Polymeric coupling agents and pharmaceutically-active...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 47/30 (2006.01) A61L 27/14 (2006.01) A61L 27/54 (2006.01)

Patent

CA 2467321

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 a.i. in vivo. Also provided are biological coupling agents useful as intermediates in the preparation of the pharmaceutically-active polymeric compounds.

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