HRP20100345T1 - Kristalne forme makrolidnih spojeva koji ispoljavaju anti-inflamatornu aktivnost - Google Patents
Kristalne forme makrolidnih spojeva koji ispoljavaju anti-inflamatornu aktivnost Download PDFInfo
- Publication number
- HRP20100345T1 HRP20100345T1 HR20100345T HRP20100345T HRP20100345T1 HR P20100345 T1 HRP20100345 T1 HR P20100345T1 HR 20100345 T HR20100345 T HR 20100345T HR P20100345 T HRP20100345 T HR P20100345T HR P20100345 T1 HRP20100345 T1 HR P20100345T1
- Authority
- HR
- Croatia
- Prior art keywords
- around
- crystalline form
- mixture
- ray diffraction
- differential scanning
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract 6
- 230000003110 anti-inflammatory effect Effects 0.000 title abstract 3
- 239000003120 macrolide antibiotic agent Substances 0.000 title abstract 3
- 238000000034 method Methods 0.000 claims abstract 6
- 239000004480 active ingredient Substances 0.000 claims abstract 3
- 208000027866 inflammatory disease Diseases 0.000 claims abstract 2
- 239000000203 mixture Substances 0.000 claims 7
- 238000002441 X-ray diffraction Methods 0.000 claims 4
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 4
- 238000002844 melting Methods 0.000 claims 4
- 230000008018 melting Effects 0.000 claims 4
- 239000000843 powder Substances 0.000 claims 4
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- 238000002560 therapeutic procedure Methods 0.000 claims 3
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 239000007900 aqueous suspension Substances 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Kristalna Forma I spoja formulenaznačena time što profil difrakcije X zraka u praškastom uzorku obuhvaća vrijednosti 2θ kutova od oko 4.9; oko 8.5; oko 9.1; oko 10.3; oko 11.1; oko 14.5; oko 17.0; oko 18.2; oko 19.3. Patent sadrži još 19 patentnih zahtjeva.
Claims (20)
1. Kristalna Forma I spoja formule
[image]
naznačena time što profil difrakcije X zraka u praškastom uzorku obuhvaća vrijednosti 2θ kutova od oko 4.9; oko 8.5; oko 9.1; oko 10.3; oko 11.1; oko 14.5; oko 17.0; oko 18.2; oko 19.3.
2. Kristalna forma prema zahtjevu 1, naznačena time što ispoljava profil difrakcije X zraka u praškastom uzorku koji je suštinski suglasan sa onim što je prikazano na Sl 1.
3. Kristalna forma, prema nekom od prethodnih zahtjeva, naznačena time što krivulja diferencijalne skenirajuće kalorimetrije ima početak topljenja u opsegu 163-174ºC.
4. Kristalna forma, prema zahtjevu 3, naznačena time što krivulja diferencijalne skenirajuće kalorimetrije ima početak topljenja u opsegu 163-168ºC.
5. Kristalna Forma II spoja formule I, naznačena time što profil difrakcije X zraka u praškastom uzorku obuhvaća vrijednosti 2θ kuteva od oko 11.9; oko 13.4; oko 13.9; oko 14.6; oko 15.3; oko 16.4; oko 17.4; oko 18.8; oko 19.0; oko 19.5; oko 21.1; oko 22.7.
6. Kristalna forma prema zahtjevu 5, naznačena time što je profil difrakcije X zraka u praškastom uzorku suštinski suglasan sa onim što je prikazano na Sl. 2.
7. Kristalna forma prema zahtjevima 5 i 6, naznačena time što krivulja diferencijalne skenirajuće kalorimetrije ima početak topljenja u opsegu 218-226ºC.
8. Kristalna forma prema zahtjevu 7, naznačena time što krivulja diferencijalne skenirajuće kalorimetrije ima početak topljenja u opsegu 218-223ºC.
