AR082599A1 - COMPOSICIONES FARMACEUTICAS DE ANTAGONISTAS DEL RECEPTOR METABOTROPICO DE GLUTAMATO 5 (mGlu5) - Google Patents
COMPOSICIONES FARMACEUTICAS DE ANTAGONISTAS DEL RECEPTOR METABOTROPICO DE GLUTAMATO 5 (mGlu5)Info
- Publication number
- AR082599A1 AR082599A1 ARP110102881A ARP110102881A AR082599A1 AR 082599 A1 AR082599 A1 AR 082599A1 AR P110102881 A ARP110102881 A AR P110102881A AR P110102881 A ARP110102881 A AR P110102881A AR 082599 A1 AR082599 A1 AR 082599A1
- Authority
- AR
- Argentina
- Prior art keywords
- layer containing
- polymer
- cycloalkyl
- lower alkyl
- optionally substituted
- Prior art date
Links
Classifications
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- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
-
- 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
- A61P25/24—Antidepressants
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Materials For Medical Uses (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se describen composiciones farmacéuticas de antagonistas del receptor metabotrópico de glutamato 5 (mGlu5) o una sal farmacológicamente aceptable de los mismos, las composiciones contienen el compuesto terapéuticamente activo junto con un polímero no iónico y polímero iónico, aglutinante y cargas de relleno ya sea en forma de bola de matriz (matrix pellet), tableta de matriz o bolas recubiertas, las composiciones proporcionan un perfil de liberación “in vitro” independiente del ph con un nmt del 70% en una hora, nmt del 85% en 4 horas y nmt del 80% en 8 horas, las composiciones son útiles para el tratamiento de trastornos del SNC, por ejemplo la depresión resistente al tratamiento (trd) y el síndrome de la X frágil.Reivindicación 1: Una composición farmacéutica en forma de bola multicapa (layered pellet), que consta de: a) un núcleo inerte; b) una capa que contiene un compuesto de la fórmula (1) en la que uno de A o E es N y el otro es C; R1 es halógeno o ciano; R2 es alquilo inferior; R3 es arilo o heteroarilo, cada uno de ellos está opcionalmente sustituido por uno, dos o tres sustituyentes elegidos entre halógeno, alquilo inferior, alcoxi inferior, cicloalquilo, haloalquilo inferior, haloalcoxi inferior, ciano y NR’R’’, o por 1-morfolinilo, 1-pirrolidinilo, opcionalmente sustituido por (CH2)mOR, piperidinilo, opcionalmente sustituido por (CH2)mOR, 1,1-dioxo-tiomorfolinilo o piperazinilo, opcionalmente sustituido por alquilo inferior o (CH2)m-cicloalquilo; R es hidrógeno, alquilo inferior o (CH2)m-cicloalquilo; R’ y R’’ son con independencia entre sí hidrógeno, alquilo inferior, (CH2)m-cicloalquilo o (CH2)nOR; m es el número 0 ó 1; n es el número 1 ó 2; y R4 es CHF2, CF3, C(O)H o CH2R5, en el que R5 es hidrógeno, OH, alquilo C1-6 o cicloalquilo C3-12; y sus sales farmacéuticamente aceptables; c) una capa de liberación controlada que contiene un polímero controlador de la velocidad; y d) una capa que contiene un polímero que se disuelve en función del pH. Reivindicación 2: Una composición según la reivindicación 1, que consta de: a) un núcleo inerte; b) una capa que contiene un compuesto de la fórmula (1); c) opcionalmente, una capa de separación; d) una capa de liberación controlada que contiene un polímero controlador de la velocidad; e) una capa que contiene un polímero que se disuelve en función del pH; y f) opcionalmente, una capa que contiene un polímero no termoplástico. Reivindicación 8: La composición según una cualquiera de las reivindicaciones de 1 a 7, en la que el antagonista del receptor metabotrópico de glutamato 5 es la 2-cloro-4-[1-(4-flúor-fenil)-2,5-dimetil-1H-imidazol-4-iletinil]-piridina.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37270510P | 2010-08-11 | 2010-08-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR082599A1 true AR082599A1 (es) | 2012-12-19 |
