BRPI1005979A8 - Derivados de rifamicina - Google Patents

Derivados de rifamicina

Info

Publication number
BRPI1005979A8
BRPI1005979A8 BRPI1005979A BRPI1005979A BRPI1005979A8 BR PI1005979 A8 BRPI1005979 A8 BR PI1005979A8 BR PI1005979 A BRPI1005979 A BR PI1005979A BR PI1005979 A BRPI1005979 A BR PI1005979A BR PI1005979 A8 BRPI1005979 A8 BR PI1005979A8
Authority
BR
Brazil
Prior art keywords
alkyl
compounds
hydroxy
hydrogen
pharmaceutical compositions
Prior art date
Application number
BRPI1005979A
Other languages
English (en)
Inventor
Claudio Viscomi Giuseppe
Campana Manuela
Folegatti Mahena
Cannata Vicenzo
Righi Paolo
Rosini Goffredo
Original Assignee
Alfa Wassermann Spa
Alfasigma Spa
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 Alfa Wassermann Spa, Alfasigma Spa filed Critical Alfa Wassermann Spa
Publication of BRPI1005979A2 publication Critical patent/BRPI1005979A2/pt
Publication of BRPI1005979A8 publication Critical patent/BRPI1005979A8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/20—Spiro-condensed systems
    • 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
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/7036—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/08—Bridged systems
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/18—Bridged systems
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/20—Spiro-condensed systems
    • 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

  • 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)
  • Communicable Diseases (AREA)
  • Oncology (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

COMPOSTO DERIVADO DE RIFAMICINA, SEUS PROCESSOS DE PRODUÇÃO E COMPOSIÇÕES FARMACÊUTICAS. A presente invenção refere-se a compostos incluindo derivados de rifamicina tendo atividades antibacterianas, em que os compostos têm a seguinte fórmula geral (I): (I) em que: R é hidrogênio ou acetila, R1 e R2 são selecionados de modo independente entre o grupo consistindo em hidrogênio, ( C1-4) alquila, benzilóxi, mono- e di-(C1-3) alquilamino-(C1-4)alquila, (C1-3)alcóxi, (C1-4) alquila, hidroximetila, hidroxi-(C2-4)-alquila, e nitro ou R1 e R2 tomados juntos com dois átomos de carbono consecutivos do núcleo de piridina formam um anel benzeno opcionalmente substituído por um ou dois grupos metila ou etila e R3 é hidrozialquila (C1-4). A invenção refere-se, além disso, a processos para obter estes compostos e a composições farmacêuticas compreendendo os mesmos. Os compostos têm atividade antibacteriana.
BRPI1005979A 2009-04-20 2010-03-18 Derivados de rifamicina BRPI1005979A8 (pt)

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
BRPI1005979A2 BRPI1005979A2 (pt) 2016-02-10
BRPI1005979A8 true BRPI1005979A8 (pt) 2017-12-26

Family

ID=41228810

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI1005979A BRPI1005979A8 (pt) 2009-04-20 2010-03-18 Derivados de rifamicina

Country Status (28)

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

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1698630T3 (da) 2005-03-03 2014-12-08 Alfa Wassermann Spa Nye polymorfe former af rifaximin, fremgangsmåde for deres fremstilling og anvendelse deraf i de medicinske præparater
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.
JP2015531347A (ja) * 2012-09-12 2015-11-02 サリックス ファーマスーティカルズ，インコーポレーテッド 抗生物質耐性を生じることなくリファキシミンを投与する方法
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
ES2810010T3 (es) * 2014-05-12 2021-03-08 Alfasigma Spa Preparación y uso de la forma cristalina tau de rifaximina solvatada con DEGME
PL3645539T3 (pl) * 2017-06-26 2021-10-25 Biofer S.P.A. Pochodne pirydoimidazoryfamycyny jako środek przeciwbakteryjny

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE751182A (fr) * 1969-05-30 1970-11-03 Takeda Chemical Industries Ltd Procede de fabrication d'antibiotiques
SU465795A3 (ru) * 1972-05-05 1975-03-30 Группо Лепетит (Фирма) Способ получени рифамицина в.
US3847903A (en) * 1973-03-01 1974-11-12 Archifar Ind Chim Trentino Method for extracting and isolating rifamycin o from fermentation broths of rifamycins
CH571064A5 (en) * 1973-03-01 1975-12-31 Archifar Ind Chim Trentino Recovery of rieamycin from broths - by oxidn to an insol form
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
US20130287692A1 (en) 2013-10-31
SG171989A1 (en) 2011-07-28
HK1163663A1 (en) 2012-09-14
WO2010122436A1 (en) 2010-10-28
BRPI1005979A2 (pt) 2016-02-10
PL2421869T3 (pl) 2015-08-31
AR076340A1 (es) 2011-06-01
CA2743801C (en) 2017-03-07
TWI422372B (zh) 2014-01-11
CO6362013A2 (es) 2012-01-20
HRP20110437A2 (hr) 2011-09-30
UA105775C2 (uk) 2014-06-25
EP2421869A1 (en) 2012-02-29
KR101555860B1 (ko) 2015-09-25
TN2011000265A1 (en) 2012-12-17
NZ595884A (en) 2012-12-21
US8318763B2 (en) 2012-11-27
ITMI20090653A1 (it) 2010-10-21
CN102405223A (zh) 2012-04-04
MX338334B (es) 2016-04-11
AU2010240638B2 (en) 2014-06-05
IL212942A0 (en) 2011-07-31
MX2011011026A (es) 2011-11-02
DK2421869T3 (da) 2015-06-08
EP2421869B1 (en) 2015-03-11
KR20120014110A (ko) 2012-02-16
ES2535327T3 (es) 2015-05-08
CL2011002597A1 (es) 2012-03-23
EA020201B1 (ru) 2014-09-30
IL212942A (en) 2015-06-30
EA201190216A1 (ru) 2012-02-28
JP2012524060A (ja) 2012-10-11
TW201039819A (en) 2010-11-16
PT2421869E (pt) 2015-04-29
US8765778B2 (en) 2014-07-01
MA33320B1 (fr) 2012-06-01
CA2743801A1 (en) 2010-10-28
US20100267654A1 (en) 2010-10-21
JP5661100B2 (ja) 2015-01-28
AU2010240638A1 (en) 2010-10-28
IT1397617B1 (it) 2013-01-18

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B25A Requested transfer of rights approved

Owner name: ALFASIGMA S.P.A. (IT)

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06I Publication of requirement cancelled [chapter 6.9 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: MANTIDO O INDEFERIMENTO UMA VEZ QUE NAO FOI APRESENTADO RECURSO DENTRO DO PRAZO LEGAL

B350 Update of information on the portal [chapter 15.35 patent gazette]