9. Proces dobijanja kristalne Forme I, prema zahtjevima 1-4, naznačen time što obuhvaća: dodavanje metil-terc-butil etera otopini spoja formule I u etil acetatu, hlađenje dobijene reakcijske smjese, filtriranje i sušenje kristaliziranog proizvoda.
10. Postupak dobijanja kristalne Forme II, prema zahtjevima 5-8, naznačen time što obuhvaća konverziju kristalne Forme I, prema zahtjevima 1-4, u kristalnu Formu II, zagrijanjem vodene suspenzije navedene kristalne Forme I.
11. Postupak prema zahtjevu 10, naznačen time što se suspenzija zagrijava do temperature između 30 i 35ºC.
12. Postupak dobijanja kristalne Forme II, prema zahtjevima 5-8, naznačen time što se sastoji od kristalizacije spoja formule I iz metil etil ketona.
13. Postupak prema zahtjevu 12, naznačen time što dalje obuhvaća obogaćivanje otopine kristalnom Formom II.
14. Kristalna Forma I, prema zahtjevima 1-4, naznačena time što se primjenjuje kao medikament.
15. Kristalna Forma II, prema zahtjevima 5-8, naznačena time što se primjenjuje kao medikament.
16. Farmaceutska smjesa, naznačena time što sadrži farmaceutski efektivne količine kristalne Forme I, prema zahtjevima 1-4, kao aktivnog sastojka, u smjesi sa farmaceutski prihvatljivim nosačem.
17. Farmaceutska smjesa, naznačena time što sadrži terapeutski efektivne količine kristalne Forme II, prema zahtjevima 5-8, kao aktivnog sastojka, u smjesi sa farmaceutski aktivnim nosačem.
18. Farmaceutska smjesa prema zahtjevima 16 ili 17, naznačena time što se primjenjuje u terapiji inflamatornih bolesti.
19. Farmaceutska smjesa prema zahtjevu 18, naznačena time što se primjenjuje u terapiji respiratornih bolesti.
20. Farmaceutska smjesa prema zahtjevu 18, naznačena time što se primjenjuje u terapiji gastrointestinalnih bolesti.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05106123 | 2005-07-06 | ||
| PCT/EP2006/006541 WO2007003422A1 (en) | 2005-07-06 | 2006-07-05 | Crystalline forms of macrolide compounds endowed with antiinflammatory activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20100345T1 true HRP20100345T1 (hr) | 2010-07-31 |
Family
ID=37398772
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20100345T HRP20100345T1 (hr) | 2005-07-06 | 2010-06-18 | Kristalne forme makrolidnih spojeva koji ispoljavaju anti-inflamatornu aktivnost |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US7956042B2 (hr) |
| EP (1) | EP1907406B1 (hr) |
| JP (1) | JP2008544970A (hr) |
| CN (2) | CN101291947B (hr) |
| AT (1) | ATE466019T1 (hr) |
| AU (1) | AU2006265277A1 (hr) |
| BR (1) | BRPI0612598A2 (hr) |
| CA (1) | CA2613911C (hr) |
| CY (1) | CY1110192T1 (hr) |
| DE (1) | DE602006013986D1 (hr) |
| DK (1) | DK1907406T3 (hr) |
| EA (1) | EA013082B1 (hr) |
| ES (1) | ES2343748T3 (hr) |
| HR (1) | HRP20100345T1 (hr) |
| IL (1) | IL188400A (hr) |
| IT (1) | ITMI20061305A1 (hr) |
| PL (1) | PL1907406T3 (hr) |
| PT (1) | PT1907406E (hr) |
| RS (1) | RS51299B (hr) |
| SI (1) | SI1907406T1 (hr) |
| WO (1) | WO2007003422A1 (hr) |
| ZA (1) | ZA200800414B (hr) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20021726A1 (it) * | 2002-08-01 | 2004-02-02 | Zambon Spa | Macrolidi ad attivita' antiinfiammatoria. |
| US20080249034A1 (en) * | 2005-03-21 | 2008-10-09 | Zambon S.P.A. | Use of Macrolides for Treating Intestinal Inflammation |
-
2006
- 2006-07-05 CN CN2006800244137A patent/CN101291947B/zh not_active Expired - Fee Related
- 2006-07-05 AT AT06791531T patent/ATE466019T1/de active
- 2006-07-05 EP EP06791531A patent/EP1907406B1/en active Active
- 2006-07-05 EA EA200800266A patent/EA013082B1/ru not_active IP Right Cessation
- 2006-07-05 SI SI200630715T patent/SI1907406T1/sl unknown
- 2006-07-05 PL PL06791531T patent/PL1907406T3/pl unknown
- 2006-07-05 WO PCT/EP2006/006541 patent/WO2007003422A1/en active Application Filing
- 2006-07-05 PT PT06791531T patent/PT1907406E/pt unknown
- 2006-07-05 US US11/994,784 patent/US7956042B2/en not_active Expired - Fee Related
- 2006-07-05 DK DK06791531.4T patent/DK1907406T3/da active
- 2006-07-05 RS RSP-2010/0268A patent/RS51299B/sr unknown
- 2006-07-05 JP JP2008518762A patent/JP2008544970A/ja active Pending
- 2006-07-05 DE DE602006013986T patent/DE602006013986D1/de active Active
- 2006-07-05 ES ES06791531T patent/ES2343748T3/es active Active
- 2006-07-05 CN CN201110157119.6A patent/CN102295671B/zh not_active Expired - Fee Related
- 2006-07-05 CA CA2613911A patent/CA2613911C/en not_active Expired - Fee Related
- 2006-07-05 AU AU2006265277A patent/AU2006265277A1/en not_active Abandoned
- 2006-07-05 BR BRPI0612598-0A patent/BRPI0612598A2/pt not_active IP Right Cessation
- 2006-07-06 IT IT001305A patent/ITMI20061305A1/it unknown
-
2007
- 2007-12-25 IL IL188400A patent/IL188400A/en not_active IP Right Cessation
-
2008
- 2008-01-14 ZA ZA200800414A patent/ZA200800414B/xx unknown
-
2010
- 2010-06-18 HR HR20100345T patent/HRP20100345T1/hr unknown
- 2010-07-07 CY CY20101100633T patent/CY1110192T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102295671B (zh) | 2014-01-29 |
| EP1907406B1 (en) | 2010-04-28 |
| CN101291947B (zh) | 2012-08-22 |
| CY1110192T1 (el) | 2015-01-14 |
| WO2007003422A9 (en) | 2007-04-19 |
| AU2006265277A1 (en) | 2007-01-11 |
| US7956042B2 (en) | 2011-06-07 |
| CA2613911A1 (en) | 2007-01-11 |
| ES2343748T3 (es) | 2010-08-09 |
| DE602006013986D1 (de) | 2010-06-10 |
| PT1907406E (pt) | 2010-07-05 |
| JP2008544970A (ja) | 2008-12-11 |
| DK1907406T3 (da) | 2010-08-09 |
| EP1907406A1 (en) | 2008-04-09 |
| WO2007003422A1 (en) | 2007-01-11 |
| CA2613911C (en) | 2013-10-22 |
| EA200800266A1 (ru) | 2008-06-30 |
| EA013082B1 (ru) | 2010-02-26 |
| ITMI20061305A1 (it) | 2007-01-07 |
| PL1907406T3 (pl) | 2010-10-29 |
| RS51299B (sr) | 2010-12-31 |
| IL188400A0 (en) | 2008-08-07 |
| ATE466019T1 (de) | 2010-05-15 |
| SI1907406T1 (sl) | 2010-08-31 |
| IL188400A (en) | 2012-08-30 |
| US20090018089A1 (en) | 2009-01-15 |
| ZA200800414B (en) | 2009-02-25 |
| CN102295671A (zh) | 2011-12-28 |
| CN101291947A (zh) | 2008-10-22 |
| BRPI0612598A2 (pt) | 2010-11-23 |
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