HRP20200927T1 - Kompleksi agomelatina i sulfonskih kiselina, postupak njihove proizvodnje i proizvodnje farmaceutskih pripravaka koji ih sadržavaju - Google Patents
Kompleksi agomelatina i sulfonskih kiselina, postupak njihove proizvodnje i proizvodnje farmaceutskih pripravaka koji ih sadržavaju Download PDFInfo
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- HRP20200927T1 HRP20200927T1 HRP20200927TT HRP20200927T HRP20200927T1 HR P20200927 T1 HRP20200927 T1 HR P20200927T1 HR P20200927T T HRP20200927T T HR P20200927TT HR P20200927 T HRP20200927 T HR P20200927T HR P20200927 T1 HRP20200927 T1 HR P20200927T1
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- 229960002629 agomelatine Drugs 0.000 title claims 20
- YJYPHIXNFHFHND-UHFFFAOYSA-N agomelatine Chemical compound C1=CC=C(CCNC(C)=O)C2=CC(OC)=CC=C21 YJYPHIXNFHFHND-UHFFFAOYSA-N 0.000 title claims 19
- 239000002253 acid Substances 0.000 title claims 8
- 238000000034 method Methods 0.000 title claims 5
- 150000007513 acids Chemical class 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims 6
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims 4
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 206010022437 insomnia Diseases 0.000 claims 4
- 230000007170 pathology Effects 0.000 claims 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 239000002244 precipitate Substances 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 208000027559 Appetite disease Diseases 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 2
- 208000011688 Generalised anxiety disease Diseases 0.000 claims 2
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 206010033664 Panic attack Diseases 0.000 claims 2
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 210000002249 digestive system Anatomy 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 208000029364 generalized anxiety disease Diseases 0.000 claims 2
- 239000004615 ingredient Substances 0.000 claims 2
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims 2
- 208000024714 major depressive disease Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000001193 melatoninergic effect Effects 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 208000019906 panic disease Diseases 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 208000012672 seasonal affective disease Diseases 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 230000035882 stress Effects 0.000 claims 2
- 208000000044 Amnesia Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010039966 Senile dementia Diseases 0.000 claims 1
- 201000001880 Sexual dysfunction Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 229940092714 benzenesulfonic acid Drugs 0.000 claims 1
- 238000009835 boiling Methods 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 239000003433 contraceptive agent Substances 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 150000004682 monohydrates Chemical class 0.000 claims 1
- 230000036651 mood Effects 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
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- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
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- 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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- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
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- 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
- C07C233/18—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 a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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- C07C303/02—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof
- C07C303/22—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof from sulfonic acids, by reactions not involving the formation of sulfo or halosulfonyl groups; from sulfonic halides by reactions not involving the formation of halosulfonyl groups
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Claims (16)
1. Kompleksi agomelatina i sultanske kiseline, naznačeni time, da su predstavljeni formulom (I):
[image]
pri čemu je x 0 ili 1, a RSO3H predstavlja 1,5-naftalendisulfonsku kiselinu ili benzensultansku kiselinu.
2. Kompleks agomelatina formule (I) u skladu s patentnim zahtjevom 1, naznačen time, da je to kompleks agomelatin / 1,5-naftalendisulfonske kiseline (2/1).
3. Kompleks agomelatina formule (I) u skladu s patentnim zahtjevom 2, naznačen time, da ima dijagram rendgenske difrakcije praha, izražen u interplanarnoj udaljenosti d, Braggov kut 2 theta (izražen u ° ±0,2) i relativni intenzitet, kako slijedi:
[image]
uključujući oblike čiji kutovi difrakcije odgovaraju vrijednostima unutar ± 0,2 °.
4. Kompleks agomelatina formule (I) u skladu s patentnim zahtjevom 1, naznačen time, da je to kompleks agomelatin / 1,5-naftalendisulfonska kiselina (2/1) monohidrat.
