NZ595335A - Pharmaceutical comprising (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide with enhanced bioavailability and solubility - Google Patents
Pharmaceutical comprising (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide with enhanced bioavailability and solubilityInfo
- Publication number
- NZ595335A NZ595335A NZ595335A NZ59533510A NZ595335A NZ 595335 A NZ595335 A NZ 595335A NZ 595335 A NZ595335 A NZ 595335A NZ 59533510 A NZ59533510 A NZ 59533510A NZ 595335 A NZ595335 A NZ 595335A
- Authority
- NZ
- New Zealand
- Prior art keywords
- trifluoropentanamide
- oxadiazol
- chlorophenyl
- sulfonyl
- fluoro
- Prior art date
Links
- 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 title abstract 2
- 239000002202 Polyethylene glycol Substances 0.000 abstract 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 abstract 3
- 229920001223 polyethylene glycol Polymers 0.000 abstract 3
- 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 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 206010019196 Head injury Diseases 0.000 abstract 1
- 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 abstract 1
- 208000030886 Traumatic Brain injury Diseases 0.000 abstract 1
- 229930003427 Vitamin E Natural products 0.000 abstract 1
- 150000003869 acetamides Chemical class 0.000 abstract 1
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 229920001531 copovidone Polymers 0.000 abstract 1
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- 208000017004 dementia pugilistica Diseases 0.000 abstract 1
- 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 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 208000027061 mild cognitive impairment Diseases 0.000 abstract 1
- 229920002689 polyvinyl acetate Polymers 0.000 abstract 1
- 239000011118 polyvinyl acetate Substances 0.000 abstract 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 abstract 1
- 230000009529 traumatic brain injury Effects 0.000 abstract 1
- 229940046009 vitamin E Drugs 0.000 abstract 1
- 235000019165 vitamin E Nutrition 0.000 abstract 1
- 239000011709 vitamin E Substances 0.000 abstract 1
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16906109P | 2009-04-14 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| NZ595335A true NZ595335A (en) | 2013-03-28 |
Family
ID=42235859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ595335A NZ595335A (en) | 2009-04-14 | 2010-04-13 | Pharmaceutical comprising (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide with enhanced bioavailability and solubility |
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 |
|---|---|---|---|---|
| DK1465861T3 (da) | 2001-12-20 | 2009-08-31 | Bristol Myers Squibb Co | Alpha-(N-sulfonamid)acetamidderivater som beta-amyloidhæmmere |
| 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 |
| EP2651450B1 (en) * | 2010-12-16 | 2015-12-16 | Borje S. Andersson | Azole pharmaceutical formulations for parenteral administration and methods for preparing and using the same as treatment of diseases sensitive to azole compounds |
| US9364433B2 (en) | 2011-04-28 | 2016-06-14 | Borje S. Andersson | Parenteral formulations of lipophilic pharmaceutical agents and methods for preparing and using the same |
| 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 |
| WO2020169738A1 (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 |
| MX2023002116A (es) * | 2020-08-21 | 2023-03-15 | Janssen Pharmaceutica Nv | Formulaciones farmaceuticas que comprenden un inhibidor de malt1 y una mezcla de polietilenglicol con un acido graso. |
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 |
| PT874836E (pt) | 1995-11-17 | 2003-02-28 | Warner Lambert Co | Inibidores com sulfonamida de metaloproteinases de matriz |
