US2005255082A1PendingUtilityA1

Polymeric coupling agents and pharmaceutically-active polymers made therefrom

60
Individually held — no corporate assignee on recordPriority: May 14, 2004Filed: May 16, 2005Published: Nov 17, 2005
Est. expiryMay 14, 2024(expired)· nominal 20-yr term from priority
Inventors:Paul SanterreMei LiFrank Laronde
A61K 9/0024C08G 18/73A61L 2300/41A61L 2300/406A61K 47/60C08G 18/4277A61L 27/14A61L 27/54A61K 47/56A61L 2300/604A61L 2300/42A61K 47/59A61L 2300/416A61L 2300/45A61K 47/55A61K 47/50A61K 47/30
60
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

A pharmaceutically-active polymeric compound of the general formula (I), Y-[Y n -LINK B-X] m -LINK B  (I) wherein (i) X is a coupled biological coupling agent of the general formula (II) Bio-LINK A-Bio  (II) wherein Bio is a biologically active agent fragment or precursor thereof linked to LINK A through a hydrolysable covalent bond; and LINK A is a coupled central flexible linear first segment of <2000 theoretical molecular weight linked to each of said Bio fragments; (ii) Y is LINK B-OLIGO; wherein (a) LINK B is a coupled second segment linking one OLIGO to another OLIGO and an OLIGO to X or precursor thereof; and (b) OLIGO is a short length of polymer segment having a molecular weight of less than 5,000 and comprising less than 100 monomeric repeating units; (iii) m is 1-40; and (iv) n is selected from 2-50. The compounds are useful as biomaterials, particularly, providing antibacterial activity in vivo. Also provided are biological coupling agents useful as intermediates in the preparation of the pharmaceutically-active polymeric compounds.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutically-active polymeric compound of the general formula (I),  
       Y-[Y n -LINK B-X] m -LINK B  (I)  
     wherein (i) X is a coupled biological coupling agent of the general formula (II)  
       Bio-LINK A-Bio  (II)  
     wherein Bio is a biologically active agent fragment or precursor thereof linked to LINK A through a hydrolysable covalent bond;  
     and LINK A is a coupled central flexible linear first segment of <2000 theoretical molecular weight linked to each of said Bio fragments; 
 (ii) Y is LINK B-OLIGO; wherein  
 (a) LINK B is a coupled second segment linking one OLIGO to another OLIGO and an OLIGO to X or precursor thereof; and  
 (b) OLIGO is a short length of polymer segment having a molecular weight of less than 5,000 and comprising less than 100 monomeric repeating units;  
 (iii) m is 1-40; and  
 (iv) n is selected from 2-50.  
 
   
   
       2 . A compound as defined in  claim 1  wherein LINK A is linked to Bio by carboxylic ester, amide or sulfonamide links.  
   
   
       3 . A compound as defined in  claim 1  wherein LINK A contains within itself polyalkyl, polyethylene oxide, polyalkylene oxide, polyamides, polyester, polyvinyl, polycarbonate, polyanhydrides or polysiloxanes.  
   
   
       4 . A compound as defined in  claim 1  wherein LINK A has a molecular weight selected from 60-700  
   
   
       5 . A compound as defined in  claim 1  wherein Y n  has a theoretical molecular weight of less than 15,000,  
   
   
       6 . A compound as defined in  claim 5  wherein Y n  has a molecular weight of <10,000.  
   
   
       7 . A compound as defined in  claim 6  wherein Y n  has a molecular weight of <5,000.  
   
   
       8 . A compound as defined in  claim 1  wherein LINK B has a molecular weight selected from 60-2000.  
   
   
       9 . A compound as defined in  claim 8  wherein LINK B has a molecular weight selected from 60-700.  
   
   
       10 . A compound as defined in  claim 1  wherein LINK B is linked to other segments via urethanes, esters, ureas, sulfonamides, carbonates, anhydrides or amides.  
   
   
       11 . A compound as defined in  claim 1  having at least two Bio fragments or precursors thereof of different biological activities.  
   
   
       12 . A compound as defined in  claim 1  wherein said Bio has a molecular weight of <4000.  
   
   
       13 . A compound as defined in  claim 12  wherein said Bio has a molecular weight of <2000.  
   
