EA201190216A1 - Производные рифамицина - Google Patents

Производные рифамицина

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Publication number
EA201190216A1
EA201190216A1 EA201190216A EA201190216A EA201190216A1 EA 201190216 A1 EA201190216 A1 EA 201190216A1 EA 201190216 A EA201190216 A EA 201190216A EA 201190216 A EA201190216 A EA 201190216A EA 201190216 A1 EA201190216 A1 EA 201190216A1
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
compounds
hydroxy
hydrogen
antibacterial activity
Prior art date
Application number
EA201190216A
Other languages
English (en)
Other versions
EA020201B1 (ru
Inventor
Джузеппе Клаудио Вискоми
Мануэла Кампана
Маена Фолегатти
Винченцо Канната
Паоло Риги
Гоффредо Росини
Original Assignee
Альфа Вассерманн С.П.А.
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 Альфа Вассерманн С.П.А. filed Critical Альфа Вассерманн С.П.А.
Publication of EA201190216A1 publication Critical patent/EA201190216A1/ru
Publication of EA020201B1 publication Critical patent/EA020201B1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/7036Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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 two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/20Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (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)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Curing Cements, Concrete, And Artificial Stone (AREA)

Abstract

Раскрыты соединения, включая производные рифамицина, обладающие антибактериальной активностью, где соединения имеют формулу I, где R представляет собой водород или ацетил, Rи Rнезависимо выбраны из группы, состоящей из водорода, (С)алкила, бензилокси, моно- и ди-(С)алкиламино(С)алкила, (С)алкокси(С)алкила, гидроксиметила, гидрокси(С)алкила и нитро, или Rи R, взятые вместе с двумя последовательными атомами углерода пиридинового кольца, образуют бензольное кольцо, возможно замещенное одной или двумя метильными или этильными группами, и Rпредставляет собой гидрокси(С)алкил. Кроме того, описаны способы получения этих соединений. Соединения обладают антибактериальной активностью.
EA201190216A 2009-04-20 2010-03-18 Производные рифамицина EA020201B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI2009A000653A IT1397617B1 (it) 2009-04-20 2009-04-20 Nuovi derivati della rifamicina
PCT/IB2010/051183 WO2010122436A1 (en) 2009-04-20 2010-03-18 Rifamycin derivatives

Publications (2)

Publication Number Publication Date
EA201190216A1 true EA201190216A1 (ru) 2012-02-28
EA020201B1 EA020201B1 (ru) 2014-09-30

Family

ID=41228810

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201190216A EA020201B1 (ru) 2009-04-20 2010-03-18 Производные рифамицина

Country Status (28)

Country Link
US (2) US8318763B2 (ru)
EP (1) EP2421869B1 (ru)
JP (1) JP5661100B2 (ru)
KR (1) KR101555860B1 (ru)
CN (1) CN102405223A (ru)
AR (1) AR076340A1 (ru)
AU (1) AU2010240638B2 (ru)
BR (1) BRPI1005979A8 (ru)
CA (1) CA2743801C (ru)
CL (1) CL2011002597A1 (ru)
CO (1) CO6362013A2 (ru)
DK (1) DK2421869T3 (ru)
EA (1) EA020201B1 (ru)
ES (1) ES2535327T3 (ru)
HK (1) HK1163663A1 (ru)
HR (1) HRP20110437A2 (ru)
IL (1) IL212942A (ru)
IT (1) IT1397617B1 (ru)
MA (1) MA33320B1 (ru)
MX (1) MX338334B (ru)
NZ (1) NZ595884A (ru)
PL (1) PL2421869T3 (ru)
PT (1) PT2421869E (ru)
SG (1) SG171989A1 (ru)
TN (1) TN2011000265A1 (ru)
TW (1) TWI422372B (ru)
UA (1) UA105775C2 (ru)
WO (1) WO2010122436A1 (ru)

Families Citing this family (9)