5. Kompleks agomelatina formule (I) u skladu s patentnim zahtjevom 4, naznačen time, da ima dijagram rendgenske difrakcije praha, izražen u interplanarnoj udaljenosti d, Braggov kut 2 theta (izražen u ° ±0,2) i relativni intenzitet, kako slijedi:
[image]
uključujući oblike čiji kutovi difrakcije odgovaraju vrijednostima unutar ± 0,2 °.
6. Kompleks agomelatina formule (I) u skladu s patentnim zahtjevom 1, naznačen time, da je to kompleks agomelatin / benzensulfonska kiselina (2/1).
7. Kompleks agomelatina formule (I) u skladu s patentnim zahtjevom 6, naznačen time, da ima dijagram rendgenske difrakcije praha, izražen u interplanarnoj udaljenosti d, Braggov kut 2 theta (izražen u ° ± 0,2) i relativni intenzitet, kako slijedi:
[image]
uključujući oblike čiji kutovi difrakcije odgovaraju vrijednostima unutar ± 0,2
8. Postupak za dobivanje kompleksa agomelatina i sulfonske kiseline u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time, da:
- agomelatin i sulfonska kiselina se pomiješaju u organskom ili vodeno-organskom otapalu u željenim omjerima;
- dobivena otopina se miješa i po želji zagrijava na temperaturi ne većoj od vrelišta odabranog otapala;
- smjesa se hladi, uz miješanje, i kokristal se taloži prirodno ili se taloži nakon što je uklonjena u drugo otapalo;
- dobiveni talog se filtrira i suši.
9. Postupak za pripravu kompleksa agomelatina i sultanske kiseline u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time, da se dva sastojka zajedno melju.
10. Postupak za pripravu kompleksa agomelatina i sultanske kiseline u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time, da se dva sastojka miješaju u organskom ili vodeno-organskom otapalu, a zatim zamrzavaju i suše na vrlo niskoj temperaturi.
11. Postupak za pripravu kompleksa agomelatina i sultanske kiseline u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time, da se praškovi agomelatina i dotične kiseline pomiješaju u miješalici i smjesa se zatim ekstrudira dvostrukim vijkom bez matrice kako bi se dobilo čvrsto zrno izravno na izlazu ekstrudera.
12. Farmaceutski pripravci, naznačeni time, da sadržavaju kao aktivni sastojak jedan od kompleksa agomelatina i sultanske kiseline u skladu s bilo kojim od patentnih zahtjeva 1 do 7, u kombinaciji s jednim ili više inertnih, netoksičnih, farmaceutski prihvatljivih nosača.
13. Upotreba farmaceutskih pripravaka u skladu s patentnim zahtjevom 12, naznačena time, da se koriste u proizvodnji lijekova za liječenje poremećaja melatoninergičkog sustava.
14. Upotreba farmaceutskih pripravaka u skladu s patentnim zahtjevom 12, naznačena time, da se koriste u proizvodnji lijekova za liječenje stresa, poremećaja spavanja, anksioznih poremećaja i posebno generaliziranog anksioznog poremećaja, opsesivno- kompulzivnih poremećaja, poremećaja raspoloženja i posebno bipolarnih poremećaja, velike depresije, sezonskog afektivnog poremećaja, kardiovaskularnih patologija, patologije probavnog sustava, nesanice i umora zbog jet-laga, shizofrenije, napada panike, melankolije, poremećaja apetita, pretilosti, nesanice, boli, psihotičnih poremećaja, epilepsije, dijabetesa, Parkinsonove bolesti, senilne demencije, različitih poremećaja povezanih s normalnim ili patološkim starenjem, migrene, gubitka pamćenja, Alzheimerove bolesti, kao i kod poremećaja cerebralne cirkulacije, te kod seksualnih disfunkcija, kao inhibitora ovulacije i imunomodulatora i u liječenju karcinoma.
