DK2690087T3 - Ny krystalform vii af agomelatin, fremgangsmåde til fremstilling og anvendelse deraf og lægemiddelammensætning der indeholder samme - Google Patents
Ny krystalform vii af agomelatin, fremgangsmåde til fremstilling og anvendelse deraf og lægemiddelammensætning der indeholder samme Download PDFInfo
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- DK2690087T3 DK2690087T3 DK12760538.4T DK12760538T DK2690087T3 DK 2690087 T3 DK2690087 T3 DK 2690087T3 DK 12760538 T DK12760538 T DK 12760538T DK 2690087 T3 DK2690087 T3 DK 2690087T3
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- DK
- Denmark
- Prior art keywords
- agomelatine
- crystalline form
- acetate
- water
- temperature
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/22—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- 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
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
- A61P25/20—Hypnotics; Sedatives
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- 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
- A61P25/22—Anxiolytics
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/22—Separation; Purification; Stabilisation; Use of additives
- C07C231/24—Separation; Purification
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Anesthesiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Battery Electrode And Active Subsutance (AREA)
- Glass Compositions (AREA)
- Analysing Materials By The Use Of Radiation (AREA)
Claims (13)
1. Krystallinsk form af agomelatin, hvis røntgendiffraktionsdiagram har følgende værdier for interplanar krystalafstand d, Bragg-vinkel 2Θ og relativ intensitet:
herunder krystaller, hvis topdiffraktionsvinkler er inden for 2Θ ± 0,2 ° af ovenstående.
2. Fremgangsmåden til fremstilling af den krystallinske form af agomelatin ifølge krav 1, hvor agomelatinforbindelser med formel (II) eller (III) opløses i eddikesyre, hvortil acetat derpå tilsættes, efterfulgt af dråbevis tilsætning af vand til denne reaktionsblanding, som derefter omrøres ved en temperatur på 17-23 °C for at opnå krystallisation, hvorefter krystallerne separeres fra opløsningen.
3. Fremgangsmåden til fremstilling ifølge krav 2, hvor molforholdet mellem agomelatinforbindelser med formel (II) eller (III) og acetat er i størrelsesordenen 1:1-1,5, mest optimalt 1 :1-1,1.
4. Fremgangsmåde til fremstilling ifølge krav 2 eller 3, hvor forholdet mellem volumen eddikesyre og vand er 1 : 10-30.
5. Fremgangsmåde til fremstilling ifølge et hvilket som helst af kravene 2-4, hvor det nævnte acetat er kaliumacetat eller ammoniumacetat.
6. Fremgangsmåde til fremstilling ifølge et hvilket som helst af kravene 2-5, hvorved, når temperaturen af den resulterende reaktionsblanding når 19-25 °C og især ca. 22 °C eller 23 °C, vand tilsættes dråbevist for at frembringe krystallisation.
7. Fremgangsmåde til fremstilling ifølge et hvilket som helst af kravene 2-6, hvor vand tilsættes dråbevis til den resulterende reaktionsblanding, som derefter omrøres ved en temperatur på 20 °C for at opnå krystallisation.
8. Fremgangsmåde til fremstilling ifølge et hvilket som helst af kravene 2-7, hvorved, efter tilsætningen af acetatet, reaktionsblandingen opvarmes til 30-50 °C, hvilket resulterer i en klar opløsning; hvilken nævnte opløsning derefter lades afkøle af sig selv, og hvorefter vand tilsættes dråbevist for at fremkalde krystallisation.
9. Farmaceutisk sammensætning, der indbefatter den krystallinske form af agomelatin ifølge krav 1 og farmaceutisk acceptable adjuvanser eller excipienser.
10. Farmaceutisk sammensætning ifølge krav 9, hvilken sammensætning anvendes ved fremstilling af et medikament, der anvendes til behandling af sygdomme i det melatoninergiske system.
11. Farmaceutisk sammensætning ifølge krav 9, hvilken sammensætning anvendes til fremstilling af et medikament, der anvendes til behandling af søvnforstyrrelser, stress, angst, sæsonbetinget affektiv lidelse, alvorlig depression, hjerte-kar-sygdomme, fordøjelsessystemsygdomme, søvnløshed og træthed, der er forårsaget af jetlag, skizofreni, fobier eller depression.
