AU2015209411A1 - Modified release formulations of pridopidine - Google Patents
Modified release formulations of pridopidine Download PDFInfo
- Publication number
- AU2015209411A1 AU2015209411A1 AU2015209411A AU2015209411A AU2015209411A1 AU 2015209411 A1 AU2015209411 A1 AU 2015209411A1 AU 2015209411 A AU2015209411 A AU 2015209411A AU 2015209411 A AU2015209411 A AU 2015209411A AU 2015209411 A1 AU2015209411 A1 AU 2015209411A1
- Authority
- AU
- Australia
- Prior art keywords
- pridopidine
- solid oral
- dosage form
- oral dosage
- pharmaceutically acceptable
- 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.)
- Abandoned
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| US201462050626P | 2014-09-15 | 2014-09-15 | |
| US62/050,626 | 2014-09-15 | ||
| PCT/US2015/012248 WO2015112601A1 (en) | 2014-01-22 | 2015-01-21 | Modified release formulations of pridopidine |
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| USRE46117E1 (en) | 1999-12-22 | 2016-08-23 | Teva Pharmaceuticals International Gmbh | Modulators of dopamine neurotransmission |
| SG188298A1 (en) | 2010-09-03 | 2013-04-30 | Ivax Int Gmbh | Deuterated analogs of pridopidine useful as dopaminergic stabilizers |
| MX347209B (es) | 2011-12-08 | 2017-04-19 | Teva Pharmaceuticals Int Gmbh | La sal de bromhidrato de pridopidina. |
| US11090297B2 (en) | 2013-06-21 | 2021-08-17 | Prilenia Neurotherapeutics Ltd. | Pridopidine for treating huntington's disease |
| PE20160195A1 (es) | 2013-06-21 | 2016-05-14 | Teva Pharmaceuticals Int Gmbh | Uso de pridopidina en dosis altas para el tratamiento de enfermedad de huntington |
| PE20161220A1 (es) | 2014-01-22 | 2016-11-23 | Teva Pharmaceuticals Int Gmbh | Formulaciones de pridopidina de liberacion modificada |
| TW201613859A (en) | 2014-06-30 | 2016-04-16 | Teva Pharma | Analogs of PRIDOPIDINE, their preparation and use |
| EP3236964A4 (en) | 2014-12-22 | 2018-09-19 | Teva Pharmaceuticals International GmbH | L-tartrate salt of pridopidine |
| US11471449B2 (en) | 2015-02-25 | 2022-10-18 | Prilenia Neurotherapeutics Ltd. | Use of pridopidine to improve cognitive function and for treating Alzheimer's disease |
| EP4282479A3 (en) | 2015-02-25 | 2024-02-21 | Prilenia Neurotherapeutics Ltd. | Use of pridopidine to treat depression or anxiety |
| CA2993183A1 (en) * | 2015-07-22 | 2017-01-26 | Teva Pharmaceuticals International Gmbh | Pridopidine base formulations and their use |
| AR105434A1 (es) | 2015-07-22 | 2017-10-04 | Teva Pharmaceuticals Int Gmbh | Proceso para preparar pridopidina |
| US11738012B2 (en) | 2016-02-24 | 2023-08-29 | Prilenia Neurotherapeutics Ltd. | Treatment of neurodegenerative eye disease using pridopidine |
| ES3025836T3 (en) | 2016-08-24 | 2025-06-09 | Prilenia Neurotherapeutics Ltd | Use of pridopidine for treating functional decline |
| WO2018039475A1 (en) * | 2016-08-24 | 2018-03-01 | Teva Pharmaceuticals International Gmbh | Use of pridopidine for treating dystonias |
