The invention relates to (among other things) oligomer-foscarnet conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated foscarnet compounds.

The present invention relates to a process for preparing polyoxyalkylene polyester polyols by reacting a starter compound having Zerewitinoff-active H atoms, a cyclic dicarboxylic acid anhydride and a fatty acid ester with an alkylene oxide in the presence of a basic catalyst. The invention further relates to polyoxyalkylene polyester polyols resulting from the method and to a preparation method for polyurethanes by reaction of the polyoxyalkylene polyester polyols according to the invention.

The present invention relates to the field of drug carrier systems and polymer therapeutics and diagnostics. It provides derivatized unimolecular polyols with a hydrophobic core moiety and a polyanionic, preferably, sulfated hydrophilic shell, N in particular to unimolecular hyperbranched sulfated polyglycerol micelles having a hydrophilic shell and a hydophrobic core. These may be used for the supramolecular encapsulation and transport of hydrophobic guest molecules into biological systems. The micelles can be applied as a drug carrier system for therapy and for diagnosis. They may also be therapeutic agents on their own. The invention also relates to preparation of said micelles.

A compound comprising a cyclodextrin and a monoalkoxy polyethylene glycol linked thereto through an ether bond (a pegylated cyclodextrin) is disclosed, as are drug delivery vehicles and pharmaceutical formulations including the same, and methods for making the compound and the drug delivery vehicle and for delivering the drug to a patient in need thereof. The method of making includes the steps of creating either a tosylated monoalkoxy polyethylene glycol or a tosylated cyclodextrin, and either reacting the tosylated monoalkoxy polyethylene glycol with a deprotonated cyclodextrin, or reacting the tosylated cyclodextrin with a deprotonated monoalkoxy polyethylene glycol. The present pegylated cyclodextrin readily forms an inclusion compound with certain drugs to protect the drug against adverse interactions with mucin (e.g., in a mucus membrane).

The present invention provides, among other things, compounds that include a water-soluble and non-peptidic polymer as well as a maleimidyl group. The compounds are useful as, among other things, polymeric reagents.

A number of cationic antimicrobial polymers have been synthesized by a condensation polymerization in bulk. The initial polymer formed has backbone tertiary nitrogens, which are subsequently quaternized using a suitable quaternizing agent (e.g., alkyl halide). The cationic polymers include polyamides, polycarbonates, polypolyureas and polyguanidiniums having a cationic repeat unit comprising the quaternary ammonium nitrogen as a backbone nitrogen. The cationic polymers can be active against Gram-negative, Gram-positive microbes, and/or fungi.

In nonionic surfactants that contain blocks of hydrophobic poly(alkylene oxide) polymer linked to blocks of hydrophilic poly(alkylene oxide) polymer, the biodegradability of the polymer is improved if the hydrophobic blocks are polymerized in the presence of carbon dioxide to add poly (alkylene carbonate) units into the hydrophobic block, in which the alkylene carbonate units make up from 1 to 40 weight percent of the hydrophobic polymer blocks. The resulting nonionic surfactants can have similar surfactant performance but improved biodegradability, as compared to related surfactants without alkylene carbonate units.

A number of cationic antimicrobial polymers have been synthesized by a condensation polymerization in bulk. The initial polymer formed has backbone tertiary nitrogens, which are subsequently quaternized using a suitable quaternizing agent (e.g., alkyl halide). The cationic polymers include polyamides, polycarbonates, polypolyureas and polyguanidiniums having a cationic repeat unit comprising the quaternary ammonium nitrogen as a backbone nitrogen. The cationic polymers can be active against Gram-negative, Gram-positive microbes, and/or fungi.

The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent. According to the method, a therapeutically effective amount of a therapeutic composition of the invention is administered to a mammal (e.g. person or animal) in recognized need of the therapeutic. Also disclosed are compounds having the formula:

##STR00001##

A compound having the formula:

##STR00001## wherein n, y, R.sub.1 and R.sub.2 are defined herein, and others, methods of making of and using, and compositions made thereby which have an antimicrobial resistance effect are described.