US2013195954A1PendingUtilityA1

Films and particles

Assignee: BRIGHAM & WOMENS HOSPITALPriority: May 31, 2006Filed: Nov 8, 2012Published: Aug 1, 2013
Est. expiryMay 31, 2026(expired)· nominal 20-yr term from priority
A61P 35/00A61P 35/02A61P 29/00A61P 31/00A61P 31/12C07D 319/06A61P 11/06A61P 21/06A61K 31/519C08F 124/00A61K 31/337A61P 17/02A61K 38/50A61K 47/32A61P 23/00Y10T428/2982A61K 38/14
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Claims

Abstract

Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses.

Claims

exact text as granted — not AI-modified
1 . An oligomer or polymer having a repeat unit represented by Formula XX: 
       
         
           
           
               
               
           
         
         wherein:
 Q is selected from O, S, Se, and NH; 
 G is selected from among the following structures: 
 
       
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           R 2  is selected from hydrogen, a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, and fluorocarbon chain of 1-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, arylalkyl, or fluorocarbon chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen substituents; 
           R 3  is selected from hydrogen, methoxy, ethoxy, amino, a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, and arylalkyl chain of 1-10 carbons; 
           R 4 , R 5 , and R 6  are each independently selected from a straight or branched alkyl, cycloalkyl, aryl, olefin, silyl, alkylsilyl, arylsilyl, alkylaryl, and arylalkyl chain of 1-10 carbons; and 
           R 7  and R 8  are each independently selected from hydrogen, a straight or branched alkyl, cycloalkyl, aryl, olefin, alkylaryl, and arylalkyl chain of 1-50 carbons, wherein each alkyl, cycloalkyl, aryl, olefin, alkylaryl, or arylalkyl chain is optionally substituted internally or terminally by one or more hydroxyl, hydroxyether, carboxyl, carboxyester, carboxyamide, amino, mono- or di-substituted amino, thiol, thioester, sulfate, phosphate, phosphonate, or halogen substituents. 
         
       
     
     
         2 . The oligomer or polymer of  claim 1 , wherein the oligomer or polymer is represented by Formula XX′: 
       
         
           
           
               
               
           
         
         wherein:
 n is an integer from 2-750, and wherein each oligomeric or polymeric chain has a terminal group, the terminal group being selected from among amines, thiols, amides, phosphates, sulphates, hydroxides, alkenes, and alkynes. 
 
       
     
     
         3 . The oligomer or polymer of  claim 1 , wherein R 2  is hydrogen or methyl. 
     
     
         4 . The oligomer or polymer of  claim 1 , wherein Q is oxygen. 
     
     
         5 . A composition comprising the oligomer or polymer of  claim 1 . 
     
     
         6 . A polymeric film or particle comprising an oligomer or polymer of  claim 1 . 
     
     
         7 . A polymeric particle of  claim 6 , comprising a microparticle or nanoparticle. 
     
     
         8 . A polymeric particle of  claim 7 , wherein the particle has a diameter between about 2 nm and 1 micron. 
     
     
         9 . The polymeric particle of  claim 7  comprising a first volume at a first pH, and a second volume at a second pH, different from the from the first pH. 
     
     
         10 . The polymeric particle of  claim 9 , wherein the second volume is 1× or more greater than the first volume when the second pH is lower than the first pH. 
     
     
         11 . The polymeric particle of  claim 9 , wherein the second volume is 4× or more greater than the first volume when the second pH is lower than the first pH. 
     
     
         12 . The polymeric particle of  claim 9 , wherein the second volume is 8× or more greater than the first volume when the second pH is lower than the first pH. 
     
     
         13 . The polymeric particle of  claim 9 , wherein the second volume is greater than the first volume and the change in volume is sufficient that the particle when within a cell during the volume change ruptures the cell or a cellular compartment. 
     
     
         14 . The polymeric particle of  claim 9 , wherein the second volume is greater than the first volume and the change in volume is sufficient to cause the particle to become lodged, embedded, or immobilized in an anatomic location, such as a lymph node, airway, cavity, capillary, or other tissue. 
     
     
         15 . The polymeric film or particle of  claim 6 , further comprising an agent. 
     
     
         16 . The polymeric film or particle of  claim 15 , wherein the agent is a biologically active agent comprising one or more of an anti-cancer agent, an anti-biotic, an anti-neoplastic agent, an analgesic, an angiogenic, or an agent that promotes wound healing. 
     
     
         17 . The polymeric film or particle of  claim 15 , wherein the biologically active agent comprises one or more of asparaginase; bleomycin; busulfan; capecitabine; carboplatin; carmustine chlorambucil; cisplatin; cyclophosphamide; cytarabine; dacarbazine; dactinomycin; daunorubicin; dexrazoxane; docetaxel; doxorubicin; etoposide; floxuridine; fludarabine; fluorouracil; gemcitabine; hydroxyurea; idarubicin; ifosfamide; irinotecan; lomustine; mechlorethamine; melphalan; mercaptopurine; methotrexate; mitomycin; mitotane; mitoxantrone; paclitaxel; pemetrexed; pentostatin; plicamycin; procarbazine; rituximab; streptozocin; teniposide; thioguanine; thiotepa; vinblastine; vincristine; and vinorelbine. 
     
     
         18 . (canceled) 
     
     
         19 . The film of  claim 6 , wherein the film is a single layered film. 
     
     
         20 . The film of  claim 15 , further comprising two or more layers to form a multi-layered film. 
     
     
         21 . The film of  claim 15 , comprising a first layer comprising a first polymer of Formula XX, and a second layer comprising a second polymer different from Formula XX. 
     
     
         22 . The film of  claim 21 , wherein the second polymer comprises one or more of poly(lactic acid), poly(glycolic acid), poly(lactic-co-glycolic acid), polycaprolactone, poly(trimethylene carbonate), polyester, polycarbonate, and polyamide. 
     
     
         23 - 41 . (canceled)

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