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)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (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 (https=) |
| EP (1) | EP2419090B1 (https=) |
| JP (1) | JP2012524092A (https=) |
| KR (1) | KR20120022766A (https=) |
| CN (1) | CN102395361A (https=) |
| AR (1) | AR076305A1 (https=) |
| AU (1) | AU2010236602A1 (https=) |
| BR (1) | BRPI1015483A2 (https=) |
| CA (1) | CA2758847A1 (https=) |
| EA (1) | EA201101286A1 (https=) |
| MX (1) | MX2011010514A (https=) |
| NZ (1) | NZ595335A (https=) |
| TW (1) | TW201041609A (https=) |
| WO (1) | WO2010120755A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2471099C (en) | 2001-12-20 | 2011-04-12 | Bristol-Myers Squibb Company | .alpha.-(n-sulphonamido)acetamide derivatives as .beta.-amyloid inhibitors |
| 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 |
| WO2011040797A2 (ko) | 2009-10-02 | 2011-04-07 | 엘지전자 주식회사 | 하향링크 참조신호의 전송방법 및 장치 |
| ES2565353T3 (es) | 2010-12-16 | 2016-04-04 | Borje S. Andersson | Formulaciones farmacéuticas de azol para administración parenteral y métodos para la preparación y el uso de las mismas como tratamiento de enfermedades sensibles a los compuestos de azol |
| DK2701684T3 (en) | 2011-04-28 | 2017-09-18 | Platform Brightworks Two Ltd | Improved parenteral formulations of lipophilic pharmaceuticals and methods for their preparation and use |
| 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 |
| US20220175760A1 (en) * | 2019-02-22 | 2022-06-09 | Janssen Pharmaceutica Nv | Pharmaceutical formulations |
| EP3953345B1 (en) | 2019-04-11 | 2023-04-05 | Janssen Pharmaceutica NV | Pyridine rings containing derivatives as malt1 inhibitors |
| JP2023538099A (ja) * | 2020-08-21 | 2023-09-06 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｍａｌｔ１阻害剤と、ポリエチレングリコールの脂肪酸との混合物と、を含む、医薬製剤 |
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 |
| SK282833B6 (sk) | 1995-11-17 | 2002-12-03 | Warner-Lambert Company | Sulfónamidové inhibítory matricových metaloproteináz a farmaceutická kompozícia obsahujúca tieto inhibítory |
| JP2000515153A (ja) | 1996-07-22 | 2000-11-14 | モンサント カンパニー | チオールスルホンアミド メタロプロテアーゼインヒビター |
| JP2001523221A (ja) * | 1996-09-01 | 2001-11-20 | ファーモス コーポレイション | 親油性物質の促進された生物学的利用能のための固形共沈物 |
| 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 |
| AU766192B2 (en) | 1999-01-27 | 2003-10-09 | Wyeth Holdings Corporation | Acetylenic sulfonamide thiol tace inhibitors |
| US6313123B1 (en) | 1999-01-27 | 2001-11-06 | American Cyanamid Company | Acetylenic sulfonamide thiol tace inhibitors |
| NZ514453A (en) | 1999-02-26 | 2003-04-29 | Merck & Co Inc | Novel sulfonamide compounds and uses thereof |
| IL160761A0 (en) * | 2001-10-19 | 2004-08-31 | Isotechnika Inc | Novel cyclosporin analog microemulsion preconcentrates |
| CA2471099C (en) | 2001-12-20 | 2011-04-12 | Bristol-Myers Squibb Company | .alpha.-(n-sulphonamido)acetamide derivatives as .beta.-amyloid inhibitors |
| KR20060002908A (ko) | 2003-03-31 | 2006-01-09 | 와이어쓰 | 베타 아밀로이드 생산 억제제인 플루오로- 및트리플루오로알킬-함유 헤테로사이클릭 설폰아미드 및 이의유도체 |
| 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 |
| CA2595116A1 (en) * | 2004-04-28 | 2005-11-10 | Procarrier, Inc. | Oral formulation for delivery of poorly absorbed drugs |
| EP1768960A1 (en) | 2004-07-13 | 2007-04-04 | F.Hoffmann-La Roche Ag | Sulfonamide derivatives |
| US7144894B2 (en) | 2004-09-23 | 2006-12-05 | Bristol-Myers Squibb Company | Sulfonamide bicyclic compounds |
| WO2006065710A1 (en) * | 2004-12-14 | 2006-06-22 | Wyeth | Use of a 5-ht6 agonist for the treatment and prevention of neurodegenerative disorders |
| AR059517A1 (es) | 2006-02-17 | 2008-04-09 | Wyeth Corp | N- sulfonilacion selectiva de alcoholes sustituidos con 2- aminotrifluoralquilo |
| EP1984321A1 (en) | 2006-02-17 | 2008-10-29 | 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 |
| 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 |
| WO2009137657A1 (en) | 2008-05-08 | 2009-11-12 | Bristol-Myers Squibb Company | 2-aryl glycinamide derivatives |
| 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 |
| CN102438622A (zh) | 2009-03-19 | 2012-05-02 | 百时美施贵宝公司 | 作为β淀粉样肽产生抑制剂的新颖α-(N-磺酰氨基)乙酰胺化合物 |
| 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 CN CN2010800164919A patent/CN102395361A/zh active Pending
- 2010-04-13 CA CA2758847A patent/CA2758847A1/en not_active Abandoned
- 2010-04-13 EP EP10714418A patent/EP2419090B1/en not_active Not-in-force
- 2010-04-13 BR BRPI1015483A patent/BRPI1015483A2/pt not_active IP Right Cessation
- 2010-04-13 JP JP2012506123A patent/JP2012524092A/ja active Pending
- 2010-04-13 MX MX2011010514A patent/MX2011010514A/es active IP Right Grant
- 2010-04-13 EA EA201101286A patent/EA201101286A1/ru unknown
- 2010-04-13 AU AU2010236602A patent/AU2010236602A1/en not_active Abandoned
- 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 WO PCT/US2010/030862 patent/WO2010120755A1/en not_active Ceased
- 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 |
|---|---|
| MX2011010514A (es) | 2011-11-29 |
| CN102395361A (zh) | 2012-03-28 |
| JP2012524092A (ja) | 2012-10-11 |
| EP2419090A1 (en) | 2012-02-22 |
| KR20120022766A (ko) | 2012-03-12 |
| TW201041609A (en) | 2010-12-01 |
| BRPI1015483A2 (pt) | 2016-04-26 |
| AR076305A1 (es) | 2011-06-01 |
| EA201101286A1 (ru) | 2012-04-30 |
| US8252821B2 (en) | 2012-08-28 |
| AU2010236602A1 (en) | 2011-10-13 |
| US20100260837A1 (en) | 2010-10-14 |
| EP2419090B1 (en) | 2013-02-13 |
| CA2758847A1 (en) | 2010-10-21 |
| WO2010120755A1 (en) | 2010-10-21 |
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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 |