HRP20140752T1 - Kristalni oblici 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli, farmaceutski pripravci koji ih sadrže i postupak za njihovu proizvodnju - Google Patents
Kristalni oblici 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli, farmaceutski pripravci koji ih sadrže i postupak za njihovu proizvodnju Download PDFInfo
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- HRP20140752T1 HRP20140752T1 HRP20140752AT HRP20140752T HRP20140752T1 HR P20140752 T1 HRP20140752 T1 HR P20140752T1 HR P20140752A T HRP20140752A T HR P20140752AT HR P20140752 T HRP20140752 T HR P20140752T HR P20140752 T1 HRP20140752 T1 HR P20140752T1
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- 238000004519 manufacturing process Methods 0.000 title claims 9
- 238000000034 method Methods 0.000 title claims 9
- JKEBMURXLKGPLR-UHFFFAOYSA-N 5-amino-2,3-dihydrophthalazine-1,4-dione;sodium Chemical compound [Na].O=C1NNC(=O)C2=C1C(N)=CC=C2 JKEBMURXLKGPLR-UHFFFAOYSA-N 0.000 title claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 title claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 16
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 12
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 12
- 239000000047 product Substances 0.000 claims 6
- 239000013078 crystal Substances 0.000 claims 5
- 238000002156 mixing Methods 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 5
- HWYHZTIRURJOHG-UHFFFAOYSA-N luminol Chemical compound O=C1NNC(=O)C2=C1C(N)=CC=C2 HWYHZTIRURJOHG-UHFFFAOYSA-N 0.000 claims 4
- 238000004090 dissolution Methods 0.000 claims 2
- 238000001035 drying Methods 0.000 claims 2
- 239000012065 filter cake Substances 0.000 claims 2
- 238000001914 filtration Methods 0.000 claims 2
- 210000000987 immune system Anatomy 0.000 claims 2
- 239000002244 precipitate Substances 0.000 claims 2
- 238000005406 washing Methods 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 238000000354 decomposition reaction Methods 0.000 claims 1
- 238000010586 diagram Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 238000011301 standard therapy Methods 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
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- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
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- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
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Claims (13)
1. Kristalni oblici I ili II 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli, naznačen time što su kristalografske vrijednosti utvrđene rendgenskim zrnastim dijagramom:
d-vrijednosti: 13,5; 6,9; 5,2; 4,6; 3,9; 3,5; 3,4; 3,3; 3,1; 3,0 i
2-teta-vrijednosti: 6,5; 12,7; 16,9; 19,3; 22,8; 25,8; 26,6; 27,2; 28,7; 30,3
za oblik I
i
d-vrijednosti: 12,9; 7,9; 7,1; 6,5; 5,3; 4,0; 3,7; 3,6; 3,3; 3,2 i
2-teta-vrijednosti: 6,8; 11,2; 12,5; 13,7; 16,7; 22,4; 24,3; 24,9; 27,2; 27,8
za oblik II,
nadalje naznačen time što je temperatura razlaganja ≥ 335 °C ± 10 °C.
2. Kristalni oblik I ili II prema zahtjevu 1, naznačen time što je sadržaj vode od kristalizacije ≤ 0,4 %.
3. Postupak za proizvodnju kristalnog oblika I 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli prema zahtjevu 1 ili 2, naznačen miješanjem 5-amino-2,3-dihidroftalazin-1,4-diona s otopinom natrijeva hidroksida i dodavanjem etanola, čime se produkt topljivosti nastalog 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli spušta tako da se isti taloži, pri čemu se nataloženi kristalni produkt odvaja i suši, pri čemu je kristalni oblik I višestruko suspendiran u etanolu, miješan ponovno ispiran etanolom, i potom ponovno sušen.
4. Postupak za proizvodnju kristalnog oblika I prema zahtjevu 3, naznačen time što se dodaje etanol stupnja čistoće ≥ 98 %, osobito poželjno ≥ 99 %, na sobnoj temperaturi unutar 10 - 40 minuta, poželjno 20 minuta.
