Anti-HIV achiral polyurea oligomers, a process for creating them

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

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564 50, 564 51, 564 52, 564 53, 574588, 574595, C07C27300, C61K 3117

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057288747

ABSTRACT:
The present invention relates to achiral polyurea oligomers, their uses and formulations as anti-HIV pharmaceuticals and to a process for the preparation of narrow mono- and polydispersed oligomers as an emodiment of the invention. The achiral oligomers are derived from repeating units of the monomer 4,4'-diamino-biphenyl-3,3'-disulfonic acid and are water soluble, have a rigid backbone, possess ordered anionic spacing and have a number average molecular weight of <20,000. The process relates to the synthesis of narrow poly- and mono-dipersed oligomers comprising the steps of: 1) restricting the crude olydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture; and/or 2) isolating the monodispersed anionic oligomer; and 3) optionally converting the narrow poly- or mono-dispersed anionic oligomer salt from Step 1 or 2 to a desired pharmaceutically-acceptable salt, especially a solim or potassium salt. The process steps may be executed whereby step 1 or 2 is done alone, each in combination with Step 3, or all three steps are done.

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