EA022490B1 - Новые формы рифаксимина и их применение - Google Patents
Новые формы рифаксимина и их применение Download PDFInfo
- Publication number
- EA022490B1 EA022490B1 EA201270808A EA201270808A EA022490B1 EA 022490 B1 EA022490 B1 EA 022490B1 EA 201270808 A EA201270808 A EA 201270808A EA 201270808 A EA201270808 A EA 201270808A EA 022490 B1 EA022490 B1 EA 022490B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- rifaximin
- piperazine
- mixed
- mixed crystals
- peaks
- Prior art date
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- 229910000342 sodium bisulfate Inorganic materials 0.000 description 1
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- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- CSMWJXBSXGUPGY-UHFFFAOYSA-L sodium dithionate Chemical compound [Na+].[Na+].[O-]S(=O)(=O)S([O-])(=O)=O CSMWJXBSXGUPGY-UHFFFAOYSA-L 0.000 description 1
- VILMUCRZVVVJCA-UHFFFAOYSA-M sodium glycolate Chemical compound [Na+].OCC([O-])=O VILMUCRZVVVJCA-UHFFFAOYSA-M 0.000 description 1
- 239000012064 sodium phosphate buffer Substances 0.000 description 1
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- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
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- 238000002076 thermal analysis method Methods 0.000 description 1
- AOBORMOPSGHCAX-DGHZZKTQSA-N tocofersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-DGHZZKTQSA-N 0.000 description 1
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- UMFCIIBZHQXRCJ-NSCUHMNNSA-N trans-anol Chemical compound C\C=C\C1=CC=C(O)C=C1 UMFCIIBZHQXRCJ-NSCUHMNNSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35128110P | 2010-06-03 | 2010-06-03 | |
| US35750510P | 2010-06-22 | 2010-06-22 | |
| US36324110P | 2010-07-10 | 2010-07-10 | |
| US36351110P | 2010-07-12 | 2010-07-12 | |
| US36718510P | 2010-07-23 | 2010-07-23 | |
| US41659310P | 2010-11-23 | 2010-11-23 | |
| PCT/US2011/039085 WO2011153444A1 (en) | 2010-06-03 | 2011-06-03 | New forms of rifaximin and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201270808A1 EA201270808A1 (ru) | 2013-04-30 |
| EA022490B1 true EA022490B1 (ru) | 2016-01-29 |
Family
ID=45067089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201270808A EA022490B1 (ru) | 2010-06-03 | 2011-06-03 | Новые формы рифаксимина и их применение |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US8513275B2 (https=) |
| EP (1) | EP2575464A4 (https=) |
| JP (1) | JP2013527246A (https=) |
| KR (1) | KR20130086338A (https=) |
| CN (1) | CN103269587A (https=) |
| AU (1) | AU2011261283B2 (https=) |
| BR (1) | BR112012030783A2 (https=) |
| CA (1) | CA2800668A1 (https=) |
| CR (1) | CR20120620A (https=) |
| EA (1) | EA022490B1 (https=) |
| IL (1) | IL222900A (https=) |
| MX (1) | MX2012013945A (https=) |
| NZ (2) | NZ710780A (https=) |
| PH (1) | PH12012502393A1 (https=) |
| SG (2) | SG185490A1 (https=) |
| TN (1) | TN2012000533A1 (https=) |
| WO (1) | WO2011153444A1 (https=) |
| ZA (1) | ZA201208770B (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025170483A1 (ru) * | 2024-02-07 | 2025-08-14 | Общество с ограниченной ответственностью "БИННОФАРМ ГРУПП" | Фармацевтическая композиция, обладающая антибиотической активностью |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1698630E (pt) | 2005-03-03 | 2014-09-15 | Alfa Wassermann Spa | Novas formas polimorfas de rifaximina, processos para a sua produção e a sua utilização nas preparações medicinais |
| US8486956B2 (en) | 2008-02-25 | 2013-07-16 | Salix Pharmaceuticals, Ltd | Forms of rifaximin and uses thereof |
| UA113275C2 (xx) | 2008-02-25 | 2017-01-10 | ζ-ФОРМА РИФАКСИМІНУ І ЇЇ ЗАСТОСУВАННЯ | |