5. Postupak za izradu kristalnog oblika I prema zahtjevu 3 ili 4, koji obuhvaća faze:
a) Proizvodnje smjese od 1.0 - 1.4 ekvivalenta natrijeva hidroksida, poželjno 1.2 ekvivalenta, sa 4 - 7 ekvivalenata (vol/m) vode, poželjno 6 ekvivalenata (vol/m) vode;
b) Dodavanje 1 ekvivalenta luminola u ovu smjesu i miješanje do potpunog otapanja;
c) Dodavanje 50 - 70 ekvivalenata, poželjno 60 ekvivalenata (vol/m) etanola stupnja čistoće ≥ 98 %, naročito poželjno ≥ 99 %, na sobnoj temperaturi (25 °C ± 5 °C) unutar 10 - 40 minuta, poželjno 20 minuta;
d) Nakon potpunog dodavanja etanola, ponovno miješanje reakcijske smjese na sobnoj temperaturu maksimalno 20 sati, poželjno 2 - 8 sati, osobito poželjno 8 sati, i filtriranje ove smjese;
e) Pranje filterskog kolača sa 10 - 15 ekvivalenata (vol/m) etanola, poželjno 13 ekvivalenata (vol/m) etanola stupnja čistoće ≥ 98 %, osobito poželjno ≥ 99 %;
f) Sušenje proizvoda u vakuumskoj sušari na 50 - 90 °C /1 - 3 mbara, poželjno 70 °C - 90 °C, osobito poželjno 80 °C - 90 °C, ili na rotacijskom isparivaču na 20 ± 10 mbara i 50 °C - 90 °C, poželjno 70 °C - 90 °C, osobito poželjno 80 °C - 90 °C, do ostvarivanja konstantnosti masa.
6. Postupak za proizvodnju kristalnog oblika II 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli prema zahtjevu 1 ili 2, naznačen time što se miješa 5-amino-2,3-dihidroftalazin-1,4-dion s otopinom natrijeva hidroksida i dodaje 2-propanol, uslijed čega se produkt topljivosti nastalog 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli spušta tako da se na kraju taloži, pri čemu se nataloženi kristalni produkt odvaja i suši.
7. Postupak za izradu kristalnog oblika II prema zahtjevu 6, naznačen dodavanjem 2-propanola stupnja čistoće ≥ 98 %, osobito poželjno ≥ 99 %, na sobnoj temperaturi unutar 10 - 40 minuta, poželjno 20 minuta.
8. Postupak za izradu kristalnog oblika II prema zahtjevu 6 ili 7, koji obuhvaća faze:
a) Proizvodnja smjese od 1.0 - 2.0 ekvivalenta natrijeva hidroksida, poželjno 1.1 - 1.4 ekvivalenta, osobito poželjno 1.2 ekvivalenta, sa 6 - 7.5 ekvivalenta (vol/m) vode, poželjno 6 ekvivalenata (vol/m) vode;
b) Dodavanje 0.5 - 1 ekvivalenta luminola i miješanje smjese do ostvarivanja potpunog otapanja;
c) Dodavanje 60 ekvivalenata (vol/m) 2-propanola stupnja čistoće ≥ 98 %, osobito poželjno ≥ 99 %, unutar 20 ± 10 minuta, na sobnoj temperaturi (25 °C ± 5 °C);
d) Miješanje suspenzije na sobnoj temperaturi (25 °C ± 5 °C) najmanje 1 sat;
e) Filtriranje i ispiranje filterskog kolača sa 13 - 15 ekvivalenata (vol/m) 2 - propanola stupnja čistoće ≥ 98 %, osobito poželjno ≥ 99 %;
f) Sušenje produkta u vakuumskoj sušari na 85 °C - 120 °C /1 - 3 mbara, poželjno 90 °C - 100 °C, osobito poželjno 90 °C, ili na rotacijskom isparivaču na 20 ± 10 mbara i 85 °C - 120 °C, poželjno 90 °C - 100 °C, osobito poželjno 90 °C, do ostvarivanja konstantnosti mase.
9. Farmaceutski pripravak, naznačen time što sadrži kristalni oblik I i / ili kristalni oblik II prema zahtjevu 1 ili 2.
10. Farmaceutski pripravak prema zahtjevu 9, naznačen kombinacijom sa drugim aktivnim sastojcima i / ili dodacima.
11. Farmaceutski pripravak prema zahtjevu 9 ili 10, naznačen time što je moguće uključiti farmaceutski prihvatljive pomoćne tvari.
