CN103269587A - 利福昔明的新形式及其用途 - Google Patents

利福昔明的新形式及其用途 Download PDF

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Publication number
CN103269587A
CN103269587A CN2011800382176A CN201180038217A CN103269587A CN 103269587 A CN103269587 A CN 103269587A CN 2011800382176 A CN2011800382176 A CN 2011800382176A CN 201180038217 A CN201180038217 A CN 201180038217A CN 103269587 A CN103269587 A CN 103269587A
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CN
China
Prior art keywords
rifaximin
cocrystal
piperazine
substantially similar
peaks
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN2011800382176A
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English (en)
Chinese (zh)
Inventor
Y.吴
S.D.佩伦特
N.C.舒尔泰斯
M.J.贝维尔
P.弗拉霍瓦
T.L.霍斯顿
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Salix Pharmaceuticals Inc
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Salix Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Salix Pharmaceuticals Inc filed Critical Salix Pharmaceuticals Inc
Publication of CN103269587A publication Critical patent/CN103269587A/zh
Pending legal-status Critical Current

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    • 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
    • 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

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  • 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)
CN2011800382176A 2010-06-03 2011-06-03 利福昔明的新形式及其用途 Pending CN103269587A (zh)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US35128110P 2010-06-03 2010-06-03
US61/351281 2010-06-03
US35750510P 2010-06-22 2010-06-22
US61/357505 2010-06-22
US36324110P 2010-07-10 2010-07-10
US61/363241 2010-07-10
US36351110P 2010-07-12 2010-07-12
US61/363511 2010-07-12
US36718510P 2010-07-23 2010-07-23
US61/367185 2010-07-23
US41659310P 2010-11-23 2010-11-23
US61/416593 2010-11-23
PCT/US2011/039085 WO2011153444A1 (en) 2010-06-03 2011-06-03 New forms of rifaximin and uses thereof

Publications (1)

Publication Number Publication Date
CN103269587A true CN103269587A (zh) 2013-08-28

Family

ID=45067089

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2011800382176A Pending CN103269587A (zh) 2010-06-03 2011-06-03 利福昔明的新形式及其用途

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=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
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
WO2025170483A1 (ru) * 2024-02-07 2025-08-14 Общество с ограниченной ответственностью "БИННОФАРМ ГРУПП" Фармацевтическая композиция, обладающая антибиотической активностью

Citations (5)

* Cited by examiner, † Cited by third party
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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
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
US8486956B2 (en) * 2008-02-25 2013-07-16 Salix Pharmaceuticals, Ltd Forms of rifaximin and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
G. C. VISCOMI ET AL.: "Crystal forms of rifaximin and their effect on pharmaceutical properties", 《CRYSTENGCOMM》 *
STEPHEN BYRN: "pharmaceutical solids: a strategic approach to regulatory consiferations", 《PHARMACEUTICAL RESEARCH》 *

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
EA022490B1 (ru) 2016-01-29
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
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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