JP2012524092A5 - - Google Patents
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- Publication number
- JP2012524092A5 JP2012524092A5 JP2012506123A JP2012506123A JP2012524092A5 JP 2012524092 A5 JP2012524092 A5 JP 2012524092A5 JP 2012506123 A JP2012506123 A JP 2012506123A JP 2012506123 A JP2012506123 A JP 2012506123A JP 2012524092 A5 JP2012524092 A5 JP 2012524092A5
- Authority
- JP
- Japan
- Prior art keywords
- capsule
- pharmaceutical composition
- peg
- crystallization inhibitor
- inhibitor component
- 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
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 21
- 239000002775 capsule Substances 0.000 claims 20
- 239000002202 Polyethylene glycol Substances 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 229920001223 polyethylene glycol Polymers 0.000 claims 18
- 238000002425 crystallisation Methods 0.000 claims 15
- 230000008025 crystallization Effects 0.000 claims 15
- 239000003112 inhibitor Substances 0.000 claims 15
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 14
- AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 9
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 8
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 8
- XEAOPVUAMONVLA-QGZVFWFLSA-N Avagacestat Chemical compound C=1C=C(Cl)C=CC=1S(=O)(=O)N([C@H](CCC(F)(F)F)C(=O)N)CC(C(=C1)F)=CC=C1C=1N=CON=1 XEAOPVUAMONVLA-QGZVFWFLSA-N 0.000 claims 7
- 229920001531 copovidone Polymers 0.000 claims 6
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 4
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 4
- 108010010803 Gelatin Proteins 0.000 claims 2
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 2
- 229930003427 Vitamin E Natural products 0.000 claims 2
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims 2
- 229920000159 gelatin Polymers 0.000 claims 2
- 239000008273 gelatin Substances 0.000 claims 2
- 239000007903 gelatin capsule Substances 0.000 claims 2
- 235000019322 gelatine Nutrition 0.000 claims 2
- 235000011852 gelatine desserts Nutrition 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 claims 2
- 229920002689 polyvinyl acetate Polymers 0.000 claims 2
- 239000011118 polyvinyl acetate Substances 0.000 claims 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 2
- 229940046009 vitamin E Drugs 0.000 claims 2
- 235000019165 vitamin E Nutrition 0.000 claims 2
- 239000011709 vitamin E Substances 0.000 claims 2
- FYLZPFSWVMMCQC-UHFFFAOYSA-N 5,5,5-trifluoropentanamide Chemical compound NC(=O)CCCC(F)(F)F FYLZPFSWVMMCQC-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 229920002534 Polyethylene Glycol 1450 Polymers 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16906109P | 2009-04-14 | 2009-04-14 | |
| US61/169,061 | 2009-04-14 | ||
| PCT/US2010/030862 WO2010120755A1 (en) | 2009-04-14 | 2010-04-13 | Bioavailable capsule compositions of amorphous alpha-(n-sulfonamido)acetamide compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012524092A JP2012524092A (ja) | 2012-10-11 |
| JP2012524092A5 true JP2012524092A5 (enExample) | 2013-03-28 |
Family
ID=42235859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012506123A Pending JP2012524092A (ja) | 2009-04-14 | 2010-04-13 | アモルファスアルファ−（ｎ−スルホンアミド）アセトアミド化合物の生物学的に利用可能なカプセル組成物 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8252821B2 (enExample) |
| EP (1) | EP2419090B1 (enExample) |
| JP (1) | JP2012524092A (enExample) |