12. Kristalni oblik I i / ili kristalni oblik II prema zahtjevu 1 ili 2 i / ili farmaceutski pripravak prema najmanje jednom od zahtjeva 9 do 11 za primjenu u postupku modulacije imunološkog sustava.
13. Kristalni oblik I i / ili kristalni oblik II prema zahtjevu 1 ili 2 i / ili farmaceutska priprema prema najmanje jednom od zahtjeva 9 do 11 za primjenu u postupku modulacije imunološkog sustava u kombinaciji sa standardnim terapijama.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10002067 | 2010-03-01 | ||
EP10075744 | 2010-11-25 | ||
PCT/EP2011/001124 WO2011107295A1 (de) | 2010-03-01 | 2011-03-01 | Kristalline formen zu 5-amino-2,3-dihydrophthalazin-1,4-dion natriumsalz, diese enthaltende pharmazeutische zubereitungen und verfahren zu ihrer herstellung |
Publications (1)
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HRP20140752T1 true HRP20140752T1 (hr) | 2014-10-24 |
Family
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HRP20140752AT HRP20140752T1 (hr) | 2010-03-01 | 2014-08-06 | Kristalni oblici 5-amino-2,3-dihidroftalazin-1,4-dion natrijeve soli, farmaceutski pripravci koji ih sadrže i postupak za njihovu proizvodnju |
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Country | Link |
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US (2) | US8772294B2 (hr) |
EP (2) | EP2774920A1 (hr) |
JP (2) | JP6061081B2 (hr) |
KR (1) | KR101770011B1 (hr) |
CN (3) | CN105726541A (hr) |
AU (1) | AU2011223226B2 (hr) |
BR (1) | BR112012021857B1 (hr) |
CA (1) | CA2791327C (hr) |
CH (1) | CH704794B1 (hr) |
CY (1) | CY1115585T1 (hr) |
DK (1) | DK2542535T3 (hr) |
ES (1) | ES2487221T3 (hr) |
HK (2) | HK1223929A1 (hr) |
HR (1) | HRP20140752T1 (hr) |
IL (1) | IL221680A (hr) |
NZ (1) | NZ601689A (hr) |
PL (1) | PL2542535T3 (hr) |
PT (1) | PT2542535E (hr) |
RS (1) | RS53492B1 (hr) |
RU (1) | RU2585677C2 (hr) |
SI (1) | SI2542535T1 (hr) |
WO (1) | WO2011107295A1 (hr) |
ZA (1) | ZA201206264B (hr) |
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EP2774920A1 (de) * | 2010-03-01 | 2014-09-10 | MetrioPharm AG | Kristalline formen von 5-amino-2,3-dihydrophthalazin-1,4-dion natriumsalz und ihre medizinische verwendung |
WO2016096143A1 (de) | 2014-12-18 | 2016-06-23 | Metriopharm Ag | Kristalline form von 5-amino-2,3-dihydrophthalazin-1,4-dion natriumsalz, diese enthaltende pharmazeutische zubereitungen und verfahren zu ihrer herstellung |
ES2797299T3 (es) * | 2016-02-16 | 2020-12-01 | Metriopharm Ag | Forma cristalina de 5-amino-2,3-dihidroftalazina-1,4-diona |
US11203575B2 (en) * | 2016-02-16 | 2021-12-21 | Metriopharm Ag | Methhod for producing a crystalline form of 5-amino-2,3-dihydrophthalazine-1,4-dione |
EP3248602A1 (en) | 2016-05-26 | 2017-11-29 | MetrioPharm AG | Use of 5-amino-2,3-dihydro-1,4-phthalazinedione in the treatment of inflammatory and/or degenerative disorders of the tendons, ligaments of the joints, articular capsules and bursae |
RU2625267C1 (ru) * | 2016-09-22 | 2017-07-12 | Общество с ограниченной ответственностью "АБИДАФАРМА" | Способ производства нестерильных субстанций безводного "тамерита" и/или двухводного "галавита" - натриевых солей 5-амино-2,3-дигидрофталазин-1,4-диона (варианты) и способы дальнейшей их переработки в стерильные лекарственные препараты |
