JP2012524090A5 - - Google Patents
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- Publication number
- JP2012524090A5 JP2012524090A5 JP2012506089A JP2012506089A JP2012524090A5 JP 2012524090 A5 JP2012524090 A5 JP 2012524090A5 JP 2012506089 A JP2012506089 A JP 2012506089A JP 2012506089 A JP2012506089 A JP 2012506089A JP 2012524090 A5 JP2012524090 A5 JP 2012524090A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- trifluoropentanamide
- oxadiazol
- chlorophenyl
- sulfonyl
- 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
- 239000000203 mixture Substances 0.000 claims 34
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 11
- FYUWIEKAVLOHSE-UHFFFAOYSA-N ethenyl acetate;1-ethenylpyrrolidin-2-one Chemical compound CC(=O)OC=C.C=CN1CCCC1=O FYUWIEKAVLOHSE-UHFFFAOYSA-N 0.000 claims 6
- FYLZPFSWVMMCQC-UHFFFAOYSA-N 5,5,5-trifluoropentanamide Chemical compound NC(=O)CCCC(F)(F)F FYLZPFSWVMMCQC-UHFFFAOYSA-N 0.000 claims 5
- 239000007962 solid dispersion Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 2
- 238000001694 spray drying Methods 0.000 claims 2
- 238000009474 hot melt extrusion Methods 0.000 claims 1
Claims (23)
- （２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミドおよびＰＶＰ−ＶＡを含むアモルファス固形分散組成物。
- 約１０−５０ｗ／ｖ％の（２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミド、および約９０−５０ｗ／ｖ％のＰＶＰ−ＶＡを含む請求項１に記載の組成物。
- 約２０−４０ｗ／ｖ％の（２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミド、および約８０−６０ｗ／ｖ％のＰＶＰ−ＶＡを含む請求項２に記載の組成物。
- 約２５ｗ／ｖ％の（２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミド、および約７５％のＰＶＰ−ＶＡを含む請求項３に記載の組成物。
- 少なくとも約３ヶ月間物理化学的に安定な組成物である、請求項１に記載の組成物。
- 少なくとも約６ヶ月間物理化学的に安定な組成物である、請求項５に記載の組成物。
- ホットメルト押出成形または噴霧乾燥により製造される組成物である、請求項１に記載の組成物。
- 錠剤化された組成物である、請求項７に記載の組成物。
- 経口投与可能な組成物である、請求項８に記載の組成物。
- 経口投与可能な組成物である、請求項１に記載の組成物。
- （２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミドおよびＨＰＭＣ−ＡＳを含むアモルファス固形分散組成物。
- 約１０−５０のｗ／ｖ％（２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミド、および約９０−５０ｗ／ｖ％のＨＰＭＣ−ＡＳを含む請求項１１に記載の組成物。
- 約２０−４０ｗ／ｖ％の（２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミド、および約８０−６０ｗ／ｖ％のＨＰＭＣ−ＡＳを含む請求項１２に記載の組成物。
- 約２５ｗ／ｖ％の（２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミド、および約７５％のＨＰＭＣ−ＡＳを含む請求項１３の組成物。
- 少なくとも約３ヶ月間物理化学的に安定である、請求項１１に記載の組成物。
- 少なくとも約６ヶ月間物理化学的に安定である、請求項１５に記載の組成物。
- 噴霧乾燥により製造された組成物である、請求項１１に記載の組成物。
- 打錠された組成物である、請求項１７に記載の組成物。
- 経口投与可能な組成物である、請求項１８に記載の組成物。
- 経口投与可能な組成物である、請求項１１に記載の組成物。
- （２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミド、ならびにＰＶＰ−ＶＡおよびＨＰＭＣ−ＡＳからなる群から選択される１つの成分を含む医薬錠剤。
- （２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミドをＰＶＰ−ＶＡと共にホットメルト押出成形することを特徴とする、アモルファス固形分散組成物の製造方法。
- （２Ｒ）−２−［［（４−クロロフェニル）スルホニル］［［２−フルオロ−４−(１，２，４−オキサジアゾール−３−イル）フェニル］メチル］アミノ］−５，５，５−トリフルオロペンタンアミドをＨＰＭＣ−ＡＳと共に噴霧乾燥することを特徴とする、アモルファス固形分散組成物の製造方法。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16906609P | 2009-04-14 | 2009-04-14 | |
| US61/169,066 | 2009-04-14 | ||
| PCT/US2010/030679 WO2010120662A2 (en) | 2009-04-14 | 2010-04-12 | Bioavailable compositions of amorphous alpha-(n-sulfonamido)acetamide compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012524090A JP2012524090A (ja) | 2012-10-11 |
| JP2012524090A5 true JP2012524090A5 (ja) | 2013-03-28 |
