HRP20170023T1 - Kristalni oblik pemirolasta - Google Patents
Kristalni oblik pemirolasta Download PDFInfo
- Publication number
- HRP20170023T1 HRP20170023T1 HRP20170023TT HRP20170023T HRP20170023T1 HR P20170023 T1 HRP20170023 T1 HR P20170023T1 HR P20170023T T HRP20170023T T HR P20170023TT HR P20170023 T HRP20170023 T HR P20170023T HR P20170023 T1 HRP20170023 T1 HR P20170023T1
- Authority
- HR
- Croatia
- Prior art keywords
- sodium
- pemirolast
- compound according
- solvent
- crystallization
- Prior art date
Links
- HIANJWSAHKJQTH-UHFFFAOYSA-N pemirolast Chemical compound CC1=CC=CN(C2=O)C1=NC=C2C=1N=NNN=1 HIANJWSAHKJQTH-UHFFFAOYSA-N 0.000 title claims 3
- 229960004439 pemirolast Drugs 0.000 title claims 3
- 150000001875 compounds Chemical class 0.000 claims 5
- KYIZZXKWRKKFSQ-UHFFFAOYSA-N sodium 9-methyl-3-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)pyrido[1,2-a]pyrimidin-4-one Chemical compound [Na+].CC1=CC=CN(C2=O)C1=NC=C2C1=NN=N[N-]1 KYIZZXKWRKKFSQ-UHFFFAOYSA-N 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical group OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 239000003125 aqueous solvent Substances 0.000 claims 2
- 238000002425 crystallisation Methods 0.000 claims 2
- 230000008025 crystallization Effects 0.000 claims 2
- 238000004090 dissolution Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 229910052708 sodium Inorganic materials 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 239000012296 anti-solvent Substances 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 230000018044 dehydration Effects 0.000 claims 1
- 238000006297 dehydration reaction Methods 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- -1 sodium alkoxide Chemical class 0.000 claims 1
- 159000000000 sodium salts Chemical class 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
-
- 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
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Claims (8)
1. Hemihidratni oblik natrijeve soli pemirolasta.
2. Spoj prema zahtjevu 1, koji je više od 60% kristalan.
3. Spoj prema zahtjevu 1 ili zahtjevu 2, koji sadrži manje od 5% drugih kristalnih oblika pemirolast natrija.
4. Spoj prema bilo kojem od prethodnih zahtjeva naznačen X-ray difrakcijskim uzorkom praška koji sadrži karakteristične kristalne pikove sa 2-theta vrijednosti (u stupnjevima) od oko 26.6, 25.3, 13.0, 15.3, 18.2 i/ili 28.4.
5. Postupak za proizvodnju spoja prema bilo kojem od zahtjeva 1-4, koji sadrži reagiranje pemirolasta sa bazom koja sadrži natrij, prije kristalizacije iz otapala.
6. Postupak prema zahtjevu 5 gdje je baza natrij hidroksid ili natrij alkoksid, i/ili je otapalo metanol ili etanol.
7. Postupak prema zahtjevu 5 ili zahtjevu 6, gdje kristalizacija sadrži:
(a) djelomično otapanje pemirolast natrija u otapalu, u prisutnosti ne više od 9% (w/w, kao razmjer otapala) vode;
(b) djelomično otapanje pemirolast natrija u vodenom otapalu i filtracija pri 64.8°C ili više; ili
(c) otapanje pemirolast natrija u vodenom otapalu popraćeno dodavanjem suviška antiotapala.