| US9018684B2 (en) | 2009-11-23 | 2015-04-28 | California Institute Of Technology | Chemical sensing and/or measuring devices and methods |
| IT1398550B1 (it) | 2010-03-05 | 2013-03-01 | Alfa Wassermann Spa | Formulazioni comprendenti rifaximina utili per ottenere un effetto prolungato nel tempo |
| AU2011225810B2 (en) * | 2010-03-10 | 2014-11-06 | Lupin Limited | Rifaximin ready-to-use suspension |
| SG192122A1 (en) * | 2011-02-11 | 2013-08-30 | Salix Pharmaceuticals Ltd | Forms of rifaximin and uses thereof |
| WO2012150561A1 (en) * | 2011-05-02 | 2012-11-08 | Ranbaxy Laboratories Limited | Rifaximin dimethylformamide solvate |
| ITBO20110461A1 (it) | 2011-07-29 | 2013-01-30 | Alfa Wassermann Spa | Composizioni farmaceutiche comprendenti rifaximina, processi per la loro preparazione e loro uso nel trattamento di infezioni vaginali. |
| CA2854380A1 (en) | 2011-11-02 | 2013-05-10 | Salix Pharmaceuticals, Ltd. | Methods for treating irritable bowel syndrome (ibs) and infections |
| CA2876737A1 (en) | 2012-06-13 | 2013-12-19 | Apotex Pharmachem Inc. | Polymorphic forms of rifaximin |
| ITBO20120368A1 (it) | 2012-07-06 | 2014-01-07 | Alfa Wassermann Spa | Composizioni comprendenti rifaximina e amminoacidi, cristalli di rifaximina derivanti da tali composizioni e loro uso. |
| MX2015002934A (es) * | 2012-09-13 | 2015-10-29 | Salix Pharmaceuticals Inc | Metodos de administracion de rifaximina para perdida de peso y tratamiento de obesidad. |
| CN105142636A (zh) | 2013-03-15 | 2015-12-09 | 意大利阿尔法韦士曼制药公司 | 用于治疗阴道感染的利福昔明 |
| WO2014140995A2 (en) | 2013-03-15 | 2014-09-18 | Alfa Wassermann S.P.A. | Method for diagnosing vaginal infections |
| EP2983647B1 (en) | 2013-04-12 | 2020-09-09 | Alfasigma S.p.A. | Nsaid administration and related compositions, methods and systems |
| ITMI20131307A1 (it) * | 2013-08-02 | 2015-02-02 | A M S A Anonima Materie Sint & Affini S P A | Processo per la preparazione di refaximina k |
| ES2621557T3 (es) | 2014-03-31 | 2017-07-04 | Euticals S.P.A. | Mezcla polimórfica de rifaximina y su uso para la preparación de formulaciones sólidas |
| EP3140313B1 (en) | 2014-05-04 | 2020-02-26 | Salix Pharmaceuticals, Inc. | Ibs microbiota and uses thereof |
| NZ723571A (en) * | 2014-05-12 | 2020-02-28 | Alfasigma Spa | New solvated crystal form of rifaximin, production, compositions and uses thereof |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050181041A1 (en) * | 2003-12-09 | 2005-08-18 | Medcrystalforms, Llc | Method of preparation of mixed phase co-crystals with active agents |
| US20070026078A1 (en) * | 2002-02-15 | 2007-02-01 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions |
| US20090082558A1 (en) * | 2007-09-20 | 2009-03-26 | Apotex Pharmachem Inc. | Amorphous form of rifaximin and processes for its preparation |
| WO2009108730A2 (en) * | 2008-02-25 | 2009-09-03 | Salix Pharmaceuticals, Ltd. | Forms of rifaximin and uses thereof |
| US20090234114A1 (en) * | 2003-11-07 | 2009-09-17 | Alfa Wasserman S.P..A. | Polymorphic forms alpha, beta, and gamma of rifaximin |
| US20100174064A1 (en) * | 2008-02-25 | 2010-07-08 | Salix Pharmaceuticals, Ltd. | Forms of rifaximin and uses thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20032144A1 (it) * | 2003-11-07 | 2005-05-08 | Alfa Wassermann Spa | Forme polimorfe di rifaximina, processi per ottenerle e |
| WO2006007448A2 (en) * | 2004-06-17 | 2006-01-19 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions and related methods of use |
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2011
