Bioresponsive pharmacologically-active polymers and articles made therefrom

{
  "publication_number": "US5798115A",
  "country": "US",
  "kind": "A",
  "title": "Bioresponsive pharmacologically-active polymers and articles made therefrom",
  "abstract": "This invention relates to pharmacologically-active polymeric compounds; to substrates, such as implantable medical devices formed thereof or coated therewith; and to methods of using said compounds or said substrates for providing pharmacological agents released in response to in vivo activation at a desired location in a mammal. The polymeric material has a backbone comprising a pharmacologically-active fragment covalently linked through at least two functional groups within the backbone, wherein the backbone comprises, preferably, polyamide, polyurethane and/or polyurea linkages with, optionally, polyester, polycarbonate, polyether and/or polyvinyl linkages. The preferred pharmacological compounds are fluoroquinolines, particularly, ciprofloxacin. The pharmacologically-active compounds provide in vivo enhanced long term anti-inflammatory, anti-bacterial, anti-microbial and/or anti-fungal activity.",
  "claims": [
    "1. A bioresponsive, pharmacologically-active, polymeric material having a polystyrene equivalent molecular weight selected from 2,000-200,000 and a backbone comprising a pharmacologically-active fragment formed from a fluoroquinolone covalently linked through two functional groups selected from a polyamide, polyurea, polyurethane and polysulfonamide formed from two or isocyanate functional groups within said backbone.",
    "2. A polymeric material as defined in claim 1 further comprising one or more polyester, and polyether linkages.",
    "3. A polymeric material as defined in claim 2 wherein said polyester linkage is made from polycaprolactone-diol.",
    "4. A polymeric material as defined in claim 2 wherein said polyether linkage is made from polyether-diamine.",
    "5. A polymeric material as defined in any one of the preceding claims wherein said backbone comprises 1,6-diamidohexane--or 1,12-diamidododecane-polyurethane, - polyurea, polyamide or polysulphonamide linkages.",
    "6. A polymeric material as defined in claim 1 wherein said phannacologically-active fragment provides biological activity selected from the group consisting of anti-inflammatory, anti-bacterial, anti-microbial and anti-fingal activity under in vivo biochemical action.",
    "7. A polymeric material as defined in claim 1 wherein said fluoroquinolin is ciprofloxacin (1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-piperazine-quinolone-3-carboxylic acid).",
    "8. A polymeric material as defined in claim 1 made by the reaction of a polyisocyanate, an oligomeric α-ω diol, diamine or amino-alcohol, and a covalently linkable pharmacologically-active compound.",
    "9. A polymeric material as defined in claim 1 wherein said polyisocyanate is selected from hexamethylene diisocyanate and dodecyl-diisocyanate; said oligomeric diol is polycaprolactone-diol; and said pharmacologically-active compound is an antibacterial fluoroquinolone.",
    "10. A polymeric material as defined in claim 9 made by (a) reacting said hexamethylene diisocyanate or dodecyl-diisocyanate with polycaprolactone-diol to form a prepolymer; and (b) reacting said prepolymer with ciprofloxacin.",
    "11. A solid substrate comprising in whole or in part a bioresponsive pharmacologically-active polymeric material as defined in claim 1.",
    "12. A solid substrate wholly or partially coated with a bioresponsive pharmacologically-active polymeric material as defined in claim 1.",
    "13. A substrate as defined in claim 11 from the group consisting of an access device, suture, film, patch and dental fibre.",
    "14. A method of delivering a bioresponsive pharmacologically-active compound to a selected site in a mammal, said method comprising, locating or disposing a polymeric material as defined in claim 1, at or adjacent the locus of said site.",
    "15. A method of delivering a bioresponsive pharmacologically-active compound to a selected site in a mammal, said method comprising, locating or disposing a substrate as defined in claim 11 at or adjacent the locus of said site."
  ],
  "cpc": [
    "C08G 18/73",
    "A61K 47/59",
    "A61K 47/595",
    "A61L 2300/404",
    "A61L 2300/406",
    "A61L 2300/41",
    "A61L 27/34",
    "A61L 27/54",
    "A61L 29/085",
    "A61L 29/16",
    "A61P 31/04",
    "C08G 18/5024"
  ],
  "filing_date": "1997-02-13",
  "publication_date": "1998-08-25",
  "grant_date": "1998-08-25",
  "priority_date": "1996-02-15",
  "application_number": "US-79993897-A",
  "family_id": "26682693",
  "citations": [
    "EP0710689A2",
    "US4670444A",
    "US4670444B1",
    "US5219564A",
    "US5405919A",
    "US5449720A",
    "US5455027A",
    "US5474765A"
  ]
}