8. Postupak za proizvodnju spoja prema bilo kojem od zahtjeva 1 do 4, koji sadrži dehidraciju višeg hidrata pemirolast natrija.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18734809P | 2009-06-16 | 2009-06-16 | |
| US18735509P | 2009-06-16 | 2009-06-16 | |
| PCT/GB2010/001168 WO2010146348A2 (en) | 2009-06-16 | 2010-06-15 | New crystalline form of pemirolast |
| EP10732402.2A EP2443120B1 (en) | 2009-06-16 | 2010-06-15 | Crystalline form of pemirolast |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170023T1 true HRP20170023T1 (hr) | 2017-03-10 |
Family
ID=43264726
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170023TT HRP20170023T1 (hr) | 2009-06-16 | 2017-01-10 | Kristalni oblik pemirolasta |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US20120157415A1 (hr) |
| EP (2) | EP2443120B1 (hr) |
| JP (2) | JP5722317B2 (hr) |
| KR (2) | KR20120032530A (hr) |
| CN (1) | CN102596202B (hr) |
| AR (1) | AR077915A1 (hr) |
| AU (1) | AU2010261540B2 (hr) |
| BR (1) | BRPI1015559A2 (hr) |
| CA (1) | CA2765408A1 (hr) |
| CY (1) | CY1118413T1 (hr) |
| DK (1) | DK2443120T3 (hr) |
| EA (1) | EA025865B1 (hr) |
| ES (1) | ES2613059T3 (hr) |
| HR (1) | HRP20170023T1 (hr) |
| HU (1) | HUE032978T2 (hr) |
| IL (1) | IL216670A (hr) |
| LT (1) | LT2443120T (hr) |
| ME (1) | ME02685B (hr) |
| MX (1) | MX2011013676A (hr) |
| NZ (1) | NZ596747A (hr) |
| PL (1) | PL2443120T3 (hr) |
| PT (1) | PT2443120T (hr) |
| RS (1) | RS55558B1 (hr) |
| SA (1) | SA114350792B1 (hr) |
| SG (1) | SG176295A1 (hr) |
| SI (1) | SI2443120T1 (hr) |
| SM (1) | SMT201700085B (hr) |
| TW (1) | TWI504599B (hr) |
| UY (1) | UY32711A (hr) |
| WO (2) | WO2010146348A2 (hr) |
| ZA (1) | ZA201109045B (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2012005513A (es) * | 2009-11-13 | 2012-06-19 | Cardoz Ab | Pemirolast para el tratamiento de inflamacion sistemica de bajo grado. |
| WO2016063085A1 (en) | 2014-10-23 | 2016-04-28 | Rspr Pharma Ab | Use of pemirolast in the treatment of acute asthma |
| WO2016102941A1 (en) | 2014-12-22 | 2016-06-30 | Rspr Pharma Ab | New combination of pemirolast and montelukast |
| GB201518831D0 (en) | 2015-10-23 | 2015-12-09 | Rspr Pharma Ab | New use |
| BR112019006429A2 (pt) * | 2016-10-03 | 2019-06-25 | Brivention Pharmaceutical Shanghai Inc | composição compreendendo combinação de análogo de trh com ácido arúndico, e sal farmaceuticamente aceitável de ácido arúndico |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4122274A (en) * | 1977-05-25 | 1978-10-24 | Bristol-Myers Company | 3-Tetrazolo-5,6,7,8-substituted-pyrido[1,2-a]pyrimidin-4-ones |
| JP2504788B2 (ja) | 1987-11-10 | 1996-06-05 | 東京田辺製薬株式会社 | ９−メチル−３−（１Ｈ−テトラゾ―ル−５−イル）−４Ｈ−ピリド［１，２−ａ］ピリミジン−４−オンカリウム塩の水性製剤 |
| JP2837449B2 (ja) * | 1989-08-11 | 1998-12-16 | 東京田辺製薬株式会社 | ピリド［１，２―ａ］ピリミジン誘導体の製造法 |
| ITMI20011764A1 (it) | 2001-08-10 | 2003-02-10 | Dinamite Dipharma Spa | Metodo per l'ottenimento del pemirolast ad elevata purezza |
| WO2007032498A1 (ja) | 2005-09-16 | 2007-03-22 | Daiichi Sankyo Company, Limited | 光学活性なジアミン誘導体およびその製造方法 |
