ES2911800T3 - Formulaciones de liberación modificada de pridopidina - Google Patents
Formulaciones de liberación modificada de pridopidina Download PDFInfo
- Publication number
- ES2911800T3 ES2911800T3 ES15740303T ES15740303T ES2911800T3 ES 2911800 T3 ES2911800 T3 ES 2911800T3 ES 15740303 T ES15740303 T ES 15740303T ES 15740303 T ES15740303 T ES 15740303T ES 2911800 T3 ES2911800 T3 ES 2911800T3
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- Spain
- Prior art keywords
- dosage form
- pridopidine
- oral dosage
- solid oral
- 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.)
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| CA2913781C (en) | 2013-06-21 | 2022-05-10 | Teva Pharmaceutical Industries Ltd. | Use of pridopidine for treating huntington's disease |
| CA2937243C (en) | 2014-01-22 | 2023-07-18 | Teva Pharmaceuticals International Gmbh | Modified release formulations of pridopidine |
| TW201613859A (en) | 2014-06-30 | 2016-04-16 | Teva Pharma | Analogs of PRIDOPIDINE, their preparation and use |
| WO2016106142A1 (en) | 2014-12-22 | 2016-06-30 | 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 |
| EP3854785A1 (en) | 2015-02-25 | 2021-07-28 | Prilenia Neurotherapeutics Ltd. | Use of pridopidine to treat depression or anxiety |
| EP3324967A4 (en) * | 2015-07-22 | 2019-03-20 | Prilenia Therapeutics Development Ltd. | PRIDOPIDINE-BASED FORMULATIONS AND USE OF THE SAME |
| AR105434A1 (es) | 2015-07-22 | 2017-10-04 | Teva Pharmaceuticals Int Gmbh | Proceso para preparar pridopidina |
| EP3419622B1 (en) | 2016-02-24 | 2024-03-06 | Prilenia Neurotherapeutics Ltd. | Treatment of neurodegenerative eye disease using pridopidine |
| IL311081A (en) | 2016-08-24 | 2024-04-01 | Prilenia Neurotherapeutics Ltd | Use of pyridofidine to treat functional decline |
| CN110012661A (zh) * | 2016-08-24 | 2019-07-12 | 普瑞尼亚医疗发展有限公司 | 普利多匹定用于治疗肌张力障碍的用途 |
| ES2909557T3 (es) * | 2016-09-16 | 2022-05-09 | Prilenia Neurotherapeutics Ltd | Utilización de la pridopidina para el tratamiento del síndrome de Rett |
| US12102627B2 (en) | 2016-09-16 | 2024-10-01 | Prilenia Neurotherapeutics Ltd. | Use of pridopidine for treating rett syndrome |
| ES2972205T3 (es) | 2017-01-20 | 2024-06-11 | Prilenia Neurotherapeutics Ltd | Pridopidina para el tratamiento del síndrome x frágil |
| HUE061505T2 (hu) | 2017-08-14 | 2023-07-28 | Prilenia Neurotherapeutics Ltd | Módszer amyothrophiás lateralsclerosis kezelésére pridopidinnel |
| JP2020532517A (ja) * | 2017-08-30 | 2020-11-12 | プリレニア ニューロセラピューティクス リミテッド | 高濃度プリドピジン製剤 |
| US12036213B2 (en) | 2017-09-08 | 2024-07-16 | Prilenia Neurotherapeutics Ltd. | Pridopidine for treating drug induced dyskinesias |
| CA3075020C (en) | 2017-09-08 | 2021-12-07 | 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 |
| JP7585561B2 (ja) * | 2019-02-04 | 2024-11-19 | プリレニア ニューロセラピューティクス リミテッド | パーキンソン病およびパーキンソニズムに関連する他の疾患のための低用量プリドピジン |
| AU2020243692B2 (en) | 2019-03-15 | 2023-03-02 | Prilenia Neurotherapeutics Ltd. | Treatment of mitochondrial associated diseases and disorders, including symptoms thereof using pridopidine |
| 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 |
| KR20030019326A (ko) * | 2000-03-21 | 2003-03-06 | 니뽄 신야쿠 가부시키가이샤 | 방출 제어형 경구 투여 제제 |
| 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 |
| KR20060115350A (ko) * | 2003-09-02 | 2006-11-08 | 화이자 프로덕츠 인크. | 지프라시돈의 지속 방출형 투여 형태 |
| ES2659577T3 (es) | 2004-10-13 | 2018-03-16 | Teva Pharmaceuticals International Gmbh | Proceso para la síntesis de 4-(3-metanosulfonilfenil)-1-N-propil-piperidina |
| US20110206782A1 (en) * | 2010-02-24 | 2011-08-25 | Auspex Pharmaceuticals, Inc. | Piperidine modulators of dopamine receptor |
| EP2787997A4 (en) * | 2011-12-08 | 2015-05-27 | Ivax Int Gmbh | HYDROBROMIDE SALT OF PRIDOPIDINE |
| BR112014024672A8 (pt) * | 2012-04-04 | 2018-04-03 | Ivax Int Gmbh | Composições farmacêuticas para terapia de combinação |
| CA2913781C (en) * | 2013-06-21 | 2022-05-10 | Teva Pharmaceutical Industries Ltd. | Use of pridopidine for treating huntington's disease |
| CA2937243C (en) | 2014-01-22 | 2023-07-18 | Teva Pharmaceuticals International Gmbh | Modified release formulations of pridopidine |
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