POSACONAZOLE POLYMER CONJUGATES AND METHODS OF TREATMENT USING POSACONAZOLE AND POLYMER CONJUGATES THEREOF
First Claim
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1. A polymeric conjugate comprising posaconazole and a substantially non-antigenic polymer.
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Abstract
Improved posaconazole-based compositions and methods of treating and preventing fungal infections, cancer or metastatic diseases are disclosed. In preferred aspects, the conjugates are PEG-posaconazole conjugates in which the PEG has a molecular weight of about 20,000 daltons.
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Citations
28 Claims
- 1. A polymeric conjugate comprising posaconazole and a substantially non-antigenic polymer.
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15. A method of preparing a polymeric conjugate, comprising
a) reacting a compound of the structure in the presence of a base wherein Z21 and Z22 are independently selected from the group consisting of O, S and NR21; -
Y21 is O, S, SO, SO2, CR22R23 or NR24; R21, R22, R23 and R24 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-19 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 hetero-alkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and b) reacting the resulting product of step a) with an amine-terminated polyalkylene oxide in the presence of a base and a coupling agent under conditions sufficient to form a polymeric conjugate. - View Dependent Claims (16)
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Specification