| KR (1) | KR20120022766A (enExample) |
| CN (1) | CN102395361A (enExample) |
| AR (1) | AR076305A1 (enExample) |
| AU (1) | AU2010236602A1 (enExample) |
| BR (1) | BRPI1015483A2 (enExample) |
| CA (1) | CA2758847A1 (enExample) |
| EA (1) | EA201101286A1 (enExample) |
| MX (1) | MX2011010514A (enExample) |
| NZ (1) | NZ595335A (enExample) |
| TW (1) | TW201041609A (enExample) |
| WO (1) | WO2010120755A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE430727T1 (de) | 2001-12-20 | 2009-05-15 | Bristol Myers Squibb Co | Alpha-(n-sulfonamid)acetamidderivate als beta- amyloidinhibitoren |
| US8044077B2 (en) | 2009-03-19 | 2011-10-25 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production |
| US7977362B2 (en) | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
| EP2485416A4 (en) | 2009-10-02 | 2017-04-05 | LG Electronics Inc. | Transmission method and device for a downlink reference signal |
| RU2734128C2 (ru) * | 2010-12-16 | 2020-10-13 | Плэтформ Брайтворкс Ту,Лтд | Фармацевтические препараты азолов для парентерального введения и способы их получения и применения для лечения заболеваний, чувствительных к азольным соединениям |
| DK3238709T3 (da) | 2011-04-28 | 2020-09-28 | Platform Brightworks Two Ltd | Forbedrede parenterale formuleringer af lipofile farmaceutiske midler og fremgangsmåder til fremstilling og anvendelse af samme |
| US20130302414A1 (en) * | 2012-05-07 | 2013-11-14 | Bristol-Myers Squibb Company | Solubilized capsule formulation of 1,1-dimethylethyl [(1s)-1-carbamoyl)pyrrolidin-1-yl]carbonyl}-2,2-dimethylpropyl]carbamate |
| TWI795381B (zh) | 2016-12-21 | 2023-03-11 | 比利時商健生藥品公司 | 作為ｍａｌｔ１抑制劑之吡唑衍生物 |
| CA3129356A1 (en) * | 2019-02-22 | 2020-08-27 | Janssen Pharmaceutica Nv | Pharmaceutical formulations |
| KR20210151880A (ko) | 2019-04-11 | 2021-12-14 | 얀센 파마슈티카 엔.브이. | Malt1 억제제로서의 피리딘 고리 함유 유도체 |
| US20230310413A1 (en) * | 2020-08-21 | 2023-10-05 | Janssen Pharmaceutica Nv | Pharmaceutical formulations comprising a malt1 inhibitor and a mixture of polyethylene glycol with a fatty acid |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5274094A (en) | 1990-08-15 | 1993-12-28 | British Bio-Technology Limited | Production of heterobicyclic containing benzene sulfonamides |
| GB9202791D0 (en) | 1992-02-11 | 1992-03-25 | British Bio Technology | Compounds |
| PL326700A1 (en) | 1995-11-17 | 1998-10-26 | Warner Lambert Co | Sulphonamide-based inhibitors of intercellular substance metaloproteinases |
| RU2202540C2 (ru) | 1996-07-22 | 2003-04-20 | Монсанто Компани | Тиолсульфонамидные ингибиторы металлопротеазы |
| CA2264718C (en) * | 1996-09-01 | 2006-05-30 | Pharmos Corporation | Solid coprecipitates for enhanced bioavailability of lipophilic substances |
| JPH11343279A (ja) | 1998-03-16 | 1999-12-14 | Shionogi & Co Ltd | スルホンアミド誘導体およびそれらを含有するＴＮＦ―α産生抑制剤 |
| US6313123B1 (en) | 1999-01-27 | 2001-11-06 | American Cyanamid Company | Acetylenic sulfonamide thiol tace inhibitors |
| NZ512306A (en) | 1999-01-27 | 2003-10-31 | American Cyanamid Co | Acetylenic sulfonamide thiol tace inhibitors |
| EP1159263A1 (en) | 1999-02-26 | 2001-12-05 | Merck & Co., Inc. | Novel sulfonamide compounds and uses thereof |
| JP2005506990A (ja) * | 2001-10-19 | 2005-03-10 | アイソテクニカ インコーポレーテッド | 新規のシクロスポリン類似体のマイクロエマルションプレコンセントレート |
| ATE430727T1 (de) | 2001-12-20 | 2009-05-15 | Bristol Myers Squibb Co | Alpha-(n-sulfonamid)acetamidderivate als beta- amyloidinhibitoren |