15. Kompleksi agomelatina i sulfonske kiseline formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačeni time, da se liječe poremećaji melatoninergičkog sustava.
16. Kompleksi agomelatina i sulfonske kiseline formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačeni time, da se koriste za liječenje stresa, poremećaja spavanja, anksioznih poremećaja i posebno generaliziranog anksioznog poremećaja, opsesivno-kompulzivnih poremećaja, poremećaja raspoloženja i posebno bipolarnih poremećaja, velike depresije, sezonskog afektivnog poremećaja, kardiovaskularne patologije, patologije probavnog sustava, nesanice i umora zbog jet- laga, shizofrenije, napada panike, melankolije, poremećaja apetita, pretilosti, nesanice, boli, psihotičnih poremećaja, epilepsije, dijabetesa, Parkinsonove bolesti, senilne demencije, raznih poremećaja povezanih s normalnim ili patološkim starenjem, migrene, gubitka pamćenja, Alzheimerove bolesti, kao i kod poremećaja cerebralne cirkulacije, te kod seksualnih disfunkcija, kao inhibitora ovulacije i imunomodulatora i u liječenju karcinoma.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2013/080337 WO2015013865A1 (en) | 2013-07-29 | 2013-07-29 | Agomelatine sulfonic acids complexes and preparation thereof |
| FR1360124A FR3012142B1 (fr) | 2013-10-17 | 2013-10-17 | Nouveaux complexes d'agomelatine et d'acides sulfoniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| PCT/FR2014/051944 WO2015015102A2 (fr) | 2013-07-29 | 2014-07-28 | Nouveaux complexes d'agomelatine et d'acides sulfoniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| EP14758162.3A EP3027588B1 (fr) | 2013-07-29 | 2014-07-28 | Complexes d'agomélatine et d'acides sulfoniques, procédé de leur préparation et compositions pharmaceutiques qui les contiennent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20200927T1 true HRP20200927T1 (hr) | 2020-09-18 |
Family
ID=51453772
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20200927TT HRP20200927T1 (hr) | 2013-07-29 | 2020-06-10 | Kompleksi agomelatina i sulfonskih kiselina, postupak njihove proizvodnje i proizvodnje farmaceutskih pripravaka koji ih sadržavaju |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US9573891B2 (hr) |
| EP (1) | EP3027588B1 (hr) |
| JP (1) | JP6595990B2 (hr) |
| CN (1) | CN105473547B (hr) |
| AU (1) | AU2014298304B2 (hr) |
| CA (1) | CA2919601C (hr) |
| CY (1) | CY1123214T1 (hr) |
| DK (1) | DK3027588T3 (hr) |
| EA (1) | EA031237B1 (hr) |
| ES (1) | ES2792248T3 (hr) |
| HK (2) | HK1218745A1 (hr) |
| HR (1) | HRP20200927T1 (hr) |
| HU (1) | HUE049928T2 (hr) |
| LT (1) | LT3027588T (hr) |
| ME (1) | ME03741B (hr) |
| MX (1) | MX369303B (hr) |
| NZ (1) | NZ716151A (hr) |
| PL (1) | PL3027588T3 (hr) |
| PT (1) | PT3027588T (hr) |
| RS (1) | RS60440B1 (hr) |
| RU (1) | RU2673080C2 (hr) |
| SG (1) | SG11201600006RA (hr) |
| SI (1) | SI3027588T1 (hr) |
| UA (1) | UA116811C2 (hr) |
| WO (1) | WO2015015102A2 (hr) |