12. Krystallinsk form af agomelatin ifølge krav 1 til anvendelse i en fremgangsmåde til behandling af sygdomme i det melatoninergiske system.
13. Krystallinsk form af agomelatin ifølge krav 1 til anvendelse i en fremgangsmåde til behandling af søvnforstyrrelser, stress, angst, sæsonbetinget affektiv lidelse, alvorlig depression, kardiovaskulære sygdomme, fordøjelsessystemsygdomme, søvnløshed og træthed forårsaget af jetlag, skizofreni, fobier, eller depression.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2011100708280A CN102690210A (zh) | 2011-03-23 | 2011-03-23 | 阿戈美拉汀的新晶型ⅶ、其制备方法、应用和包含其的药物组合物 |
PCT/CN2012/072816 WO2012126385A1 (zh) | 2011-03-23 | 2012-03-22 | 阿戈美拉汀的新晶型ⅶ、其制备方法、应用和包含其的药物组合物 |
Publications (1)
Publication Number | Publication Date |
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DK2690087T3 true DK2690087T3 (da) | 2017-12-04 |
Family
ID=46855966
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK12760538.4T DK2690087T3 (da) | 2011-03-23 | 2012-03-22 | Ny krystalform vii af agomelatin, fremgangsmåde til fremstilling og anvendelse deraf og lægemiddelammensætning der indeholder samme |
Country Status (32)
Country | Link |
---|---|
US (1) | US9527803B2 (da) |
EP (1) | EP2690087B1 (da) |
JP (1) | JP6203170B2 (da) |
KR (1) | KR20130136544A (da) |
CN (2) | CN102690210A (da) |
AR (1) | AR085543A1 (da) |
AU (1) | AU2012231547B2 (da) |
BR (1) | BR112013024219A2 (da) |
CA (1) | CA2829687C (da) |
CY (1) | CY1119625T1 (da) |
DK (1) | DK2690087T3 (da) |
EA (1) | EA023297B1 (da) |
ES (1) | ES2650604T3 (da) |
GE (1) | GEP20156386B (da) |
HK (1) | HK1193087A1 (da) |
HR (1) | HRP20171831T1 (da) |
HU (1) | HUE037264T2 (da) |
LT (1) | LT2690087T (da) |
MA (1) | MA34958B1 (da) |
MD (1) | MD4391C1 (da) |
ME (1) | ME02921B (da) |
MX (1) | MX355552B (da) |
MY (1) | MY185235A (da) |
NO (1) | NO2690087T3 (da) |
PL (1) | PL2690087T3 (da) |
PT (1) | PT2690087T (da) |
RS (1) | RS56444B1 (da) |
SG (1) | SG193300A1 (da) |
SI (1) | SI2690087T1 (da) |
UA (1) | UA113058C2 (da) |
WO (1) | WO2012126385A1 (da) |
ZA (1) | ZA201306760B (da) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PH12012000132B1 (en) * | 2011-06-09 | 2014-10-20 | Servier Lab | New co-crystals of agomelatine, a process for their preparation and pharmaceutical compositions containing them |
CA2919601C (fr) * | 2013-07-29 | 2018-02-27 | Les Laboratoires Servier | Nouveaux complexes d'agomelatine et d'acides sulfoniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
KR101470794B1 (ko) * | 2014-06-30 | 2014-12-08 | 순천향대학교 산학협력단 | 아고멜라틴 공결정의 제조 방법 및 이를 포함하는 조성물 |
ES2959460T3 (es) | 2015-03-31 | 2024-02-26 | Fis Fabbrica Italiana Sintetici Spa | Forma sólida de agomelatina |
EP3466923A1 (en) | 2017-10-09 | 2019-04-10 | KRKA, d.d., Novo mesto | Process for the preparation of agomelatine in crystalline form |
EP3466413A1 (en) | 2017-10-09 | 2019-04-10 | KRKA, d.d., Novo mesto | Pharmaceutical composition containing agomelatine and process for the preparation thereof |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
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FR2658818B1 (fr) * | 1990-02-27 | 1993-12-31 | Adir Cie | Nouveaux derives a structure naphtalenique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
