CA2417799A1 - Inhibiteurs de pompes d'efflux cellulaire de microbes - Google Patents

Inhibiteurs de pompes d'efflux cellulaire de microbes Download PDF

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Publication number
CA2417799A1
CA2417799A1 CA002417799A CA2417799A CA2417799A1 CA 2417799 A1 CA2417799 A1 CA 2417799A1 CA 002417799 A CA002417799 A CA 002417799A CA 2417799 A CA2417799 A CA 2417799A CA 2417799 A1 CA2417799 A1 CA 2417799A1
Authority
CA
Canada
Prior art keywords
oxo
dihydro
carboxylic acid
fluoro
salts
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.)
Abandoned
Application number
CA002417799A
Other languages
English (en)
Inventor
Noel J. De Souza
Mahesh V. Patel
Shrikant V. Gupte
Dilip J. Upadhyay
Milind C. Shukla
Nishith C. Chaturvedi
Satish B. Bhawsar
Sheela C. Nair
Mohammed A. Jafri
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wockhardt Ltd
Original Assignee
Individual
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
Priority claimed from US09/640,947 external-priority patent/US6750224B1/en
Priority claimed from US09/850,669 external-priority patent/US6608078B2/en
Priority claimed from PCT/IN2001/000100 external-priority patent/WO2001085728A2/fr
Application filed by Individual filed Critical Individual
Publication of CA2417799A1 publication Critical patent/CA2417799A1/fr
Abandoned legal-status Critical Current

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Classifications

    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
    • 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
    • A61K31/65—Tetracyclines
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/04—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne des composés inhibiteurs de pompes d'efflux cellulaire de microbes. L'invention se rapporte également à des procédés de préparation desdits composés, des procédés d'utilisation de ces composés inhibiteurs de pompes d'efflux et des compositions pharmaceutiques contenant lesdits composés.
CA002417799A 2000-08-01 2001-07-31 Inhibiteurs de pompes d'efflux cellulaire de microbes Abandoned CA2417799A1 (fr)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US22220100P 2000-08-01 2000-08-01
US60/222,201 2000-08-01
US09/640,947 US6750224B1 (en) 1999-05-07 2000-08-17 Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment
US09/640,947 2000-08-19
INPCT/IN00/00111 2000-11-21
IN0000111 2000-11-22
US28629101P 2001-04-25 2001-04-25
US60/286,291 2001-04-25
US09/850,669 US6608078B2 (en) 2000-05-08 2001-05-07 Antibacterial chiral 8-(substituted piperidino)-benzo [i,j] quinolizines, processes, compositions and methods of treatment
US09/850,669 2001-05-07
INPCT/IN01/00100 2001-05-08
PCT/IN2001/000100 WO2001085728A2 (fr) 2000-05-08 2001-05-08 Piperidino-benzo [i, j] quinolizines a substitution de piperidino en 8 chirales antibacteriennes, procedes, compositions et methodes de traitement
PCT/IN2001/000139 WO2002009758A2 (fr) 2000-08-01 2001-07-31 Inhibiteurs de pompes d'efflux cellulaire de microbes

Publications (1)

Publication Number Publication Date
CA2417799A1 true CA2417799A1 (fr) 2002-02-07

Family

ID=27517699

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002417799A Abandoned CA2417799A1 (fr) 2000-08-01 2001-07-31 Inhibiteurs de pompes d'efflux cellulaire de microbes

Country Status (4)