Family
ID=44514702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110102881A AR082599A1 (es) | 2010-08-11 | 2011-08-09 | COMPOSICIONES FARMACEUTICAS DE ANTAGONISTAS DEL RECEPTOR METABOTROPICO DE GLUTAMATO 5 (mGlu5) |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20120040008A1 (es) |
| EP (1) | EP2603203A2 (es) |
| JP (2) | JP2013536186A (es) |
| KR (1) | KR20130038419A (es) |
| CN (1) | CN103068372B (es) |
| AR (1) | AR082599A1 (es) |
| AU (1) | AU2011288556B2 (es) |
| BR (1) | BR112013003094A2 (es) |
| CA (1) | CA2806459A1 (es) |
| HK (1) | HK1181654A1 (es) |
| MX (1) | MX2013001601A (es) |
| MY (1) | MY162779A (es) |
| NZ (1) | NZ606801A (es) |
| RU (1) | RU2013108056A (es) |
| SG (1) | SG187179A1 (es) |
| TW (1) | TW201211025A (es) |
| WO (1) | WO2012019990A2 (es) |
| ZA (1) | ZA201300657B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120039999A1 (en) * | 2010-08-11 | 2012-02-16 | Ashish Chatterji | Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists |
| EP2732815A1 (en) | 2012-11-16 | 2014-05-21 | Neurochlore | Modulators of intracellular chloride concentration for treating fragile X syndrome |
| JP6444996B2 (ja) * | 2013-06-12 | 2018-12-26 | ノバルティス アーゲー | 調節放出製剤 |
| AU2018270505B2 (en) * | 2017-05-19 | 2023-09-21 | Biscayne Neurotherapeutics, Inc. | Modified release pharmaceutical compositions of huperzine and methods of using the same |
| IL308650A (en) | 2017-06-21 | 2024-01-01 | Minerva Neurosciences Inc | Stomach-resistant controlled-release oral dosage forms |
| KR20200035035A (ko) | 2017-07-31 | 2020-04-01 | 노파르티스 아게 | 코카인 사용 감소 또는 코카인 사용 재발 예방에 있어서 마보글루란트의 용도 |
| JP2023504177A (ja) * | 2019-12-02 | 2023-02-01 | エフ．ホフマン－ラ ロシュ アーゲー | アルキニル－（ヘテロアリール）－カルボキサミドｈｃｎ１阻害剤 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA881301B (en) * | 1987-02-27 | 1989-10-25 | Lilly Co Eli | Sustained release matrix formulations |
| FR2677886B1 (fr) | 1991-06-18 | 1995-03-31 | Adir | Comprime matriciel permettant la liberation prolongee d'indapamide apres administration par voie orale. |
| US5656291A (en) * | 1994-03-16 | 1997-08-12 | Pharmacia & Upjohn Aktiebolag | Controlled release preparation |
| US6004996A (en) | 1997-02-05 | 1999-12-21 | Hoffman-La Roche Inc. | Tetrahydrolipstatin containing compositions |
| SE9803871D0 (sv) * | 1998-11-11 | 1998-11-11 | Pharmacia & Upjohn Ab | Therapeutic method and formulation |
| DE19927688A1 (de) * | 1999-06-17 | 2000-12-21 | Gruenenthal Gmbh | Mehrschichttablette zur Verabreichung einer fixen Kombination von Tramadol und Diclofenac |
| US6627223B2 (en) * | 2000-02-11 | 2003-09-30 | Eurand Pharmaceuticals Ltd. | Timed pulsatile drug delivery systems |
| WO2001076557A1 (fr) * | 2000-04-10 | 2001-10-18 | Sumitomo Pharmaceuticals Co., Ltd. | Preparations a liberation prolongee |
| DE10209982A1 (de) * | 2002-03-07 | 2003-09-25 | Boehringer Ingelheim Pharma | Oral zu applizierende Darreichungsform für schwerlösliche basische Wirkstoffe |