   
       14 . A compound as defined in  claim 1  wherein said Bio is a biologically-active entity selected from an anti-coagulant, an anti-inflammatory agent, an anti-proliferative agent, an antimicrobial agent, an anti-thrombic agent and a hydrolysable precursor fragment thereof.  
   
   
       15 . A compound as defined in  claim 1  having at least two of said Bio entities and/or said hydrolysable precursor fragment thereof.  
   
   
       16 . A compound as defined in  claim 14  wherein said Bio is an antimicrobial agent or hydrolysable precursor fragment thereof.  
   
   
       17 . A compound defined in  claim 16  wherein said antimicrobial agent is selected from Cipofloxacin and Norfloxacin.  
   
   
       18 . A compound as defined in  claim 14  wherein said anti-flammatory agent is selected from Amfenac, Aceclofenac, Oxaceprol and Enoxolone.  
   
   
       19 . A compound as defined in  claim 14  wherein said anti-thrombic agent is selected from Bromofenac, Tirofiban and Lotrafiban.  
   
   
       20 . A compound as defined in  claim 14  wherein said anti-proliferation agent is selected from Acivicin and Alkeren.  
   
   
       21 . A biological coupling agent of the general formula (III)  
       PBio-LINK A-PBio  (III)  
     wherein PBio is a biologically active agent fragment or precursor thereof linked to LINK A through a hydrolysable covalent bond and having at least one functional group to permit step growth polymerization;  
     and LINK A is a coupled central flexible linear first segment of <2000 theoretical molecular weight linked to each of said PBio fragments.  
   
   
       22 . A coupling agent as defined in  claim 21  wherein LINK A is linked to Bio by carboxylic ester, amide or sulfonamide links.  
   
   
       23 . A coupling agent as defined in  claim 21  wherein LINK A has a molecular weight selected from 60-700.  
   
   
       24 . A coupling agent as defined in  claim 21  wherein said Bio is a biologically-active entity selected from an anti-coagulant, an anti-inflammatory agent, an anti- proliferative agent, an antimicrobial agent, an anti-thrombic agent and a hydrolysable precursor fragment thereof.  
   
   
       25 . A coupling agent as defined in  claim 24  wherein said anti-microbial agent is selected from Cipofloxacin and Norfloxacin.  
   
   
       26 . A coupling agent as defined in  claim 24  wherein said antiflammatory agent is selected from Amfenac, Aceclofenac, Oxacepro and Enoxolone.  
   
   
       27 . A coupling as defined in  claim 24  wherein said anti-thrombic agent is selected from Oxaceprol, Bromofenac, Tirofiban and Lotrafiban.  
   
   
       28 . A coupling agent as defined in  claim 24  wherein said anti-proliferation agent is selected from Acivicin and Alkeren.  
   
   
       29 . A pharmaceutically-active polymeric composition comprising a pharmaceutically- active polymeric compound as defined in  claim 1  in admixture with a compatible base polymer.  
   
   
       30 . A composition as defined in  claim 29  wherein said base polymer is selected from the group consisting of polyurethanes, polysulfones, polycarbonates, polyesters, polyethylene, polypropylene, polystyrene, polysilicone, poly(acrylonitrile- butadienestyrene), polybutadiene, polyisoprene, polymethylmethacrylate, polyamine, polyvinylacetate, polyacrylonitrile, polyvinyl chloride, polyethylene, terephthalate, cellulose and other polysacharides.  
   
   
       31 . A composition as defined in  claim 29  wherein said base polymer is a segmented polyurethane, a polyester, a polycarbonate, polysaccharide or polyamide or polysilicone.  
   
   
       32 . A composition as defined in  claim 29  in the form of a shaped article.  
   
   
       33 . A shaped article as defined in  claim 32  in the form of an implantable medical device, self-supporting film, or fiber.  
   
   
       34 . A compound as defined in  claim 1  in the form of a shaped article.  
   
   
       35 . A shaped article as defined in  claim 34  in the form of an implantable medical device, self-supporting film or fiber.

Join the waitlist — get patent alerts

Track US2005255082A1 — get alerts on status changes and closely related new filings.

We store only your email — no account needed. See our privacy policy.