Country Link
EP (1) EP1305048A2 (fr)
AU (1) AU2001280091A1 (fr)
CA (1) CA2417799A1 (fr)
WO (1) WO2002009758A2 (fr)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6608078B2 (en) 2000-05-08 2003-08-19 Wockhardt Limited Antibacterial chiral 8-(substituted piperidino)-benzo [i,j] quinolizines, processes, compositions and methods of treatment
US7098219B2 (en) 2000-08-01 2006-08-29 Wockhart Limited Inhibitors of cellular efflux pumps of microbes
WO2011101710A1 (fr) * 2010-02-16 2011-08-25 Wockhardt Research Centre Inhibiteurs de pompe à écoulement
US6878713B2 (en) 2001-04-25 2005-04-12 Wockhardt Limited Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
US6964966B2 (en) 2001-04-25 2005-11-15 Wockhardt Limited Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
JP2005511743A (ja) * 2001-12-13 2005-04-28 ウォックハート・リミテッド 新世代の三重標的化したキラルな広域スペクトラム抗菌性の７位置換ピペリジノ−キノロンカルボン酸誘導体、その調製方法、組成物、および医薬としての使用
US6664267B1 (en) 2002-05-28 2003-12-16 Wockhardt Limited Crystalline fluoroquinolone arginine salt form
EP1918289A3 (fr) * 2002-05-28 2009-08-19 Wockhardt Limited Forme cristalline de sel d'arginine de fluoroquinolone
WO2004062674A2 (fr) 2003-01-07 2004-07-29 Paratek Pharmaceuticals, Inc. Polyamines substituees inhibant les pompes a efflux des bacteries
GB2403653A (en) * 2003-07-10 2005-01-12 Secr Defence Use of fluoroquinone antibiotics for the treatment of plague
JP5255183B2 (ja) 2003-09-04 2013-08-07 ウォックハート リミテッド ベンゾキノリジン−２−カルボン酸アルギニン塩四水和物
WO2005026145A2 (fr) * 2003-09-12 2005-03-24 Warner-Lambert Company Llc Agents antibacteriens a base de quinolone
WO2005070940A2 (fr) * 2004-01-13 2005-08-04 Cumbre Pharmaceuticals Inc. Derives de rifamycine efficaces contre des microbes pharmacoresistants
EP1723150A1 (fr) 2004-01-13 2006-11-22 Cumbre Pharmaceuticals Inc. Derives de rifamycine imino efficaces contres des microbes pharmacoresistants
US7994225B2 (en) 2004-03-17 2011-08-09 Rempex Pharmaceuticals, Inc. Bacterial efflux pump inhibitors for the treatment of ophthalmic and otic infections
JP2008500965A (ja) * 2004-03-17 2008-01-17 エムペックス・ファーマシューティカルズ・インコーポレーテッド 細菌の排出ポンプ阻害剤の使用および投与
DE102004035203A1 (de) 2004-07-21 2006-02-16 Bayer Healthcare Ag Substituierte Chinolone
DE102005030524A1 (de) 2005-06-30 2007-01-18 Aicuris Gmbh & Co. Kg Substituierte Chinolone II
DE102006005861A1 (de) 2006-02-09 2007-08-23 Aicuris Gmbh & Co. Kg Substituierte Chinolone III
US20090264342A1 (en) 2006-02-13 2009-10-22 Trustees Of Boston University Compositions and methods for antibiotic potentiation and drug discovery
AU2007222115B2 (en) * 2006-03-07 2011-05-12 Wockhardt Ltd Prodrugs of benzoquinolizine-2-carboxylic acid
CA2645376C (fr) * 2006-03-13 2017-06-20 Activx Biosciences, Inc. Aminoquinolones utilisees comme inhibiteurs de la gsk-3
US20100234348A1 (en) * 2006-08-04 2010-09-16 Trustees Of Boston University Compositions and methods for potentiating antibiotic activity
US7902227B2 (en) 2007-07-27 2011-03-08 Janssen Pharmaceutica Nv. C-7 isoxazolinyl quinolone / naphthyridine derivatives useful as antibacterial agents
CN102351880B (zh) * 2007-09-11 2014-11-12 杏林制药株式会社 作为gsk-3 抑制剂的氰基氨基喹诺酮和四唑并氨基喹诺酮
US8476261B2 (en) 2007-09-12 2013-07-02 Kyorin Pharmaceutical Co., Ltd. Spirocyclic aminoquinolones as GSK-3 inhibitors
MX2011009414A (es) 2009-03-11 2011-10-19 Kyorin Seiyaku Kk 7-cicloalquiloaminoquinolonas como inhibidores de gsk-3.
SG2014004162A (en) 2011-08-31 2014-03-28 Otsuka Pharma Co Ltd Quinolone compound
CN103183684B (zh) * 2011-12-29 2015-11-18 杭州师范大学 一种喹喏酮内酯化合物及其制备方法和应用
CN109486739B (zh) * 2018-11-23 2022-02-01 上海海洋大学 一种诱导副溶血性弧菌产生左氧氟沙星耐药性的方法
WO2023002011A1 (fr) * 2021-07-23 2023-01-26 Institut National De La Sante Et De La Recherche Medicale (Inserm) Inhibiteurs de pompe d'efflux de bactéries à gram négatif

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU200917B (en) * 1987-07-20 1990-09-28 Chinoin Gyogyszer Es Vegyeszet Process for producing pharmaceutical compositions comprising quinoline or naphthyridinecarboxylic acid and tetracycline derivatives as active ingredient
US5753269A (en) * 1995-12-27 1998-05-19 Bayer Corporation Otic microbial combinations

Also Published As

Publication number Publication date
AU2001280091A1 (en) 2002-02-13
WO2002009758A3 (fr) 2002-12-27
EP1305048A2 (fr) 2003-05-02
WO2002009758A2 (fr) 2002-02-07

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FZDE Discontinued