| US12102627B2 (en) | 2016-09-16 | 2024-10-01 | Prilenia Neurotherapeutics Ltd. | Use of pridopidine for treating rett syndrome |
| ES2909557T3 (es) * | 2016-09-16 | 2022-05-09 | Prilenia Neurotherapeutics Ltd | Utilización de la pridopidina para el tratamiento del síndrome de Rett |
| CA3050700C (en) | 2017-01-20 | 2023-10-03 | Prilenia Neurotherapeutics Ltd. | Use of pridopidine for the treatment of fragile x syndrome |
| HRP20251431T1 (hr) | 2017-08-14 | 2026-01-02 | Prilenia Neurotherapeutics Ltd. | Liječenje amiotrofične lateralne skleroze pridopidinom |
| EP3675830A1 (en) | 2017-08-30 | 2020-07-08 | Prilenia Neurotherapeutics Ltd. | High concentration dosage forms of pridopidine |
| AU2018329628B2 (en) | 2017-09-08 | 2021-04-22 | Prilenia Neurotherapeutics Ltd. | Pridopidine for treating drug induced dyskinesias |
| US12036213B2 (en) | 2017-09-08 | 2024-07-16 | Prilenia Neurotherapeutics Ltd. | Pridopidine for treating drug induced dyskinesias |
| KR20200056071A (ko) | 2018-11-14 | 2020-05-22 | 한화토탈 주식회사 | 내열성, 강성 및 용융 강도가 우수한 폴리올레핀 수지 조성물 |
| EP3920924A4 (en) | 2019-02-04 | 2022-11-16 | Prilenia Neurotherapeutics Ltd. | LOW-DOSE PRIDOIDIN FOR THE TREATMENT OF PARKINSON'S DISEASE AND OTHER PARKINSONIC-RELATED DISEASES |
| CN116472043A (zh) * | 2020-10-20 | 2023-07-21 | 普瑞尼亚神经治疗有限公司 | 普利多匹定和类似物用于治疗焦虑和抑郁的用途 |
| WO2024258929A1 (en) * | 2023-06-12 | 2024-12-19 | Unravel Biosciences, Inc. | Methods for treating diseases associated with taf1 loss of function |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4020983B2 (ja) * | 1995-07-07 | 2007-12-12 | 帝國製薬株式会社 | 持続性製剤およびその製法 |
| SE9904724D0 (sv) | 1999-12-22 | 1999-12-22 | Carlsson A Research Ab | New modulators of dopamine neurotransmission I |
| CN1193754C (zh) | 2000-03-21 | 2005-03-23 | 日本新药株式会社 | 释放控制型口服制剂 |
| AR030557A1 (es) * | 2000-04-14 | 2003-08-27 | Jagotec Ag | Una tableta en multicapa de liberacion controlada y metodo de tratamiento |
| GB0125088D0 (en) | 2001-10-18 | 2001-12-12 | Smithkline Beecham Cork Ltd | New use |
| KR20090080143A (ko) * | 2003-09-02 | 2009-07-23 | 화이자 프로덕츠 인크. | 지프라시돈의 지속 방출형 투여 형태 |
| CA2584831C (en) | 2004-10-13 | 2013-09-17 | Neurosearch Sweden Ab | Process for the synthesis of 4-(3-methanesulfonylphenyl)-1-n-propyl-piperidine |
| US20110206782A1 (en) * | 2010-02-24 | 2011-08-25 | Auspex Pharmaceuticals, Inc. | Piperidine modulators of dopamine receptor |
| MX347209B (es) * | 2011-12-08 | 2017-04-19 | Teva Pharmaceuticals Int Gmbh | La sal de bromhidrato de pridopidina. |
| HK1206297A1 (en) * | 2012-04-04 | 2016-01-08 | Teva Pharmaceuticals International Gmbh | Pharmaceutical compositions for combination therapy |
| PE20160195A1 (es) * | 2013-06-21 | 2016-05-14 | Teva Pharmaceuticals Int Gmbh | Uso de pridopidina en dosis altas para el tratamiento de enfermedad de huntington |
| PE20161220A1 (es) | 2014-01-22 | 2016-11-23 | Teva Pharmaceuticals Int Gmbh | Formulaciones de pridopidina de liberacion modificada |
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