Family
ID=42664672
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012506089A Pending JP2012524090A (ja) | 2009-04-14 | 2010-04-12 | アモルファスα−（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組成物 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20100261768A1 (ja) |
| EP (1) | EP2419086B1 (ja) |
| JP (1) | JP2012524090A (ja) |
| KR (1) | KR20120027142A (ja) |
| CN (1) | CN102387788B (ja) |
| AR (1) | AR076306A1 (ja) |
| AU (1) | AU2010236701A1 (ja) |
| BR (1) | BRPI1012523A2 (ja) |
| CA (1) | CA2758709A1 (ja) |
| DK (1) | DK2419086T3 (ja) |
| EA (1) | EA201171207A1 (ja) |
| ES (1) | ES2426403T3 (ja) |
| HR (1) | HRP20130807T1 (ja) |
| MX (1) | MX2011010513A (ja) |
| NZ (1) | NZ595411A (ja) |
| PL (1) | PL2419086T3 (ja) |
| PT (1) | PT2419086E (ja) |
| SI (1) | SI2419086T1 (ja) |
| SM (1) | SMT201300106B (ja) |
| TW (1) | TW201043269A (ja) |
| WO (1) | WO2010120662A2 (ja) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL162498A0 (en) | 2001-12-20 | 2005-11-20 | Bristol Myers Squibb Co | (N-sulphonamido) acetamide derivatives and pharmaceutical compositions containing the same |
| 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 |
| US8252821B2 (en) | 2009-04-14 | 2012-08-28 | Bristol-Myers Squibb Company | Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| US9095585B2 (en) * | 2011-07-21 | 2015-08-04 | Bristol-Myers Squibb Company | Bioavailable compositions of amorphous piperidinyl compounds |
| US20150045353A1 (en) * | 2013-08-09 | 2015-02-12 | Neurogenetic Pharmaceuticals, Inc. | Formulations containing gamma secretase modulators, methods for preparation and delivery thereof |
| TWI718102B (zh) | 2014-08-08 | 2021-02-11 | 日商中外製藥股份有限公司 | ４環性化合物的非晶質體 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3999007A (en) * | 1975-10-09 | 1976-12-21 | Carl Joseph Crane | Aircraft visual approach/landing reproducer device and system |
| US5136301A (en) * | 1989-08-30 | 1992-08-04 | Rockwell International Corporation | Primary flight display system having a vertical linear altimeter |
| 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 |
| EP0750238B1 (en) * | 1995-06-20 | 2000-03-01 | Honeywell Inc. | Integrated ground collision avoidance system |
| IL123901A (en) * | 1995-11-17 | 2003-06-24 | Warner Lambert Co | Sulfonamide inhibitors of matrix metalloproteinases and pharmaceutical compositions comprising them |
| US6233522B1 (en) * | 1998-07-06 | 2001-05-15 | Alliedsignal Inc. | Aircraft position validation using radar and digital terrain elevation database |
| US6313123B1 (en) * | 1999-01-27 | 2001-11-06 | American Cyanamid Company | Acetylenic sulfonamide thiol tace inhibitors |
| US6570531B1 (en) * | 2000-04-27 | 2003-05-27 | Rockwell Collins, Inc. | Satellite navigation receiver designed for compatibility with aircraft automatic landing systems |
| US6483454B1 (en) * | 2000-11-28 | 2002-11-19 | Bae Systems Aerospace Inc. | Close formation aircraft collision avoidance |
| IL162498A0 (en) * | 2001-12-20 | 2005-11-20 | Bristol Myers Squibb Co | (N-sulphonamido) acetamide derivatives and pharmaceutical compositions containing the same |