| JP2006522126A (ja) | 2003-03-31 | 2006-09-28 | ワイス | βアミロイド生産のフルオロ含有およびトリフルオロアルキル含有複素環スルホンアミド阻害物質およびその誘導体 |
| CA2544350A1 (en) | 2003-10-29 | 2005-05-12 | Elan Pharmaceuticals, Inc. | N-substituted benzene sulfonamides |
| US7163942B2 (en) | 2004-04-01 | 2007-01-16 | Pfizer Inc. | Sulfonamide compounds for the treatment of neurodegenerative disorders |
| AU2005237580B2 (en) * | 2004-04-28 | 2011-06-16 | Procarrier, Inc. | Oral formulation for delivery of poorly absorbed drugs |
| CA2573372A1 (en) | 2004-07-13 | 2006-01-19 | F. Hoffmann-La Roche Ag | Sulfonamide derivatives |
| US7144894B2 (en) | 2004-09-23 | 2006-12-05 | Bristol-Myers Squibb Company | Sulfonamide bicyclic compounds |
| JP2008523146A (ja) * | 2004-12-14 | 2008-07-03 | ワイス | 神経変性障害の処置および予防のための５−ｈｔ６アゴニストの使用 |
| US7687666B2 (en) | 2006-02-17 | 2010-03-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
| BRPI0707742A2 (pt) | 2006-02-17 | 2011-05-10 | Wyeth Corp | processo para preparar um composto |
| CN101400349A (zh) * | 2006-03-01 | 2009-04-01 | 罗斯坎普研究有限责任公司 | 抑制β-淀粉样蛋白产生的化合物 |
| WO2008112249A1 (en) | 2007-03-13 | 2008-09-18 | Trustees Of Columbia University In The City Of New York | Synergistic interaction of notch-1 inhibitors with glucocorticoids |
| WO2009005688A2 (en) | 2007-06-29 | 2009-01-08 | Trustees Of Columbia University In The City Of New York | Activating mutations in notch-1 |
| US8084477B2 (en) * | 2007-10-31 | 2011-12-27 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
| CN102088855A (zh) | 2008-05-08 | 2011-06-08 | 百时美施贵宝公司 | 2-芳基甘氨酰胺衍生物 |
| US8044077B2 (en) | 2009-03-19 | 2011-10-25 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production |
| MX2011009271A (es) | 2009-03-19 | 2011-09-26 | Bristol Myers Squibb Co | Nuevo compuesto de alfa-(n-sulfonamido)acetamida como inhibidor de la produccion del peptido beta amiloide. |
| US7977362B2 (en) | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
| US20110071199A1 (en) | 2009-03-20 | 2011-03-24 | Bristol-Myers Squibb Company | Thiophenyl Sulfonamides for the Treatment of Alzheimer's Disease |
| TW201043269A (en) | 2009-04-14 | 2010-12-16 | Bristol Myers Squibb Co | Bioavailable compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
-
2010
- 2010-04-12 US US12/758,385 patent/US8252821B2/en not_active Expired - Fee Related
- 2010-04-13 AU AU2010236602A patent/AU2010236602A1/en not_active Abandoned
- 2010-04-13 NZ NZ595335A patent/NZ595335A/xx not_active IP Right Cessation
- 2010-04-13 KR KR1020117024036A patent/KR20120022766A/ko not_active Withdrawn
- 2010-04-13 JP JP2012506123A patent/JP2012524092A/ja active Pending
- 2010-04-13 BR BRPI1015483A patent/BRPI1015483A2/pt not_active IP Right Cessation
- 2010-04-13 MX MX2011010514A patent/MX2011010514A/es active IP Right Grant
- 2010-04-13 EP EP10714418A patent/EP2419090B1/en not_active Not-in-force
- 2010-04-13 EA EA201101286A patent/EA201101286A1/ru unknown
- 2010-04-13 CA CA2758847A patent/CA2758847A1/en not_active Abandoned
- 2010-04-13 CN CN2010800164919A patent/CN102395361A/zh active Pending
- 2010-04-13 WO PCT/US2010/030862 patent/WO2010120755A1/en not_active Ceased
- 2010-04-14 AR ARP100101257A patent/AR076305A1/es not_active Application Discontinuation
- 2010-04-14 TW TW099111671A patent/TW201041609A/zh unknown
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