CA3042956A1 (en) * | 2016-11-07 | 2018-05-11 | Metriopharm Ag | Use of 5-amino-2,3-dihydro-1,4-phthalazinedione in the treatment of chronic progressive multiple sclerosis |
CN106810501B (zh) * | 2017-01-23 | 2019-09-10 | 湖北新德晟材料科技有限公司 | 一种利用一锅法合成鲁米诺或异鲁米诺的方法 |
RU2635769C1 (ru) * | 2017-02-08 | 2017-11-15 | Адмир Мусаевич Абидов | Лекарственный препарат на основе 5-амино-2,3-дигидрофталазин-1,4-диона в виде быстрорастворимой пленки для трансбуккального введения |
RU2673452C1 (ru) * | 2017-08-15 | 2018-11-27 | Межрегиональное общественное учреждение "Институт инженерной физики" | Способ получения активной фармацевтической субстанции, представляющей собой аминодигидрофталазиндион натрия |
EP3511325A1 (en) | 2018-01-11 | 2019-07-17 | MetrioPharm AG | Method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione |
EP3870175A1 (en) * | 2018-10-26 | 2021-09-01 | Immunopharma Plus D.o.o | Oral aminodihydrophthalazinedione compositions and their use the treatment of non-viral hepatitis |
EP3858358A1 (en) | 2020-01-31 | 2021-08-04 | MetrioPharm AG | Use of 5-amino-2,3-dihydro-1,4-phthalazinedione in the treatment of rare chronic inflammatory pulmonary diseases |
EP3858328A1 (en) | 2020-01-31 | 2021-08-04 | MetrioPharm AG | Use of 5-amino-2,3-dihydro-1,4-phthalazinedione in the inhalatory treatment of inflammatory pulmonary diseases |
WO2021190783A1 (en) | 2020-03-25 | 2021-09-30 | Metriopharm Ag | 5-amino-2,3-dihydro-1,4-phthalazinedione for treatment of acute lung injury |
EP3981405A1 (en) | 2020-10-08 | 2022-04-13 | MetrioPharm AG | Compound for the treatment of coronaviral infections |
JP2023529022A (ja) | 2020-06-10 | 2023-07-06 | メトリオファーム アーゲー | コロナウイルス感染症の治療のための化合物 |
KR20230038228A (ko) | 2020-07-09 | 2023-03-17 | 메트리오팜 아게 | 글루코코르티코이드 절약제 |
JP2024516340A (ja) | 2020-12-02 | 2024-04-15 | メトリオファーム アーゲー | Sars-cov-2感染の後遺症の予防と治療のためのルミノール |
RU2756568C1 (ru) * | 2021-03-24 | 2021-10-01 | Акционерное общество "Щелково Агрохим" | Способ получения натриевой соли 5-амино-2,3-дигидро-1,4-фталазиндиона в гидратированной или безводной форме |
EP4193994A1 (en) | 2021-12-08 | 2023-06-14 | MetrioPharm AG | Combination of 5-amino-2,3-dihydro-1,4-phtalazinedione and a 6'-methoxycinchonan-9-ol for use in the treatment of coronaviral infections |
EP4209219A1 (en) | 2022-01-07 | 2023-07-12 | MetrioPharm AG | Combination of budesonide and 5-amino-2,3-dihydro-1,4-phtalazinedione |
EP4248963A1 (en) | 2022-03-25 | 2023-09-27 | MetrioPharm AG | Combination of 5-amino-2,3-dihydro-1,4-phtalazinedione and a fumaric acid ester |
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CN1089086C (zh) * | 1988-03-31 | 2002-08-14 | 兰德尔·L·米尔斯 | 鲁米纳得类药物 |
CH683965A5 (it) | 1993-02-19 | 1994-06-30 | Limad Marketing Exp & Imp | Composti della classe dei ftalidrazidici come sostanza attiva in agenti antinfiammatori ed antitossici. |
CH683966A5 (it) | 1993-02-19 | 1994-06-30 | Limad Marketing Exp & Imp | Composti della classe dei ftalidrazidici come sostanze attive in agenti anti-ipossici e di difesa. |
RU2113222C1 (ru) * | 1997-09-30 | 1998-06-20 | Закрытое акционерное общество "Центр современной медицины "Медикор" | Иммуномодулирующее средство |
RU2138264C1 (ru) | 1999-05-06 | 1999-09-27 | Абидов Муса Тажудинович | Способ получения лекарственного препарата галавит |
US6489326B1 (en) * | 2000-03-28 | 2002-12-03 | Anatoliy Ivanovich Pavlov | Medicinal preparation and process for manufacturing thereof |