| TWI336698B (en) * | 2003-03-31 | 2011-02-01 | Wyeth Corp | Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof |
| US20050048112A1 (en) * | 2003-08-28 | 2005-03-03 | Jorg Breitenbach | Solid pharmaceutical dosage form |
| FR2870605B1 (fr) * | 2004-05-18 | 2010-10-08 | Airbus France | Procede et dispositif de guidage automatique d'un aeronef, pour un vol au moins en partie a basse altitude |
| FR2880456B1 (fr) * | 2005-01-03 | 2007-02-23 | Airbus France Sas | Procede et dispositif d'alerte sonore lors de la desactivation d'un pilote automatique d'un aeronef |
| FR2886439B1 (fr) * | 2005-05-24 | 2010-11-05 | Eurocopter France | Procede et dispositif d'aide au pilotage d'un aeronef a basse altitude |
| KR101374928B1 (ko) * | 2005-11-09 | 2014-03-14 | 노파르티스 아게 | 일시적 가소제를 사용한 약학 조성물의 제조 방법 |
| FR2897448B1 (fr) * | 2006-02-14 | 2008-03-14 | Airbus France Sas | Procede et systeme d'aide au pilotage d'un aeronef. |
| KR20080093126A (ko) * | 2006-02-17 | 2008-10-20 | 와이어쓰 | 술폰아미드 치환된 알코올 및 이의 중간체의 제조 방법 |
| RU2008131051A (ru) * | 2006-02-17 | 2010-03-27 | Вайет (Us) | Избирательное n-сульфонилирование 2-амино трифторалкильнзамещенных спиртов |
| RS20090406A (en) * | 2006-03-20 | 2010-12-31 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions |
| WO2007109604A2 (en) * | 2006-03-20 | 2007-09-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions |
| FR2911988B1 (fr) * | 2007-01-26 | 2016-03-25 | Airbus France | Procede et dispositif pour determiner une hauteur maximale de stabilisation lors de la phase finale de vol d'un avion |
| 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 |
-
2010
- 2010-04-08 TW TW099110918A patent/TW201043269A/zh unknown
- 2010-04-09 US US12/757,304 patent/US20100261768A1/en not_active Abandoned
- 2010-04-12 CN CN2010800160778A patent/CN102387788B/zh not_active Expired - Fee Related
- 2010-04-12 EP EP10714413.1A patent/EP2419086B1/en not_active Not-in-force
- 2010-04-12 BR BRPI1012523A patent/BRPI1012523A2/pt not_active Application Discontinuation
- 2010-04-12 PL PL10714413T patent/PL2419086T3/pl unknown
- 2010-04-12 NZ NZ595411A patent/NZ595411A/xx not_active IP Right Cessation
- 2010-04-12 DK DK10714413.1T patent/DK2419086T3/da active
- 2010-04-12 SI SI201030355T patent/SI2419086T1/sl unknown
- 2010-04-12 JP JP2012506089A patent/JP2012524090A/ja active Pending
- 2010-04-12 EA EA201171207A patent/EA201171207A1/ru unknown
- 2010-04-12 MX MX2011010513A patent/MX2011010513A/es unknown
- 2010-04-12 AU AU2010236701A patent/AU2010236701A1/en not_active Abandoned
- 2010-04-12 KR KR1020117024035A patent/KR20120027142A/ko not_active Application Discontinuation
- 2010-04-12 CA CA2758709A patent/CA2758709A1/en not_active Abandoned
- 2010-04-12 WO PCT/US2010/030679 patent/WO2010120662A2/en active Application Filing
- 2010-04-12 PT PT107144131T patent/PT2419086E/pt unknown
- 2010-04-12 ES ES10714413T patent/ES2426403T3/es active Active
- 2010-04-14 AR ARP100101258A patent/AR076306A1/es unknown
-
2013
- 2013-08-27 HR HRP20130807AT patent/HRP20130807T1/hr unknown
- 2013-09-24 SM SM201300106T patent/SMT201300106B/xx unknown
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