| PT2120919E (pt) * | 2006-12-18 | 2012-11-12 | Cardoz Ab | Nova combinação para utilização no tratamento de perturbações inflamatórias |
| CA2673214A1 (en) | 2006-12-20 | 2008-06-26 | Cardoz Ab | New combination for use in the treatment of inflammatory disorders |
-
2010
- 2010-06-15 JP JP2012515552A patent/JP5722317B2/ja not_active Expired - Fee Related
- 2010-06-15 SG SG2011088655A patent/SG176295A1/en unknown
- 2010-06-15 LT LTEP10732402.2T patent/LT2443120T/lt unknown
- 2010-06-15 US US13/378,787 patent/US20120157415A1/en not_active Abandoned
- 2010-06-15 DK DK10732402.2T patent/DK2443120T3/en active
- 2010-06-15 CA CA2765408A patent/CA2765408A1/en not_active Abandoned
- 2010-06-15 RS RS20170003A patent/RS55558B1/sr unknown
- 2010-06-15 WO PCT/GB2010/001168 patent/WO2010146348A2/en active Application Filing
- 2010-06-15 PT PT107324022T patent/PT2443120T/pt unknown
- 2010-06-15 TW TW099119396A patent/TWI504599B/zh not_active IP Right Cessation
- 2010-06-15 MX MX2011013676A patent/MX2011013676A/es active IP Right Grant
- 2010-06-15 CN CN201080026883.3A patent/CN102596202B/zh not_active Expired - Fee Related
- 2010-06-15 KR KR1020127001227A patent/KR20120032530A/ko active Application Filing
- 2010-06-15 ME MEP-2017-8A patent/ME02685B/me unknown
- 2010-06-15 ES ES10732402.2T patent/ES2613059T3/es active Active
- 2010-06-15 BR BRPI1015559A patent/BRPI1015559A2/pt not_active IP Right Cessation
- 2010-06-15 PL PL10732402T patent/PL2443120T3/pl unknown
- 2010-06-15 EP EP10732402.2A patent/EP2443120B1/en active Active
- 2010-06-15 AU AU2010261540A patent/AU2010261540B2/en not_active Ceased
- 2010-06-15 EA EA201200017A patent/EA025865B1/ru not_active IP Right Cessation
- 2010-06-15 SI SI201031380A patent/SI2443120T1/sl unknown
- 2010-06-15 KR KR1020177012036A patent/KR20170049645A/ko not_active Application Discontinuation
- 2010-06-15 HU HUE10732402A patent/HUE032978T2/hu unknown
- 2010-06-15 UY UY0001032711A patent/UY32711A/es not_active Application Discontinuation
- 2010-06-15 WO PCT/GB2010/001159 patent/WO2010146341A2/en active Application Filing
- 2010-06-15 NZ NZ596747A patent/NZ596747A/en not_active IP Right Cessation
- 2010-06-15 EP EP16194237.0A patent/EP3141549A1/en not_active Withdrawn
- 2010-06-16 AR ARP100102136A patent/AR077915A1/es unknown
- 2010-06-16 SA SA114350792A patent/SA114350792B1/ar unknown
-
2011
- 2011-11-29 IL IL216670A patent/IL216670A/en not_active IP Right Cessation
- 2011-12-08 ZA ZA2011/09045A patent/ZA201109045B/en unknown
-
2014
- 2014-05-12 US US14/274,951 patent/US9006431B2/en not_active Expired - Fee Related
-
2015
- 2015-03-24 JP JP2015060587A patent/JP2015120750A/ja active Pending
-
2016
- 2016-12-28 US US15/392,497 patent/US20170202839A1/en not_active Abandoned
-
2017
- 2017-01-10 HR HRP20170023TT patent/HRP20170023T1/hr unknown
- 2017-01-11 CY CY20171100039T patent/CY1118413T1/el unknown
- 2017-02-08 SM SM201700085T patent/SMT201700085B/it unknown
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