FR2866335B1 (fr) * | 2004-02-13 | 2006-05-26 | Servier Lab | Nouveau procede de synthese de l'agomelatine |
US7498466B2 (en) * | 2004-02-13 | 2009-03-03 | Les Laboratoires Servier | Process for the synthesis and crystalline form of agomelatine |
FR2889523B1 (fr) * | 2005-08-03 | 2007-12-28 | Servier Lab | Nouvelle forme cristalline v de l'agomelatine, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
FR2889522B1 (fr) | 2005-08-03 | 2007-12-28 | Servier Lab | Nouvelle forme cristalline iv de l'agomelatine, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
FR2889521B1 (fr) * | 2005-08-03 | 2007-12-28 | Servier Lab | Nouvelle forme cristalline iii de l'agomelatine, son procede de preparation et les compositions pharmaceutiques qui la contiennent |
US7358395B2 (en) * | 2005-08-03 | 2008-04-15 | Les Laboratories Servier | Crystalline form V of agomelatine, a process for its preparation and pharmaceutical compositions containing it |
CN101585779B (zh) * | 2009-03-10 | 2014-04-02 | 上海医药工业研究院 | 阿戈美拉汀的晶型vi及其制备方法和应用 |
CN101781225A (zh) | 2009-11-21 | 2010-07-21 | 浙江华海药业股份有限公司 | 一种阿戈美拉汀晶形a制备方法 |
EP2319827A1 (en) * | 2009-11-09 | 2011-05-11 | Ratiopharm GmbH | Process for the production of polymorph form I of agomelatine |
CN101704763B (zh) | 2009-11-25 | 2012-03-28 | 天津泰普药品科技发展有限公司 | 阿戈美拉汀i型晶体的制备方法 |
CN101781226B (zh) * | 2009-12-23 | 2012-03-28 | 天津泰普药品科技发展有限公司 | 阿戈美拉汀及其药物组合物 |
CN101792400B (zh) * | 2010-03-16 | 2013-01-30 | 华东师范大学 | 一种阿戈美拉汀的合成方法 |
CN101921205B (zh) | 2010-08-30 | 2013-11-20 | 江苏恩华药业股份有限公司 | 阿戈美拉汀ⅰ晶型的制备方法 |
CN102452951B (zh) * | 2010-10-25 | 2014-02-19 | 天津泰普药品科技发展有限公司 | 阿戈美拉汀及其药物组合物 |
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2011
- 2011-03-23 CN CN2011100708280A patent/CN102690210A/zh active Pending
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- 2012-03-22 PL PL12760538T patent/PL2690087T3/pl unknown
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- 2012-03-22 HU HUE12760538A patent/HUE037264T2/hu unknown
- 2012-03-22 KR KR1020137027637A patent/KR20130136544A/ko not_active Application Discontinuation
- 2012-03-22 JP JP2014500243A patent/JP6203170B2/ja not_active Expired - Fee Related
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- 2012-03-22 EA EA201301066A patent/EA023297B1/ru not_active IP Right Cessation
- 2012-03-22 BR BR112013024219A patent/BR112013024219A2/pt not_active Application Discontinuation
- 2012-03-22 SI SI201231112T patent/SI2690087T1/sl unknown
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- 2012-03-22 MX MX2013010702A patent/MX355552B/es active IP Right Grant
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- 2012-03-22 NO NO12760538A patent/NO2690087T3/no unknown
- 2012-03-22 CN CN201280013421.7A patent/CN103476742B/zh active Active
- 2012-03-22 US US14/006,468 patent/US9527803B2/en active Active
- 2012-03-22 EP EP12760538.4A patent/EP2690087B1/en active Active
- 2012-03-22 AU AU2012231547A patent/AU2012231547B2/en not_active Ceased
- 2012-03-22 WO PCT/CN2012/072816 patent/WO2012126385A1/zh active Application Filing
- 2012-03-22 MA MA36225A patent/MA34958B1/fr unknown
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- 2014-06-24 HK HK14106353.2A patent/HK1193087A1/xx not_active IP Right Cessation
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