The invention includes taxoid compounds represented by the formula: ##STR00001##
wherein: R.sup.1 represents a methyl group or a fluorine; R.sup.2 represents an alkyl or alkenyl group having one to six carbon atoms; or a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; R.sup.3 represents an alkyl, alkenyl, dialkylamino, alkylamino, or alkoxy group having one to six carbon atoms; a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; an aryl group having six to eighteen ring carbon atoms; or a heteroaryl group having three to seventeen ring carbon atoms; R.sup.4 represents hydrogen or a methyl group; and X represents hydrogen or fluorine.

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.

Provided in the present disclosure are complexes and solutions demonstrating improved aqueous solubility of derivatized cytotoxic taxane drug moieties. In some other aspects, the disclosure provides methods of using such complexes and solutions for the treatment of cancer. In some further aspects, the disclosure provides combination therapies that may be suitable when used in combination with the use of the complexes disclosed herein.

Provided in the present disclosure are complexes and solutions demonstrating improved aqueous solubility of derivatized cytotoxic taxane drug moieties. In some other aspects, the disclosure provides methods of using such complexes and solutions for the treatment of cancer. In some further aspects, the disclosure provides combination therapies that may be suitable when used in combination with the use of the complexes disclosed herein.

The present disclosure provides bioorthogonal linkers and reagents, including trans-cyclooctene (TCO)- and tetrazine (Tz)-containing compounds. In a general aspect, the present disclosure provides reagents, conjugates, and bioactive molecules containing a trans-cyclooctene (TCO) fragment. Examples of TCO fragments include: Formulae (I) and (II).

##STR00001##

Reactor systems and processes produce organic acids through thermolysis of polylactones. The reactor systems and processes introduce at least one epoxide reagent and carbon monoxide reagent to at least one reaction vessel through at least one feed stream inlet. The epoxide reagent and carbon monoxide reagent contact at least one carbonylation catalyst to produce at least one beta-lactone intermediate. The beta-lactone intermediate is polymerized with at least one initiator in the presence of a metal cation to produce at least one polylactone product. The polylactone product is heated under thermolysis conditions to produce at least one organic acid product. The processes control the presence of contaminates, impurities, catalytic materials, and/or reagents to provide for highly pure organic acid products.

Reactor systems and processes produce organic acids through thermolysis of polylactones. The reactor systems and processes introduce at least one epoxide reagent and carbon monoxide reagent to at least one reaction vessel through at least one feed stream inlet. The epoxide reagent and carbon monoxide reagent contact at least one carbonylation catalyst to produce at least one beta-lactone intermediate. The beta-lactone intermediate is polymerized with at least one initiator in the presence of a metal cation to produce at least one polylactone product. The polylactone product is heated under thermolysis conditions to produce at least one organic acid product. The processes control the presence of contaminates, impurities, catalytic materials, and/or reagents to provide for highly pure organic acid products.

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 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.