* 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
ITBO20050123A1 (it) 2005-03-07 2005-06-06 Alfa Wassermann Spa Formulazioni farmaceutiche gastroresistenti contenenti rifaximina
IT1398550B1 (it) 2010-03-05 2013-03-01 Alfa Wassermann Spa Formulazioni comprendenti rifaximina utili per ottenere un effetto prolungato nel tempo
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.
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.
MX2015003108A (es) * 2012-09-12 2015-09-10 Salix Pharmaceuticals Inc Metodos de administracion de rifaximina sin producir resistencia a los antibioticos.
CN103709177B (zh) * 2013-12-20 2016-02-24 武汉工程大学 利福霉素类沃尼妙林杂合抗生素及其制备方法
JP6576953B2 (ja) * 2014-05-12 2019-09-18 アルファシグマ ソシエタ ペル アチオニ リファキシミンの新規溶媒和物結晶形、生成物、組成物及びそれらの使用
DK3645539T3 (da) 2017-06-26 2021-05-10 Biofer Spa Pyrido-imidazo-rifamycin-derivater som antibakterielt middel

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2043847A1 (ru) 1969-05-30 1971-02-19 Takeda Chemical Industries Ltd
SU465795A3 (ru) * 1972-05-05 1975-03-30 Группо Лепетит (Фирма) Способ получени рифамицина в.
CH571064A5 (en) * 1973-03-01 1975-12-31 Archifar Ind Chim Trentino Recovery of rieamycin from broths - by oxidn to an insol form
US3847903A (en) * 1973-03-01 1974-11-12 Archifar Ind Chim Trentino Method for extracting and isolating rifamycin o from fermentation broths of rifamycins
US4267274A (en) * 1973-04-26 1981-05-12 Gruppo Lepetit S.P.A. Streptomyces mediterranei mutant capable of production of rifamycin B
GB1470426A (en) * 1974-08-30 1977-04-14 Lepetit Spa Rifamycins
IT1154655B (it) * 1980-05-22 1987-01-21 Alfa Farmaceutici Spa Derivati imidazo-rifamicinici metodi per la loro preparazione e loro uso come sostanza ad azione antibatterica
IT1199374B (it) * 1984-05-15 1988-12-30 Alfa Farmaceutici Spa Processo per la preparazione di pirido-imidazo-rifamicine
US7923553B2 (en) * 2003-11-07 2011-04-12 Alfa Wassermann, S.P.A. Processes for the production of polymorphic forms of rifaximin
ITMI20032144A1 (it) * 2003-11-07 2005-05-08 Alfa Wassermann Spa Forme polimorfe di rifaximina, processi per ottenerle e

Also Published As

Publication number Publication date
CL2011002597A1 (es) 2012-03-23
HRP20110437A2 (hr) 2011-09-30
KR20120014110A (ko) 2012-02-16
CO6362013A2 (es) 2012-01-20
UA105775C2 (ru) 2014-06-25
MX338334B (es) 2016-04-11
CA2743801A1 (en) 2010-10-28
TW201039819A (en) 2010-11-16
CN102405223A (zh) 2012-04-04
CA2743801C (en) 2017-03-07
IL212942A (en) 2015-06-30
ITMI20090653A1 (it) 2010-10-21
US20130287692A1 (en) 2013-10-31
AU2010240638B2 (en) 2014-06-05
MX2011011026A (es) 2011-11-02
KR101555860B1 (ko) 2015-09-25
IT1397617B1 (it) 2013-01-18
PT2421869E (pt) 2015-04-29
BRPI1005979A8 (pt) 2017-12-26
US8318763B2 (en) 2012-11-27
JP5661100B2 (ja) 2015-01-28
EA020201B1 (ru) 2014-09-30
TN2011000265A1 (en) 2012-12-17
BRPI1005979A2 (pt) 2016-02-10
WO2010122436A1 (en) 2010-10-28
AU2010240638A1 (en) 2010-10-28
TWI422372B (zh) 2014-01-11
US20100267654A1 (en) 2010-10-21
IL212942A0 (en) 2011-07-31
MA33320B1 (fr) 2012-06-01
JP2012524060A (ja) 2012-10-11
EP2421869B1 (en) 2015-03-11
NZ595884A (en) 2012-12-21
PL2421869T3 (pl) 2015-08-31
DK2421869T3 (da) 2015-06-08
ES2535327T3 (es) 2015-05-08
HK1163663A1 (en) 2012-09-14
US8765778B2 (en) 2014-07-01
AR076340A1 (es) 2011-06-01
SG171989A1 (en) 2011-07-28
EP2421869A1 (en) 2012-02-29

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