Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K38/00—Medicinal preparations containing peptides
  • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
  • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
  • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
  • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
  • A61K47/61—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P11/00—Drugs for disorders of the respiratory system
• • 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
• • 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

Definitions

• the monomeric residues in the alginate oligomer may be the same or different and not all need carry electrically charged groups although it is preferred that the majority (e.g. at least 60%, preferably at least 80% more preferably at least 90%) do. It is preferred that a substantial majority, e.g. at least 80%, more preferably at least 90% of the charged groups have the same polarity.
• the ratio of hydroxyl groups to charged groups is preferably at least 2:1 , more especially at least 3:1.
• G residues/G and M residues/M or to guluronic acid or mannuronic acid, or guluronate or mannuronate are to be read interchangeably as references to guluronic acid/guluronate and mannuronic acid/mannuronate
• Non-limiting examples thereof may include ester, carbonate ester, orthoester, ketone, ketal, hemiketal, ketene, ether, acetal, hemiacteal, peroxy, methylenedioxy, carbamate, amide, amine, amine oxide, hydroxamic acid, imine, imide, imidate, azide, azo, oxime, carbodiimide, carbazone, hydrozone, sulfide, disulfide, sulfinyl, sulfonyl, carbonothioyi, thioamide, thioester, thioether, thioketone, thioketal, sulphonate ester, dithiocarbamate, semicarbazone, phosphine or phosphodiester functional groups. As shown in the Examples, the formation of amide and ester bonds may be convenient and advantageous.
• covalent linker molecules include but are not limited to acetyl, succinyl, aconityl (c/ ' s or trans), glutaryl, methylsuccinyl, trimellityl cysteamine, penicillamine, N-(2-mercaptopropionyl)glycine, 2-mercaptopropionic acid, homocysteine, 3-mercaptopropionic acid and deamino-penicillamine groups.
• the covalent linker molecule may be a plurality of the molecules and/or groups described above.
• the invention further provides a polymyxin-alginate oligomer conjugate of the invention as defined herein, for use in the treatment or prevention of a bacterial infection in a subject with, suspected to have, or at risk of, a bacterial infection.
• bacterial infection (or "infected by” or “infected with” and the like) is used broadly herein to indicate that the subject may comprise, or contain, or carry, the bacteria in question, i.e. that the bacteria may simply be present in or on the subject, and this may include any site or location in or on the body of the subject. It is not necessary that the infection of the subject be manifest as a clinical disease (i.e. that the infection result in clinical symptoms in the subject), although this is of course encompassed.
• Acidaminococcus Acidovorax, Acinetobacter, Actinobacillus, Actinobaculum, Actinomadura, Actinomyces, Aerococcus, Aeromonas, Afipia, Agrobacterium, Alcaligenes, Alloiococcus, Alteromonas, Amycolata, Amycolatopsis,
• Brachyspira Brevibacillus, Brevibacterium, Brevundimonas, Brucella, Burkholderia, Buttiauxella, Butyrivibrio, Calymmatobacterium, Campylobacter, Capnocytophaga, Cardiobacterium, Catonella, Cedecea, Cellulomonas, Centipeda, Chlamydia,
• Non-fermenting Gram-negative bacteria include, but are not limited to, bacteria from the genera Pseudomonas, Acinetobacter, Stenotrophomonas and Burkholderia, Achromobacter, Algaligenes, Bordetella, Brevundimonas,
• the invention may provide for the treatment or prevention of respiratory infections or conditions associated therewith (e.g. cystic fibrosis, pneumonia, COPD, COAD, COAP, bronchitis, sinusitis, an infection in a chronic wound (including burns), a device related infection associated with implantable or prosthetic medical devices, bacteraemia, septicaemia, septic shock, or sepsis.
• respiratory infections or conditions associated therewith e.g. cystic fibrosis, pneumonia, COPD, COAD, COAP, bronchitis, sinusitis, an infection in a chronic wound (including burns), a device related infection associated with implantable or prosthetic medical devices, bacteraemia, septicaemia, septic shock, or sepsis.
• a subject is used broadly herein to include sites or locations inside a subject or on a subject, e.g. an external body surface, and may include in particular infection of a medical device e.g. an implanted or "in-dwelling" medical device.
• a medical device e.g. an implanted or "in-dwelling” medical device.
• the term “in a patient” should be interpreted consistently with this.
• Enteric coated granules may be prepared in accordance with the teachings of WO 1989008448 and Al-Khedairy, E.B.H, 2006, Iraqi J.Pharm.Sci., Vol.15 (1 ) 49, the contents of which are
• allylamines e.g. terbinafine, amorolfine, naftifine, butenafine
• echinocandins e.g. anidulafungin, caspofungin, micafungin.
• aceclofenac diclofenac, etodolac, indomethacin, ketorolac, nabumetone, tolmetin, sulindac
• the enolic acid derivatives e.g. droxicam, isoxicam, lornoxicam, meloxicam, piroxicam, tenoxicam
• the anthranilic acid derivatives e.g. flufenamic acid, meclofenamic acid, mefenamic acid, tolfenamic acid
• COX-2 inhibitors e.g.
• mucus viscosity reducing agent As used herein, the terms “mucolytic agent” and “mucus viscosity reducing agent” are intended to encompass agents which reduce the intrinsic viscosity of mucus and agents which reduce the attachment of mucus to underlying epithelium, in particular agents which directly or indirectly disrupt the molecular interactions within or between the components of mucus, agents which affect the hydration of mucus and agents which modulate the ionic microenvironment of the mucosal epithelium (particularly the levels of divalent cations, e.g. calcium).
• suitable mucus viscosity reducing agents include, but are not limited to, a nucleic acid cleaving enzyme (e.g.
• Suitable CFTR potentiators include, but are not limited to, ivacaftor (VX-770; N-(2,4-di-tert-butyl-5-hydroxyphenyl)-1 ,4-dihydro-4- oxoquinoline-3-carboxamide) and VRT-532 (4-methyl-2-(5-phenyl-1 H-pyrazol-3-yl)- phenol) of Vertex PharmaceuticalsTM).
• the model system was prepared under aseptic conditions in a class 2 laminar airflow cabinet and transferred to a shaking incubator set at 37°C in ambient air and constant orbital agitation at 70 rpm for 48 h.
• Acinetobacter baumanii (V19) in Mueller-Hinton broth (5 x 10 5 CFU/ml) was transferred to the OC and the IC was loaded with the agent under test (Batch 6) in PBS at previously determined MIC or double said MIC (Example 3; Batch 6 - colistin MIC: 0.25 g/ml; OligoG-E-colistin MIC: 0.125 g/ml; OligoG-A-colistin MIC: 0.125 g/ml). Samples were collected from the OC at various time points and characterised by bacterial colony counts (CFU/ml) using Miles and Misra Method.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Epidemiology (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Communicable Diseases (AREA)
• Oncology (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Immunology (AREA)
• Gastroenterology & Hepatology (AREA)
• Pulmonology (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Peptides Or Proteins (AREA)
• Medicinal Preparation (AREA)