| UA80888C2 (en) * | 2003-06-05 | 2007-11-12 | Hoffmann La Roche | Imidazole derivatives as glutmate receptor antagonists |
| WO2005118568A1 (en) * | 2004-06-01 | 2005-12-15 | F. Hoffmann-La Roche Ag | Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists |
| BRPI0511678A (pt) * | 2004-06-01 | 2008-01-08 | Hoffmann La Roche | piridin-4-il-etinil-imidazóis e pirazóis como antagonistas de receptor de mglu5 |
| US20090208579A1 (en) * | 2004-12-27 | 2009-08-20 | Eisai R & D Management Co., Ltd. | Matrix Type Sustained-Release Preparation Containing Basic Drug or Salt Thereof, and Method for Manufacturing the Same |
| EP1681056A1 (en) * | 2005-01-14 | 2006-07-19 | Krka Tovarna Zdravil, D.D., Novo Mesto | Process for preparing lansoprazole |
| US20070087056A1 (en) * | 2005-08-09 | 2007-04-19 | Claudia Guthmann | Pharmaceutical form with sustained pH-independent active ingredient release for active ingredients having strong pH-dependent solubility |
| KR100591142B1 (ko) * | 2005-11-04 | 2006-06-20 | 지엘팜텍 주식회사 | 파록세틴을 활성물질로 함유하는 장용성 서방형 정제 |
-
2011
- 2011-08-04 US US13/197,822 patent/US20120040008A1/en not_active Abandoned
- 2011-08-08 KR KR1020137006062A patent/KR20130038419A/ko not_active Application Discontinuation
- 2011-08-08 WO PCT/EP2011/063604 patent/WO2012019990A2/en active Application Filing
- 2011-08-08 NZ NZ606801A patent/NZ606801A/en not_active IP Right Cessation
- 2011-08-08 CA CA2806459A patent/CA2806459A1/en not_active Abandoned
- 2011-08-08 RU RU2013108056/15A patent/RU2013108056A/ru not_active Application Discontinuation
- 2011-08-08 AU AU2011288556A patent/AU2011288556B2/en not_active Ceased
- 2011-08-08 SG SG2013005384A patent/SG187179A1/en unknown
- 2011-08-08 BR BR112013003094A patent/BR112013003094A2/pt active Search and Examination
- 2011-08-08 MY MYPI2013700229A patent/MY162779A/en unknown
- 2011-08-08 EP EP11749137.3A patent/EP2603203A2/en not_active Withdrawn
- 2011-08-08 CN CN201180038645.9A patent/CN103068372B/zh not_active Expired - Fee Related
- 2011-08-08 MX MX2013001601A patent/MX2013001601A/es not_active Application Discontinuation
- 2011-08-08 JP JP2013523582A patent/JP2013536186A/ja active Pending
- 2011-08-09 AR ARP110102881A patent/AR082599A1/es unknown
- 2011-08-10 TW TW100128605A patent/TW201211025A/zh unknown
-
2013
- 2013-01-24 ZA ZA2013/00657A patent/ZA201300657B/en unknown
- 2013-08-01 HK HK13108973.9A patent/HK1181654A1/zh not_active IP Right Cessation
-
2014
- 2014-12-24 JP JP2014259978A patent/JP2015107977A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| HK1181654A1 (zh) | 2013-11-15 |
| MY162779A (en) | 2017-07-14 |
| ZA201300657B (en) | 2013-09-25 |
| CN103068372B (zh) | 2016-02-17 |
| CA2806459A1 (en) | 2012-02-16 |
| WO2012019990A3 (en) | 2012-08-02 |
| AU2011288556B2 (en) | 2014-05-22 |
| EP2603203A2 (en) | 2013-06-19 |
| CN103068372A (zh) | 2013-04-24 |
| KR20130038419A (ko) | 2013-04-17 |
| AU2011288556A1 (en) | 2013-01-31 |
| TW201211025A (en) | 2012-03-16 |
| WO2012019990A2 (en) | 2012-02-16 |
| JP2015107977A (ja) | 2015-06-11 |
| RU2013108056A (ru) | 2014-09-20 |
| NZ606801A (en) | 2015-01-30 |
| BR112013003094A2 (pt) | 2016-06-28 |
| SG187179A1 (en) | 2013-02-28 |
| MX2013001601A (es) | 2013-03-22 |
| US20120040008A1 (en) | 2012-02-16 |
| JP2013536186A (ja) | 2013-09-19 |
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| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |