ME02480B - Optimizirana sinteza čistih, nepolimorfnih, kristalnih žučnih kiselina sa određenom veličinom čestica - Google Patents
Optimizirana sinteza čistih, nepolimorfnih, kristalnih žučnih kiselina sa određenom veličinom česticaInfo
- Publication number
- ME02480B ME02480B MEP-2016-230A MEP23016A ME02480B ME 02480 B ME02480 B ME 02480B ME P23016 A MEP23016 A ME P23016A ME 02480 B ME02480 B ME 02480B
- Authority
- ME
- Montenegro
- Prior art keywords
- polymorph
- udca
- pharmaceutical composition
- less
- liver disease
- Prior art date
Links
- 239000002245 particle Substances 0.000 title claims 6
- 239000002253 acid Substances 0.000 title 1
- 150000007513 acids Chemical class 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- QYYDXDSPYPOWRO-JHMCBHKWSA-N (3r)-3-[(3r,5s,7s,8r,9s,10s,13r,14s,17r)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]butanoic acid Chemical compound C([C@H]1C[C@@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CC(O)=O)C)[C@@]2(C)CC1 QYYDXDSPYPOWRO-JHMCBHKWSA-N 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 206010008635 Cholestasis Diseases 0.000 claims 2
- 206010068786 Overlap syndrome Diseases 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 230000001476 alcoholic effect Effects 0.000 claims 2
- 239000012535 impurity Substances 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 230000002503 metabolic effect Effects 0.000 claims 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 230000008021 deposition Effects 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/29—Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
- Y10T428/2982—Particulate matter [e.g., sphere, flake, etc.]
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
Claims (11)
- Hemijski čist polimorf Nor-UDCA, u kame je ukupna količina hemijskih nečistoća manja od 0,5%, u odnosu na ukupnu težinu Nor-UDCA, i bar 60% polimorfnih čestica ima veličinu < 10 µm, i pri čemu je pomenuti polimorf, naznačen time, što ima XRPD signale na 11,9, 14,4,15,3, 15,8,i 16,6 ± 0,2 stepena 2-teta i što amorfni Nor-UDCA nije detektovan u pomenutom polimorfu pomoću XPRD.
- Polimorf prema zahtevu 1, u kojem je ukupna količina hemijksih nečistoća manja od 0,1%, poželjno manja od 0,05 %.
- Poiimorf prema zahtevu 1 ili 2, u kame je pomenuti Nor-UDCA u svom anhidorvanom obiiku.
- Poiimorf prema zahtevu 1, naznačen time, što ima XPRD uzorak prikazan na slici
- Polimorf prema bilo kom od zahteva 1 do 4, koji ima zapreminski određenu srednju vrednost prečnika čestica D50 manju od 10 µm i/ili zapreminski određenu srednju vrednost prečnika čestica D95 manju od 30µm.
- Farmaceutska kompozicija koja sadrži polimorf prema bilo kom od zahteva 1 do 5.
- Farmaceutska kompozicija prema zahtevu 6, gde je raspored veličine čestica u farmaceutskoj kompoziciji bar 60% čestica veličine < 10 µm.
- Polimorf prema bilo kom od zahteva 1 do 5, ili farmaceutska kompozicija prema zahtevu 6 ili 7, za upotrebu u lečenju holestatičke bolesti jetre, gde je holestatička bolest jetre poželjno izabrana iz grupe koju čine primarna bilijarna ciroza (PBC), primarni sklerozirajući holangitis (PSC), autoimuni hepatitis (AIH) i sindromi preklapanja, uključujući AIH sindrom preklapanja.
- Polimorf prema bilo kom od zahteva 1 do 5 ili farmaceutska kompozicija prema zahtevu 6 ili 7, za upotrebu u lečenju metaboličke bolesti jetre i/ili arteroskleroze, gde je metabolička bolest jetre požeijno izabrana iz nealkoholnog stearohepatitisa i alkoholnog stearo hepatitisa.
- Farmaceutska kompozicija prema bilo kom od zahteva 6 do 9, koja je formulisana za oralno, parenteralno, subkutanozno, intravensko, intramuskularno, nazalno, lokalno ili rektalno davanje, i/iii koja sadrzi jedan ili više farmaceutski prihvatijivih ekscipijenata.
- 11. Postupak za dobijanje čistog polimorfnog Nor-UDCA, koji obuhvata sledeće korake: kristalizaciju kalijumove soli Nor-UDCA; i opciono rastvaranje kalijumove soli u rastvaraču i zakiseljavanje rastvora da bi se dobio čist Nor-UDCA.Postupak prema zahtevu 11, gde je pomenuti rastvarač smeša vode i acetona, i gde je pomenuto taloženje izvedeno zakiseljavanjem rastvora do pH u opsegu 1 do 2.Postupak prema bilo kom od zahteva 11 do 13, naznačen time, što ne obuhvata korak mlevenja i/ili korak mikronizacije.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10193143A EP2468762A1 (en) | 2010-11-30 | 2010-11-30 | Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size |
| PCT/EP2011/071406 WO2012072689A1 (en) | 2010-11-30 | 2011-11-30 | Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size |
| EP11788533.5A EP2646457B1 (en) | 2010-11-30 | 2011-11-30 | Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02480B true ME02480B (me) | 2017-02-20 |
Family
ID=44275998
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-230A ME02480B (me) | 2010-11-30 | 2011-11-30 | Optimizirana sinteza čistih, nepolimorfnih, kristalnih žučnih kiselina sa određenom veličinom čestica |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US9512167B2 (me) |
| EP (2) | EP2468762A1 (me) |
| JP (2) | JP6276592B2 (me) |
| CN (1) | CN103298825B (me) |
| AU (1) | AU2011334928B2 (me) |
| BR (1) | BR112013013179B1 (me) |
| CA (1) | CA2818984C (me) |
| CY (1) | CY1118036T1 (me) |
| DK (1) | DK2646457T3 (me) |
| EA (1) | EA025586B1 (me) |
| ES (1) | ES2597652T3 (me) |
| HR (1) | HRP20161187T1 (me) |
| HU (1) | HUE029847T2 (me) |
| IL (1) | IL226616A (me) |
| LT (1) | LT2646457T (me) |
| ME (1) | ME02480B (me) |
| NZ (2) | NZ610862A (me) |
| PL (1) | PL2646457T3 (me) |
| PT (1) | PT2646457T (me) |
| RS (1) | RS55211B1 (me) |
| SI (1) | SI2646457T1 (me) |
| UA (1) | UA112764C2 (me) |
| WO (1) | WO2012072689A1 (me) |
| ZA (1) | ZA201303820B (me) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1392714T3 (da) | 2001-03-12 | 2006-01-09 | Intercept Pharmaceuticals Inc | Steroider som agonister for FXR |
| EP2468762A1 (en) * | 2010-11-30 | 2012-06-27 | Dr. Falk Pharma Gmbh | Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size |
| EP3518937A4 (en) * | 2016-09-30 | 2020-04-29 | Intercept Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF A BILIARY ACID DERIVATIVE |
| EP3461485A1 (en) * | 2017-09-28 | 2019-04-03 | Dr. Falk Pharma Gmbh | Use of nor-ursodeoxycholic acid for reducing liver fat |
| WO2021130232A1 (en) | 2019-12-23 | 2021-07-01 | Medizinische Universität Wien | Bile acid derivatives in the medical intervention of anxieties and/or stress symptoms |
| US11655240B1 (en) * | 2022-05-10 | 2023-05-23 | Beijing Grand Johamu Pharmaceutical Company, Ltd. | Crystal form of compound and fumaric acid, pharmaceutical composition and method for treating coronavirus-induced diseases |
| KR20250040943A (ko) * | 2022-07-25 | 2025-03-25 | 실파 메디케어 리미티드 | 노르-udca의 약제학적 조성물 |
| WO2024245370A1 (zh) * | 2023-05-31 | 2024-12-05 | 上海复宏汉霖生物技术股份有限公司 | 一种组合产品、盐及其用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW289020B (me) * | 1993-05-08 | 1996-10-21 | Hoechst Sktiengesellschaft | |
| ITMI20012572A1 (it) | 2001-12-06 | 2003-06-06 | Istituto Biochimico Italiano | Microgranuli di acido ursodesossicolico |
| EP2392335B1 (en) * | 2005-05-12 | 2015-06-24 | Medizinische Universität Graz | Use of 24-norUDCA |
| CN100513415C (zh) * | 2005-08-03 | 2009-07-15 | 中国人民解放军军事医学科学院毒物药物研究所 | 胆汁酸衍生物及其医药用途 |
| SI2182954T1 (sl) * | 2007-07-25 | 2019-04-30 | Medizinische Universitat Graz | Uporaba nor-žolčnih kislin pri zdravljenju arterioskleroze |
| EP2468762A1 (en) * | 2010-11-30 | 2012-06-27 | Dr. Falk Pharma Gmbh | Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size |
-
2010
- 2010-11-30 EP EP10193143A patent/EP2468762A1/en not_active Withdrawn
-
2011
- 2011-11-30 EA EA201300647A patent/EA025586B1/ru unknown
- 2011-11-30 BR BR112013013179-9A patent/BR112013013179B1/pt active IP Right Grant
- 2011-11-30 DK DK11788533.5T patent/DK2646457T3/en active
- 2011-11-30 RS RS20160858A patent/RS55211B1/sr unknown
- 2011-11-30 AU AU2011334928A patent/AU2011334928B2/en active Active
- 2011-11-30 PL PL11788533T patent/PL2646457T3/pl unknown
- 2011-11-30 UA UAA201308173A patent/UA112764C2/uk unknown
- 2011-11-30 NZ NZ610862A patent/NZ610862A/en unknown
- 2011-11-30 ES ES11788533.5T patent/ES2597652T3/es active Active
- 2011-11-30 ME MEP-2016-230A patent/ME02480B/me unknown
- 2011-11-30 PT PT117885335T patent/PT2646457T/pt unknown
- 2011-11-30 LT LTEP11788533.5T patent/LT2646457T/lt unknown
- 2011-11-30 WO PCT/EP2011/071406 patent/WO2012072689A1/en not_active Ceased
- 2011-11-30 SI SI201130954A patent/SI2646457T1/sl unknown
- 2011-11-30 HU HUE11788533A patent/HUE029847T2/en unknown
- 2011-11-30 EP EP11788533.5A patent/EP2646457B1/en active Active
- 2011-11-30 CN CN201180063073.XA patent/CN103298825B/zh active Active
- 2011-11-30 US US13/989,012 patent/US9512167B2/en active Active
- 2011-11-30 JP JP2013541332A patent/JP6276592B2/ja active Active
- 2011-11-30 NZ NZ708988A patent/NZ708988A/en unknown
- 2011-11-30 HR HRP20161187TT patent/HRP20161187T1/hr unknown
- 2011-11-30 CA CA2818984A patent/CA2818984C/en active Active
-
2013
- 2013-05-24 ZA ZA2013/03820A patent/ZA201303820B/en unknown
- 2013-05-28 IL IL226616A patent/IL226616A/en active IP Right Grant
-
2016
- 2016-09-15 CY CY20161100918T patent/CY1118036T1/el unknown
- 2016-11-11 US US15/349,541 patent/US10000526B2/en active Active
-
2017
- 2017-01-13 JP JP2017003772A patent/JP6594917B2/ja active Active
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