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- 2011-06-03 BR BR112012030783A patent/BR112012030783A2/pt not_active Application Discontinuation
- 2011-06-03 PH PH1/2012/502393A patent/PH12012502393A1/en unknown
- 2011-06-03 SG SG2012082541A patent/SG185490A1/en unknown
- 2011-06-03 EP EP11790471.4A patent/EP2575464A4/en not_active Ceased
- 2011-06-03 CN CN2011800382176A patent/CN103269587A/zh active Pending
- 2011-06-03 NZ NZ710780A patent/NZ710780A/en unknown
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- 2011-06-03 AU AU2011261283A patent/AU2011261283B2/en active Active
- 2011-06-03 JP JP2013513376A patent/JP2013527246A/ja active Pending
- 2011-06-03 KR KR1020137000060A patent/KR20130086338A/ko not_active Ceased
- 2011-06-03 NZ NZ603590A patent/NZ603590A/en unknown
- 2011-06-03 MX MX2012013945A patent/MX2012013945A/es not_active Application Discontinuation
- 2011-06-03 US US13/152,804 patent/US8513275B2/en active Active
- 2011-06-03 WO PCT/US2011/039085 patent/WO2011153444A1/en not_active Ceased
- 2011-06-03 CA CA2800668A patent/CA2800668A1/en not_active Abandoned
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2012
- 2012-11-06 IL IL222900A patent/IL222900A/en active IP Right Grant
- 2012-11-09 TN TNP2012000533A patent/TN2012000533A1/en unknown
- 2012-11-21 ZA ZA2012/08770A patent/ZA201208770B/en unknown
- 2012-12-10 CR CR20120620A patent/CR20120620A/es unknown
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| US20070026078A1 (en) * | 2002-02-15 | 2007-02-01 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions |
| US20090234114A1 (en) * | 2003-11-07 | 2009-09-17 | Alfa Wasserman S.P..A. | Polymorphic forms alpha, beta, and gamma of rifaximin |
| US20050181041A1 (en) * | 2003-12-09 | 2005-08-18 | Medcrystalforms, Llc | Method of preparation of mixed phase co-crystals with active agents |
| US20090082558A1 (en) * | 2007-09-20 | 2009-03-26 | Apotex Pharmachem Inc. | Amorphous form of rifaximin and processes for its preparation |
| WO2009108730A2 (en) * | 2008-02-25 | 2009-09-03 | Salix Pharmaceuticals, Ltd. | Forms of rifaximin and uses thereof |
| US20100174064A1 (en) * | 2008-02-25 | 2010-07-08 | Salix Pharmaceuticals, Ltd. | Forms of rifaximin and uses thereof |
| US20100239664A1 (en) * | 2008-02-25 | 2010-09-23 | Salix Pharmaceuticals, Ltd. | Forms of rifaximin and uses thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025170483A1 (ru) * | 2024-02-07 | 2025-08-14 | Общество с ограниченной ответственностью "БИННОФАРМ ГРУПП" | Фармацевтическая композиция, обладающая антибиотической активностью |
Also Published As
| Publication number | Publication date |
|---|---|
| ZA201208770B (en) | 2013-07-31 |
| US20120108620A1 (en) | 2012-05-03 |
| EP2575464A4 (en) | 2013-10-02 |
| PH12012502393A1 (en) | 2013-02-11 |
| AU2011261283A1 (en) | 2012-12-06 |
| US8815888B2 (en) | 2014-08-26 |
| WO2011153444A1 (en) | 2011-12-08 |
| SG185490A1 (en) | 2012-12-28 |
| NZ603590A (en) | 2015-08-28 |
| CA2800668A1 (en) | 2011-12-08 |
| KR20130086338A (ko) | 2013-08-01 |
| AU2011261283B2 (en) | 2015-05-14 |
| CN103269587A (zh) | 2013-08-28 |
| NZ710780A (en) | 2017-02-24 |
| US8513275B2 (en) | 2013-08-20 |
| MX2012013945A (es) | 2013-05-06 |
| TN2012000533A1 (en) | 2014-04-01 |
| EP2575464A1 (en) | 2013-04-10 |
| SG10201507035UA (en) | 2015-10-29 |
| IL222900A0 (en) | 2012-12-31 |
| US20130317225A1 (en) | 2013-11-28 |
| BR112012030783A2 (pt) | 2015-09-29 |
| JP2013527246A (ja) | 2013-06-27 |
| CR20120620A (es) | 2014-05-23 |
| IL222900A (en) | 2017-11-30 |
| EA201270808A1 (ru) | 2013-04-30 |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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