Priority Applications (12)

Applications Claiming Priority (4)

Publications (1)

Family

ID=60186268

Family Applications (1)

Country Status (13)

Cited By (5)

Families Citing this family (4)

Citations (5)

Family Cites Families (2)

• 2017
  • 2017-10-20 US US16/343,568 patent/US20190328833A1/en not_active Abandoned
  • 2017-10-20 RU RU2019109719A patent/RU2019109719A/ru unknown
  • 2017-10-20 EP EP17791037.9A patent/EP3528830B1/en active Active
  • 2017-10-20 DK DK17791037.9T patent/DK3528830T3/da active
  • 2017-10-20 WO PCT/EP2017/076927 patent/WO2018073449A1/en not_active Ceased
  • 2017-10-20 ES ES17791037T patent/ES2933983T3/es active Active
  • 2017-10-20 JP JP2019521049A patent/JP2020503253A/ja active Pending
  • 2017-10-20 AU AU2017345295A patent/AU2017345295A1/en not_active Abandoned
  • 2017-10-20 KR KR1020197014050A patent/KR20190072579A/ko not_active Abandoned
  • 2017-10-20 CN CN201780065109.5A patent/CN109843315A/zh active Pending
  • 2017-10-20 FI FIEP17791037.9T patent/FI3528830T3/fi active
  • 2017-10-20 BR BR112019007927A patent/BR112019007927A2/pt not_active IP Right Cessation
  • 2017-10-20 CA CA3040795A patent/CA3040795A1/en active Pending

Patent Citations (5)

Non-Patent Citations (1)

Also Published As

Similar Documents

Legal Events