| PL331338A1 (en) | 1996-07-22 | 1999-07-05 | Monsanto Co | Thiosulphonamidic metaloprotease inhibitors |
| WO1998008490A1 (en) * | 1996-09-01 | 1998-03-05 | 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 |
| DK1149074T3 (da) | 1999-01-27 | 2005-01-10 | Wyeth Corp | Acetyleniske sulfonamid-thiol-TACE-inhibitirer |
| AU773273B2 (en) | 1999-02-26 | 2004-05-20 | Bristol-Myers Squibb Company | Novel sulfonamide compounds and uses thereof |
| DE60233150D1 (de) * | 2001-10-19 | 2009-09-10 | Isotechnika Inc | Neue cyclosporin-analoge mikroemulsionsvorkonzentrate |
| DK1465861T3 (da) | 2001-12-20 | 2009-08-31 | Bristol Myers Squibb Co | Alpha-(N-sulfonamid)acetamidderivater som beta-amyloidhæmmere |
| RU2342374C2 (ru) | 2003-03-31 | 2008-12-27 | Уайт | Фтор- и трифторалкилсодержащие гетероциклические сульфонамидные ингибиторы образования бета-амилоида и их производные |
| 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 |
| JP2007535545A (ja) * | 2004-04-28 | 2007-12-06 | プロキャリア・インコーポレーテッド | 難吸収性薬剤の経口投与のための製剤 |
| AU2005261932B2 (en) | 2004-07-13 | 2011-10-13 | F. Hoffmann-La Roche Ag | Sulfonamide derivatives |
| US7144894B2 (en) | 2004-09-23 | 2006-12-05 | Bristol-Myers Squibb Company | Sulfonamide bicyclic compounds |
| RU2007122450A (ru) * | 2004-12-14 | 2009-01-27 | Вайет (Us) | Применение агониста рецептора 5-нт6 для лечения и профилактики нейродегенеративных заболеваний |
| EP1984347A1 (en) | 2006-02-17 | 2008-10-29 | Wyeth a Corporation of the State of Delaware | Selective n-sulfonylation of 2-amino trifluoroalkyl substituted alcohols |
| WO2007098029A1 (en) | 2006-02-17 | 2007-08-30 | Wyeth | Methods for preparing sulfonamide substituted alcohols and intermediates thereof |
| WO2007103683A2 (en) * | 2006-03-01 | 2007-09-13 | Roskamp Research Llc | Compounds for inhibiting beta-amyloid production |
| US8633179B2 (en) | 2007-03-13 | 2014-01-21 | The 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 |
| BRPI0924404A2 (pt) | 2009-03-19 | 2019-04-02 | Bristol-Myers Squibb Company | composto alfa-(n-sulfonamido) acetamida como um inibidor de produção de peptídeo beta amilóide |
| 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 KR KR1020117024036A patent/KR20120022766A/ko not_active Withdrawn
- 2010-04-13 NZ NZ595335A patent/NZ595335A/xx not_active IP Right Cessation
- 2010-04-13 CN CN2010800164919A patent/CN102395361A/zh active Pending
- 2010-04-13 EA EA201101286A patent/EA201101286A1/ru unknown
- 2010-04-13 JP JP2012506123A patent/JP2012524092A/ja active Pending
- 2010-04-13 AU AU2010236602A patent/AU2010236602A1/en not_active Abandoned
- 2010-04-13 WO PCT/US2010/030862 patent/WO2010120755A1/en not_active Ceased
- 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 CA CA2758847A patent/CA2758847A1/en not_active Abandoned
- 2010-04-14 TW TW099111671A patent/TW201041609A/zh unknown
- 2010-04-14 AR ARP100101257A patent/AR076305A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EA201101286A1 (ru) | 2012-04-30 |
| US20100260837A1 (en) | 2010-10-14 |
| JP2012524092A (ja) | 2012-10-11 |
| WO2010120755A1 (en) | 2010-10-21 |
| AR076305A1 (es) | 2011-06-01 |
| CN102395361A (zh) | 2012-03-28 |
| EP2419090A1 (en) | 2012-02-22 |
| KR20120022766A (ko) | 2012-03-12 |
| AU2010236602A1 (en) | 2011-10-13 |
| CA2758847A1 (en) | 2010-10-21 |
| EP2419090B1 (en) | 2013-02-13 |
| MX2011010514A (es) | 2011-11-29 |
| US8252821B2 (en) | 2012-08-28 |
| TW201041609A (en) | 2010-12-01 |
| BRPI1015483A2 (pt) | 2016-04-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 3 YEARS UNTIL 13 APR 2017 BY CPA GLOBAL Effective date: 20140306 |
|
| LAPS | Patent lapsed |