSRAM) |
| KR (1) | KR20100017648A (OSRAM) |
| CN (1) | CN101711174A (OSRAM) |
| AU (1) | AU2008247508B2 (OSRAM) |
| BR (1) | BRPI0810697A2 (OSRAM) |
| CA (1) | CA2686396A1 (OSRAM) |
| CO (1) | CO6241136A2 (OSRAM) |
| CR (1) | CR11117A (OSRAM) |
| EA (1) | EA200971025A1 (OSRAM) |
| EC (1) | ECSP099777A (OSRAM) |
| IL (1) | IL201934A0 (OSRAM) |
| MA (1) | MA31664B1 (OSRAM) |
| MX (1) | MX2009011929A (OSRAM) |
| NI (1) | NI200900196A (OSRAM) |
| NZ (1) | NZ581351A (OSRAM) |
| TN (1) | TN2009000461A1 (OSRAM) |
| WO (1) | WO2008137778A2 (OSRAM) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090041841A1 (en) * | 2003-05-02 | 2009-02-12 | Cardiome Pharma Corp. | Controlled release tablet formulations for the prevention of arrhythmias |
| US7345086B2 (en) * | 2003-05-02 | 2008-03-18 | Cardiome Pharma Corp. | Uses of ion channel modulating compounds |
| US20110198492A1 (en) * | 2010-02-18 | 2011-08-18 | Black David L | Detection and Quantitation of Pain Medications in Oral Fluid Specimens |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2103756T3 (es) * | 1990-06-22 | 1997-10-01 | Hoffmann La Roche | Deteccion de metabolizadores ineficaces de farmacos. |
| US5891696A (en) | 1996-08-02 | 1999-04-06 | Panvera Corporation | Compositions for cytochrome P450 biotransformation reactions |
| JP3176342B2 (ja) * | 1997-08-13 | 2001-06-18 | ファイザー製薬株式会社 | 薬剤代謝の評価方法及び前記方法用の試薬組成物 |
| PT1087934E (pt) * | 1998-04-01 | 2004-07-30 | Cardiome Pharma Corp | Compostos de eter de aminociclo-hexilo e as suas utilizacoes |
| US7507545B2 (en) * | 1999-03-31 | 2009-03-24 | Cardiome Pharma Corp. | Ion channel modulating activity method |
| US7057053B2 (en) * | 2000-10-06 | 2006-06-06 | Cardiome Pharma Corp. | Ion channel modulating compounds and uses thereof |
| US7524879B2 (en) * | 2000-10-06 | 2009-04-28 | Cardiome Pharma Corp. | Ion channel modulating compounds and uses thereof |
| EP1281755A3 (en) * | 2001-07-31 | 2003-06-18 | Pfizer Products Inc. | Variants of the human cyp2d6 gene |
| US7148226B2 (en) * | 2003-02-21 | 2006-12-12 | Agouron Pharmaceuticals, Inc. | Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same |
| US20080063707A1 (en) * | 2003-05-02 | 2008-03-13 | Cardiome Pharma Corp. | Controlled release tablet formulations for the prevention of arrhythmias |
| US7345086B2 (en) * | 2003-05-02 | 2008-03-18 | Cardiome Pharma Corp. | Uses of ion channel modulating compounds |
| CA2524323C (en) * | 2003-05-02 | 2012-05-15 | Cardiome Pharma Corp. | Aminocyclohexyl ether compounds and uses thereof |
| WO2004098525A2 (en) * | 2003-05-02 | 2004-11-18 | Cardiome Pharma Corp. | Uses of ion channel modulating compounds |
| US20090041841A1 (en) * | 2003-05-02 | 2009-02-12 | Cardiome Pharma Corp. | Controlled release tablet formulations for the prevention of arrhythmias |
| WO2005018635A2 (en) * | 2003-08-07 | 2005-03-03 | Cardiome Pharma Corp. | Ion channel modulating activity i |
| US7345087B2 (en) | 2003-10-31 | 2008-03-18 | Cardiome Pharma Corp. | Aminocyclohexyl ether compounds and uses thereof |
| US7705036B2 (en) * | 2004-04-01 | 2010-04-27 | Cardiome Pharma Corp. | Deuterated aminocyclohexyl ether compounds and processes for preparing same |
| US7754897B2 (en) * | 2005-06-15 | 2010-07-13 | Cardiome Pharma Corp. | Synthetic processes for the preparation of aminocyclohexyl ether compounds |
| CA2586918C (en) * | 2004-11-08 | 2021-01-19 | Cardiome Pharma Corp. | Use of ion channel modulating compounds for treating acute atrial fibrillation in a human |
| WO2009018547A1 (en) * | 2007-08-01 | 2009-02-05 | Cardiome Pharma Corp. | Extended release formulations containing an ion-channel-modulating compound for the prevention of arrhythmias |
-
2008
- 2008-05-02 EP EP08755034A patent/EP2155334A2/en not_active Withdrawn
- 2008-05-02 EP EP12001278A patent/EP2468278A1/en not_active Withdrawn
- 2008-05-02 EA EA200971025A patent/EA200971025A1/ru unknown
- 2008-05-02 AU AU2008247508A patent/AU2008247508B2/en not_active Ceased
- 2008-05-02 WO PCT/US2008/062551 patent/WO2008137778A2/en not_active Ceased
- 2008-05-02 JP JP2010506692A patent/JP2010526102A/ja active Pending
- 2008-05-02 BR BRPI0810697A patent/BRPI0810697A2/pt not_active IP Right Cessation
- 2008-05-02 EP EP12001273A patent/EP2462933A1/en not_active Withdrawn
- 2008-05-02 MX MX2009011929A patent/MX2009011929A/es not_active Application Discontinuation
- 2008-05-02 NZ NZ581351A patent/NZ581351A/en not_active IP Right Cessation
- 2008-05-02 KR KR1020097025421A patent/KR20100017648A/ko not_active Withdrawn
- 2008-05-02 CA CA002686396A patent/CA2686396A1/en not_active Abandoned
- 2008-05-02 CN CN200880021022A patent/CN101711174A/zh active Pending
- 2008-05-02 US US12/114,652 patent/US20080312309A1/en not_active Abandoned
-
2009
- 2009-11-04 IL IL201934A patent/IL201934A0/en unknown
- 2009-11-04 NI NI200900196A patent/NI200900196A/es unknown
- 2009-11-04 TN TNP2009000461A patent/TN2009000461A1/fr unknown
- 2009-11-18 CR CR11117A patent/CR11117A/es unknown
- 2009-11-26 MA MA32379A patent/MA31664B1/fr unknown
- 2009-12-02 CO CO09137710A patent/CO6241136A2/es not_active Application Discontinuation
- 2009-12-02 EC EC2009009777A patent/ECSP099777A/es unknown
-
2014
- 2014-06-17 US US14/306,915 patent/US20150099788A1/en not_active Abandoned
-
2015
- 2015-12-02 US US14/957,109 patent/US20160089361A1/en not_active Abandoned
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