The present invention discloses a water-soluble docetaxel anticancer drug compound having the structure of Formula I below:

##STR00001## in which R=CH.sub.3, CH.sub.2CH.sub.3, CH.sub.2CH.sub.2CH.sub.3, or CH.sub.2CH.sub.2CH.sub.2CH.sub.3; and n=5-500.

The active moiety docetaxel in the anticancer drug compound is covalently conjugated to a polyethylene glycol monoalkyl ether through a linker diglycoloyl (carbonyl methoxyacetyl) to form the water-soluble docetaxel anticancer drug compound.

The present invention also relates to a preparation method of the drug compound and use thereof.

The present invention is directed to reactor systems and processes for producing organic acids through thermolysis of polylactones. In preferred embodiments, the reactor systems and processes are capable of introducing at least one epoxide reagent and carbon monoxide reagent to at least one reaction vessel through at least one feed stream inlet; contacting the at least one epoxide reagent and carbon monoxide reagent with at least one carbonylation catalyst to produce at least one beta-lactone intermediate; polymerizing the at least one beta-lactone intermediate with at least one initiator in the presence of a metal cation to produce at least one polylactone product; and heating the at least one polylactone product under thermolysis conditions to produce at least one organic acid product. Advantageously, the processes of the present invention may control the presence of contaminates, impurities, catalytic materials, and/or reagents to provide for highly pure organic acid products.

Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of taxane-based compounds and/or fluorinated forms thereof. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the taxane-based compound is achieved.

Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of taxane-based compounds and/or fluorinated forms thereof. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the taxane-based compound is achieved.

The present invention is directed to reactor apparatus and processes for thermolysis of polypropiolactone to produce highly pure acrylic acid. In preferred embodiments of the present invention, the processes comprise introducing a feed stream comprising polypropiolactone to a thermolysis process vessel through an inlet; maintaining a concentration of active salt by adding and removing portions of active salt by at least one inlet and at least one outlet; heating the thermolysis process vessel; and recovering a product including acrylic acid from an outlet. In certain preferred embodiments, the active salt may be present as a catalyst used for polymerization of the polypropiolactone in the feed stream. In some embodiments, one or more active salts may be added to the feed stream and/or the thermolysis process vessel.

A method for analyzing related substances in a pharmaceutical composition containing an amphiphilic block copolymer comprising a hydrophilic block and a hydrophobic block as a polymeric drug carrier, related substances identified thereby, and a method for evaluating a pharmaceutical composition by using the same are provided.

Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.

Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.

The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.

The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.