| ZA (1) | ZA201600448B (hr) |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0706044D0 (en) * | 2007-03-28 | 2007-05-09 | Syngenta Ltd | C0-Crystals |
| WO2009140466A2 (en) * | 2008-05-14 | 2009-11-19 | Dr. Reddy's Laboratories Ltd. | Linezolid co-crystals |
| CN101481321B (zh) * | 2009-02-27 | 2012-04-18 | 上海医药工业研究院 | 阿戈美拉汀卤化氢复合物及其制备方法 |
| CN102690209A (zh) * | 2011-03-23 | 2012-09-26 | 上海医药工业研究院 | 阿戈美拉汀的混晶(形式-ⅷ)、其制备方法、应用和包含其的药物组合物 |
| CN102690210A (zh) * | 2011-03-23 | 2012-09-26 | 上海医药工业研究院 | 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 |
| PL2517700T3 (pl) * | 2011-04-28 | 2013-12-31 | Zentiva Ks | Farmaceutyczne dopuszczalne kokryształy n-[2-(7-metoksy-1-naftylo]acetamidu i sposoby ich wytwarzania |
| 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 |
| CN102702041B (zh) * | 2012-05-14 | 2013-08-14 | 上海右手医药科技开发有限公司 | 阿戈美拉汀苯磺酸类复合物及其制备方法 |
| CN102718675B (zh) * | 2012-06-07 | 2015-03-25 | 上海右手医药科技开发有限公司 | 阿戈美拉汀甲磺酸复合物及其制备方法 |
| US9409857B2 (en) | 2012-05-14 | 2016-08-09 | Shanghai Righthand Pharmtech, Co., Ltd. | Agomelatine sulfuric acid complex, and preparation method and application thereof |
-
2014
- 2014-07-28 DK DK14758162.3T patent/DK3027588T3/da active
- 2014-07-28 MX MX2016001219A patent/MX369303B/es active IP Right Grant
- 2014-07-28 AU AU2014298304A patent/AU2014298304B2/en not_active Ceased
- 2014-07-28 ES ES14758162T patent/ES2792248T3/es active Active
- 2014-07-28 JP JP2016530580A patent/JP6595990B2/ja not_active Expired - Fee Related
- 2014-07-28 NZ NZ716151A patent/NZ716151A/en not_active IP Right Cessation
- 2014-07-28 EA EA201600142A patent/EA031237B1/ru not_active IP Right Cessation
- 2014-07-28 HU HUE14758162A patent/HUE049928T2/hu unknown
- 2014-07-28 LT LTEP14758162.3T patent/LT3027588T/lt unknown
- 2014-07-28 UA UAA201601715A patent/UA116811C2/uk unknown
- 2014-07-28 SG SG11201600006RA patent/SG11201600006RA/en unknown
- 2014-07-28 SI SI201431601T patent/SI3027588T1/sl unknown
- 2014-07-28 CN CN201480042633.7A patent/CN105473547B/zh active Active
- 2014-07-28 WO PCT/FR2014/051944 patent/WO2015015102A2/fr active Application Filing
- 2014-07-28 RS RS20200720A patent/RS60440B1/sr unknown
- 2014-07-28 PL PL14758162T patent/PL3027588T3/pl unknown
- 2014-07-28 EP EP14758162.3A patent/EP3027588B1/fr active Active
- 2014-07-28 CA CA2919601A patent/CA2919601C/fr not_active Expired - Fee Related
- 2014-07-28 RU RU2016106958A patent/RU2673080C2/ru active
- 2014-07-28 US US14/907,670 patent/US9573891B2/en active Active
- 2014-07-28 PT PT147581623T patent/PT3027588T/pt unknown
- 2014-07-28 ME MEP-2020-125A patent/ME03741B/me unknown
-
2016
- 2016-01-20 ZA ZA2016/00448A patent/ZA201600448B/en unknown
- 2016-06-13 HK HK16106760.7A patent/HK1218745A1/zh unknown
- 2016-09-27 HK HK16111309.5A patent/HK1223088A1/zh unknown
-
2020
- 2020-06-10 HR HRP20200927TT patent/HRP20200927T1/hr unknown
- 2020-06-19 CY CY20201100565T patent/CY1123214T1/el unknown
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