RU2167659C1 (ru) | 2000-08-02 | 2001-05-27 | Закрытое акционерное общество "Центр современной медицины "Медикор" | Способ коррекции иммунной системы живого организма |
RU2169139C1 (ru) | 2000-08-02 | 2001-06-20 | Закрытое акционерное общество "Центр современной медицины "Медикор" | Способ получения щелочных и щелочноземельных солей 5-амино-2,3-дигидро-1,4-фталазиндиона |
RU2211036C2 (ru) | 2001-11-20 | 2003-08-27 | Общество с ограниченной ответственностью "Абидофарма" | Лекарственный препарат (варианты) и способ его производства |
RU2222327C2 (ru) | 2002-03-22 | 2004-01-27 | Общество с ограниченной ответственностью "Абидофарма" | Способ получения лекарственного препарата |
US7326690B2 (en) | 2002-10-30 | 2008-02-05 | Bach Pharma, Inc. | Modulation of cell fates and activities by phthalazinediones |
RU2238730C1 (ru) | 2003-02-17 | 2004-10-27 | Абидов Муса Тажудинович | Лекарственный препарат |
RU2233161C1 (ru) | 2003-04-18 | 2004-07-27 | Общество с ограниченной ответственностью "Абидофарма" | Лекарственный препарат (варианты) и способ его производства |
CN1217193C (zh) * | 2003-07-30 | 2005-08-31 | 中国药科大学 | 心肌肌钙蛋白鲁米诺化学发光免疫分析检测方法 |
US8592421B2 (en) | 2003-08-04 | 2013-11-26 | Valery Khazhmuratovich Zhilov | Cyclic bioisosters of purine system derivatives and a pharmaceutical composition based thereon |
PL231885B1 (pl) | 2009-01-16 | 2019-04-30 | Abidopharma Spolka Z Ograniczona Odpowiedzialnoscia | Sposób wytwarzania soli 5-amino-2,3-dihydroftalazyno-1,4-di onu z metalami alkalicznymi, ich kompozycje farmaceutyczne i ich zastosowanie |
US20100222584A1 (en) | 2009-02-06 | 2010-09-02 | Bach Pharma, Inc. | Pharmaceutical grade phthalazinediones, process for their preparation and pharmaceutical compositions containing them |
EP2774920A1 (de) * | 2010-03-01 | 2014-09-10 | MetrioPharm AG | Kristalline formen von 5-amino-2,3-dihydrophthalazin-1,4-dion natriumsalz und ihre medizinische verwendung |
-
2011
- 2011-03-01 EP EP14001134.7A patent/EP2774920A1/de not_active Withdrawn
- 2011-03-01 CN CN201610087203.8A patent/CN105726541A/zh active Pending
- 2011-03-01 US US13/582,522 patent/US8772294B2/en active Active
- 2011-03-01 CH CH01123/12A patent/CH704794B1/de not_active IP Right Cessation
- 2011-03-01 ES ES11710423.2T patent/ES2487221T3/es active Active
- 2011-03-01 DK DK11710423.2T patent/DK2542535T3/da active
- 2011-03-01 AU AU2011223226A patent/AU2011223226B2/en active Active
- 2011-03-01 SI SI201130233T patent/SI2542535T1/sl unknown
- 2011-03-01 CN CN201610087179.8A patent/CN105859634B/zh active Active
- 2011-03-01 NZ NZ601689A patent/NZ601689A/en unknown
- 2011-03-01 EP EP11710423.2A patent/EP2542535B1/de active Active
- 2011-03-01 RU RU2012141274/04A patent/RU2585677C2/ru active
- 2011-03-01 JP JP2012555335A patent/JP6061081B2/ja active Active
- 2011-03-01 PL PL11710423T patent/PL2542535T3/pl unknown
- 2011-03-01 KR KR1020127025234A patent/KR101770011B1/ko active IP Right Grant
- 2011-03-01 CA CA2791327A patent/CA2791327C/en active Active
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- 2011-03-01 CN CN201180011760.7A patent/CN102971300B/zh active Active
- 2011-03-01 WO PCT/EP2011/001124 patent/WO2011107295A1/de active Application Filing
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